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Glimepiride dispersible tablet composition and preparation method thereof

A technology for glimepiride and dispersible tablets, which is applied in the field of medicine, can solve the problems of uneven dispersion, poor dissolution effect, influence on drug efficacy and the like, and achieves the effects of simple production process, good process tolerance and stable clinical efficacy

Active Publication Date: 2021-04-09
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The dissolution rate of the dispersible tablet in 200ml of 0.02% tris solution in 45 minutes was 75%, and the dissolution effect was poor
[0008] Chinese patent CN102379855 discloses a preparation method of glimepiride dispersible tablets, and every 10,000 tablets of said dispersible tablets consist of 10-20g of glimepiride, 120-1500g of diluent, 40-200g of disintegrant, adhesive 15-90g of lubricant, 5-10g of lubricant, etc., the dissolution rate is improved by controlling the particle size of the raw material glimepiride, but only the dissolution rate in the pH7.8 phosphate buffer solution is improved, and the other aspects are not investigated. Dissolution in other media
[0010] Glimepiride belongs to BCSII (low solubility-high penetration) drugs, and the specifications of glimepiride preparations are 1 mg and 2 mg, and the content of active ingredients of the main drug is relatively low. Therefore, glimepiride dispersible tablets have uneven content, Problems such as uneven dispersion have a great impact on the efficacy of the drug

Method used

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  • Glimepiride dispersible tablet composition and preparation method thereof
  • Glimepiride dispersible tablet composition and preparation method thereof
  • Glimepiride dispersible tablet composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment 1: Glimepiride Dispersible Tablets

[0058] 1. Prescription composition:

[0059]

[0060] Feed intake according to the prescription quantity of 200000 tablets, prepare glimepiride dispersible tablet, the same below.

[0061] 2. Preparation method:

[0062] (1) Preparation of adhesive: polyvinylpyrrolidone K -29 / 32 Dissolved in water to prepare a 6.0% (w / w) binder solution;

[0063] (2) Premixing and wet granulation: add glimepiride and sodium carboxymethyl starch as an internal auxiliary material into the wet mixing granulator for premixing 1, add lactose into the wet mixing granulator for premixing 2. Then add the binder solution under stirring conditions, and wet granulate; the process parameters are as follows:

[0064]

[0065] (3) Drying: Dry the granules at 48-53°C until the water content is 1.5%;

[0066] (4) Grain sizing: add the dried granules to the sizing machine for sizing;

[0067] (5) Mixing: add microcrystalline cellulose PH302 and...

Embodiment 2

[0079] Embodiment 2: Glimepiride Dispersible Tablets

[0080] One, prescription composition: with embodiment 1

[0081] 2. Preparation method:

[0082] Preparation method: step (1)-step (5) is the same as embodiment 1;

[0083] (6) Tablet compression: the tablet compression pressure is 10KN; each tablet contains 1 mg of glimepiride in dispersible tablets.

[0084] 3. Test results:

[0085] 1. The friability, content uniformity and dispersion uniformity of the prepared glimepiride dispersible tablets were measured, and the results are shown in Table 4.

[0086] Table 2: Results of friability, content uniformity, and dispersion uniformity of glimepiride dispersible tablets in Example 2

[0087]

[0088] 2. The dissolution rate of the prepared glimepiride dispersible tablets was tested, and the results are shown in Table 5.

[0089] Table 5: Dissolution results of Glimepiride Dispersible Tablets in Example 2

[0090]

Embodiment 3

[0091] Embodiment 3: Glimepiride Dispersible Tablets

[0092] 1. Prescription composition:

[0093]

[0094] 2. Preparation method:

[0095] (1) Preparation of adhesive: polyvinylpyrrolidone K -29 / 32 Dissolved in water to prepare a 7.0% binder solution;

[0096] (2) Premixing and wet granulation: add glimepiride and sodium carboxymethyl starch as an internal auxiliary material into the wet mixing granulator for premixing 1, add lactose into the wet mixing granulator for premixing 2. Then add the binder solution under stirring conditions, and wet granulate; the process parameters are as follows:

[0097]

[0098] (3) Drying: Dry the granules at 45-50°C until the moisture content is 1.7%;

[0099] (4) Grain sizing: add the dried granules to the sizing machine for sizing;

[0100] (5) Mixing: add microcrystalline cellulose PH302 and the excipient sodium carboxymethyl starch to the granules, stir and mix for 8 minutes, then add magnesium stearate, and mix for 8 minutes;...

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Abstract

The invention provides a glimepiride dispersible tablet and a preparation method thereof. The glimepiride dispersible tablet comprises the following components in percentage by weight of 1%-1.5% of glimepiride, 75%-80% of lactose, 5%-10% of carboxymethyl starch sodium, 0.4%-1.0% of polyvinylpyrrolidone, 10%-15% of microcrystalline cellulose and 0.1%-1.0% of magnesium stearate. The glimepiride dispersible tablet prepared by the invention has dissolution rates of more than 85% in dissolution media with pH values of 1.2 and 7.8, and is high in dissolution rate and stable in clinical curative effect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a glimepiride dispersible tablet composition and a preparation method thereof. Background technique [0002] Glimepiride is the third-generation sulfonylurea oral 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, suitable for type 2 diabetes mellitus whose blood sugar cannot be adequately controlled by diet control, exercise therapy and weight loss , the structural formula is as follows. [0003] [0004] Glimepiride tablets were developed by Sanofi and imported to China in 2005. The trade name is Yamoli (reference preparation). Glimepiride can lower fasting blood sugar and postprandial blood sugar. The main mechanism of action is to stimulate pancreatic islet β Cells secrete insulin, and can increase the sensitivity of peripheral tissues to insulin, that is, it binds to...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/64A61K47/38A61K47/36A61K47/26A61K47/32A61P3/10
CPCA61K9/2095A61K9/2054A61K9/2059A61K9/2027A61K9/2018A61K9/0095A61K31/64A61P3/10
Inventor 王洁敏张彩娟刘文静张芳杨婷婷
Owner CSPC OUYI PHARM CO LTD
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