Glipizide controlled release tablets and preparation method thereof

Abstract

The invention provides a glipizide loaded controlled release preparation, which comprises a pastille layer and a boosting layer with the weight ratio of 1:0.5 to 3, the pastille layer comprises glipizide and carrier, the carrier is ethane ketopyrrolidine homopolymer and / or ethane ketopyrrolidine copolymer occupying 40 to 99 percent of the weight of the pastille layer; the boosting layer at least comprises infiltration promoting polymer occupying 10 to 80 percent of the weight of the boosting layer, 10 to 80 percent of insoluble polymer and residual osmotic pressure accelerant; the glipizide of the invention can be controlled to release a drug so as to lead the preparation to attain the purpose that the drug is administrated one time a day, and the glipizide can be released in 24 hours.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an osmotic pump drug delivery preparation containing the active drug glipizide and a preparation method thereof. Glipizide can be delivered in a controlled release manner. Background technique [0002] Glipizide (Glipizide, chemical name: 5-methyl-N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl]phenyl]ethyl]-pyrazinecarboxamide) , a second-generation sulfonylurea hypoglycemic drug, mainly used for the treatment of non-insulin-dependent diabetes mellitus. In vivo and in vitro experiments have shown that the main mechanism of action of glipizide is to stimulate the pancreatic β cells to secrete insulin, showing an acute hypoglycemic effect; in addition, the drug also has two important extrapancreatic effects: increasing insulin sensitivity and reducing insulin sensitivity. Glycogenesis. The common oral preparations of glipizide are rapidly and completely absorbed i...

AI Technical Summary

Problems solved by technology

However, the osmotic pump controlled-release tablet with PEO as the main auxiliary material has inherent disadvantages: (1) the water absorption rate and hydration rate of polyoxyethylene are relatively slow, so the time lag of drug release is long, so that the drug cannot be rapidly recovered after taking it. (2) The typical glass transition temperature range of polyoxyethylene is 65°C to 67°C, so PEO does not have ideal thermal stability, and there are the following problems in the preparation and storage process of industrial production: during the granulation process Solvent drying is more difficult

Since the drying temperature should not usually exceed 40°C, it is easy to cause a high residual amount of organic solvent; if the drying is to be relatively complete, a relatively long drying time is required; the storage temperature of the tablet should not be too high, and the high storage temperature is easy to cause The physical and chemical properties of polyoxyethylene change, which affects the release behavior of the tablet; during high-speed tablet compression, if the die is used repeatedly to generate heat and the temperature reaches about 50°C, adverse phenomena such as sticking and punching are prone to occur. Special cooling facilities are required to control the temperature of the die

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