Fluticasone propionate lipidosome cream

Abstract

The invention relates to a lipidosome medical composition which uses fluticasone propionate as an active component, and a cyst diameter of lipidosome is smaller than 800 nm. The composition comprises 0.025 percent to 0.2 percent of fluticasone propionate as the active component, 0.5 percent to 6 percent of phospholipid, 0 percent to 1 percent of lipophilic additive, 0.01 percent to 1 percent of antioxidant which is used for preserving the medical composition, a pH buffering agent which is used for retaining the pH value from 5 to 7.5, 3 percent to 15 percent of humectant, 20 percent to 30 percent of oil phrase component, 0.01 percent to 0.1 percent of antimicrobial preservative and the balanced of water. The fluticasone propionate lipidosome cream is used for treating skin diseases of human beings or animals.

Description

field of invention [0001] The invention relates to a skin composition containing fluticasone propionate liposome. Background technique [0002] Fluticasone propionate (fluticasone propionate, CAS: 80474-14-2), its molecular formula is as follows: [0003] [0004] The trade name of fluticasone propionate cream is CUTIVATE, which was first developed and listed by Glaxo (GSK) in 1988. At present, there is only one specification of 0.05% content, and the specification of CUTIVATE cream (http: / / 69.20.19.211 / cder / pediatric / labels / Fluticasone-Cutivate.pdf) discloses that its main ingredient is: fluticasone propionate 0.05%; Excipients: liquid paraffin, microcrystalline wax, propylene glycol, and sorbitan sesquioleate. However, this drug also has side effects of general skin corticosteroid preparations, such as inhibition of the HPA axis, long-term large-scale use The resulting Cushing's syndrome (Cushing's) can cause skin thinning, skin display telangiectasia, and cause skin ...

AI Technical Summary

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)

From the content disclosed in this application, we can conclude that it is difficult for hydrophobic glucocorticoids such as fluticasone propionate to be loaded into liposomes.

[0008] 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 amount of cholesterol and phospholipids as a lipophilic additive is only 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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