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Compound clobetasol propionate lipid composite ointment and preparation method thereof

A technology of clobetasol propionate and lipid complex, which is applied in the direction of ointment delivery, effective ingredients of hydroxyl compounds, drug combination, etc., can solve problems such as difficult simultaneous uniform dispersion, tretinoin instability, and unconsidered, etc. Achieve the effect of small particle size, good skin relative targeting, particle size and uniformity

Active Publication Date: 2015-06-24
JIANGSU SEMPOLL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, because tretinoin is unstable and prone to oxidative degradation, although the above invention added antioxidant components to delay the degradation of the drug during the further preparation of the preparation, it did not take into account that when using composite oxidants, different composite oxidants have different solubility and are difficult to disperse uniformly at the same time in the same preparation system

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1: the preparation of drug lipoplex

[0039] The prescription form of table 1 drug lipoplex

[0040] name

Dosage

Clobetasol Propionate

5mg

Tretinoin

2.5mg

Hydrogenated Phosphatidylcholine

50mg

Stearamide

100mg

pH 5.0 phosphate buffer was added to

1000mg

[0041] Preparation process: Dissolve clobetasol propionate, retinoic acid, hydrogenated phosphatidylcholine, and stearylamide in 10 times the weight of ethanol; at 50°C, spin dry the organic solvent to obtain a drug-phospholipid co-precipitate Film: add pH 5.0 phosphate buffer, oscillate and hydrate until the drug-mixed micelle co-precipitate film is completely dissolved, and the drug-lipid complex is obtained.

[0042] The encapsulation efficiency of clobetasol propionate in the obtained lipoplex is 94.7%; the encapsulation efficiency of retinoic acid is 98.7%; and the average particle size is 30.7nm.

Embodiment 2

[0043] Embodiment 2: Composite antioxidant solid dispersion

[0044] The preparation of table 2 composite antioxidant solid dispersion

[0045] name

[0046] The preparation steps are as follows: take lanolin, paraffin, Tween 80, heat and melt at 70°C, add composite antioxidant, rapidly cool to below the minimum eutectic point temperature, and prepare a solid dispersion.

Embodiment 3

[0047] Embodiment 3: the preparation of compound clobetasovitrin A acid ointment

[0048] Table 3 Prescription table of compound clobetasol propionate ointment

[0049] name

[0050] Preparation process: Take stearic acid, liquid paraffin, stearyl alcohol, and vaseline, heat and melt at 80°C, add Span 60 to dissolve in the oil phase matrix, and take the compound antioxidant solid dispersion of Example 2, dissolve it in the oil phase In the matrix, melt evenly; take the drug lipid complex of Example 1, add it to the above oil phase matrix in a thin stream at 80°C, add sodium lauryl sulfate, and emulsify evenly to obtain the compound clobetasol propionate Vitamin A ointment.

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Abstract

The present invention provides a clobetasol propionate and tretinoin ointment agent. According to the present invention, a phospholipid and a positively charged lipid are mainly adopted to wrap drugs to prepare a lipid complex, wherein the positively charged lipid complex can concurrently wrap two drugs, encapsulation efficiency is high, and leakage is not easily generated; with the lipid complex, drug absorption can be promoted, and drug retention in skin can be increased; the multi-component low co-melting system is adopted to prepare the solid dispersion, such that the composite antioxidant component in the formula is uniformly dispersed in the same system; an oil phase matrix and an emulsifying agent are added so as to further prepare into a cream agent or an ointment agent in one step; and the preparation has characteristics of good emulsifying uniformity and high stability, and can be used for treatment of psoriasis, chronic dermatitis and eczema, skin papule type amyloidopathia, lichen planus, and non-atopic dermatitis.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a compound clobetasol propionate and all-trans retinoic acid lipid complex and a preparation method thereof. The lipid complex has the characteristics of high skin penetration and high skin drug retention Features, can be further prepared into cream, ointment, mainly used for the treatment of psoriasis vulgaris, dermatitis, eczema and other diseases. Background technique [0002] Both clobetasol propionate and retinoic acid are commonly used topical dermatological treatments with definite curative effects. Clobetasol propionate (CP) is a powerful hormone, long-term use can cause side effects such as skin atrophy, and the side effect commonly used in the use of tretinoin is skin irritation. In addition, transdermal absorption of drugs into the blood circulation system will produce systemic toxic and side effects. Therefore existing open technology is devoted to utilizing c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/573A61K9/06A61P17/06A61P17/00A61K31/203
Inventor 尹莉芳何伟
Owner JIANGSU SEMPOLL PHARMA
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