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Metformin hydrochloride sustained-release tablet and preparation method thereof

A technology of metformin hydrochloride and sustained-release tablets, applied in the field of medicine, can solve problems such as unfavorable swallowing, high temperature, and sudden release phenomenon, and achieve the effects of overcoming incomplete release, reducing impurity content, and reducing adverse reactions

Active Publication Date: 2019-10-22
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The original research product of metformin hydrochloride sustained-release tablets "Glucophage XR" is a gel barrier type hydrophilic product made of hydroxypropyl methylcellulose, sodium carboxymethylcellulose, microcrystalline cellulose, magnesium stearate, etc. Sexual matrix sustained-release preparation, the tablet weight is 1g, the effective drug is 0.5g, and the dose is relatively large. When taking it, you need to swallow the whole tablet and not crush it. It is very inconvenient to have to swallow a tablet that is too heavy. Especially for the elderly is more inconvenient
Chinese patent documents CN102440975A and CN103816130A adopt the following problems in the preparations of the present common skeleton slow-release materials such as hydroxypropyl methylcellulose and sodium carboxymethylcellulose: 1. The tablet is heavy, and the amount of skeleton slow-release material used is too large, resulting in The tablet is heavy, which is not conducive to swallowing; 2. Uneven drug release, sudden release or incomplete release
Metformin hydrochloride sustained-release tablets are prepared by hot-melt extrusion technology. Due to the high temperature during the preparation process of melt granulation and hot-melt extrusion, the instability of drugs and excipients will be increased, which will lead to more impurities in the preparation products.
Although the invention patent reduces the generation of impurities by adding the auxiliary material PVP-VA64, it is not ideal enough

Method used

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  • Metformin hydrochloride sustained-release tablet and preparation method thereof
  • Metformin hydrochloride sustained-release tablet and preparation method thereof
  • Metformin hydrochloride sustained-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Embodiment 1 prepares metformin hydrochloride sustained-release tablet of the present invention

[0064] prescription:

[0065]

[0066] Preparation:

[0067] 1. Preparation of sustained-release granules by dry method:

[0068] a. Mixing: add metformin hydrochloride, hypromellose and copovidone in the prescribed amount into the mixer and mix for 10 minutes;

[0069] b. Dry granulation: transfer the mixed material to a dry granulation roller press for granulation to obtain metformin hydrochloride sustained-release granules.

[0070] 2. Preparation of sustained-release microcapsules by spray drying method:

[0071] a. Prepare bletilla striata polysaccharide solution: weigh the bletilla striata polysaccharide in the prescribed amount, add 470ml of distilled water, heat and stir in a water bath at 50°C to dissolve;

[0072] b. Prepare gum arabic solution: weigh the gum arabic of the prescribed amount, add 938ml of distilled water, heat and stir in a water bath at 50°...

Embodiment 2

[0080] Embodiment 2 prepares metformin hydrochloride sustained-release tablet of the present invention

[0081] prescription:

[0082]

[0083] Preparation:

[0084] 1. Preparation of sustained-release granules by dry method:

[0085] a. Mixing: Add metformin hydrochloride, hypromellose and microcrystalline cellulose in the prescribed amount into the mixer and mix for 10 minutes;

[0086] b. Dry granulation: transfer the mixed material to a dry granulation roller press for granulation to obtain metformin hydrochloride sustained-release granules.

[0087] 2. Preparation of sustained-release microcapsules by spray drying method:

[0088] a. Prepare bletilla striata polysaccharide solution: weigh the bletilla striata polysaccharide in the prescribed amount, add 330ml of distilled water, heat and stir in a water bath at 50°C to dissolve;

[0089] b. Preparation of gum arabic solution: weigh the gum arabic of the prescribed amount, add 910ml of distilled water, heat and stir...

Embodiment 3

[0097] Embodiment 3 prepares metformin hydrochloride sustained-release tablet of the present invention

[0098] prescription:

[0099]

[0100] Preparation:

[0101] 1. Preparation of sustained-release granules by dry method:

[0102] a. Mixing: Add metformin hydrochloride, hypromellose and microcrystalline cellulose in the prescribed amount into the mixer and mix for 10 minutes;

[0103] b. Dry granulation: transfer the mixed material to a dry granulation roller press for granulation to obtain metformin hydrochloride sustained-release granules.

[0104] 2. Preparation of sustained-release microcapsules by spray drying method:

[0105] a. Prepare bletilla striata polysaccharide solution: weigh the bletilla striata polysaccharide in the prescribed amount, add 265ml of distilled water, heat and stir in a water bath at 50°C to dissolve;

[0106] b. Preparation of gum arabic solution: weigh the gum arabic of the prescribed amount, add 1100ml of distilled water, heat and sti...

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Abstract

The invention relates to a metformin hydrochloride sustained-release tablet and a preparation method thereof, and belongs to the technical field of medicine. The metformin hydrochloride sustained-release tablet is composed of sustained-release granules, sustained-release microcapsules and a lubricant, and is prepared through tabletting, wherein the weight ratio of the metformin hydrochloride in the sustained-release granules and the metformin hydrochloride in the sustained-release microcapsules is (3:7)-(6:4), and the lubricant is selected from superfine silica powder or magnesium stearate. According to the preparation method, a traditional spray drying method is improved, by combining a dry granulation process, the sustained-release microcapsules and sustained-release granules of different processes are prepared, tabletting is further carried out to prepare the metformin hydrochloride sustained-release tablet, the specific ratio of the sustained-release microcapsules prepared by the spray drying process to the sustained-release granules prepared by the dry granulation process is explored, and the metformin hydrochloride sustained-release tablet of which the inner portion has the structure of the sustained-release microcapsules and the sustained-release granules is finally obtained. The metformin hydrochloride sustained-release tablet and the preparation method thereof achievea good release behavior of the sustained-release tablet, overcome the shortcomings of sudden release and incomplete release, obtain a better release curve, and also greatly reduce the impurity content.

Description

technical field [0001] The invention relates to a metformin hydrochloride sustained-release tablet and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Metformin hydrochloride is the only oral biguanide antihyperglycemic drug that is still used in developed countries in the world. It is a commonly used drug for the treatment of type 2 diabetes, and its clinical application of sustained-release tablets has become common. Metformin hydrochloride is a Class III drug in the biopharmaceutical classification system (BCS), and it has high solubility and low permeability in the human body. Gastrointestinal adverse reactions such as bloating, diarrhea, nausea, and abdominal discomfort to varying degrees, and metformin hydrochloride sustained-release tablets have a certain gastric retention effect, which can increase the residence time of the drug in the stomach, improve the bioavailability of the drug, and reduce the The fluct...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/26A61K47/12A61K9/16A61K47/38A61K47/32A61K9/50A61K47/36A61K31/155A61P3/10
CPCA61K9/1635A61K9/1652A61K9/2013A61K9/2081A61K9/5036A61K31/155A61P3/10
Inventor 马慧丽白艳玲张萌王晨光
Owner CSPC OUYI PHARM CO LTD
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