2013年10月26日星期六

Bezafibrate Interactions with other drug

Bezafibrate is prescribed for the treatment of high blood cholesterol when dietary measures have proven ineffective. The medication lowers lipid (fat) levels in the blood and is particularly effective when the levels of HDL-cholesterol - often termed "good" cholesterol because it tends to carry cholesterol away from the arteries and back to the liver, where it's passed from the body - is low, and triglycerides - a type of fat that is normally present in the blood, and of which high levels are linked to heart disease and atherosclerosis - are raised.


Bezafibrate(CAS.NO:41859-67-0) improves markers of combined hyperlipidemia, effectively reducing LDL and triglycerides and improving HDL levels. The main effect on cardiovascular morbidity is in patients with the metabolic syndrome, the features of which are attenuated by bezafibrate. Studies show that in patients with impaired glucose tolerance, bezafibrate may delay progress to diabetes, and in those with insulin resistance it slowed progress in the HOMA severity marker. In addition, a prospective observational study of dyslipidemic patients with diabetes or hyperglycemia showed that bezafibrate significantly reduces haemoglobin A1c (HbA1c) concentration as a function of baseline HbA1c levels, regardless of concurrent use of antidiabetic drugs.
Drug interactions

Warfarin:  Possible increased warfarin toxicity

Monoamine oxidase inhibitors (MAOIs):  Possible liver damage

Antidiabetic drugs:  Possible increased blood sugar lowering effect

Statin-type cholesterol-lowering drugs:Possible muscle damage

Orlistat: Manufacturer advises against concomitant use

Cholestyramine: Should be taken at least 2 hours apart from bezafibrate

Phenytoin: Possible increased phenytoin toxicity

Disease interactions : Consult your doctor before using this drug if you have 
severe kidney or liver disease, an overactive thyroid gland, gallstones or a gall bladder disorder, a stomach ulcer, or if you have heart disease.


Overdose action  : A small overdose is no cause for concern. In case of intentional large overdose, seek emergency medical attention.

1,4-Butanediol properties

1,4-Butanediol is the organic compound with the formula HOCH2CH2CH2CH2OH. This colorless viscous liquid is derived from butane by placement of alcohol groups at each end of the chain. It is one of four stable isomers of butanediol.

              
1.1,4-Butanediol Property
Name:1,4-Butanediol

EINECS:203-786-5

Molecular Formula:C4H10O2

CAS Registry Number:110-63-4

Synonyms:1,4-Butyleneglycol; 1,4-Dihydroxybutane; 1,4-Tetramethylene glycol; DabcoDBO; Diol 14B; NSC 406696; Polycure D; Sucol B; Tetramethylene 1,4-diol; Tetramethylene glycol; Vibracure A 250; ZM 0025;

InChI:InChI=1/C4H10O2/c5-3-1-2-4-6/h5-6H,1-4H2

HS Code:29053980

Appearance:viscous colourless liquid

Molecular Weight:90.12

Density:1.017 g/mL at 25 °C(lit.)

Boiling Point:229.2℃ (759.8513 mmHg)

Melting Point:20℃

Flash Point:135℃

Storage Temperature:2-8°C

Refractive index:1.4442-1.4462

Solubility:Miscible with water

Stability:Stable. Combustible. Incompatible with strong oxidizing agents, mineral acids, acid chlorides, acid anhydrides.

Usage:Chemical intermediate for tetrahydrofuran, and other acetylenic chems (gamma butyrolactone), monomer for polybutylene terephthalate
resins, chain extender for polyurethane resins.

CBNumber:CB4452184

vapor density : 3.1 (vs air)

Sensitive :Hygroscopic

BRN :1633445


2.Safety information
Hazard Codes :Xn

Risk Statements :22

Safety Statements : 36

WGK Germany :1

RTECS :EK0525000

HS Code : 29053980

Hazardous Substances Data: 110-63-4(Hazardous Substances Data)

Chemical Properties:viscous colourless liquid

General Description:Odorless colorless liquid or solid (depending upon temperature).

Air & Water Reactions:Highly flammable. 1,4-Butanediol is hygroscopic. Water soluble.

Reactivity Profile:1,4-Butanediol is heat and light sensitive. 1,4-Butanediol reacts with acid chlorides, acid anhydrides and chloroformates. 1,4-Butanediol also reacts with oxidizing agents and reducing agents. 1,4-Butanediol is incompatible with isocyanates and acids. 1,4-Butanediol is also
incompatible with peroxides, perchloric acid, sulfuric acid, hypochlorous acid, nitric acid, caustics, acetaldehyde, nitrogen peroxide and chlorine.

Health Hazard:Ingestion of large amounts needed to produce any symptoms.

The application of 1,4-Butanediol

The bifunctional alcohol 1,4-butanediol is a versatile intermediate for the chemical industry. It reacts with dicarboxylic acids to yield polyesters, with diisocyanates to yield polyurethanes, and with phosgene to yield chloroformates. The main applications for butanediol are the production of cellular plastics, thermoplastic polyesters, hot-melt adhesives and plasticizers.


In the textile industry, 1,4-butanediol is an additive in sizes and finishing baths. Similar to glycerol, it acts as a plasticizer for water-soluble binders. Plasticized products are less tacky in a humid atmosphere than those treated with glycerol because 1,4-butanediol is not as hygroscopic.
Polybutyleneterephthalate (PBT) is a thermoplastic polyester produced by the polycondensation of 1,4-butanediol with terephthalic acid or dimethylterephthalate. Preference is usually given to the reaction with the ester, which can be purified more easily to the degree required for polycondensation.


1,4-Butanediol is used industrially as a solvent and in the manufacture of some types of plastics, elastic fibers and polyurethanes. In organic chemistry, 1,4-butanediol is used for the synthesis of γ-butyrolactone (GBL). In the presence of phosphoric acid and high temperature, it dehydrates to the important solvent tetrahydrofuran. At about 200 °C in the presence of soluble ruthenium catalysts, the diol undergoes dehydrogenation to form butyrolactone.

FDA warning against products containing GHB and its prodrugs, such as 1,4-butanediol. It is also used as a recreational drug known by some users as "One Comma Four", "One Four Bee" or "One Four B-D-O". It exerts effects similar to γ-hydroxybutyrate (GHB), which is a metabolic product of 1,4-butanediol. Misuse has also resulted in addiction and death.


Meimei is a website edit person of the guidechem.com.Guidechem.com was established with the aim to build the most comprehensive database of chemical products and contain most complete suppliers, making chemical trading more efficient, convenient and safe. facilitate global chemical trading and bring chemical buyers & sellers from all over the world to one common chemical platform.And now guidechem.com B2B network has been named "2010 China's e-commerce website industry TOP100".

2013年10月25日星期五

Dromostanolone propionate

Dromostanolone propionate's trade name is  masteron.it  is an anabolic/androgenic steroid which is the propionate ester of drostanolone.



Dromostanolone propionate  is a popular steroid among competitive bodybuilders. The average dosage of Dromostanolone propionate is 100 mg injected every other day.

Drostanolone propionate is an injectable anabolic steroid derived from dihydrotestosterone (DHT). Here, the DHT backbone has been modified with a 2-methyl group to increase its anabolic properties, making Dromostanolone propionate significantly more effective at promoting the growth of muscle tissue than its non-methylated parent. Drostanolone Propionate is described in product literature as a "steroid with powerful anabolic and anti-estrogenic properties," and indeed Dromostanolone propionate does seem to share some of both properties. Admittedly, however, its anabolic properties are more properly described as moderate, especially when placed in the context of other agents. Dromostanolone propionate is most often used by dieting bodybuilders and athletes in speed sports, where it is highly favored for its ability to produce solid increases in lean muscle mass and strength, which are usually accompanied by reductions in body fat level and minimal side effects.


Dromostanolone propionate is commonly used in contest preparation for many reasons. To begin with, Drostanolone Propionate is a derivative of DHT (Dihydrotestosterone), and therefore, it will not aromatize into estrogen. Competing bodybuilders find this extremely beneficial because aromatization typically causes excess water retention which may give the muscles a smooth appearance. Another advantage of Dromostanolone propionate is its strong androgenic component. The androgenic effect can cause a noticeable improvement in muscle density and hardness which can help the bodybuilder obtain the "ripped" look if his body fat percentage is low enough. The androgenic effect is also crucial because it helps to provide sufficient "kick" or "drive" for intense training when an athlete has lowered his caloric intake for contest preparation. Dromostanolone propionate can also be used successfully by bodybuilders preparing for a drug-tested show. Drostanolone Propionate is fast acting and quickly broken down. The athlete can therefore use Dromostanolone propionate up to about ten days before a drug test. The average dosage of Drostanolone Propionate is 100 mg injected every other day. It is best to inject Dromostanolone propionate every 2-3 days, because Dromostanolone propionate has a short duration of effect. Popular steroids for Dromostanolone propionate stack include Parabolan (Trenbolone hexahydrobencylcarbonate), Winstrol (Stanozolol), and Anavar (Oxandrolone). Athletes rarely experience any side effects with Drostanolone Propionate. Dromostanolone propionate is not hepatotoxic, and gynecomastia should not be a concern since Dromostanolone propionate does not convert into estrogen.

