Repaglinide troche and preparation method thereof

Abstract

The invention relates to an oral troche which contains repaglinide or pharmaceutically acceptable derivatives of repaglinide as well as a preparation method of the oral troche. According to the preparation method, powder of repaglinide or pharmaceutically acceptable derivatives of repaglinide is directly pressed into troche, so that the production cost is remarkably lowered, and the disintegration and the dissolution rate are greatly improved. The bioavailability and the stability of the medicine can be improved, and the problem of low content uniformity of existing small-dose medicines formed by the direct pressing method is overcome, so that the quality of the troche is better guaranteed.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an oral tablet containing repaglinide or a pharmaceutically acceptable derivative thereof, and a method for preparing the oral tablet. Background technique [0002] Whether it is a developed country or a developing country, diabetes, especially type II diabetes, has developed into an epidemic in modern society and a worldwide public health problem that seriously threatens human health. [0003] Repaglinide is a first-line oral hypoglycemic drug developed by Germany's Novo Nordisk for the treatment of type 2 diabetes. It was first launched in the United States in 1997. Its trade name is: Later, it was listed in Europe and my country successively. The trade name is: It is a methylbenzylamine benzoic acid (CBMA) derivative with the following structural formula: [0004] [0005] The drug binds to a specific site on the β-cell membrane, closes the ATP-depen...

AI Technical Summary

Problems solved by technology

Despite satisfactory dissolution, this wet granulation method has many disadvantages

For example, the operation steps in production are complicated, including binder solution preparation, soft material preparation, granule sizing, granule drying, mixture mixing and blending powder tableting; more equipment is required in production, including liquid preparation device, wet granulation Machines, granulators, ovens, mixers and tablet presses increase labor costs and prolong operating time; the drying temperature of wet granules is not easy to control, and the uneven particle size distribution can easily cause content differences between granules, content decline and related substances ( For example, the problem of increased impurities; after wet granulation, the tablet disintegrates into granulated particles, which are not primary particles, which is not conducive to the dissolution of active drugs; in addition, it is important that the wet granulation step introduces A large amount of water, and the introduction of water will cause the active substance to decompose or undergo crystal transformation during the manufacturing or storage process, thus affecting the stability of the drug

[0009] The conceivable preparation methods used to solve the above problems may be dry granulation tableting method and powder direct tableting method, however, limited by the particularity of repaglinide's own physical and chemical properties and the requirements of oral small dose preparations, since Since its listing 15 years ago, there have been no successful dry granulation tableting and powder direct tableting products, and there are no literature reports in this regard

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