Pharmaceutical Bulk Tauroursodeoxycholic Acid Powder

CAS:14605-22-2

MF: C26H45NO6S

MW:499.7

EINECS:1308068-626-2

Specification: 99% min Tauroursodeoxycholic Acid Powder

Sample: Tauroursodeoxycholic Acid Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Tauroursodeoxycholic Acid Powder Usage and Synthesis.

Tauroursodeoxycholate(TUDCA) suppressesbothviabilityandmigrationofvascularsmoothmusclecells(VSMCs)throughinhibitionofERKphosphorylation,byinductionofmitogen-activatedproteinkinasephosphatase-1(MKP-1)viaPKCα.TauroursodeoxycholateinhibitsboththeproliferationandmigrationofVSMCsviainhibitionofERK,throughCa2+-dependentPChemicalbookKCαtranslocation.Tauroursodeoxycholatepreventsplatelet-derivedgrowthfactor(PDGF)andvascularinjury-inducedMMP-9expression.Theknock-downofMKP-1usingspecificsi-RNArestoresthereducedVSMCviabilitybyTauroursodeoxycholate(200μM),whichsuggeststhatanti-proliferativeeffectofTauroursodeoxycholatedependedontheMKP-1expression.

Uses and functions of Tauroursodeoxycholic Acid.

Tauroursodeoxycholic acid has the functions of spasmolytic, anticonvulsive, anti-inflammatory and cholelithiolytic. It is mainly used in the treatment of gallbladder cholesterol stones, primary sclerosing cholangitis, primary biliary cirrhosis and chronic hepatitis C.

Pharmacological Effects of Tauroursodeoxycholic Acid .

Tauroursodeoxycholic acid sodium, also known as tauroursodeoxycholic acid, taurodeoxycholic acid, chemical name 3a, 7β dihydroxycholanyl-n-taurine, mainly exists in black bear bile, is a symbolic active ingredient in bear bile. It can relieve spasmodic, anticonvulsant, anti-inflammatory and cholelithiolysis.The modern synthetic drug taurodeoxycholic acid is a binding bile acid formed from the shrinkage between the fusio group of ursodeoxycholic acid and the amino group of taurine. Taurodeoxycholic acid capsules have been listed abroad and were approved for sale in China as imported drugs in 2007. They are mainly used in the treatment of gallbladder cholesterol stones, primary sclerosing cholangitis, primary biliary cirrhosis and chronic viral hepatitis C. At present, taurodeoxycholic acid apis and their preparations have not been registered in China.Ursodeoxycholate sodium is a natural bile acid separated from energy bile, is a chemical preparation, in the body and taurine combined in bile, is a hydrophilic bile acid, a cholesterol stone dissolving agent. It can reduce the liver's secretion of cholesterol, reduce the saturation of cholesterol in bile, promote the secretion of bile acid, increase the solubility of cholesterol in bile, dissolve cholesterol stones or prevent the formation of stones. It can increase the volume of bile secretion, relax the sphincter of bile duct and produce cholelitic effect, which is conducive to the discharge of stones. This product does not dissolve other types of gallstones. It is suitable for the treatment of cholesterol lithiasis, hyperlipidemia, biliary dysplasia, primary biliary cirrhosis, chronic hepatitis, bile reflux gastritis and prevention of acute rejection and reaction of liver transplantation. The stone dissolving effect of this product is slightly weaker than that of goodeoxycholic acid.

Preparation method of Bulk Tauroursodeoxycholic Acid Powder.

1) The preparation of taurodeoxycholic acid crude is carried out according to the following steps:In the reactor, 4.0KG ursodeoxycholic acid was added, 19KG acetone was added, 1650ml triethylamine was added after stirring, the jacket refrigeration was opened, and the temperature of the mixture was reduced to -10℃. Add 1120ml ethyl chloroformate, control the addition rate of ethyl chloroformate, so that the temperature of the reaction liquid is maintained between -5-0℃, after 30 minutes, continue to maintain the temperature and stir reaction for 40 minutes, to obtain the mixed anhydride of ursodeoxycholic acid and ethyl chloroformate. The reaction liquid of the mixed anhydride is filtered through the filter with nitrogen pressure to contain 4.2KG purified water. 1.4KG taurine and 0.4KG sodium hydroxide were mixed in a 50-liter reactor for 3 hours to further prepare 4.0KG tauroursodeoxycholic acid crude.2) The refining of taurodeoxycholic acid crude is carried out according to the following steps:(1) Put 4.0KG taurursodeoxycholic acid into a 50L reactor, add 4KG water and 580ml acetone, heat and stir until completely dissolved;(2) stirring and cooling to -5-0° C, crystallization for 30 hours;(3) Put the material into the filter and drain it, wash the filter cake with ice water (-3-0℃) and drain it again to obtain 3.3KG taurodeoxycholic acid (purity 99.6%, HPLC), of which the content of taurodeoxycholic acid was 0.3% and the maximum content of other impurities was 0.05%(liquid chromatography).