Glimepiride tablet and preparation method thereof

Abstract

The invention discloses a glimepiride tablet and a preparation method thereof. The preparation method comprises the following steps: dissolving glimepiride in a sodium hydroxide solution; adding mesoporous silica and carrying out uniform mixing under stirring; adding glacial acetic acid into a solution obtained in the previous step under stirring; allowing a compound of glimepiride and mesoporous silica to be precipitated and carrying out filtering and drying; then mixing the dried compound with a filler and a disintegrating agent and carrying out granulation and drying; and adding a lubricant into dry particles and then carrying out tabletting. Compared with the prior art, the glimepiride tablet prepared in the invention can be rapidly dissolved out in water, and the preparation method is simple in process and suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a glimepiride tablet and a preparation method thereof. Background technique [0002] Glimepiride is a new sulfonylurea hypoglycemic drug, the chemical name is 1-[4-[2-(3-ethyl-4-methyl-2-oxo-3-pyrroline) -1-formamido)ethyl]benzenesulfonyl]-3-(trans-4-methylcyclohexyl)urea, the structural formula is as follows: [0003] [0004] Molecular formula: C 24 h 34 N 4 o 5 S molecular weight: 490.62 [0005] Glimepiride was developed by the German company Hoechst Marion Roussel (HMR). It was first launched in Sweden under the trade name Amaryl in September 1995. It was approved by the FDA to enter the US market in 1996. It is used for the treatment of uncontrolled diet and exercise. Type 2 diabetes, it is the first FDA-approved sulfonylurea drug that can be used simultaneously with insulin. Because the drug has a short action time with the receptor, it shortens the ...

AI Technical Summary

Problems solved by technology

However, because glimepiride is an insoluble drug and is almost insoluble in water, the actual production of glimepiride oral solid preparations often encounters the problem that the dissolution rate is low or even unqualified; and because the content of glimepiride in the preparation Low, it is difficult to fully mix during preparation, and there are often problems of high and low, and large dissolution differences between tablets when performing dissolution testing

When there is an urgent need for quick-acting and high-efficiency preparations in clinical practice, solving the problem of low bioavailability of insoluble drugs due to low solubility and slow dissolution has always been a major problem in the pharmaceutical industry

[0009] CN102512388B provides a glimepiride orally disintegrating tablet, the orally disintegrating tablet is prepared by inclusion technology, glimepiride is clathrated with polypropylene resin S100, the prepared tablet disintegrates rapidly, but the dissolution effect is not good good

[0010] CN102600106A relates to glimepiride nanoparticle capsules and a preparation method thereof, which can effectively solve the problems of poor water solubility of glimepiride, short half-life, instability, low bioavailability, and poor effect of targeted therapy. The technical solution is: It is composed of 1 part of glimepiride, 1-30 parts of surfactant, and 3-60 parts of lyoprotectant in terms of weight ratio; the preparation method is to combine glimepiride or glimepiride with the said The mixture of surfactants is dissolved in an organic solvent to prepare a primary suspension, and a suspension with an average particle size of 300±60nm is obtained by using a high-pressure homogenization method or an emulsification diffusion method; the nanosuspension is freeze-dried and sieved , filled in the capsule shell

However, after the drug is micronized, it is easy to aggregate, and it is difficult to ensure that the drug is mixed evenly; adding a large amount of surfactant will lead to increased gastrointestinal side effects

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