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Clopidogrel bisulfate liposome solid preparation

A technology of clopidogrel bisulfate lipid and clopidogrel bisulfate lipid, which is applied in the field of medicine to achieve the effects of good sustained release, excellent dissolution and high bioavailability

Inactive Publication Date: 2012-04-04
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Clopidogrel is usually administered in the form of clopidogrel sulfate (i.e. clopidogrel bisulfate), currently on the market only tablets, but this tablet has the following problems: the clopidogrel bisulfate tablet Clopidogrel is easier to convert to clopidogrel acid, and clopidogrel D-isomer is easier to convert to L-isomer
[0016] However, the challenge in preparing liposomes lies in selecting the appropriate liposome composition and formulation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Example 1 Clopidogrel bisulfate liposome tablet

[0079] The raw materials used are as follows:

[0080]

[0081] The following production process was used to prepare clopidogrel hydrogen sulfate liposomal tablets:

[0082] (1) Accurately weigh 25g clopidogrel hydrogen sulfate, 160g phosphatidylethanolamine, 40g stearamide, 100g cholesterol, 50g Tween 80, dissolve in 1200ml volume ratio and be 2:1 dichloromethane and isopropanol mixed solvent , stir to dissolve;

[0083] (2) above-mentioned solution is placed in eggplant-shaped bottle, 45 ℃ of water bath decompression removes methylene chloride and isopropanol, and forms uniform transparent film on the bottle wall;

[0084] (3) Add 1200ml of phosphate buffer solution with a pH value of 7.0 to the eggplant-shaped bottle, and continue to rotate at a normal pressure in a water bath at 45°C to swell and hydrate the film;

[0085] (4) filtering the above solution with a 0.45 microporous membrane, placing the filtrate...

Embodiment 2

[0089] Example 2 Clopidogrel bisulfate liposome tablet

[0090] The raw materials used are as follows:

[0091]

[0092]

[0093] The following production process was used to prepare clopidogrel bisulfate liposomal tablets:

[0094] (1) Accurately weigh 75g of clopidogrel hydrogen sulfate, 200g of phosphatidylethanolamine, 50g of stearamide, 200g of cholesterol, 80g of Tween 80, and dissolved in 1500ml of dichloromethane and isopropanol mixed solvent with a volume ratio of 2:1 , stir to dissolve;

[0095] (2) above-mentioned solution is placed in eggplant-shaped bottle, 45 ℃ of water bath decompression removes methylene chloride and isopropanol, and forms uniform transparent film on the bottle wall;

[0096] (3) Add 1500ml of phosphate buffer solution with pH value of 7.0 to the eggplant-shaped bottle, and continue to rotate at 45°C under normal pressure in a water bath to swell and hydrate the film;

[0097] (4) filtering the above solution with a 0.45 microporous ...

Embodiment 3

[0101] Example 3 Clopidogrel bisulfate liposome granules

[0102]

[0103]

[0104] The clopidogrel bisulfate liposome granules are prepared by the following production process:

[0105] (1) Accurately weigh 75g of clopidogrel hydrogen sulfate, 300g of phosphatidylethanolamine, 75g of stearamide, 200g of cholesterol, 120g of Tween 80 and dissolve them in 2000ml of dichloromethane and isopropanol mixed solvent whose volume ratio is 2:1 , stir to dissolve;

[0106] (2) above-mentioned solution is placed in eggplant-shaped bottle, 45 ℃ of water bath decompression removes methylene chloride and isopropanol, and forms uniform transparent film on the bottle wall;

[0107] (3) Add 2000ml of phosphate buffer solution with a pH value of 7.0 to the eggplant-shaped bottle, and continue to rotate at a normal pressure in a water bath at 45°C to swell and hydrate the film;

[0108] (4) filtering the above solution with a 0.45 microporous membrane, placing the filtrate in a -20°C r...

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Abstract

The invention discloses a clopidogrel bisulfate liposome solid preparation and a preparation method thereof. According to the invention, an active component clopidogrel bisulfate, and phosphatidyl ethanolamine, stearic amide, cholesterol and tween 80 with a certain composition are prepared into a liposome, such that the stability, dissolution rate, and bioavailability of the medicine are substantially improved. Also, the prepared medicine is advantaged in stable and durable effect, and substantial curative effect. With the preparation provided by he invention, product quality of the preparation is improved, and toxic and side-effects are reduced.

Description

technical field [0001] The invention relates to a new solid preparation of clopidogrel hydrogen sulfate, in particular to a liposome solid preparation of clopidogrel hydrogen sulfate and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Clopidogrel bisulfate (Clopidogrel Bisulfate) is a new drug—clopidogrel bisulfate (trade name: Plavix) developed by the Research and Development Department of Sanofi-Santa Delaberg, France. The chemical name of clopidogrel hydrogen sulfate is: 2-(2-chlorophenyl)-2-(6,7-dihydrothieno[3,2-c]pyridin-5-yl)acetate methyl hydrogensulfate , molecular formula: C 16 h 16 ClNO 2 S·H 2 SO 4 , molecular weight: 419.90, the structural formula is as follows: [0003] [0004] Clopidogrel bisulfate is a platelet aggregation inhibitor with a unique mechanism of action (ADP receptor antagonism), which specifically and potently inhibits ADP-induced platelet aggregation. For patients at high risk...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/16A61K9/20A61K31/4365A61K47/34A61P7/02
Inventor 陶灵刚
Owner HAINAN LINGKANG PHARMA CO LTD
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