Repaglinide/metformin combo tablet

Abstract

The invention relates to a repaglinide / metformin combo tablet, particularly a pharmaceutical composition in the form of a tablet, which comprises the following components in parts by weight: 500 parts of metformin hydrochloride, 0.5-5 parts of repaglinide and 10-200 parts of medicinal auxiliary materials. The medicinal auxiliary materials include, but are not limited to filler, disintegrant, binding agent, alkali and lubricant. The invention also relates to a method for preparing the pharmaceutical composition. The pharmaceutical composition provided by the invention has favorable pharmaceutical properties.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a tablet pharmaceutical composition with repaglinide and metformin as active ingredients and a preparation method thereof. Background technique [0002] Repaglinide (English name Repaglinide), its chemical name is: S(+)-2-ethoxy-4-{2-[(3-methyl-1-(2-(1-piperidinyl) phenyl)butyl)amino]-2-oxoethyl}benzoic acid. Molecular formula: C27H36N2O4, molecular weight: 452.59, and its structural formula is as follows: [0003] [0004] Repaglinide is a benzoic acid derivative, a non-sulfonylurea insulin secretagogue, a new type of oral hypoglycemic drug that acts rapidly, and specifically binds to the 36KDA protein on the ATP-dependent potassium ion channel outside the islet D cell membrane , to close the potassium channel, depolarize the D cell, open the calcium channel, and promote the influx of calcium ions to promote insulin secretion. [0005] Metformin (Metformin), i...

AI Technical Summary

Problems solved by technology

[0016] The disadvantage of the above-mentioned double-layer sustained-release tablets or compressed small tablets separately is that their preparation requires too much equipment and is difficult to industrialized production. Even if the products are put on the market, patients will need to pay high treatment costs; The preparation process will lead to excessive hardness of the tablet, which will affect the release of the drug, and it will be difficult to release the drug from the connecting surface of the upper and lower double-layer tablets

Moreover, because repaglinide is almost insoluble in water, the drug's in vitro dissolution rate is poor, resulting in low bioavailability.

[0017] In the compound tablet containing repaglinide and metformin, the weights of the two active ingredients differ greatly, so special consideration needs to be given to the uniformity of low-dose repaglinide, that is, the content uniformity; Glinide has poor solubility and metformin has very good solubility. There is a big difference between the two in the dissolution performance of the tablet, which may cause the onset time of the two drugs to be inconsistent after the tablet is taken.

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