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Repaglinide liposome solid preparation

A technology of liposome tablets and liposomes, which is applied in the field of repaglinide liposome solid preparations and new solid preparations of antidiabetic drug repaglinide, which can solve the problem of bioavailability and long-term stability. , the slow onset of the pharmaceutical composition and other problems, to achieve the effects of improving bioavailability, improving drug compliance, and reducing the number of administrations

Inactive Publication Date: 2014-07-02
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This patent also protects the composition of repaglinide and a pharmaceutically acceptable carrier and its preparation method, but the pharmaceutical composition it protects has a slow onset of action, which is worthwhile and needs to be improved
[0006] Patent document CN101695491A discloses a slow-release formulation of repaglinide and its preparation method. The formulation has been carefully screened to solve the problem of poor solubility of the drug, but the bioavailability and long-term stability need to be improved.

Method used

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  • Repaglinide liposome solid preparation
  • Repaglinide liposome solid preparation
  • Repaglinide liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Example 1 Preparation of Repaglinide Liposome Tablets

[0062] Prescription: (1000 tablets)

[0063]

[0064] Adopt the following production process to prepare repaglinide liposome tablet:

[0065] (1) Dissolve 0.5g repaglinide in a mixed solution of 5ml ethanol and chloroform;

[0066] (2) Dissolve 11g of egg yolk lecithin, 3g of soybean sterol and 3.25g of dilauroylphosphatidylglycerol in a mixed solution of 50ml of ethanol and chloroform, then pour (1) quickly, mix well, and keep warm at 59°C for 30-40 Minutes, then remove the organic solvent under reduced pressure with a rotary vacuum drier to obtain a liposome solid;

[0067] (3) Mix repaglinide liposome solid with 31.95g lactose, 31.95g microcrystalline cellulose and 5.325g low-substituted hydroxypropyl cellulose, pass through an 80 mesh sieve and mix evenly, add 5% povidone K30 50ml of 50% ethanol solution prepares soft materials, passes through 24 mesh sieves, granulates, and dries;

[0068] (4) Mix the...

Embodiment 2

[0069] Example 2 Preparation of Repaglinide Liposome Tablets

[0070] Prescription: (1000 tablets)

[0071]

[0072] Adopt the following production process to prepare repaglinide liposome tablet:

[0073] (1) Dissolve 1g repaglinide in a mixed solution of 5ml ethanol and chloroform;

[0074] (2) Dissolve 20g of egg yolk lecithin, 4g of soybean sterol and 5g of dilauroylphosphatidylglycerol in a mixed solution of 50ml of ethanol and chloroform, then pour (1) quickly, mix well, and keep warm at 55°C for 30-40 minutes , and then remove the organic solvent under reduced pressure with a rotary vacuum dryer to obtain a liposome solid;

[0075] (3) Mix repaglinide liposome solid with 45g lactose, 45g microcrystalline cellulose and 6g low-substituted hydroxypropyl cellulose, pass through an 80 mesh sieve and mix evenly, add 50% of 5% povidone K30 Prepare soft material with 80ml of ethanol solution, pass through a 24-mesh sieve to granulate, and dry;

[0076] (4) Mix the dry g...

Embodiment 3

[0077] Example 3 Preparation of Repaglinide Liposome Tablets

[0078] Prescription: (1000 tablets)

[0079]

[0080] Adopt the following production process to prepare repaglinide liposome tablet:

[0081] (1) Dissolve 2g repaglinide in a mixed solution of 10ml ethanol and chloroform;

[0082] (2) Dissolve 48g of egg yolk lecithin, 16g of soybean sterol and 16g of dilauroylphosphatidylglycerol in a mixed solution of 100ml of ethanol and chloroform, then pour (1) quickly, mix well, and keep warm at 60°C for 30-40 minutes , and then remove the organic solvent under reduced pressure with a rotary vacuum dryer to obtain a liposome solid;

[0083] (3) Mix repaglinide liposome solid with 174g lactose, 174g microcrystalline cellulose and 34g low-substituted hydroxypropyl cellulose, pass through an 80 mesh sieve and mix evenly, add 50% of 5% povidone K30 Prepare soft material with 200ml of ethanol solution, pass through a 24-mesh sieve to granulate, and dry;

[0084] (4) Mix t...

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Abstract

The invention provides a repaglinide liposome solid preparation, and a preparation method thereof. According to the invention, repaglinide, ovolecithin, soyasterol, and dilauroyl phosphatidyl glycerol with a certain weight ratio are prepared into repaglinide liposome with excellent quality; and the repaglinide liposome is prepared into a solid preparation with a common preparation method. Compared with existing preparations, the preparation provided by the invention is advantaged in substantially improved preparation stability, bioavailability, product quality, and release-retarding effect, and reduced toxic and side effects.

Description

technical field [0001] The invention relates to a new solid preparation of repaglinide, an antidiabetic drug, in particular to a repaglinide liposome solid preparation, which belongs to the field of pharmaceutical preparations. Background technique [0002] Repaglinide is a white or off-white crystalline powder, odorless, easily soluble in chloroform, slightly soluble in ethanol or acetone, almost insoluble in water, slightly soluble in 0.1mol / L hydrochloric acid solution. The chemical name is (S+)-2-ethoxy-4-[2-[3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]-amino]-2-carbonyl ethyl benzoic acid, molecular formula C 27 h 36 N 2 o 4 , molecular weight: 452.59, structural formula: [0003] [0004] Repaglinide is a new type of oral hypoglycemic drug of the methylbenzylamine benzoic acid family. It is a non-sulfonylurea oral hypoglycemic drug for the treatment of type 2 diabetes. Its mechanism of action is that repaglinide interacts with pancreatic beta Binding to specific...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/451A61K47/24A61K47/28A61P3/10
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA
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