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Prednicarbate lipidosome cream

A technology of prenicalate and liposomes, which is applied in the field of creams containing prednicamid liposomes, can solve the problem of affecting the penetration and absorption of drugs, unable to give full play to the advantages of liposome administration for external use on the skin, and glucocorticoids. Problems such as difficulty in loading hormones into liposomes

Inactive Publication Date: 2009-12-16
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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)
[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

Method used

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  • Prednicarbate lipidosome cream
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  • Prednicarbate lipidosome cream

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Recipe for the oil phase:

[0042] White Vaseline 100g Stearyl Alcohol 30g Liquid Paraffin 50g Glyceryl Monostearate 20g Pingpinga-2020g Methylparaben 0.5g Propylparaben 0.05g

[0043] The formula of liposome solution:

[0044] Prednicate 1g Soy lecithin 20g Cholesterol 2g Disodium ethylenediaminetetraacetic acid (EDTA-2Na) 1g α-tocopherol 1g

[0045] Buffer the liposome solution to pH=6.5 in phosphate buffer

[0046] Glycerin 50g

[0047] Distilled water to 1000g (based on the total weight of the composition)

[0048] Preparation:

[0049] (1) Preparation of oil phase

[0050] Take the prescribed amount of oil phase ingredients and heat to 70°C, add paraben dissolved in an appropriate amount of organic solvent, then take the prescribed amount of moisturizer and heat it to the same temperature and slowly add it to the oil phase, and stir until it is uniform while adding. have to.

[0051] (2) Preparation of liposome solution

[0052] Prednicate, phospholipids, c...

Embodiment 2

[0056] Oil Phase Formula:

[0057] White Vaseline 120g Stearyl Alcohol 50g Liquid Paraffin 50g Glyceryl Monostearate 40g Pingpingjia a-20 20g Methylparaben 0.5g Propylparaben 0.05g

[0058] The liposome solution formula is:

[0059] Prednicate 0.5g Hydrogenated soybean lecithin 10g Cholesterol 1g Disodium edetate 1g Glycerin 40g

[0060] Buffer the liposome solution to pH=6.5 in phosphate buffer

[0061] Distilled water to 1000g (based on the total weight of the composition)

[0062] Prepare 0.05% prednicardate liposome emulsifiable cream as the compound method of embodiment 1.

Embodiment 3

[0064] Oil Phase Formula:

[0065] White Vaseline 60g Cetyl Alcohol 40g Octadecanol 40g Liquid Paraffin 90g Glyceryl Monostearate 20g Pingpinga a-20 40g Methylparaben 0.5g Propylparaben 0.05g

[0066] Liposome Solution Formula:

[0067] Prednicate 0.25g Egg yolk lecithin 3g Cholesterol 0.6g

[0068] Buffer the liposome solution to pH=6.5 in phosphate buffer

[0069] Distilled water to 1000g (based on the total weight of the composition)

[0070] Prepare 0.025% prednicardate liposome emulsifiable cream as the compound method of embodiment 1.

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Abstract

The invention relates to a lipidosome medical composition which uses prednicarbate 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 prednicarbate 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 components, 0.01 percent to 0.1 percent of antimicrobial preservative and the balanced of water. The prednicarbate lipidosome cream is used for treating skin diseases of human beings or animals.

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] ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/06A61K31/573A61K47/24A61P5/44
Inventor 涂春玲张其婉李娜
Owner TIANJIN JINYAO GRP
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