Method for preparing ursodesoxycholic acid preparation on large scale

Abstract

The invention discloses a method for preparing an ursodesoxycholic acid preparation on a large scale, which comprises the following steps: weighing ursodesoxycholic acid, corn starch and colloidal silicon dioxide according to a weight ratio determined by a small-scale experiment, putting into amplified equipment, and carrying out wet mixing granulation, in the wet mixing granulation process, according to the Froude number, the diameter of a granulation pot and the change of the height of the granulation pot, the stirring speed determined by the small-scale experiment is amplified and converted, the amplified stirring speed is controlled to be (omega2 + / -2)-(omega2 '+ / -2), and other parameters are kept consistent with equipment parameters before amplification; and continuing to add magnesium stearate for total mixing, and then preparing the preparation. The method is simple in calculation and convenient to operate, the risk of excessive granulation of the materials can be effectively avoided in the process of large-batch wet granulation by amplifying small-scale determined parameters, the consistency of the materials in the aspects of powder characteristics and preparation dissolution can be kept, and the risk of production failure is reduced.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, in particular to a method for preparing ursodeoxycholic acid preparations in large quantities. Background technique [0002] Ursodeoxychlic acid (UDCA) is a hydrophilic bile acid, which can promote bile secretion, inhibit liver cell apoptosis, immune regulation and cell protection, and reduce the toxicity of hydrophobic bile acid. Polarity, stabilizes cell membranes. It was first isolated from the bile of Chinese bears by Japanese scientists in 1927 and named as ursodeoxycholic acid. [0003] The U.S. FDA approved the marketing application of ursodeoxycholic acid capsules (150mg and 300mg) in December 1987, and the marketing application of ursodeoxycholic acid tablets (250mg and 500mg) in October 1997. Domestically approved ursodeoxycholic acid capsules are produced in Germany with a specification of 250 mg, which is different from the specifications of the capsules approved in the...

AI Technical Summary

Problems solved by technology

[0004] Most of the original research and domestic preparation of ursodeoxycholic acid capsules are wet granulation technology (prepared by wet granulator or one-step granulator), but according to the patents and literature retrieved so far, none of them The content of the process part is described in detail

However, the inventor found that the ursodeoxycholic acid mixture prepared according to the prescription determined by the small test experiment has a high viscosity after being wetted, and it is easy to over-granulate during the granulation process, resulting in granulation failure.

Images