Preparation method of glimepiride tablet

Abstract

The invention relates to a glimepinride tablet preparation method, which comprises 1) glimepinride and microposer silica gel are ground with a micronizaion method, and the mixture powder of micronized glimepinride and microposer silica gel is obtained after passing through a screen of 80 to 100 mesh; wherein, the weight ratio of the glimepinride and microposer silica gel is 1: 1; 2) the mixture powder obtained in the step 1) is mixed with filling agent, disintegrant, lubricant, bond and 30 percent to 40 percent by volume concentration of ethanol solution for 15 minutes to 20 minutes in normal temperature, and passes through a screen with 18 to 24 meshes to obtain the particles. The particles adopts micronization technique to increase the surface area of slightly soluble main drug to facilitate glimepinride pulverization so that the wettability of the surface of the powder particles is improved and the dissolution of the raw medicine in tablets and the quality stability of the product during storage time are improved.

Description

technical field [0001] The invention belongs to the field of glimepiride tablets, in particular to a preparation method of glimepiride tablets. Background technique [0002] Glimepiride Tablet, the structural formula is It is a sulfonylurea hypoglycemic drug, which was successfully developed by the German Hoechst AG pharmaceutical company in the 1980s as a treatment for type II diabetes. As a new generation of sulfonylurea hypoglycemic drugs after tolbutamide (D860) and glibenclamide (glibenclamide), it has the characteristics of high efficiency, long-acting, small dose, and low side effects. It has been approved for marketing in Germany, Sweden, Denmark, Switzerland and other countries, and was approved for marketing by the US FDA in 1995. It has been widely used in the treatment of type II diabetes in Europe and the United States. [0003] As a new type of sulfonylurea hypoglycemic drug, glimepiride has a different action site from traditional sulfonylurea drugs, mainl...

AI Technical Summary

Problems solved by technology

When the trial production is carried out according to the prescription process in the declared production data, the dissolution rate of the product in the quality inspection always fails to meet the requirements, which is only about 50% (the standard is: 75% of the labeled amount), which affects the specification. A major problem in the production and marketing of Limepiride Tablets

[0015] In addition, our research has found that glimepiride is soluble in chloroform, slightly soluble in ethanol or methanol, and almost insoluble in water or ether. It is a hydrophobic and insoluble substance and is easy to decompose at high temperature.

Therefore, there are two major problems in its preparations: 1) in the process of producing pharmaceutical preparations, the technical difficulty is relatively large, and its dissolution rate is difficult to reach the quality standard; It is difficult to meet the relevant regulations of the quality standard

[0016] By changing the glimepiride raw material from the 100-mesh fineness in the original process data to 200-mesh fineness, but the dissolution test result is 70% to 80%, which is still unstable; after adjusting the disintegrating agent and Treatment methods such as excipients cannot improve the dissolution profile

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