2013年10月24日星期四

Why is silver nitrate used in on medicine?

Silver nitrate is a chemical compound with chemical formula AgNO3. This nitrate of silver is a light-sensitive ingredient in photographic film and is a poisonous, corrosive compound. Silver nitrate crystals can be produced by dissolving silver in nitric acid and evaporating the solution. The compound notably stains skin a greyish or black color that is made visible after exposure to sunlight.



1. AgNO3 Cautery

Silver nitrate(CAS.NO:7761-88-8) can be used in a medical environment as a chemical cauterizing agent and medicinal caustic. A typical applicator is composed of 75% silver nitrate with 25% potassium nitrate. As the silver nitrate contacts with water (in the blood) the compound goes into solution forming nitric acid. The acid subsequently is responsible for the cautery effect. As mentioned above this will typically result in a black or greyish staining of the skin. This staining is caused by the accumulation of the silver and will typically go away as the body rids itself of the mineral.

2. Possible toxicity

1) Silver nitrate when used topically has been noted to cause irritation, redness.

2) The main toxic effect of topical silver nitrate is a generalized gray pigmentation of the skin called argyria. This is very rare with chronic topical use and typically occurs more frequently with chronic systemic absorption. On average, 3.8 grams of silver nitrate given orally can cause argyria to begin to be observed.

3) Silver nitrate is mainly considered a poison with ingestion due to the corrosive nature of the compound. If ingested, silver nitrate can cause potentially fatal gastroenteritis and gastrointestinal bleed. In toxicity studies, 29mg/kg administered to humans via an unknown route caused no fatalities, however 50mg/kg given orally to mice was lethal to 50% of the subjects.


3. Effect

Silver nitrate is a powerful chemical germicide and, on contact with living tissue,

1) "Toughened silver nitrate" and "Lunar caustic" are terms to describe the combination of silver nitrate with potassium nitrate

2) Exposure to light causes the silver in the tip to turn brown, but does not affect its therapeutic action

3) Moisture has a deteriorating effect on the tip (can make it break or loosen from the applicator)

4) Improper use of silver nitrate can cause chemical burns (it is a caustic compound)

* Use in neonates (as on the umbilicus) should be of short duration

*  Do not use in the eyes

4. Indications

1) Skin

*Cauterization of wounds an sluggish ulcers

*Removal of granulation tissue and warts


2) Mucous membranes

*Oral ulcers and apthae

*Control of epistaxis by direct application to hemorrhagic site

Intro to 2-Methylimidazole

2-methylimidazole , is white needle crystal or crystalline powder under room temperature. Relative molecular mass of 82.11 . Melting point 145 ~ 146 ℃. Boiling point 267 ℃. It Can be sublimated . Flash point of 160 ℃. Insoluble in ether , cold benzene , soluble in water , alcohols , ketones . Irritant to skin and mucous membranes.


1.Overview

2-methylimidazole(CAS.NO:693-98-1) pesticide production antitrichomonal Flagyl (metronidazole) intermediates. Is epoxy resin curing agent , and other curing accelerator , an amine curing agent occupies a special position in the epoxy resin curing agent in the temperature ,which may be used alone , in a short time after heat treatment , heating can be obtained cured high temperature deformation . It is mainly used for powder molding and powder coating curing accelerator .

2.Uses

1)for pharmaceutical intermediates metronidazole , is epoxy resin curing agent , and other.

2)This product is a medication metronidazole and feed growth promoters dimethyl azole intermediates, as well epoxy and other resin curing agent. As the temperature of the solid epoxy resin through the agent may be used alone , but primarily for powder molding and powder coating curing accelerator .

3.Preparation

1)glyoxal , acetaldehyde , and ammonia as raw materials , the reaction of 2-methyl-imidazole crude, sublimation purification , can be obtained products.

2)ethylenediamine and acetonitrile as raw materials , the reaction in the presence of sulfur to produce imidazoline , again in the presence of a nickel catalyst , at 200 ℃ dehydrogenation , can be prepared from 2 - methylimidazole products.

3)to glyoxal and methylamine in the presence of formaldehyde reaction , can be obtained.

4.Production methods

From 2-methylimidazoline eliminate dehydrogenation . 2-imidazoline heating and melting (melting point 107 ℃), active nickel was added carefully , the reaction temperature was raised to 200-210 ℃ 2h. Cooling to below 150 ℃ , dissolved in water , hot pressure filtration , separation active nickel , the filtrate was concentrated to a temperature above 140 ℃ , discharge cooling that is to give 2 - methylimidazole. With the production of a purity of ≥ 98% of the product , 1t products consume ethylene diamine (95%) 1095kg, acetonitrile 975kg. A better approach is to use glyoxal and formaldehyde as raw materials .

5. 2-methylimidazole and environment


2-Methylimidazole's production and use in the manufacture of pharmaceuticals, photographic and photothermographic chemicals, dyes, pigments, agricultural chemicals and rubber may result in its release to the environment through various waste streams. If released to air, an estimated vapor pressure of 6.9X10-4 mm Hg at 25 deg C indicates 2-methylimidazole will exist solely as a vapor in the atmosphere. Vapor-phase 2-methylimidazole will be degraded in the atmosphere by reaction with photochemically-produced hydroxyl radicals; the half-life for this reaction in air is estimated to be 4.1 hours. 2-Methylimidazole does not contain chromophores that absorb at wavelengths >290 nm and therefore is not expected to be susceptible to direct photolysis by sunlight. If released to soil, 2-methylimidazole is expected to have very high mobility based upon an estimated Koc of 33. The pKa of 2-methylimidazole is 7.86, indicating that this compound will partially exist in cation form in the environment and cations generally adsorb more strongly to soils containing organic carbon and clay than their neutral counterparts. Volatilization from moist soil surfaces may be an important fate process based upon an estimated Henry's Law constant of 4.1X10-6 atm-cu m/mole. However, volatilization from moist soil may be attenuated because the compound exists partially as a cation and cations do not volatilize. Utilizing the Japanese MITI test, 1% of the Theoretical BOD was reached in four weeks indicating that biodegradation is not an important environmental fate process. If released into water, 2-methylimidazole is not expected to adsorb to suspended solids and sediment based upon the estimated Koc. Volatilization from water surfaces may be an important fate process based upon this compound's estimated Henry's Law constant. Estimated volatilization half-lives for a model river and model lake are 190 hours and 62 days, respectively. An estimated BCF of 3.2 suggests the potential for bioconcentration in aquatic organisms is low. Hydrolysis is not expected to be an important environmental fate process since this compound lacks functional groups that hydrolyze under environmental conditions. Occupational exposure to 2-methylimidazole may occur through inhalation and dermal contact with this compound at workplaces where 2-methylimidazole is produced or used. The general population may have limited exposure to this compound from consumer products containing 2-methylimidazole.

Compound: 4-Hydroxy-4-methyl-2-pentanone

 4-Hydroxy-4-methyl-2-pentanone is a clear colourless liquid with mild pleasant odor it turns yellow on ageing. It is also known as Diacetone alcohol, diketone alcohol, tyranton, 4-hydroxy-4-methylpentanone, 2-methyl-2-pentanol-4-one, 4-methyl-2-pentanon-4-ol, diacetonalkohol, 4-hydroxy-2-keto-4-methylpentane, acetonyldimethylcarbinol, 4-hydroxy-4-methyl-penta-2-on, diacetone, daa, or 4-idrossi-4-metil-pentan-2-one. 4-Hydroxy-4-methyl-2-pentanone has slow evaporation rates. Characteristics- its boiling range is 145 -170 c, purity 99% min., and specific gravity is 0. 935 at 27 c. It is used as a solvent for both hydrogen bonding and polar substances. It is miscible in water and used as a solvent for water-based coatings. It is used as a solvent extractant in purification processes for resins and waxes. 4-Hydroxy-4-methyl-2-pentanone is more suitable for use in applications as a component of gravure printing inks, with proving favorable flow and leveling characteristics.

Name:4-Hydroxy-4-methyl-2-pentanone

EINECS:204-626-7

Molecular Formula:C6H12O2

CAS Registry Number:123-42-2

Appearance:Clear, colorless liquid

Molecular Weight:116.16

Density:0.938

Boiling Point:166℃

Melting Point:-42.8℃

Flash Point:58℃

Chemical Properties: colorless flammable liquid with a pleasant odor. And ethanol , aromatics, halogenated hydrocarbons, ethers and water miscible .

