Sarpogrelate hydrochloride lipidosome solid preparation

A technology of sarcogrelate hydrochloride lipid and solid preparations, which is applied in the field of pharmaceutical preparations, can solve the problems of poor production controllability, unsatisfactory reproducibility of sustained-release effects of preparations, low bioavailability of sarcogrelate hydrochloride, etc., and achieve Improve bioavailability, improve drug compliance, and increase retention time

Inactive Publication Date: 2013-04-17
海南路易丹尼生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] There are disadvantages in the sargrelate hydrochloride drug sustained-release preparations described in the above two patents
The controllability of production is not good, the sustained-release effect reproducibility of the preparation after long-term storage is not ideal, and the bioavailability of sargrelate hydrochloride is low; thus, a new preparation process and method are urgently needed, and the liposome technology application, can solve these shortcomings of the existing formulations of sarcogrelate hydrochloride

Method used

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  • Sarpogrelate hydrochloride lipidosome solid preparation
  • Sarpogrelate hydrochloride lipidosome solid preparation
  • Sarpogrelate hydrochloride lipidosome solid preparation

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preparation example Construction

[0061] According to another aspect of the present invention, the preparation method of above-mentioned sarcogrelate hydrochloride liposome is provided, and the method comprises the following steps:

[0062] (a) Dissolve dilauroylphosphatidylcholine, phosphatidylethanolamine, phosphatidylglycerol and cholesterol in an organic solvent, mix well and sonicate for 30 minutes to prepare blank liposomes;

[0063] (b) Dissolving sarcogrelate hydrochloride in blank liposome suspension, incubating at 59° C. for 30-40 minutes, ultrasonication for 30-40 minutes, filtering through a 0.45 μm microporous membrane, and freeze-drying to obtain a solid liposome.

[0064] In a preferred embodiment of the method for preparing sarcogrelate hydrochloride liposomes according to the present invention, in step (a), the organic solvent is selected from the group consisting of ethanol, methanol, acetone, ether, chloroform, n-hexane, di One of methyl chloride, preferably ethanol solvent.

[0065] In a p...

Embodiment 1

[0091] The preparation of embodiment 1 sarcogrelate hydrochloride liposome sheet

[0092] The raw materials used are as follows:

[0093]

[0094] The preparation process is as follows:

[0095] (1) Dissolve 100g of dilauroylphosphatidylcholine, 100g of phosphatidylethanolamine, 100g of phosphatidylglycerol and 100g of cholesterol in 800ml of ethanol, mix well and sonicate for 30 minutes to make a blank liposome;

[0096] (2) Dissolve 100 g of sarcogrelate hydrochloride in the blank liposome suspension, incubate at 59° C. for 30 minutes and sonicate, filter through a 0.45 μm microporous membrane, and freeze-dry to obtain solid liposomes;

[0097] (3) Sieve the sarcogrelate hydrochloride liposome solid through an 80-mesh sieve, then mix it with 50 g of microcrystalline cellulose and 40 g of low-substituted hydroxypropyl cellulose, and mix evenly through a sieve, then add 5% povidone K30 in 50% ethanol solution Wet 100ml to prepare soft material, pass through a 24 mesh siev...

Embodiment 2

[0100] The preparation of embodiment 2 sarcogrelate hydrochloride liposome sheet

[0101] The raw materials used are as follows:

[0102]

[0103] The preparation process is as follows:

[0104] (1) Dissolve 240g of dilauroylphosphatidylcholine, 100g of phosphatidylethanolamine, 150g of phosphatidylglycerol and 150g of cholesterol in 1000ml of ethanol, mix well and sonicate for 30 minutes to make a blank liposome;

[0105] (2) Dissolve 100 g of sarcogrelate hydrochloride in the blank liposome suspension, incubate at 59° C. for 30 minutes and sonicate, filter through a 0.45 μm microporous membrane, and freeze-dry to obtain solid liposomes;

[0106] (3) Sieve the sarcogrelate hydrochloride liposome solid through an 80-mesh sieve, then mix it with 60 g of microcrystalline cellulose and 50 g of low-substituted hydroxypropyl cellulose, sieve and mix evenly, and add 5% povidone K30 in 50% ethanol solution Wet 120ml to prepare soft material, granulate through 24 mesh sieve, and ...

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Abstract

The invention relates to a sarpogrelate hydrochloride lipidosome solid preparation and a preparation method thereof. The preparation method comprises the following steps: selecting sarpogrelate hydrochloride, dilauroyl phosphatidylcholine, phosphatidyl ethanolamine, phosphatidyl glycerol and cholesterol with specific weight ratio to prepare sarpogrelate hydrochloride lipidosome with excellent quality; and preparing the solid preparation by the common preparation method. Compared with the conventional preparation, the preparation provided by the invention improves the stability, the bioavailability and the product quality of the preparation and reduces the toxic or side effect.

Description

technical field [0001] The invention relates to a liposome solid preparation and a preparation method thereof, in particular to a sargrelate hydrochloride liposome solid preparation and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. Background technique [0002] Sarpogrelate hydrochloride, chemical name: (+ / -)-2-(dimethylamino)-1-{[2-(3-methoxyphenyl)phenoxy]methyl} Ethylsuccinate monoester hydrochloride, formula C 24 h 31 NO 6 HCl, molecular weight: 466.02, structural formula: [0003] [0004] Sagrelate hydrochloride is a white or off-white powder, easily soluble in water and ethanol. It is a 5-HT receptor blocker developed by Mitsubishi Corporation, a cardiovascular drug. Launched in the market in 1993, it is clinically used to improve ischemic symptoms such as ulcers, pain and cold sensation caused by chronic arterial occlusive disease. The pharmacological characteristics are: (1) inhibition of platelet aggregatio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/225A61K47/28A61K47/24A61P9/10A61P7/02A61P9/00
Inventor 王平
Owner 海南路易丹尼生物科技有限公司
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