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Glimepiride tablet and preparation method thereof

The technology of glimepiride tablet and urea tablet is applied in the field of medicine and can solve the problems of glimepiride easily absorbing, sticky punching and splitting tablet, glimepiride tablet having low disintegration degree and being unsuitable for mass production, etc. Achieve the effect of increasing absolute bioavailability, conducive to disintegration and dissolution, and improving absolute bioavailability

Inactive Publication Date: 2019-03-08
YANGTZE RIVER PHARM GRP GUANGZHOU HAIRUI PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Patent document CN201610123929.2 provides a preparation method of glimepiride tablets, the dissolution rate of glimepiride tablets prepared in this method can reach 93.2%, and the method needs to control the particle size of glimepiride raw drug powder Glimepiride is a hygroscopic compound. It is difficult to micronize it into a powder with a particle size of less than 10 μm to ensure that it is not sticky, uniform tableting, and no cracks. It is not suitable for mass production.
[0007] Therefore, there is still a lack of glimepiride tablets on the market that effectively solve the problems of low disintegration of glimepiride tablets, slow dissolution, and glimepiride's easy hygroscopicity, stickiness, and splitting during tablet production.

Method used

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  • Glimepiride tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1, the preparation of glimepiride

[0035] S1: 3-ethyl-4-methyl-2-pyrrolidone is added in n-heptane, the mass ratio of 3-ethyl-4-methyl-2-pyrrolidone and n-heptane is 1:15, and the temperature is raised to Dissolve at 70-90°C, add phenylethyl isocyanate dropwise, the molar ratio of phenylethyl isocyanate to 3-ethyl-4-methyl-2-pyrrolidone is 1:1, heat to 90°C, react After 8 hours, it was lowered to room temperature to obtain a crude product of Compound A, and then added methyl tert-butyl ether equal in mass to n-heptane, stirred for 25 minutes, filtered, and dried to obtain a pure product of Compound A;

[0036] S2: Add the pure compound A prepared in step S1 to chlorosulfonic acid with a mass ratio of 2.8:1 to 3-ethyl-4-methyl-2-pyrrolidone, the reaction temperature is 20°C, stir for 2.5h, add 10 ℃ water, dry crystal, filter to obtain compound B;

[0037] S3: Add the compound B prepared in step S2 to 3-ethyl-4-methyl-2-pyrrolidone in saturated ammonia water...

Embodiment 2

[0039] Embodiment 2, a kind of glimepiride tablet

[0040] The glimepiride tablet comprises an immediate-release layer and a sustained-release layer:

[0041] The sustained-release layer is a hydroxypropyl-β-cyclodextrin inclusion compound, and the hydroxypropyl-β-cyclodextrin inclusion compound is composed of glimepiride and hydroxypropyl-β-cyclodextrin by weight Made with a ratio of 1:3;

[0042] The immediate-release layer is composed of the following components and parts by weight: 1 part of glimepiride, 10 parts of β-cyclodextrin, 20 parts of sodium hydroxymethyl starch, 10 parts of microcrystalline cellulose, 1 part of magnesium stearate 50 parts and lactose;

[0043] The particle size of the immediate-release layer β-cyclodextrin, sodium hydroxymethyl starch, microcrystalline cellulose, magnesium stearate and lactose is 10-90 μm;

[0044] The glimepiride is prepared from Example 1;

[0045] The weight ratio of glimepiride in the immediate-release layer and the susta...

Embodiment 3

[0049] Embodiment 3, a kind of glimepiride tablet

[0050] The glimepiride tablet comprises an immediate-release layer and a sustained-release layer:

[0051] The sustained-release layer is a hydroxypropyl-β-cyclodextrin inclusion compound, and the hydroxypropyl-β-cyclodextrin inclusion compound is composed of glimepiride and hydroxypropyl-β-cyclodextrin by weight Made with a ratio of 1:4;

[0052] The immediate-release layer is composed of the following components and parts by weight: 1 part of glimepiride, 10 parts of β-cyclodextrin, 20 parts of sodium hydroxymethyl starch, 10 parts of microcrystalline cellulose, and 1 part of magnesium stearate and lactose 50 parts.

[0053] The particle size of β-cyclodextrin, sodium hydroxymethyl starch, microcrystalline cellulose, magnesium stearate and lactose in the immediate release layer is 10-90 μm;

[0054] The glimepiride is prepared from Example 1;

[0055] The weight ratio of glimepiride in the quick-release layer and the su...

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Abstract

The invention belongs to the technical field of medicines and in particular relates to a glimepiride tablet and a preparation method thereof. The glimepiride tablet provided by the invention comprisesa quick-release layer and a slow-release layer, wherein the slow-release layer is composed of glimepiride and hydroxypropyl-beta-cyclodextrin; the quick-release layer is composed of the glimepiride,beta-cyclodextrin, sodium carboxymethyl starch, microcrystalline cellulose, magnesium stearate and lactose. According to the glimepiride tablet provided by the invention, the purity of the self-made glimepiride is high and the micronization effect is good; furthermore, the quick-release layer and the slow-release layer do not contain cyclodextrin and, so that moisture absorption and sticking phenomena can be effectively prevented; the prepared glimepiride tablet has a high dissolution rate; after the tablet is orally taken, the glimepiride of the quick-release layer is dissolved out and the glimepiride of the slow-release layer is slowly released, so that the absolute bioavailability of the glimepiride is improved; after the beta-cyclodextrin is added, the glimepiride of the quick-releaselayer and a hydroxypropyl-beta-cyclodextrin inclusion compound of the slow-release layer are uniformly distributed, the glimepiride tablet is more easily disintegrated and dissolved out, and the stability of the glimepiride tablet is improved.

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] Diabetes mellitus is a syndrome of glucose, protein, and lipid metabolism disorders caused by absolute or relative insufficiency of insulin in the body. Elevated blood sugar is the basic feature, often accompanied by chronic diseases of multiple systems such as blood lipids, cardiovascular, nerves, skin and eyes. Today, diabetes has become the "third killer" that threatens human beings after tumors and cardiovascular and cerebrovascular diseases. In 2010, "New England Journal of Medicine" reported that the number of diabetic patients in 14 provinces and municipalities in China will exceed 9200 10,000 people, accounting for about 10% of the population in these places, and showing a growing trend. [0003] Glimepiride, chemical name 1-[4-[2-(3-ethyl-4-methyl-2-oxo-3-pyrroline-1-carbo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24A61K47/69A61K47/36A61K47/40A61K47/38A61K47/26A61K31/64A61P3/10C07D207/38
CPCA61K9/2018A61K9/205A61K9/2054A61K9/2059A61K9/2086A61K31/64A61K47/6951A61P3/10C07B2200/13C07D207/38
Inventor 刘志强任亚东夏春森汪刘恒袁海成
Owner YANGTZE RIVER PHARM GRP GUANGZHOU HAIRUI PHARM CO LTD
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