Production methods: by acetone in alkaline conditions derived by condensation . Consumption per ton of product acetone 1250kg.

Category : Flammable liquid


Toxicity grading : Poisoning

Acute toxicity : Oral - Rat LD50: 4000 mg / kg ; Oral - Mouse LD50: 3950 mg / kg

Stimulus data: skin - Rabbit 500 mg mild ; Eye - Rabbit 20 mg severe

Explosive hazardous characteristics : an explosive mixtures with air

Flammable hazardous characteristics : case of fire , high temperature, strong oxidants combustible ; combustion exhaust fumes stimulus

Storage features: packaging integrity , light loading and unloading ; Treasury ventilated , away from open flames , heat, and oxidants

Extinguishing Media: Foam , dry powder, carbon dioxide, sand

Purposes:

1) 4-Hydroxy-4-methyl-2-pentanone is manufactured from acetone isopropylidene acetone , methyl isobutyl ketone , methyl isobutyl carbinol and
hexylene glycol , isophorone , isophorone intermediate in 4-Hydroxy-4-methyl-2-pentanone available to the system to metal cleaners , wood
preservatives , photographic film and drug preservatives , antifreeze, hydraulic oil solvent extraction agent and fiber finishing agent . 4-Hydroxy-4-
methyl-2-pentanone is widely used as electrostatic painting , celluloid , nitrocellulose , fat, oil , wax and resin solvent .

2) As high boiling point solvents , paint thinners , wood stains , rust agents and dyes and other materials


3) As dye materials and resin solutions

How to produce Potassium hydrogencarbonate?

Potassium hydrogencarbonate(CAS.NO:298-14-6)  is a colorless, odorless, slightly basic, salty substance. Soluble in water , insoluble in alcohol. Potassium hydrogencarbonate is "generally recognized as safe".There is no evidence of human carcinogenicity, no adverse effects of overexposure, and an undetermined LD50. Physically, Potassium hydrogencarbonate occurs as a crystal or a soft white granular powder. Potassium hydrogencarbonate is very rarely found in its natural form, the mineral called kalicinite.

1. Purposes

1) For the production of potassium carbonate, potassium acetate , potassium arsenite and other raw materials , it also used in medicine, food, fire extinguishing agent industry;

2) It can be  used as analytical reagent;

3) As acidity regulator and chemical leavening agents ,which can be used for all kinds of requirements which need to add leavening agent in food , according to production needs in moderation;

4) The production of potassium carbonate, potassium acetate , potassium arsenite materials. Petroleum and chemicals can be used for the extinguishing agent. it can also be used in medicine, baking powder.

2.Production methods

1) Carbonation
Potassium carbonate raw materials available three products. As a raw material,it can be an alkali earth , containing 40% to 60% of potassium carbonate , 10% to 15% potassium sulfate , potassium chloride 3.5% , before feeding to be calcined to remove organics , by the different solubility of potassium sulfate and potassium chloride was removed , milk of lime or magnesium can be removed by pressure filtration of silicon, aluminum , phosphorus and other impurities , and the filtrate was evaporated , the preparation of potassium carbonate solution , the total alkali concentration of 750 ~ 800 g / L ( total potassium carbonate ) , into the carbonation tower . At a temperature above 50 ℃ , reaction pressure 0.4MPa , the pass carbon dioxide ( 30% concentration ) for carbonization , with the concentration of Potassium hydrogencarbonate and continuous precipitation . 5 ~ 6h carbonation crystallization mother liquor after separation, washing , centrifugation , dried at 80 ℃ , Potassium hydrogencarbonate to obtain the finished product . Its

K2CO3 + CO2 + H2O → 2KHCO3


2) Ion exchange method

Potassium chloride solution by the addition of calcium, magnesium Walter countercurrent ion exchange column , so that sodium resin (R-Na) becomes potassium type (RK), washed with soft water chlorine ions, ammonium bicarbonate solution downstream through the resin exchange column , to obtain a mixture of Potassium hydrogencarbonate and ammonium bicarbonate dilute solution by evaporation decomposition of most of the decomposition of potassium carbonate , and the solution generated by carbonization send carbonation tower Potassium hydrogencarbonate , and then by crystallization, separation , washing and drying to obtain a Potassium hydrogencarbonate product. Its

R-Na + KCl → R-K + NaCl

R-K + NH4HCO3 → R-NH4 + KHCO3

2KHCO3 → K2CO3 + CO2 ↑ + H2O

K2CO3 + CO2 + H2O → 2KHCO3

3) Solution reaction


By potassium hydroxide in 80% ethanol solution or saturated solution of potassium carbonate to absorb carbon dioxide prepared products.
K2CO3 + CO2 + H2O → 2KHCO3

2013年10月23日星期三

Diethyl acetamidomalonate


1.Diethyl acetamidomalonate Chemical Properties

Product Name: Diethyl acetamidomalonate

Synonyms:Diethyl acetamidomatonate; Diethyl Acetaminomalonate; Acetamidomalonic acid diethyl ester; Diethylacetamidomalonate; Diethyl acetamido malonate; Acetaminomalonic Acid Diethyl Ester; ROPANEDIOIC ACID, (ACETYLAMINO)-, DIETHYL ESTER; (Acetylamino)propanedioic acid diethyl ester; (acetylamino)-propanedioicacidiethylester; 2-(Acetylamino)propanedioic acid diethyl ester; acetamido-malonicacidiethylester; Acetaminomalonicaciddiethylester; Diethyl 2-(acetylamino)malonate; PROPANEDIOIC ACID, (ACETYLAMINO)-, DIETHYL ESTER; Diethy acetamino Malonate; a-Diethyl acetamidomalonate

InChI:InChI=1/C9H15NO5/c1-4-14-8(12)7(10-6(3)11)9(13)15-5-2/h7H,4-5H2,1-3H3,(H,10,11)

CAS: 1068-90-2

MF: C9H15NO5

Molecular Weight :217.22 

Product Categories: Pharmaceutical Intermediates;Other Reagents;Amino ester;ester series;Building Blocks;C8 to C9;Carbonyl Compounds;Chemical
Synthesis;Esters;Organic Building Blocks

Mol File: 1068-90-2.mol

CAS Number: 1068-90-2 

Linear Formula: CH3CONHCH(CO2C2H5)2 

Beilstein Registry Number :783883 

EC Number :213-952-9  

MDL number: MFCD00009146

mp:  95-98 °C(lit.)

bp:  185 °C20 mm Hg(lit.)

Fp:  185°C/20mm

storage temp:  Store at RT.

BRN : 783883

NIST Chemistry Reference :Propanedioic acid, (acetylamino)-, diethyl ester(1068-90-2)

EPA Substance Registry System: Propanedioic acid, (acetylamino)-, diethyl ester(1068-90-2)


2.Safety Information
Hazard Codes:Xi

Risk Statements:36-36/37/38

Safety Statements:39-36-26

WGK Germany:3

RTECS:OO0360000

HazardClass:IRRITANT

HS Code:29241900

Hazardous Substances Data:1068-90-2

2013年10月22日星期二

Tamoxifen citrate Action

Tamoxifen citrate is used to treat breast cancer that has spread to other parts of the body , to treat breast cancer in certain patients after surgery and radiation therapy, and to reduce the chances of breast cancer in high-risk patients.


1.Mechanism of action
Tamoxifen citrate  competitively binds to estrogen receptors on tumor cells and other tissue targets, producing a nuclear complex that decreases DNA synthesis and inhibits estrogen effects. It is a nonsteroidal agent with potent antiestrogenic properties which compete with estrogen for binding sites in breast and other tissues. Tamoxifen citrate  causes cells to remain in the G0 and G1 phases of the cell cycle. Because it prevents (pre)cancerous cells from dividing but does not cause cell death, Tamoxifen citrate  is cytostatic rather than cytocidal.

Tamoxifen citrate  itself is a prodrug, having relatively little affinity for its target protein, the estrogen receptor. It is metabolized in the liver by the cytochrome P450 isoform CYP2D6 and CYP3A4 into active metabolites such as 4-hydroxytamoxifen (afimoxifene) and N-desmethyl-4-hydroxytamoxifen (endoxifen) which have 30-100 times more affinity with the estrogen receptor than Tamoxifen citrate  itself. These active metabolites compete with estrogen in the body for binding to the estrogen receptor. In breast tissue, 4-hydroxytamoxifen acts as an estrogen receptor antagonist so that transcription of estrogen-responsive genes is inhibited.
Tamoxifen citrate  binds to estrogen receptor (ER) which in turn interacts with DNA. The ER/tamoxifen complex recruits other proteins known as co-repressors to stop genes being switched on by estrogen. Some of these proteins include NCoR and SMRT. Tamoxifen citrate  function can be regulated by a number of different variables including growth factors. Tamoxifen citrate  needs to block growth factor proteins such as ErbB2/HER2 because high levels of ErbB2 have been shown to occur in Tamoxifen citrate  resistant cancers. Tamoxifen citrate  seems to require a protein PAX2 for its full anticancer effect. In the presence of high PAX2 expression, the tamoxifen/estrogen receptor complex is able to suppress the expression of the pro-proliferative ERBB2 protein. In contrast, when AIB-1 expression is higher than PAX2, tamoxifen/estrogen receptor complex upregulates the expression of ERBB2 resulting in stimulation of breast cancer growth.

