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Sarpogrelate hydrochloride sustained-release preparation and preparation method

A technology of sarpogrelate hydrochloride and preparations, which can be used in pharmaceutical formulations, medical preparations of inactive ingredients, drug delivery and other directions, and can solve problems such as rupture and foreign body sensation in the body.

Inactive Publication Date: 2011-01-05
苏州世林医药技术发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When the device is in contact with or inserted into the body, the body is prone to a foreign body sensation or even breaks, which poses a certain burden on the patient

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～3

[0017] Examples 1-3 are for comparing the effects of different water-soluble polymers on drug release. Made by direct compression method.

[0018] Put sarcogrelate hydrochloride and water-soluble polymer (hydroxypropyl methylcellulose, or carbo, polyethylene oxide), lactose, hydroxypropyl cellulose into the mixing machine and mix for 5 minutes. Magnesium stearate was added to the prepared mixture and mixed for 3 minutes to obtain the final mixture. Tablets were compressed on a rotary tablet press (KT-1000) to obtain tablets of 5 to 8 kgf.

[0019] Table 1. Composition of Examples 1-3

[0020] Raw material name

[0021] lactose

Embodiment 4～6

[0023] Examples 4-6 In order to evaluate the effect of different drug releases, water-soluble hydroxypropyl methylcellulose, and polymers of different viscosities and different grades of transesterification agents. The manufacturing method is wet granulation.

[0024] First, hydroxypropyl methylcellulose was dissolved in absolute ethanol to obtain a mixed solution. In addition, sarcogrelate hydrochloride, hydroxypropyl methylcellulose, and lactose were rotated and stirred at a high speed. After standing for 5 minutes, a mixed solution was obtained. Then slowly add the previously configured mixture, mix and granulate. The prepared granules were dried at 60° C. for 4 hours to obtain granules with a drying loss of less than 2%. Finally, after screening, 1 mm pellets were obtained. Then the granules are placed in the mixer, magnesium stearate is added, mixed for 3 minutes, and compressed with a rotary tablet machine to obtain tablets of 5-8 kgf.

[0025] The composition of tabl...

Embodiment 7～8

[0028] Examples 7-8 are comparative formulations made in order to evaluate the effect of the added amount of hydroxypropyl methylcellulose on drug release.

[0029] The manufacturing method is the same as in Examples 4-6.

[0030] The composition of table 3. embodiment 7~9 (unit: mg / T)

[0031] Raw material name

Example 7

Example 8

Sagrelate Hydrochloride

300

300

Hydroxypropyl methylcellulose 90SH100000

100

50

citric acid

15

15

lactose

50

100

Hydroxypropyl Cellulose

30

30

Magnesium stearate

5

5

total

500

500

[0032] Dissolution rate evaluation

[0033] The target dissolution rate of the sustained-release preparation is defined through pharmacokinetic characteristics and literature materials, below 30% in 1 hour, 30-60% in 4 hours, and above 80% in 10 hours. Taking Anplag (100 mg of sargrelate hydrochloride) produced by YUHAN Compan...

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PUM

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Abstract

The invention provides a low-release sarpogrelate hydrochloride medicament. The main ingredients of the medicament can be continuously released in the gastrointestinal tract for over 10h.

Description

technical field [0001] The present invention utilizes sarcogrelate hydrochloride, which has antithrombotic and vasoconstriction effects, by slowing its release rate and utilizing hydrophilic and fast water media to extend the release time of sarcogrelate hydrochloride to 8-10 hours above. Background technique [0002] The drug release technology is a well-known method of tableting with water-soluble or insoluble polymers together with the drug, and tableting after wet granulation. It has also been mentioned in many patents and papers that the main components of tablets such as water-soluble polymer cellulose derivatives, shellac, zein, etc. A method of coating with insoluble cellulose derivatives, plasticizers such as polyacrylic acid and other additives, drying, and slow release. [0003] The technology of Korean Patent No. 2001-0009439 is to mix cefaclor and hydroxypropyl cellulose, or a polymer of carboxymethyl cellulose together, and to compress the sustained release t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/225A61K47/30A61K9/22A61P7/02A61P9/00A61P9/10
Inventor 崔载胜南庚太郑载勋金志太
Owner 苏州世林医药技术发展有限公司
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