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Methylprednisolone aceponate lipidosome cream

A technology of methylprednisolone acetate and liposome, which is applied in the direction of liposome delivery, oil/fat/wax non-active ingredients, medical preparations of non-active ingredients, etc., which can solve the problem of affecting drug penetration and absorption, and cannot fully exert Advantages of liposome administration for external use on the skin, difficulties in encapsulating glucocorticoids into liposomes, etc.

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)
From the content disclosed in this application, we can draw that hydrophobic glucocorticoids such as acepromethylprednisolone are difficult 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

Method used

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  • Methylprednisolone aceponate lipidosome cream
  • Methylprednisolone aceponate lipidosome cream
  • Methylprednisolone aceponate lipidosome cream

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Recipe for the oil phase:

[0041] White Vaseline 100g Stearyl Alcohol 30g Liquid Paraffin 50g Glyceryl Monostearate 20g Pingpingjia a-2020g Methylparaben 0.5g Propylparaben 0.05g

[0042] The formula of liposome solution:

[0043] Methylprednisolone acetate 1g, soybean lecithin 20g, cholesterol 2g, disodium edetate (EDTA-2Na) 1g, α-tocopherol 1g

[0044] Glycerin 50g

[0045] The liposome solution is buffered to a phosphate buffer of pH=6.5 Distilled water to 1000g (by total weight of the composition)

[0046] Preparation:

[0047] (1) Preparation of oil phase

[0048] 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.

[0049] (2) Preparation of liposome solution

[0050] Weigh the prescribed amount of methyl...

Embodiment 2

[0054] Oil Phase Formula:

[0055] White Vaseline 120g Stearyl Alcohol 50g Liquid Paraffin 50g Glyceryl Monostearate 40g Pingpingjia a-2020g Methylparaben 0.5g Propylparaben 0.05g

[0056] Formulation of liposome solution

[0057] Methylprednisolone acetate 0.5g Hydrogenated soybean lecithin 10g Cholesterol g Disodium edetate 1g

[0058] The liposome solution is buffered to a phosphate buffer of pH=6.5 Distilled water to 1000g (by total weight of the composition)

[0059] The compound method of embodiment 1 makes 0.05% methylprednisolone acetone liposome emulsifiable cream.

Embodiment 3

[0061] Oil Phase Formula:

[0062] White Vaseline 60g Cetyl Alcohol 40g Octadecanol 40g Liquid Paraffin 90g Glyceryl Monostearate 20g Pingpinga-2040g Methylparaben 0.5g Propylparaben 0.05g

[0063] Liposome Solution Formulation

[0064] Methylprednisolone Acetate 0.25g Egg Yolk Lecithin 3g Cholesterol 0.6g

[0065] The liposome solution is buffered to a phosphate buffer of pH=6.5 Distilled water to 1000g (by total weight of the composition)

[0066] The compound method of embodiment 1 makes 0.025% methylprednisolone acetone liposome emulsifiable cream.

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Abstract

The invention relates to a lipidosome medical composition which uses methylprednisolone aceponate 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 methylprednisolone aceponate 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 methylprednisolone aceponate lipidosome cream is used for treating skin diseases of human beings or animals.

Description

field of invention [0001] The invention relates to a liposome preparation, in particular to a cream containing methylprednisolone acetone liposome. Background technique [0002] Methylprednisolone Aceponate (Methylprednisolone Aceponate, CAS: 86401-95-8), its molecular formula is as follows: [0003] [0004] Methylprednisolone acetate trade name is Advantan, which is developed and listed by Schering AG of Germany. At present, there is only one specification of 0.1%. On the instructions of Advantan cream ( http: / / www.betterhealth.vic.gov.au / bhcv2 / bhcmed.nsf / pages / cscadvan / $File / cscadvan.pdf ), we can see that its main component is: methylprednisolone acetate 0.1%; auxiliary material: decyl oleate (decyl oleate), the glycerol monostearate (glycerol monosteartae 40-55% of 40-55% content ), cetostearyl alcohol (cetostearyl alcohol), stearin (hardfat), caprylic acid / capric acid / myristic acid / stearic acid triglyceride / (Softisan 378), polyoxyl (40) stearate ( PEG-40-...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/573A61K47/24A61K47/28A61K47/34A61K47/44A61P17/00A61K47/06A61K47/14
Inventor 李静涂春玲陈松武胜赵琳
Owner TIANJIN JINYAO GRP
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