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Sarpogrelate hydrochloride tablet and preparation method thereof

A technology of sarcogrelate hydrochloride tablets and ester tablets, which is applied in the field of medicine, can solve the problems of large content of sarcogrelate hydrochloride, difficulty in ensuring the dissolution rate of preparations, and poor particle fluidity, so as to achieve low preparation cost and solve the problems of excipients and particle fluidity Contradictions, the effect of high production efficiency

Active Publication Date: 2016-07-20
SHANDONG JINHE DRUG RES DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The commonly used processing excipients of powder direct compression include microcrystalline cellulose, pregelatinized starch and direct compression lactose, but the content of sagrelorate hydrochloride in this preparation is relatively large, and its fluidity is not good
When the conventional powder is directly compressed, more excipients are added, which leads to a larger tablet weight, and it is difficult to ensure the dissolution rate of the preparation without adding a disintegrant. If less excipients are added, the fluidity of the particles will be poor, which is not conducive to tablet compression.

Method used

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  • Sarpogrelate hydrochloride tablet and preparation method thereof
  • Sarpogrelate hydrochloride tablet and preparation method thereof
  • Sarpogrelate hydrochloride tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0029] Experimental example 1. Study on particle size control of raw and auxiliary materials of sarcogrelate hydrochloride tablets

[0030] 1. Study on the type of excipients

[0031] From the results of the compatibility test of raw materials and excipients, it is known that microcrystalline cellulose is most beneficial to the stability of sarcogrelate hydrochloride, so microcrystalline cellulose is selected as the excipient of the preparation, and the model is screened.

[0032] 1. Materials: sargrel hydrochloride (Hubei Jusheng Technology Co., Ltd., 20121101); microcrystalline cellulose PH101 (batch number: 1167), microcrystalline cellulose PH102 (batch number: 2193), microcrystalline cellulose PH301 (batch number: 3194 ), microcrystalline cellulose PH302 (batch number: 6114) were purchased from Asahi Kasei (China) Investment Co., Ltd. Beijing Branch.

[0033] 2. Method: Mix the above four different types of microcrystalline cellulose and sarcogrelate hydrochloride (crushe...

experiment example 2

[0075] Experimental example 2, citric acid adding process research

[0076] 1. Materials and instruments: sargrelate hydrochloride (Hubei Jusheng Technology Co., Ltd., batch number 20121101), microcrystalline cellulose PH302 (purchased from Asahi Kasei (China) Investment Co., Ltd. Beijing Branch, batch number: 6114), citric acid ( Company: Hunan Erkang Pharmaceutical Co., Ltd., batch number: 20120601), magnesium stearate (company: Shandong Liaocheng Ahua Pharmaceutical Co., Ltd., batch number: 20100214), micropowder silica gel (company: Shanghai Yunhong Chemical Pharmaceutical Co., Ltd., batch number: VA73913), 295F680010 (Company: Shanghai Kaleokang Coating Technology Co., Ltd., batch number: THL015076); pulverizer (model: F-30B, Jiangsu Baobao Group Co., Ltd.), tablet press (model: ZP-15, manufactured by Liaocheng Wanhe Industry Co., Ltd.), coating machine (model: BG10, Baoji Nuokai Technology Development Co., Ltd.). HPLC chromatograph (detector model: SPD-20A, pump model...

experiment example 3

[0100] Experimental Example 3, Stability Study of Sagrelate Hydrochloride Tablets

[0101] Carry out scale-up tests and stability studies in accordance with the determined prescription process, focusing on changes in substances related to accelerated tests of preparations.

[0102] 1. Materials and instruments: Anbu Leke (Company: Mitsubishi Tanabe Pharmaceutical Co., Ltd., Japan, batch number: U005), sargrelate hydrochloride (Hubei Jusheng Technology Co., Ltd., batch number 20121101), microcrystalline cellulose PH302 (purchased from Asahi Kasei (China) Investment Co., Ltd. Beijing Branch, batch number: 6114), citric acid (company: Hunan Erkang Pharmaceutical Co., Ltd., batch number: 20120601), magnesium stearate (company: Shandong Liaocheng Ahua Pharmaceutical Co., Ltd., Batch number: 20100214), micropowder silica gel (company: Shanghai Yunhong Chemical Pharmaceutical Co., Ltd., batch number: VA73913), 295F680010 (Company: Shanghai Kaleokang Coating Technology Co., Ltd., ba...

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Abstract

The invention provides a sarpogrelate hydrochloride tablet. The sarpogrelate hydrochloride tablet is composed of the following raw and accessory materials by weight: 100 parts of sarpogrelate hydrochloride, 60 to 100 parts of microcrystalline cellulose PH302, 4 to 8 parts of citric acid, 2 to 6 parts of magnesium stearate, 8 to 12 parts of aerosil and 5 to 6 parts of Opadry (registeration trademark) 295F6800. The tablet has low preparation cost and better stability compared with commercially available preparations. The invention also provides a preparation method for the sarpogrelate hydrochloride tablet to overcome contradiction between minimal accessory materials and particle mobility. Research results in the invention prove that when sarpogrelate hydrochloride and citric acid are mixed and crushed to specific particle sizes in advance and then mixed with microcrystalline cellulose of a specific model, the requirement on mobility of mixed particles during direct pressing of powder is met and the dissolving-out behavior of the tablet is realized; and results of stability test show that the tablet has better stability compared with commercially available preparations.

Description

technical field [0001] The invention relates to a sargrelate hydrochloride tablet and a preparation method thereof, belonging to the technical field of medicines. Background technique [0002] Sagrelate hydrochloride, chemical name: (±)-2-(dimethylamino)-1-[[o-(m-methoxyphenethyl)phenoxy]-methyl]ethylhydrogensuccinatehydrochloride, molecular formula: C24H31NO6·HCl, molecular weight: 465.97, used in pharmacy It is used to improve ischemic symptoms such as ulcers, pain and cold sensation caused by chronic arterial occlusive disease. 2 Receptors have specific antagonism. [0003] At present, the listed preparation of sarcogrelate hydrochloride is the sarcogrelate hydrochloride tablet (trade name: ), raw and auxiliary materials include sarcogrelate hydrochloride, crystalline cellulose, carboxymethyl cellulose, hydroxypropyl cellulose, light anhydrous silicic acid, citric acid, magnesium stearate, coating powder, and its preparation method is : Mix sargrelor hydrochloride wit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K31/225A61K47/38A61P9/10
Inventor 王京凯张栋彭坤李晗刘玉芹
Owner SHANDONG JINHE DRUG RES DEV
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