prednicate liposomal cream

Abstract

A liposome pharmaceutical composition with prednicate as an active ingredient and a liposome vesicle diameter less than 800nm, the composition contains 0.025% to 0.2% of prednicate and 0.5% to 6% of phospholipids as active ingredients %, lipophilic additive 0-1%, antioxidant 0.01-1% for preserving the pharmaceutical composition, pH buffer to maintain the pH value at 5-7.5, moisturizing agent 3%-15%, oil phase components 20% to 30%, antibacterial and preservative 0.01% to 0.1%, and the rest of water, used to treat human or animal skin diseases.

Description

field of invention [0001] The present invention relates to a kind of liposome preparation, particularly a kind of emulsifiable paste containing prednicate liposome. Background technique [0002] Prednicarbate (prednicarbate, CAS: 73771-04-7), that is, prednisolone-17 ethyl carbonate, is a new high-efficiency glucocorticoid invented by HOECHSTAG (DE) in 1978. Its molecular formula is as follows: [0003] [0004] The U.S. FDA approved the 0.1% prednicarbate cream (prednicarbate ointment) of Sanofi-Aventis in March, 2007 as a dermatological drug (trade name: Dermatop). The adjuvant used in this cream is white petrolatum, octyldodecanol, glyceryl monooleate, propylene glycol, citric acid and propyl gallate, but this medicine also has side effects of general skin corticosteroid preparations, such as long-term Extensive use can cause inhibition of the HPA axis, Cushing's syndrome, etc., ( http: / / products.sanofi-aventis.us / dermatop ointment / dermatop ointment.pdf ). [0005] ...

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Problems solved by technology

[0006] Chinese patent application CN200380107482.0 discloses a liposome preparation containing water-soluble glucocorticoids, but the technical scheme of the application only discloses that it is suitable for water-soluble glucocorticoids such as dexamethasone sodium phosphate, etc.

[0007] Chinese patent application CN200580035942.2 discloses a liposome composition of glucocorticoids and glucocorticoid derivatives, yet the technical scheme of the application only discloses the liposome composition applicable to amphiphilic weakly basic glucocorticoids such as methylprednisolone succinate Sodium acid, and pointed out in this application specification that hydrophobic glucocorticoid (GC) is difficult to pack into liposome (instruction page 6)

[0009] Chinese patent ZL 01812895.5 discloses a liposome preparation containing the hydrophobic glucocorticoid clobetasol propionate. In the technical scheme disclosed by the invention, it is preferably made into a gel, but in the technical scheme disclosed in this patent , the ratio of the amount of cholesterol and phospholipids used as a lipophilic additive is 1:1 to 1:3, and the diameter of liposome vesicles is as high as 2000-5000nm. The liposome vesicle diameter of the liposome is relatively large, which affects the penetration and absorption of the drug, and cannot give full play to the advantages of liposome administration for external use on the skin

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