2.Absorption and Distribution
Following a single oral dose of 20 mg Tamoxifen citrate , an average peak plasma concentration of 40 ng/mL (range 35 to 45 ng/mL) occurred approximately 5 hours after dosing. The decline in plasma concentrations of Tamoxifen citrate  is biphasic with a terminal elimination half-life of about 5 to 7 days. The average peak plasma concentration of N-desmethyl Tamoxifen citrate  is 15 ng/mL (range 10 to 20 ng/mL). Chronic administration of 10 mg Tamoxifen citrate  given twice daily for 3 months to patients results in average steady-state plasma concentrations of 120 ng/mL (range 67-183 ng/mL) for Tamoxifen citrate  and 336 ng/mL (range 148-654 ng/mL) for N-desmethyl Tamoxifen citrate . The average steady-state plasma concentrations of Tamoxifen citrate  and N-desmethyl Tamoxifen citrate  after administration of 20 mg Tamoxifen citrate  once daily for 3 months are 122 ng/mL (range 71-183 ng/mL) and 353 ng/mL (range 152-706 ng/mL), respectively. After initiation of therapy, steady-state concentrations for Tamoxifen citrate  are achieved in about 4 weeks and steady-state concentrations for N-desmethyl Tamoxifen citrate  are achieved in about 8 weeks, suggesting a half-life of approximately 14 days for this metabolite. In a steady-state, crossover study of 10 mg Tamoxifen citrate tablets given twice a day vs. a 20 mg Tamoxifen citrate tablet given once daily, the 20 mg Tamoxifen citrate tablet was bioequivalent to the 10 mg tamoxifen citrate tablets.

3.Metabolism

Tamoxifen citrate  is extensively metabolized after oral administration. N-desmethyl Tamoxifen citrate  is the major metabolite found in patients' plasma. The biological activity of N-desmethyl Tamoxifen citrate  appears to be similar to that of Tamoxifen citrate . 4-Hydroxytamoxifen and a side chain primary alcohol derivative of Tamoxifen citrate  have been identified as minor metabolites in plasma. Tamoxifen citrate  is a substrate of cytochrome P-450 3A, 2C9 and 2D6, and an inhibitor of P-glycoprotein.

4.Excretion


Studies in women receiving 20 mg of 14C Tamoxifen citrate  have shown that approximately 65% of the administered dose was excreted from the body over a period of 2 weeks with fecal excretion as the primary route of elimination. The drug is excreted mainly as polar conjugates, with unchanged drug and unconjugated metabolites accounting for less than 30% of the total fecal radioactivity.

2013年10月21日星期一

How to get L-carnitine?

L-carnitine is a derivative of the amino acid, lysine. Its name is derived from the fact that it was first isolated from meat  in 1905. Only the L-isomer of carnitine is biologically active . L-carnitine appeared to act as a vitamin in the mealworm and was therefore termed vitamin BT . Vitamin BT, however, is actually a misnomer because humans and other higher organisms can synthesize L-carnitine . Under certain conditions, the demand for L-carnitine may exceed an individual's capacity to synthesize it, making it a conditionally essential micronutrient .


1. Endogenous Biosynthesis

Humans can synthesize L-carnitine(CAS.NO:541-15-1) from the amino acids lysine and methionine in a multi-step process. Specifically, protein-bound lysine is enzymatically methylated to form episilon-N-trimethyllysine ;  three molecules of methionine provide the methyl groups for the reaction. Epsilon-N-trimethyllysine is released for carnitine synthesis by protein hydrolysis . Several enzymes are involved in endogenous L-carnitine biosynthesis. The enzyme gamma-butyrobetaine hydroxylase, however, is absent from cardiac and skeletal muscle but highly expressed in human liver, testes, and kidney . The rate of L-carnitine biosynthesis in humans was studied in vegetarians and is estimated to be 1.2 micromol/kg of body weight/day . Changes in dietary carnitine intake or renal reabsorption do not appear to affect the rate of endogenous carnitine synthesis .

2. Absorption of Exogenous L-Carnitine

1)Dietary L-Carnitine

The bioavailability of L-carnitine from food can vary depending on dietary composition. For instance, one study reported that bioavailability of L-carnitine in individuals adapted to low-carnitine diets (i.e., vegetarians; 66%-86%) is higher than those adapted to high-carnitine diets (i.e., regular red meat eaters; 54%-72%) .

2)L-Carnitine Supplements

While bioavailability of L-carnitine from the diet is quite high , absorption from oral L-carnitine supplements is considerably lower. According to one study, bioavailability of L-carnitine from oral supplements (0.5-6 gram dosage) ranges from 14%-18% of the total dose . Less is known regarding the metabolism of the acetylated form of L-carnitine, acetyl-L-carnitine (ALCAR); however, bioavailability of ALCAR is thought to be higher than L-carnitine. The results of in vitro experiments suggest that ALCAR is partially hydrolyzed upon intestinal absorption . In humans, administration of 2 grams of ALCAR per day for 50 days increased plasma ALCAR levels by 43%, suggesting that some acetyl-L-carnitine is absorbed without hydrolysis or that L-carnitine is reacetylated in the enterocyte .
3)Elimination and Reabsorption


L-carnitine and short-chain acylcarnitines (esters of L-carnitine), such as acetyl-L-carnitine, are excreted by the kidneys. Renal reabsorption of L-carnitine is normally very efficient; in fact, an estimated 95% is thought to be reabsorbed by the kidneys . Therefore, carnitine excretion by the kidney is normally very low. However, several conditions can decrease carnitine reabsorption efficiency and, correspondingly, increase carnitine excretion. Such conditions include high-fat (low-carbohydrate) diets, high-protein diets, pregnancy, and certain disease states (see Primary Systemic Carnitine Deficiency) . In addition, when circulating L-carnitine levels increase, as in the case of oral supplementation, renal reabsorption of L-carnitine becomes saturated, resulting in increased urinary excretion of L-carnitine . Dietary or supplemental L-carnitine that is not absorbed by enterocytes is degraded by colonic bacteria to form two principal products, trimethylamine and gamma-butyrobetaine. Gamma-butyrobetaine is eliminated in the feces; trimethylamine is efficiently absorbed and metabolized to trimethylamine-N-oxide, which is excreted in the urine .

What's Sorbic acid ?

Sorbic acid is a white crystalline solid. It has a melting point of 134.5°C, a boiling point of 228°C and a pKa of 4.76.The chemistry of sorbic acid is determined by the carboxyl group and the conjugate double bonds.



Sorbic acid, or 2,4-hexadienoic acid, is a natural organic compound used as a food preservative. It has the chemical formula C6H8O2. It is a white crystalline solid that is slightly soluble in water and sublimes readily. It has a melting point of 134.5°C, a boiling point of 228°C and a pKa of 4.76. The chemistry of sorbic acid is determined by the carboxyl group and the conjugate double bonds.  It was first isolated from the unripe berries of the rowan tree (Sorbus aucuparia), hence its name.

Sorbic acid can be inactivated by oxidation and to some extent by nonionic surfactants and plastics. The activity of the sorbates may be reduced by increases in pH. Sorbic acids are relatively ineffective above a pH of 6.5.
Sorbic acid and its mineral salts, such as sodium sorbate, potassium sorbate and calcium sorbate, are antimicrobial agents often used as preservatives in food and drinks to prevent the growth of mold, yeast, and fungi. In general, the salts are preferred over the acid form because they are more soluble in water.

The un-dissociated sorbic acid molecule is responsible for the inhibitory effect of this compound. The exact mechanism of this inhibitory effect is unknown. Most scientists propose that it is not possible for food cells to develop resistance to sorbic acid. However, the break down time of sorbic acid is not known; the unknown mechanisms, expiration date, and effects of sorbic acid and its derivatives have caused concern among some people. These issues are under investigation by the scientific community.


1.Sorbic acid Chemical Properties

Product Name: Sorbic acid

Synonyms: 2-PROPENYL ACRYLIC ACID;2,4-HEXANEDIENOIC ACID;2,4-HEXADIENOIC ACID;1,3-Pentadiene-1-carboxylic acid;ACIDUM SORBICUM;(E,E) 2,4-HEXADIENOIC ACID;FEMA 3921;Hexa-2,4-dienoic acid

CAS: 110-44-1

MF: C6H8O2

MW: 112.13

EINECS: 203-768-7

mp:  132-135 °C(lit.)

bp:  228°C

density:  1,205 g/cm3

vapor pressure:  0.01 mm Hg ( 20 °C)

FEMA:  3921

Fp : 127 °C 

storage temp:2-8°C

solubility  ethanol: 0.1 g/mL, clear

Water Solubility : 1.6 g/L (20 ºC)

Merck : 14,8721

BRN : 1741831

Stability: Stability Material saturated with this acid may ignite spontaneously. Incompatible with strong oxidizing agents. May be light sensitive.

