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Pharmaceutical composition of compound clindamycin and tazarotene lipid complex

A technology of lipid complexes and tazarotene, which is applied in the directions of drug combinations, pharmaceutical formulations, and non-active ingredients medical preparations, etc., can solve the problems of unsatisfactory effects, poor skin drug retention, and drug permeability. Not ideal and other problems, to achieve the effect of increasing the drug content, prolonging the onset time, and improving the therapeutic index

Active Publication Date: 2013-11-27
CHINA RESOURCES SANJIU MEDICAL & PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the skin drug retention of this patented preparation is still relatively poor, and the drug penetration rate is not ideal. These effects are not satisfactory.

Method used

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  • Pharmaceutical composition of compound clindamycin and tazarotene lipid complex
  • Pharmaceutical composition of compound clindamycin and tazarotene lipid complex
  • Pharmaceutical composition of compound clindamycin and tazarotene lipid complex

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1- Embodiment 3

[0055] Example 1-Example 3: Compound Tazarotene Clindamycin Lipid Complex Cream

[0056]

[0057] The preparation steps are: dissolving tazarotene, phosphatidylserine and stearamide in a mixture of methylene chloride and ethanol 9-10 times the weight, the ratio of the mixture of methylene chloride and ethanol is 1:1, and then placing In a rotary evaporator, evaporate the organic solvent at 50-60°C to form a drug phospholipid film, add an appropriate volume of phosphate buffer with a pH value of 4.5-5.5, oscillate for hydration, and form a crude lipid complex suspension liquid, and then the lipoplex suspension was homogenized twice through high-pressure milk, and finally passed through a 100nm polycarbonate membrane to obtain a drug-loaded lipoplex suspension.

[0058] Take liquid paraffin and white petrolatum as the oil phase matrix and heat to 80°C to melt; take the above-mentioned drug-loaded lipid complex suspension, dilute with purified water, add Tween 80, glycerin, an...

Embodiment 4- Embodiment 6

[0059] Example 4-Example 6: Compound Tazarotene Clindamycin Lipid Complex Gel

[0060]

[0061] The preparation steps are: dissolving tazarotene, phosphatidylserine and stearamide in a mixture of methylene chloride and ethanol 9-10 times the weight, the ratio of the mixture of methylene chloride and ethanol is 1:1, and then, Place in a rotary evaporator, evaporate the organic solvent at 50-60°C to form a drug phospholipid film, add an appropriate volume of phosphate buffer with a pH value of 4.5-5.5, oscillate to hydrate, and form a lipoplex suspension solution, and then the lipoplex suspension was passed through high-pressure milk twice, and finally passed through a 100nm polycarbonate membrane.

[0062] Take the drug-encapsulated lipid complex suspension prepared above, dilute it with purified water, add Carbomer 940 gel matrix to disperse and fully swell, adjust the pH value to 7-8 with triethylamine, and add in turn Disodium diacetate and benzyl alcohol are stirred eve...

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Abstract

The invention provides a lipid complex of tazarotene and clindamycin phosphate. The lipid complex is prepared mainly by utilizing synthetic phospholipids and stearamide, is wrapped with tazarotene and is further mixed with the clindamycin to prepare cream and gel which are mainly used for treating acne vulgaris. The lipid complex is simple in preparation technique, and the stability of pharmaceuticals can be ensured in the preparation process; compared with the common cream and gel, the lipid complex has the advantages that the skin medicine retention volume is higher, the content of medicine in local skins can be increased, and the therapeutic index can be improved.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing tazarotene lipid complex and clindamycin, which is mainly used for treating acne, especially acne vulgaris. Background technique [0002] Acne is a chronic inflammatory skin disease involving the pilosebaceous glands. It is prone to occur in seborrhea, and can be manifested as comedones, papules, pustules, nodules, cysts, and scars. The exact etiology is still unknown. It is thought that the main factors associated with its cause include increased sebum secretion, development of inflammation by androgens that stimulate the sebaceous glands and Propionibacterium acnes that multiply in the pilosebaceous glands to degrade sebum to form free fatty acids, follicular parakeratosis and genetic predisposition. Acne vulgaris is a type of acne that is especially common in adolescent girls and boys. Acne vulgaris is a chronic inflammatory skin disease that occurs in the pilosebaceous glands. Its p...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/7056A61K31/455A61K9/06A61P17/10
Inventor 付劼张新明尤斌
Owner CHINA RESOURCES SANJIU MEDICAL & PHARMA
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