Glipizide osmotic pump controlled-release tablet and preparation method thereof

Abstract

Disclosed is a glipizide osmotic pump controlled release tablet. The glipizide osmotic pump controlled release tablet comprises, from inside to outside, a double-layer tablet core containing a drug layer and a promoting layer and an insoluble semi-permeable membrane; the drug layer comprises drug release holes and an optional moisture-proof film coating; the drug layer, based on the total weight, contains 1-30 wt.% of glipizide, 30-95 wt.% of a suspending agent, 2-30 wt.% of a retardant, 0-10 wt.% of an adhesive, 0-2 wt.% of a colorant and 0-2 wt.% of a lubricant; the promoting layer, based on the total weight, comprises 30-80 wt.% of an expanding agent, 1-30 wt.% of a retardant, 0-2 wt.% of a colorant, 5-40 wt.% of an osmotic pressure active substance and 0-1 wt.% of a lubricant; and the weight gain of the semi-permeable membrane is 5-20% of the weight of the tablet core. The invention also discloses a preparation method of the glipizide osmotic pump controlled release tablets. The method is convenient for production, and the product is easy to store, and can better achieve the purpose of controlled release.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an osmotic pump controlled-release tablet containing the active drug glipizide and a preparation method thereof. The controlled-release tablet can make the drug enter the gastrointestinal tract at a constant rate, so that the drug with low solubility Glipizide is released at a constant rate. Background technique [0002] Glipizide (Glipizide, chemical name: 5-methyl-N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonphthalein]phenyl]ethyl]-pyrazinecarboxamide ), a second-generation sulfonylurea oral hypoglycemic drug, mainly used for the treatment of patients with mild to moderate 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 β cells of the pancreas to secrete insulin, enhance the effect of insulin on the target tissue, and also stimulate the α cells of the pancreas ...

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Problems solved by technology

[0004] Chinese Invention Patent No. 200610114125.2 (Glipizide Controlled-release Tablets and Its Preparation Method) discloses a preparation method of Glipizide Controlled-release Tablets with a dose of 5 mg, using copolymer technology, which is the largest The characteristic is that the drug and the excipients form a copolymer, which has a certain solubilization effect on insoluble drugs. During the solubilization effect, some irrelevant impurities may also be produced, and industrialized large-scale production will also be difficult; at the same time, the drug is stored during storage. It will age in the medium, which will affect the release of the drug, and the stability of the drug will be greatly affected

[0005] In addition, Chinese invention patent application No. 038032864 (drug delivery system for sustained release of glipizide) discloses a gel matrix sustained-release tablet with carbomer as the drug release carrier. The zero-order release characteristics of sustained-release tablets are not obvious, and the drug release is easily affected by the internal environment (pH value, gastrointestinal motility, etc.)

[0006] Chinese invention patent application No. 200480016223.1 (two-way release of glipizide from a single-chamber osmotic dosage form) discloses a single-layer osmotic pump controlled-release tablet with alginate as the osmotic polymer. The tablet preparation is a single-layer osmotic pump controlled-release tablet. Although the drug release is not affected by the internal environment, this kind of single-layer osmotic pump controlled-release tablet is prone to insufficient power in the later stage of drug release and low drug release rate.

[0007] Chinese invention patent application No.201110065115.X (a preparation method of glipizide osmotic pump controlled-release tablets) adopts solid dispersion technology to improve the solubility of glipizide and improve the drug release rate to a certain extent, but Still can't fundamentally solve the problem of low drug release rate

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