CAS DataBase Reference: 110-44-1

NIST Chemistry Reference :2,4-Hexadienoic acid, (E,E)-(110-44-1)

EPA Substance Registry System: 2,4-Hexadienoic acid, (2E,4E)-(110-44-1)


2.Safety Information
Hazard Codes : Xi

Risk Statements: 36/37/38-36/38

Safety Statements : 26-36-24/25

WGK Germany : 1

RTECS : WG2100000

F: 8

HS Code:  29161930

Hazardous Substances Data: 110-44-1

Safety: Sorbic acid may be an irritant. An allergic reaction to sorbic acid may occur if it is inhaled, ingested or in contact with the skin. Inhalation or ingestion of pure sorbic acid should be considered a medical emergency.

Sorbic acid, one preservative

Sorbic acid is a natural, organic preservative frequently used to maintain the freshness of a variety of human foods, drugs, and cosmetic products. Potassium sorbate and sorbic acid possess antifungal, and to a lesser extent antibacterial, properties.



Sorbic acid(CAS.NO:110-44-1) reacts with other chemical compounds to make what are known as derivatives. Such derivatives include calcium sorbate, potassium sorbate, and sodium sorbate.

Sorbic acid was first made by the hydrolysis of oil distilled from unripe mountain-ash berries in 1859. In 1900, the first synthesis or sorbic acid was performed by Doebner. Sorbic acid was made from crotonaldehyde and malonic acid in pyridine. The antifungal effects of sorbic acid were discovered in the 1940s. Sorbic acid was not used as an additive before that time. Food applications of sorbates expanded rapidly after the issuance of the original patents in 1945.
In the United States, sorbic acid is primarily used in a wide range of food and feed products and to a lesser in certain cosmetics, pharmaceuticals and tobacco products. Sorbic acid is used as a preservative at concentrations of up to 0.2%. Sorbic acid is commonly used in the United States to preserve products such as wines, cheeses, baked goods, fresh fruits and vegetables, and refrigerated meat. Sorbic acid is also added to pharmaceuticals and cosmetic products.

Sorbic acid is tightly regulated as a food additive in Australia, and many natural health food stores do not sell products that have been treated with this chemical compound. However, the ban is usually not extended to products treated with derivatives of sorbic acid.

Sorbic acid may be used in wines to prevent secondary fermentation of sugar and recontamination by yeast. The most common methods of application for dairy products includes dipping or spraying with potassium sorbate solutions for natural cheeses, and direct addition to processed cheeses. Sorbates are commonly used to extend the life of fish and shellfish. They inhibit the development of yeast and mold in the fish product. Sorbates are applied as a fungistat for prunes, pickles, relishes, maraschino cherries, olives, and figs and are used to extend the shelf life of prepared salads. Sorbates also preserve meat and poultry. For example, country-cured hams sprayed with sorbate solution result in no mold growth for 30 days.

The antimicrobial action of sorbic acid is primarily against yeasts and molds. It's action against bacteria appears to be selective. At concentrations used in wine it does not seem to prevent spoilage from either acetic or lactic acid bacteria. Must and wine related yeasts inhibited by sorbic acid include species of genera Brettanomyces, Candida, Hansenula, Pichia, Saccharomyces, Torulaspora, and Zygosaccharomyces.


The inhibitory effect of sorbic acid on yeast strains is not uniform. Certain species are more tolerant than others. For example, according to Pitt (1974), Zygosaccharomyces bailii was not inhibited by sorbic acid at 0.06% in 10% glucose. It should be noted that the yeast Zygosaccharomyces bailii is also resistant to sulfur dioxide and diethyl pyrocarbonic acid (DEPC) and it can ferment high sugar musts such as grape juice  concentrate containing 55 to 72 percent sugar. If contaminated concentrate is used for sweetening wine, it is likely to cause a refermentation even if a normal concentration of sorbic acid is present.

2013年10月19日星期六

Application of Sorbic acid

Sorbic acid (2,4-hexadienoic acid) is a straight chain unsaturated fatty acid with a molecular weight of 112.13 and the formula: CH3 - CH = CH - CH = CH - COOH. Sorbic acid is commercially produced as a powder or granules, it has a characteristic acrid odor and acid taste. The carboxyl (COOH) group in sorbic acid is very reactive and can form salts with calcium, sodium, and potassium. The potassium salt of sorbic acid is commercially available as a powder or granules. Its molecular weight is 150.22 and it is very soluble in water.
           

Potassium sorbate is used in the production of sweet white table wines. Although BATF permits its use in wine, up to 300 ppm, it is important to remember that its taste threshold is well below the legal limit. The taste threshold for experienced tasters has been reported to be about 130 ppm. Addition of sorbic acid often results in the formation of ethyl sorbate, which is said to impart an unpleasant odor when present in a significant level.

Sorbic acid(CAS.NO:110-44-1) also inhibits mold growth. Some of the important species that are suppressed by sorbic acid belong to the genera Alternaria, Botrytis ,  Cladosporiwn,  Fusariwn , Mucor, Penicilliwn, Rhizopus, Trichoderma. Mold can be a problem in wine cellars. To control mold in the wine cellar, sorbic acid could be included in the antimicrobial compounds used for sanitizing.
Several microorganisms can metabolize sorbic acid particularly when it is present in small concentrations. For this reason, it is not a suitable preservative in foods with high microbial counts. To derive the maximum benefit from the antimicrobial action of sorbic acid, it is important to clean the wine well and keep the microbial count low in the bottled wine. It should be emphasized that sorbic acid inhibits yeast and mold, but not acetic and lactic acid bacteria. In fact, lactic acid bacteria can metabolize sorbic acid and produce off flavored compounds.

The antimicrobial action of sorbic acid is due to its inhibitory influence on various enzymes in the microbial cell. The enzymes inhibited by sorbic acid include the following:

1. Enzymes involved in carbohydrate metabolism such as enolase and lactate dehydrogenase.

2. Enzymes of citric acid cycles such as malate dehydrogenase, isocitrate dehydrogenase, ketoglutarate dehydrogenase, succinate dehydrogenase, and fumerase.

3. Several enzymes containing SH group, and other enzymes such as catalase and peroxidase.

The key points in sorbic acid use are summarized below.

1. Potassium sorbate (most soluble form of sorbic acid) should be used. However, this can cause bitartrate precipition problems.

2. The solubility of potassium sorbate is influenced by temperature, therefore, it should not be added to a cold wine.

3. Wine should be mixed well after sorbate addition.

4. Sorbate should be used in conjunction with sulfur dioxide.

5. Certain yeast and bacteria are not inhibited by sorbic acid.

6. Properly clarified wine (low yeast count), low pH, and relatively high alcohol would help in reducing the amount of sorbic acid needed for effectively controlling yeast.

7. Sorbic acid addition should never be considered as a substitute for poor sanitation. Calculating Potassium Sorbate Additions Sorbic acid is added to a wine in the form of the potassium salt. Potassium sorbate contains 73.97% sorbic acid. In order to calculate the amount of potassium sorbate, the following formula should be used.

Phosphorous acid Application

Maybe everyone of us have heard of the compounds of Phosphorous acid,It also has widely application in many spects,Next let’s learn some application of it.


1.Rust removal

Phosphoric acid(CAS.NO:13598-36-2) may be used by direct application to rusted iron, steel tools or surfaces to convert iron(III) oxide (rust) to a water soluble phosphate compound. It is usually available as a greenish liquid, suitable for dipping (acid bath), but is more generally used as a component in a gel, commonly called Naval jelly. As a thick gel, it may be applied to sloping, vertical, or even overhead surfaces. Care must be taken to avoid acid burns of the skin and especially the eyes, but the residue is easily diluted with water. When sufficiently diluted it can even be nutritious to plant life, containing the essential nutrients phosphorus and iron. It is sometimes sold under other names, such as "rust remover" or "rust killer." It should not be directly introduced into surface water such as creeks or into drains, however. After treatment, the reddish-brown iron oxide will be converted to a black iron phosphate compound coating that may be scrubbed off. Multiple applications of phosphoric acid may be required to remove all rust. The resultant black compound can provide further corrosion resistance (such protection is somewhat provided by the superficially similar Parkerizing and blued electrochemical conversion coating processes.) After application and removal of rust using phosphoric acid compounds, the metal should be oiled (if to be used bare, as in a tool) or appropriately painted, most durably by using a multiple coat process of primer, intermediate, and finish coats.

