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Compound clobetasol propionate liposome and preparation thereof

A technology of liposome preparation and compound propionate chloride, which is applied in the field of diseases, can solve the problems that unfavorable drugs can penetrate the stratum corneum, can not be prepared at the same time, and have a large particle size range, so as to achieve small particle size, improve stability, and large The effect of the envelope volume

Active Publication Date: 2012-05-02
JIANGSU SEMPOLL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Chinese patent (CN 100346773C) discloses a liposome preparation of clobetasol propionate, but the liposome preparation has a particle size range of 2000nm-5000nm, which is large in size, which is not conducive to the drug penetrating the stratum corneum to play a role
Clobetasol propionate cannot be combined with calcium ions, so this method cannot simultaneously take into account the preparation of retinoic acid and clobetasol propionate liposomes (Chinese Pharmacy, 2006, Volume 17, No. 8, page P579 )

Method used

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  • Compound clobetasol propionate liposome and preparation thereof
  • Compound clobetasol propionate liposome and preparation thereof
  • Compound clobetasol propionate liposome and preparation thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Embodiment 1: the preparation of drug liposome solution

[0030] Table 1 The prescription table of compound clobetasovitrin A acid liposome solution

[0031] name Quantity, g / 100g Clobetasol Propionate 0.10 Tretinoin 0.05 HSPCs 1.00 Dimyristoylphosphatidylcholine 1.00 Stearamide 0.40 cholesterol 1.00 pH7.4 Phosphate Buffer 96.35

[0032] Preparation process: Dissolve clobetasol propionate, retinoic acid, HSPC, dimyristoylphosphatidylcholine, stearylamide, and cholesterol in 6 times the weight of ethanol, and then slowly inject the drug solution through a syringe Heated to 50°C (and stirred by magnetic force) in the pH7.4 phosphate buffer, after the addition, kept stirring until the ethanol was completely removed, then the liposome suspension was passed through high-pressure milk twice, and finally passed through 100nm polymer Carbonate membrane to obtain liposome solution.

[0033] The encapsulation efficiency...

Embodiment 2

[0034] Embodiment 2: the preparation of drug liposome solution

[0035] Table 2 The prescription table of compound clobetasol propionate liposome solution

[0036] name Quantity, g / 100g Clobetasol Propionate 0.50 Tretinoin 0.50 Dipalmitoylphosphatidylcholine 1.50 dilauroylphosphatidylcholine 0.50 Stearamide 0.20 cholesterol 0.70 pH7.4 Phosphate Buffer 96.10

[0037] Preparation process: Dissolve clobetasol propionate, tretinoin, dipalmitoylphosphatidylcholine, dilauroylphosphatidylcholine, stearylamide, and cholesterol in 6 times the weight of ethanol, and then dissolve the liquid Slowly inject the pH 7.4 phosphate buffer solution heated to 50°C (with magnetic stirring) through the syringe. After the addition, keep stirring until the ethanol is completely removed, and then pass the liposome suspension through high-pressure milk for a second time. , and finally pass through a 100nm polycarbonate membrane to obtain a li...

Embodiment 3

[0040] Embodiment 3: the preparation of drug liposome solution

[0041] Table 3 The prescription table of compound clobetasovitrin A acid liposome solution

[0042] name Quantity, g / 100g Clobetasol Propionate 0.10 Tretinoin 0.05 HSPCs 0.50 dilauroylphosphatidylcholine 0.50 Stearamide 0.50 cholesterol 1.00 pH7.4 Phosphate Buffer 97.35

[0043] Preparation process: Dissolve clobetasol propionate, retinoic acid, HSPC, dilauroylphosphatidylcholine, stearylamide, and cholesterol in 6 times the weight of ethanol, and then slowly inject the drug solution through a syringe to heat Put it into the pH7.4 phosphate buffer at 50°C (with magnetic stirring). After the addition, keep stirring until the ethanol is completely removed, then pass the liposome suspension through high-pressure milk twice, and finally pass through 100nm polycarbonate Ester film, namely liposome solution.

[0044] The encapsulation efficiency of clobetasol ...

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Abstract

The invention provides a compound clobetasol propionate liposome and a preparation thereof, which are mainly used for treating diseases such as psoriasis vulgaris, dermatitis, eczema and the like. The liposome prepared from neutral synthetic phospholipids, lipids with positive charges, and cholesterol can coat clobetasol propionate and vitamin A acid simultaneously, and is added with a cream substrate or gel substrate to be prepared into compound clobetasol propionate liposome cream or gel. Compared with the common cream, the liposome preparation has the advantages that: the amount of the medicine retained in skin is larger, the skin penetration rate is lower, the content of the medicine in local skin can be improved, the treatment index is improved, and transdermal absorption dose is reduced, so that the toxic and side effects of the medicine are reduced.

Description

[0001] technical field [0002] The invention relates to a skin composition of compound clobetasol propionate and all-trans retinoic acid liposome, which is mainly used for treating diseases such as psoriasis vulgaris, dermatitis and eczema. Background technique [0003] Clobetasol propionate (CP) is a potent hormone with strong anti-inflammatory, anti-pruritic and vasoconstrictive effects, and is widely used in the treatment of chronic eczema, neurodermatitis, psoriasis and other corticosteroid topical treatments Effective for skin disorders. Clobetasol propionate is also the main representative of corticosteroid drugs in several commonly used methods of Western medicine treatment of psoriasis. Because it is a potent corticosteroid, clobetasol propionate will produce more obvious toxic and side effects during use, for example, irritation such as erythema, burning, itching, folliculitis, skin atrophy and thinning, capillary Symptoms such as vasodilation can also cause dry ...

Claims

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Application Information

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IPC IPC(8): A61K31/57A61K31/203A61K9/127A61K9/107A61P17/06A61P17/00
Inventor 付劼周海滨张新明
Owner JIANGSU SEMPOLL PHARMA
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