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Momestasone furoate lipidosome cream

A technology of mometasone furoate and liposome, which is applied in liposome delivery, liquid delivery, ointment delivery, etc., can solve the problem that the advantages of liposome administration for external use on the skin cannot be fully utilized, and glucocorticoids are difficult to pack into lipids. Plastids, affecting drug penetration and absorption, etc., to achieve high encapsulation efficiency, less drug dosage, and good stability

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 lipophilic additives is only 1:1~1:3, 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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  • Momestasone furoate lipidosome cream
  • Momestasone furoate lipidosome cream
  • Momestasone furoate 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 Pingpinga-2020g Methylparaben 0.5g Propylparaben 0.05g

[0042] The formula of liposome solution:

[0043] Mometasone furoate 1g Soy lecithin 20g Cholesterol 2g Disodium ethylenediaminetetraacetic acid (EDTA-2Na) 1g α-tocopherol 1g

[0044] Buffer the liposome solution to pH=6.5 in phosphate buffer

[0045] Glycerin 50g

[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 mometasone furoate, phospholipids, cholesterol, and α-tocopherol and di...

Embodiment 2

[0054] Oil Phase Formula:

[0055] White Vaseline 120g Stearyl Alcohol 50g Liquid Paraffin 50g Glyceryl Monostearate 40g Pingpingjia a-20 20g Methylparaben 0.5g Propylparaben 0.05g

[0056] The liposome solution formula is:

[0057] Mometasone furoate 0.5g Hydrogenated soybean lecithin 10g Cholesterol 1g Disodium edetate 1g

[0058] Buffer the liposome solution to pH=6.5 in phosphate buffer

[0059] Distilled water to 1000g (based on the total weight of the composition)

[0060] Glycerin 40g

[0061] Prepare 0.05% mometasone furoate liposome cream as in Example 1.

Embodiment 3

[0063] Oil Phase Formula:

[0064] White Vaseline 60g Cetyl Alcohol 40g Octadecanol 40g Liquid Paraffin 90g Glyceryl Monostearate 20g Pingpinga a-20 40g Methylparaben 0.5g Propylparaben 0.05g

[0065] Liposome Solution Formula:

[0066] Mometasone furoate 0.25g egg yolk lecithin 3g cholesterol 0.6g

[0067] Buffer the liposome solution to pH=6.5 in phosphate buffer

[0068] Distilled water to 1000g (based on the total weight of the composition)

[0069] Prepare 0.025% mometasone furoate liposome cream as in Example 1.

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Abstract

The invention relates to a lipidosome medical composition which uses momestasone furoate as an active component, and a cyst diameter of lipidosome is smaller than 800nm. The composition comprises 0.025 percent to 0.2 percent of momestasone furoate 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 a 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 momestasone furoate 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 mometasone furoate liposome. Background technique [0002] Mometasone furoate (mometasone furoate, CAS: 83919-23-7), its molecular formula is as follows: [0003] [0004] The trade name of mometasone furoate cream is Elocon, which was first developed and listed by Schering Corporation in 1988. At present, there is only one specification of 0.1%, and the manual of Elocon cream (http: / / www.fda.gov / cder / pediatric / labels / Mometasone%20Cream.pdf) discloses that its main component is: mometasone furoate 0.1 %; Excipients: hexylene glycol (hexylene glycol), phosphoric acid, propylene glycol monostearate (55% monoester), stearyl alcohol, ceteareth-20 (ceteareth-20), titanium dioxide, Aluminum octenyl succinate starch, white wax, white petrolatum, purified water, but the drug also has side effects of general skin glucocorticoid preparations, such as inhibition of the HP...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/06A61K31/58A61K47/24A61P5/44A61P17/00
Inventor 李静李娜陈松行健
Owner TIANJIN JINYAO GRP
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