2.Processed food use

It is also used to acidify foods and beverages such as various colas, but not without controversy as to its health effects. It provides a tangy taste, and being a mass-produced chemical, is available cheaply and in large quantities. The low cost and bulk availability is unlike more expensive natural seasonings that give comparable flavors, such as ginger for tangyness, or citric acid for sourness, obtainable from lemons and limes. (However most citric acid in the food industry is not extracted from citrus fruit, but fermented by Aspergillus niger mold from scrap molasses, waste starch hydrolysates and phosphoric acid.) It is labeled as E number E338.

3.Medical use

Phosphoric acid is used in dentistry and orthodontics as an etching solution, to clean and roughen the surfaces of teeth where dental appliances or fillings will be placed. Phosphoric acid is also an ingredient in over the counter anti-nausea medications which also contain high levels of sugar (glucose and fructose). It should not be used by diabetics without consultation with a doctor. Phosphoric acid is also used as a catalyst in the synthesis of aspirin because it provides a larger number of hydrogen ions with less contamination when compared to hydrochloric acid and sulfuric acid.Preparation of hydrogen halides
Phosphoric acid reacts with halides to form the corresponding hydrogen halide gas
(steamy fumes are observed on warming the reaction mixture).

4.Other applications

1)Orthophosphoric acid is used as the electrolyte in phosphoric-acid fuel cells.

2)It is used as an external standard for phosphorus-31 NMR.

3)It is used as a cleaner by construction trades to remove mineral deposits, cementitious smears, and hard water stains. It is also used as an ingredient in some household cleaners aimed at similar cleaning tasks.

4)Hot phosphoric acid is used in microfabrication to etch silicon nitride (Si3N4). It is highly selective in etching Si3N4 instead of SiO2, silicon dioxide.

5)Phosphoric acid is used as a flux by hobbyists (such as model railroaders) as an aid to soldering.

6)Phosphoric acid is also used in hydroponics to lower the pH of nutrient solutions. While other types of acids can be used, phosphorus is a nutrient used by plants, especially during flowering, making phosphoric acid particularly desirable. General Hydroponics pH Down liquid solution contains phosphoric acid in addition to citric acid and ammonium bisulfate with buffers to maintain a stable pH in the nutrient reservoir.

7)Phosphoric acid is used as a pH adjuster in cosmetics and skin care products.


8)Phosphoric acid is used as an chemical oxidizing agent for activated carbon production.

Phosphorous Acid Fungicides and Nutritional Value

Recently, a number of new fungicides that have phosphorous acid as the active ingredient have come on the market. Other names that you might hear for this are “phosphonates” or “phosphates.” Examples are ProPhyt, Phostrol, and Agri-Fos. Aliette (fosetyl-A1), an older fungicide, is the prototype for this group of fungicides. However, the long standing patent on Aliette had prevented similar fungicides from being developed up to recently.



Phosphorus-containing substances occur naturally (0.1%-0.5%) in foods such as milk, meat, poultry, fish, nuts, and egg yolks.
Phosphorous acid(CAS.NO:13598-36-2) should not be confused with phosphoric acid or phosphorous (P), a fertilizer component. In fertilizers, P is normally found in the form of phosphoric acid (H3PO4), which readily disassociates to release hydrogen phosphate (HPO42) and dihydrogen phosphate (H2PO4-). Both of these ions may be taken up by the plant and are mobile once inside the plant. Phosphorous acid is H3PO3. A single letter difference in the name of a chemical compound can make a major difference in its  properties. Phosphorous acid releases the phosphonate ion (HPO32-; also called phosphite) upon disassociation. Phosphonate is easily taken up and translocated inside the plant. Phosphorous acid does not get converted into phosphate, which is the primary  source of P for plants.


While growers are familiar with phosphorus-containing fertilizer, the abundance of terms, which are deceptively similar (such as phosphoric acid and phosphorous acid), may create some confusion on the actual content and efficacy of these products. . Some claims found in commercial literature and product descriptions refer to phosphorous acid as a “supplemental fertilizer,” while others present it as a fungicide. The purpose of this article is to explain what phosphorous acid actually is and to examine its fungicidal activity and nutritional value.
Phosphorus (abbreviated P) is one of the essential elements for normal growth and development of plants. In fertilizers, it is normally found in the form of phosphoric acid (H3PO4) (Table 1), which readily disassociates to release hydrogen phosphate (HPO42-) and dihydrogen phosphate (H2PO4-). Both of these ions may be taken up by the plant but H2PO4- more readily. Once inside the plant, both ions are mobile.


Because phosphorous acid and its derivatives do not get metabolized in plants, they are fairly stable and probably contribute little or nothing to P nutritional needs of the plants. Some researchers have investigated the ability of phosphorous acid to act as a nutrient source for plant growth and found that P-deficiency symptoms developed with phosphorous acid as a sole source of P. This means that although phosphorous acid can control diseases it is not a substitute for P fertilization. The inverse is also true: phosphate is an excellent source of P for plant growth, but is unable to control diseases other than improving the general health of the crop. So applying high amounts of P fertilizer will not work as a disease control measurer.


Researchers have found that phosphorous acid fungicides are especially effective against Oomycete pathogens, such as Phytophthora, Phythium, and Downy mildews in a number of crops. Phosphorous acid has both a direct and indirect effect on these pathogens. It inhibits a particular process (oxidative phosphorylation). In addition, some evidence suggests that phosphorous acid has an indirect effect by stimulating the plants natural defense response against pathogen attack. This probably explains the much broader spectrum of activity observed in fungicide efficacy trials in small fruit crops in Michigan.



According to the Center for Science in the Public Interest (CSPI), a consumer watchdog group not affiliated with the food industry, only a small fraction of the phosphate in the American diet comes from additives in soft drinks. Most comes from meat and dairy products. So your reason for not drinking Coke should be its sugar content and artificial food colorings, not the phosphoric acid.

2013年10月18日星期五

Atorvastatin calcium interactions and action

Atorvastatin calcium is a member of the drug class known as statins, used for lowering blood cholesterol. It also stabilizes plaque and prevents strokes through anti-inflammation and other mechanisms. Like all statins, Atorvastatin calcium works by inhibiting HMG-CoA reductase, an enzyme found in liver tissue that plays a key role in production of cholesterol in the body.


As with other statins, Atorvastatin calcium is a competitive inhibitor of HMG-CoA reductase. Unlike most others, however, it is a completely synthetic compound. HMG-CoA reductase catalyzes the reduction of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate, which is the rate-limiting step in hepatic cholesterol biosynthesis.

Inhibition of the enzyme decreases de novo cholesterol synthesis, increasing expression of low-density lipoprotein receptors (LDL receptors) on hepatocytes. This increases LDL uptake by the hepatocytes, decreasing the amount of LDL-cholesterol in the blood. Like other statins, Atorvastatin calcium also reduces blood levels of triglycerides and slightly increases levels of HDL-cholesterol.

In clinical trials, drugs that block cholesterol uptake like ezetimibe combine with and complement those that block biosynthesis like Atorvastatin calcium or simvastatin in lowering cholesterol or targeting levels of LDL.

Interactions with clofibrate, fenofibrate, gemfibrozil, which are fibrates used in accessory therapy in many forms of hypercholesterolemia, usually in combination with statins, increase the risk of myopathy and rhabdomyolysis.

Co-administration of Atorvastatin calcium with one of CYP3A4 inhibitors such as itraconazole, telithromycin, and voriconazole, may increase serum concentrations of Atorvastatin calcium, which may lead to adverse reactions. This is less likely to happen with other CYP3A4 inhibitors such as diltiazem, erythromycin, fluconazole, ketoconazole, clarithromycin, cyclosporine, protease inhibitors, or verapamil, and only rarely with other CYP3A4 inhibitors, such as amiodarone and aprepitant. Often, bosentan, fosphenytoin, and phenytoin, which are CYP3A4 inducers, can decrease the plasma concentrations of Atorvastatin calcium. Only rarely, though, barbiturates, carbamazepine, efavirenz, nevirapine, oxcarbazepine, rifampin, and rifamycin, which are also CYP3A4 inducers, can decrease the plasma concentrations of Atorvastatin calcium. Oral contraceptives increased AUC values for norethindrone and ethinyl estradiol; these increases should be considered when selecting an oral contraceptive for a woman taking Atorvastatin calcium.

Antacids can rarely decrease the plasma concentrations of Atorvastatin calcium, but do not affect the LDL-C-lowering efficacy.

Niacin also is proved to increase the risk of myopathy or rhabdomyolysis.
Statins may also alter the concentrations of other drugs, such as warfarin or digoxin, leading to alterations in effect or a requirement for clinical monitoring.

