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Compound clobetasol propionate mixed micellar solution and preparation method thereof

A technology of clobetasol propionate and compound chlorine propionate, which is applied in the field of biomedicine, can solve the problems of increased sample temperature, difficulty, and increased impurity content in the final product, and achieve the effect of increased drug retention and simple preparation process

Active Publication Date: 2012-08-22
JIANGSU SEMPOLL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantages of liposome preparations are: 1) On the one hand, the liposome preparation process is complicated. In order to ensure the uniform particle size of liposomes in the preparation process, it is necessary to use a high-pressure milk homogenizer to repeatedly high-pressure milk homogenate and granulate. A large amount of work is applied to the sample, which increases the temperature of the sample, resulting in an increase in the impurity content of the final product
Finally, the sample will be filtered through a 100nm polycarbonate membrane, and this process requires special equipment; 2) On the other hand, according to the disclosed embodiment of the patent application 201110412475.8, the average particle size of the liposomes is above 100nm. It is difficult to control the average particle size of liposomes in a smaller particle size range

Method used

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  • Compound clobetasol propionate mixed micellar solution and preparation method thereof
  • Compound clobetasol propionate mixed micellar solution and preparation method thereof

Examples

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Effect test

Embodiment 1

[0024] Embodiment 1: a kind of compound clobetasol propionate mixed micelle solution is characterized in that every 1000mg mixed micelle solution contains: clobetasol propionate 0.5mg, tretinoin 0.25mg, hydrogenated phosphatidylcholine 7.5mg mg, sodium cholate 22.5mg, and the balance is purified water.

[0025] Preparation process: take clobetasol propionate, tretinoin, hydrogenated phosphatidylcholine, sodium cholate, dissolve in 30 times the weight of ethanol; 50 ℃, rotary evaporate the organic solvent to obtain drug-mixed micelles co-precipitation Add an appropriate amount of purified water, oscillate and hydrate until the drug-mixed micelle co-precipitate film is completely dissolved, and the drug mixed micelle solution is obtained.

[0026] The encapsulation efficiency of clobetasol propionate in the obtained mixed micelle solution was 94.7%; the encapsulation efficiency of tretinoin was 98.7%; the average particle size was 30.7nm.

Embodiment 2

[0027] Embodiment 2: a kind of compound clobetasol propionate mixed micelle solution is characterized in that every 1000mg mixed micelle solution contains: clobetasol propionate 0.25mg, tretinoin 0.25mg, hydrogenated phosphatidylcholine 10mg , sodium cholate 40mg, and the balance is pH7.4 phosphate buffer.

[0028]Preparation process: Dissolve clobetasol propionate, retinoic acid, hydrogenated phosphatidylcholine, and sodium cholate in 20 times the weight of ethanol until dissolved; 50 ° C, rotary evaporate the organic solvent to obtain drug-mixed micelles Co-precipitate film: Add appropriate amount of pH 7.4 phosphate buffer, oscillate and hydrate until the drug-mixed micelle co-precipitate film is completely dissolved, and the drug mixed micelle solution is obtained.

[0029] The encapsulation efficiency of clobetasol propionate in the obtained mixed micelles solution was 93.2%; the encapsulation efficiency of tretinoin was 92.2%; the average particle size was 42.1nm.

Embodiment 3

[0030] Embodiment 3: a kind of compound clobetasol propionate mixed micelle solution is characterized in that every 1000mg mixed micelle solution contains: clobetasol propionate 0.25mg, tretinoin 0.25mg, phosphatidylethanolamine 10mg, remove Sodium oxycholate 40mg, the balance is pH7.4 phosphate buffer.

[0031] Preparation process: Dissolve clobetasol propionate, retinoic acid, phosphatidylethanolamine, and sodium deoxycholate in 40 times the weight of ethanol until dissolved; 50°C, rotary evaporate the organic solvent to dry up to obtain drug-mixed micelles Co-precipitate film: add an appropriate amount of pH7.4 phosphate buffer, oscillate and hydrate until the drug-mixed micelle co-precipitate film is completely dissolved, and the drug-mixed micelle solution is obtained.

[0032] The encapsulation efficiency of clobetasol propionate in the obtained mixed micelles solution was 85.1%; the encapsulation efficiency of tretinoin was 91.4%; the average particle size was 43.3nm. ...

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Abstract

The invention provides a compound clobetasol propionate mixed micellar solution. Phosphatide and cholate are mainly utilized to prepare the mixed micellar solution which is used for packaging clobetasol propionate and tretinoin. The mixed micelle solution can be simply prepared, and the medicament stability can be guaranteed in the process of preparation. By preparing a mixed micelle system from the phosphatide and the cholate, the problem of medicament dissolution is solved. Compared with a common ointment, the mixed micelle solution has a higher retention volume on skins, and the quantity of the medicament on local skins and the therapeutic index can be increased. The mixed micelle solution can be further prepared into an ointment and a gel, and is mainly used for treating psoriasis vulgaris, dermatitis, eczema, etc.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a compound clobetasol propionate and all-trans retinoic acid mixed micelle solution and a preparation method thereof. The micelle solution has the characteristics of high skin penetration and high skin drug retention , which can be further prepared into gels and creams, mainly used for treating psoriasis vulgaris, dermatitis, eczema and other diseases. Background technique [0002] Both clobetasol propionate and retinoic acid are commonly used topical dermatological treatments with definite curative effects. Clobetasol propionate (CP) is a powerful hormone, long-term use can cause side effects such as skin atrophy, and the common side effect of tretinoin use is skin irritation. In addition, transdermal absorption of drugs into the blood circulation system will produce systemic toxic and side effects. Therefore existing open technology is devoted to utilizing compound pres...

Claims

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Application Information

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IPC IPC(8): A61K31/573A61K9/00A61K47/28A61P17/00A61P17/06A61K31/203
Inventor 付劼周海滨张新明
Owner JIANGSU SEMPOLL PHARMA
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