Preparation method of bezoar ursodesoxycholic acid preparation

Abstract

The invention discloses a preparation method of bezoar ursodesoxycholic acid preparation. The preparation method of the bezoar ursodesoxycholic acid preparation comprises the following steps: sieving a bezoar ursodesoxycholic acid raw material and an auxiliary material for later use, wherein particle size distribution D90 of the raw material is required to be less than 150 microns, and the particle size distribution D90 of the auxiliary material is required to be less than 120 microns; mixing bezoar ursodesoxycholic acid, a diluent and a disintegrating agent, collecting a material accounting for about 10-15% of production lot size to be taken as (a) for later use; adding a lubricating agent accounting for 85-90% of the production lot size, mixing, and collecting material taken as (b) for later use; carrying out dry granulation on the material (b); straightening the material obtained in the step 3, sieving, mixing the sieved material with the material (a), carrying out dry granulation on the mixed material, and then straightening and sieving; adding the material obtained in the step 4 into the rest lubricating agent, mixing, and collecting a material; and preparing the preparation by adopting the material obtained in the step 5. The preparation method of the bezoar ursodesoxycholic acid preparation has the advantages that the problem of material fluidity can be solved and the phenomenon that no initial burst release of the bezoar ursodesoxycholic acid preparation is caused under the specified dissolution condition can be avoided.

Description

technical field [0001] The invention relates to a preparation method of a tauroursodeoxycholic acid preparation, which belongs to the field of pharmaceutical preparations. Background technique [0002] The chemical name of tauroursodeoxycholic acid (TUDCA) is 3α, 7β-dihydroxycholanoyl-N-taurine, which is formed by shrinking between the carboxyl group of ursodeoxycholic acid (UDCA) and the amino group of taurine. Conjugated bile acids. TUDCA was discovered in bear bile in 1902. It is the main bile acid in bear bile and has antispasmodic, anticonvulsant, anti-inflammatory and gallstone-dissolving effects. Tauroursodeoxycholic acid (tauroursodeoxycholic acid, 1) is the active ingredient of bear bile, the chemical name is 2-[[(3α,5β,7β)-3,7-dihydroxy-2,4-oxocholesteric acid Alkyl-24-yl] amino] ethanesulfonic acid dihydrate, developed by Italy's Besti Pharmaceutical Factory, was first listed in Italy in 1991, and was approved to be sold in China under the trade name taurolite i...

AI Technical Summary

Problems solved by technology

[0003] Tauroursodeoxycholic acid raw materials are not very stable to high humidity and high temperature, and absorb moisture seriously. This characteristic is determined by the chemical stability of this raw material drug. If it needs to be made into a preparation, it cannot be produced by conventional wet method Process; if full powder is used for production, but tauroursodeoxycholic acid accounts for about 72% of the prescription amount in the product prescription, due to the very poor fluidity of the raw material drug and its hygroscopicity, it cannot be produced

At present, Tarot capsules are produced by the screw direct pressure filling method, which has high requirements for the capsule filling machine. This equipment is expensive and needs to be imported, which restricts domestic production enterprises from using domestic capsule filling machines and using all-powder technology for production. For this capsule product, the in vitro dissolution behavior cannot be kept consistent with the reference preparation

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