Vitamin D supplementation lowers Atorvastatin calcium and active metabolite concentrations, yet synergistically reduces LDL and total cholesterol concentrations. Grapefruit juice components are known inhibitors of intestinal CYP3A4. Co-administration of grapefruit juice with Atorvastatin calcium may cause an increase in Cmax and AUC, which can lead to adverse reactions or overdose toxicity.

Atorvastatin calcium interactions and action

Atorvastatin calcium is a member of the drug class known as statins, used for lowering blood cholesterol. It also stabilizes plaque and prevents strokes through anti-inflammation and other mechanisms. Like all statins, Atorvastatin calcium works by inhibiting HMG-CoA reductase, an enzyme found in liver tissue that plays a key role in production of cholesterol in the body.


As with other statins, Atorvastatin calcium is a competitive inhibitor of HMG-CoA reductase. Unlike most others, however, it is a completely synthetic compound. HMG-CoA reductase catalyzes the reduction of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate, which is the rate-limiting step in hepatic cholesterol biosynthesis.

Inhibition of the enzyme decreases de novo cholesterol synthesis, increasing expression of low-density lipoprotein receptors (LDL receptors) on hepatocytes. This increases LDL uptake by the hepatocytes, decreasing the amount of LDL-cholesterol in the blood. Like other statins, Atorvastatin calcium also reduces blood levels of triglycerides and slightly increases levels of HDL-cholesterol.

In clinical trials, drugs that block cholesterol uptake like ezetimibe combine with and complement those that block biosynthesis like Atorvastatin calcium or simvastatin in lowering cholesterol or targeting levels of LDL.

Interactions with clofibrate, fenofibrate, gemfibrozil, which are fibrates used in accessory therapy in many forms of hypercholesterolemia, usually in combination with statins, increase the risk of myopathy and rhabdomyolysis.

Co-administration of Atorvastatin calcium with one of CYP3A4 inhibitors such as itraconazole, telithromycin, and voriconazole, may increase serum concentrations of Atorvastatin calcium, which may lead to adverse reactions. This is less likely to happen with other CYP3A4 inhibitors such as diltiazem, erythromycin, fluconazole, ketoconazole, clarithromycin, cyclosporine, protease inhibitors, or verapamil, and only rarely with other CYP3A4 inhibitors, such as amiodarone and aprepitant. Often, bosentan, fosphenytoin, and phenytoin, which are CYP3A4 inducers, can decrease the plasma concentrations of Atorvastatin calcium. Only rarely, though, barbiturates, carbamazepine, efavirenz, nevirapine, oxcarbazepine, rifampin, and rifamycin, which are also CYP3A4 inducers, can decrease the plasma concentrations of Atorvastatin calcium. Oral contraceptives increased AUC values for norethindrone and ethinyl estradiol; these increases should be considered when selecting an oral contraceptive for a woman taking Atorvastatin calcium.

Antacids can rarely decrease the plasma concentrations of Atorvastatin calcium, but do not affect the LDL-C-lowering efficacy.

Niacin also is proved to increase the risk of myopathy or rhabdomyolysis.
Statins may also alter the concentrations of other drugs, such as warfarin or digoxin, leading to alterations in effect or a requirement for clinical monitoring.

Vitamin D supplementation lowers Atorvastatin calcium and active metabolite concentrations, yet synergistically reduces LDL and total cholesterol concentrations. Grapefruit juice components are known inhibitors of intestinal CYP3A4. Co-administration of grapefruit juice with Atorvastatin calcium may cause an increase in Cmax and AUC, which can lead to adverse reactions or overdose toxicity.

Androsta-1,4-dien-3-one,17-[(1-oxo-10-undecenyl)oxy]-, (17b)-



Name:Androsta-1,4-dien-3-one,17-[(1-oxo-10-undecenyl)oxy]-, (17b)-

EINECS:236-024-5

Molecular Formula:C30H44O3

CAS Registry Number:13103-34-9

Molecular Structure:



Superlist Name:Boldenone undecylenate

Molecular Weight:452.67

Synonyms:Androsta-1,4-dien-3-one,17b-hydroxy-, 10-undecenoate(7CI,8CI);10-Undecenoic acid, ester with 17b-hydroxyandrosta-1,4-dien-3-one
(8CI);Ba 29038;Ba9038;Boldefarm;Boldenone 10-undecenoate;Equipoise;Parenabol;Vebonol;

Flash Point:232.2 °C

Appearance:Light yellow oily matter

Molecular Weight:452.6686

Density:1.055g/cm3

Boiling Point:553.243°C at 760 mmHg

Flash Point:232.215°C

Refractive index:1.537

Phthalic anhydride

Phthalic anhydride is the anhydride of phthalic acid. This colorless solid is an important industrial chemical, especially for the large–scale production of plasticizers for plastics. It is presently obtained by catalytic oxidation of ortho–xylene or naphthalene. Phthalic anhydride can also be prepared from phthalic acid.


It is a white, crystalline, slightly water-soluble solid, C8H4O3, used chiefly in the manufacture of dyes, alkyd resins, and plasticizers.

Phthalic anhydride(CAS.NO:85-44-9) is a versatile intermediate in organic chemistry,It is used in the production of unsaturated polyester resins and alkyd resins used in the coatings industry.  in part because it is bifunctional and readily available. The primary use of phthalic anhydride (PA) is as a chemical intermediate in the production of plasticizers from polyvinyl chloride (PVC).
Phthalic anhydride is a versatile intermediate in organic chemistry, in part because it is bifunctional and cheaply available. It undergoes hydrolysis and alcoholysis. Hydrolysis by hot water forms ortho-phthalic acid. This process is reversible: Phthalic anhydride re-forms upon heating the acid above 180 °C. Hydrolysis of anhydrides is not typically a reversible process. However, phthalic acid is easily dehydrated to form phthalic anhydride due to the creation of a thermodynamically favorable 5-membered ring.

Phthalic anhydride reacted with cellulose acetate forms cellulose acetate phthalate (CAP), a common enteric coating excipient that has also been shown to have antiviral activity.Phthalic anhydride is a degradation product of CAP.

Phthalic anhydride is the catalyst for oxidation and dehydrogenation.


It's colourless, aromatic chemical solid, which forms needle shaped crystals. The chemical starts to solve at a temperature of 131°degrees and changes over to gas state at 256° degrees. The majority of phthalic anhydride is used for the production and plasticizers, especially PVC. As an important synthetic resign resource the chemical bond is utilized for the surface coating of wood, for the manufacture of copper phthalocyanine in the beta crystalline form and synthetic resin. The chemical bond of phthalic anhydride is also only an important chemical component for producing colorants. Colour pigments produced with phthalic anhydride are remanufactured in dispersions, artistic colour or in finish.

What's Adefovir dipivoxil?

Adefovir dipivoxil's tradename is hepsera, a diester prodrug of adefovir. Adefovir is an acyclic nucleotide analog with activity against human hepatitis B virus (HBV).

The chemical name of adefovir dipivoxil is 9-[2-[[bis[(pivaloyloxy)methoxy]-phosphinyl]methoxy]ethyl]adenine. It has a molecular formula of C20H32N5O8P, a molecular weight of 501.48.


Adefovir dipivoxil (CAS.NO:142340 -99- 6) is a white to off-white crystalline powder with an aqueous solubility of 19 mg/mL at pH 2.0 and 0.4 mg/mL at pH 7.2. It has an octanol/aqueous phosphate buffer (pH 7) partition coefficient (log p) of 1.91.

Adefovir dipivoxil tablets are for oral administration. Each tablet contains 10 mg of adefovir dipivoxil and the following inactive ingredients: croscarmellose sodium, lactose monohydrate, magnesium stearate, pregelatinized starch, and talc.

This medication is used to treat a chronic viral infection of the liver (hepatitis B) in people 12 years of age and older. It works by slowing the growth of the virus. It is not a cure for hepatitis B and does not prevent the passing of hepatitis B to others. This medication is a nucleotide analog.


Name:Adefovir dipivoxil

EINECS:200-001-8

Molecular Formula:C20H32N5O8P

CAS Registry Number:142340-99-6

Molecular Weight:501.48

Density:1.35 g/cm3

Boiling Point:641 °C at 760 mmHg

Melting Point:98-102℃

Flash Point:641 °C at 760 mmHg

Storage Temperature:20°C

Refractive index:1.569

Merck  14,151

Hazard Codes  Xn

Risk Statements  20/21/22

Safety Statements  36/37

Gabapentin hydrochloride

Gabapentin hydrochloride is a White Crystalline Solid. It  is used as conventional anti-epileptic drugs, for who can not be satisfied with control or can not tolerate the limitations of seizures in patients with epilepsy, as well as additional treatment with the limitations, subsequently the body-oriented attack in patients with epilepsy.


1. Uses

Gabapentin hydrochloride(CAS.NO:60142-96-3) is used primarily to treat seizures, neuropathic pain, including concussions, and hot flashes.

2. Biological Activity

Anticonvulsant with several possible mechanisms of action. Increases GABA in the brain and binds to a novel site associated with voltage-sensitive Ca 2  channels. Prevents neuronal death and is antinociceptive and anxiolytic.

3. Mechanism of action

Gabapentin hydrochloride interacts with voltage-sensitive calcium channels in cortical neurons. Gabapentin hydrochloride increases the synaptic concentration of GABA, enhances GABA responses at non-synaptic sites in neuronal tissues, and reduces the release of mono-amine neurotransmitters. One of the mechanisms implicated in this effect of Gabapentin hydrochloride is the reduction of the axon excitability measured as an amplitude change of the presynaptic fibre volley (FV) in the CA1 area of the hippocampus. This is mediated through its binding to presynaptic NMDA receptors. Other studies have shown that the antihyperalgesic and antiallodynic effects of Gabapentin hydrochloride are mediated by the descending noradrenergic system, resulting in the activation of spinal alpha2-adrenergic receptors. Gabapentin hydrochloride has also been shown to bind and activate the adenosine A1 receptor.

3.Side effect

Get emergency medical help if you have any of these signs of an allergic reaction to Gabapentin hydrochloride: hives; fever; swollen glands; painful sores in or around your eyes or mouth; difficulty breathing; swelling of your face, lips, tongue, or throat.


Common Gabapentin hydrochloride side effects may include:

dizziness, drowsiness;

dry mouth, blurred vision;

headache;

diarrhea; or

swelling in your hands or feet.

2013年10月17日星期四

Something about D-Ribose

D-ribose is a simple sugar which has been used to help improve energy and muscle support. D- Ribose provides cellular energy to the body which is the source of power that all the body’s cells need to function and perform cellular repair effectively. D-ribose helps to fine tune the body to function at its optimum level providing the body’s muscles and cells with sustained energy and also helping them recover faster. Many customers such as chronic fatigue syndrome ME sufferers find their energy levels are higher and can function in daily life more efficient. Bodybuilders, sports professionals and athletes can benefit in their physical exercise and work outs as the muscles will fatigue at a slower rate in turn the performance in energy levels are more efficient and can improve performance and endurance.


1.D-Ribose Dosage


D-Ribose is typically well tolerated. Patients with decreased exercise ability due to a weakened heart could also consider D-Ribose. As a supplement, it is typically comes as a powder to mix in water or juice. The dosage is 5 g taken 3 times a day, for 3-4 weeks. After this time, patients can try going to the same dose twice a day, maintaining the amount that keeps the improvement in symptoms. No major interactions for D-ribose are known, and side effects are limited to minor GI disturbance in some.

2.D-Ribose in Your Diet


D-Ribose is naturally present in foods but only in very small amounts. Red meat is at the top of the list but the amount is insignificant. Dr Stephen Sinatra in his book ‘Metabolic Cardiology’ says “The dietary intake of D-Ribose is insufficient to provide any nutritional support, especially to those people suffering heart disease, neuromuscular disease and those hoping to recover quickly after exercise”.

Foods don't actually contain free d-ribose, so supplementation is the typical way to increase d-ribose levels. Your body uses vitamin B-12 to produce it, so a B-12 deficiency could contribute to a d-ribose deficiency. However, supplementation is the typical way to increase d-ribose levels.

3.Side Effects of D-Ribose


Side effects of d-ribose may include:

1)Digestive problems, such as nausea, stomach ache and diarrhea

2)Headache

3)Low blood sugar (not recommended for diabetics because it can lower blood sugar too much when combined with medications)

4)D-ribose is generally considered safe for short-term use. So far, we don't have much safety information about long-term use or use during
pregnancy and breast feeding.

D-Ribose Properties

What is d-ribose? D-ribose is a naturally occurring sugar that's showing promise as a natural energy stimulator. It's been shown to increase cellular levels of an energy producing substance known as ATP in both muscle cells and heart cells in the human body. ATP is considered to be the primary source of energy for the living cell. While intuitively it would make sense that ribose supplements would increase energy levels since they alter cellular levels of ATP.
 
Name:D-Ribose

EINECS:200-059-4

Molecular Formula:C5H10O5

CAS Registry Number:
50-69-1

Appearance:white to off-white crystalline powder

Molecular Weight:150.13

Density:1.681 g/cm3

Boiling Point:375.4 °C at 760 mmHg

Melting Point:88-92

Flash Point:180.8 °C

Alpha:-20.8 o (C=4, H2O)

Refractive index:1.612

Solubility:Appearance:white to off-white crystalline powder

Transport Information:HAZARD

Hazard Symbols:UN NO.

Deleted CAS:93781-19-2

Usage: It is produced by microorganism fermentation of glucose in a fermentation culture medium without adding calcium carbonate.

Uses:


D-ribose is a simple sugar which has been used to help improve energy and muscle support. D- Ribose provides cellular energy to the body which is the source of power that all the body’s cells need to function and perform cellular repair effectively. D-ribose helps to fine tune the body to function at its optimum level providing the body’s muscles and cells with sustained energy and also helping them recover faster.

Have you ever heard of D-Ribose?

For many people this may have been the first time they have heard of D-Ribose.Just like me.Then let's see what's D-Ribose next.

So what is D-Ribose (chemical name – alpha-D-ribofuranose)? It’s a simple 5 carbon sugar (glucose is a 6 carbon sugar) that is found in every cell in the human body. D-Ribose is a vital nutrient with a very significant role to play. Unlike sugars such as glucose which are metabolised to contribute to energy turnover – D-Ribose is not ‘burned’ for energy but is conserved by the cell for rebuilding the energy pool. It’s the only compound used by the body to manage cellular energy restoration.

D-ribose(CAS.NO:50-69-1), also called ribose or Beta-D-ribofuranose, is a type of sugar that your body produces naturally. It helps produce energy in the form of ATP (adenosine triphosphate.) Medicinally, it's most often used to increase muscle energy and improve exercise performance.
When we consume D-Ribose, the body recognizes that it is different from other sugars and preserves it for the vital work of actually making the energy molecule (ATP) that powers our hearts, muscles, brains, and every other tissue in the body. ATP (Adenosine Triphosphate) is the energy ‘currency’ of the cell and D-Ribose provides the key building block for ATP. Without sufficient D-Ribose the cell cannot make ATP.

In some illnesses, D-ribose is used to help improve exercise tolerance or prevent post-exercise pain, cramping and stiffness. Some evidence suggests that it's effective in people with conditions that impair the body's ability to produce energy. In people with heart disease, it may also help get energy to the heart during exercise.


D-ribose is a simple sugar which has been used to help improve energy and muscle support. D- Ribose provides cellular energy to the body which is the source of power that all the body’s cells need to function and perform cellular repair effectively. D-ribose helps to fine tune the body to function at its optimum level providing the body’s muscles and cells with sustained energy and also helping them recover faster. Many customers such as chronic fatigue syndrome ME sufferers find their energy levels are higher and can function in daily life more efficient. Bodybuilders, sports professionals and athletes can benefit in their physical exercise and work outs as the muscles will fatigue at a slower rate in turn the performance in energy levels are more efficient and can improve performance and endurance.

Is methenamine a prescription medication?

Methenamine is a heterocyclic organic compound with the formula (CH2)6N4. This white crystalline compound is highly soluble in water and polar organic solvents. It has a cage-like structure similar to adamantane. It is useful in the synthesis of other chemical compounds, e.g. plastics, pharmaceuticals, rubber additives. It sublimes in a vacuum at 280 °C. The compound was discovered by Aleksandr Butlerov in 1859.


A prescription drug (also prescription medication or prescription medicine) is a licensed medicine that is regulated by legislation to require a medical prescription before it can be obtained.
Methenamine has an FDA labeled indication for the treatment or prevention of recurrent urinary tract infections or urinary tract discomfort.  This medication is considered an antibiotic and works by forming compounds in the body, more specifically in the urine, to suppress bacterial growth and increase urine acidity to help get rid of bacteria causing the UTI.

Methenamine is considered a prescription medication, but at much higher doses than what is contained in OTC products.  For example, methenamine used in a hospital setting or as a prescription medication has a dosage of 1 gram, two to four times daily.  In an OTC product, such as Cystex(containing aspirin, benzocaine, and methenamine), the dosage is equivalent to 162.5 milligrams of methenamine four times a day.  So, the amount of methenamine in over-the-counter products is less than the amount in a prescription from a physician. 
In conclusion, methenamine could be viewed as a prescription medication or an OTC medication.  Large doses (usually 1gram or more) of the medication are considered prescription only, whereas low doses of methenamine (usually 160-170 milligrams) are considered an OTC product and do not require a prescription. Although this medication is an antibiotic used for the treatment of urinary tract infections, an OTC medication containing methenamine will not cure a UTI.  The low dose of methenamine contained in OTC medications is solely used to help prevent the progression of infection until you can see a doctor.


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