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Compound ketoconazole cream and preparation method thereof

A technology of compound ketoconazole cream and ketoconazole, which is applied in the field of medicine, can solve the problems of complex preparation process, large side effects, poor stability, etc., and achieve the effects of simple preparation process, long action time and low cost

Pending Publication Date: 2018-05-25
JIANGSU LINGBAO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In view of the current situation that there is no anti-superficial fungal infection drug that uses ketoconazole and paeonol in combination, and the existing compound ketoconazole preparations have problems such as large side effects, many ingredients, complicated preparation process, and poor stability. , the present invention aims to provide a compound ketoconazole cream and preparation method thereof

Method used

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  • Compound ketoconazole cream and preparation method thereof
  • Compound ketoconazole cream and preparation method thereof
  • Compound ketoconazole cream and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-9

[0051] Embodiment 1-9: Preparation of ketoconazole-paeonol liposome and test of drug encapsulation efficiency in liposome.

[0052] First, carry out the orthogonal test according to the factor-level design in Table 1, place the weighed ketoconazole, paeonol, lecithin and cholesterol in a small beaker, and add 20mL chloroform to dissolve, then transfer the oily solution to In the round-bottomed flask, use a rotary evaporator equipped with a vacuum pump to rotate and evaporate under reduced pressure under the condition of a water bath at 45°C until the chloroform is completely removed, and finally form a uniform and transparent oily film;

[0053] Next, hydrate the above-mentioned oily film with an appropriate amount of phosphate buffer solution containing polysorbate-80 (using sodium dihydrogen phosphate / disodium hydrogen phosphate as a buffer pair) until no insoluble matter exists to obtain a dispersion system;

[0054] Then, above-mentioned dispersion system ultrasonic treatm...

Embodiment 10-12

[0069] Examples 10-12: Preparation of compound ketoconazole cream.

[0070] The liposome prepared in Example 5 was used to prepare the cream, and its components and dosage are shown in Table 5.

[0071] Table 5. The formula list of compound ketoconazole cream

[0072]

[0073] The specific preparation method is as follows:

[0074] (1) Prepare the oil phase: take stearyl alcohol, cetyl alcohol, white petrolatum or liquid paraffin as the base of the oil phase, heat and melt it and keep it warm at 75°C to form the oil phase;

[0075] (2) Preparation of the water phase: Weigh ethyl paraben as a preservative and sodium lauryl sulfate as an emulsifier, Ping Pinga O or glyceryl monostearate, add to glycerin and / or propylene glycol and purified water Dissolve in the water phase matrix formed after mixing and keep warm at 75°C, which is the water phase;

[0076] (3) Preparation of emulsifiable cream: under the condition of mechanical stirring, the above-mentioned oil phase is sl...

experiment example 1

[0077] Experimental Example 1: Skin irritation test of compound ketoconazole cream

[0078] Adopt the compound ketoconazole cream in embodiment 10 to embodiment 12 to carry out skin irritation test.

[0079] The specific experimental process is as follows: select a rabbit with a body weight of 2.0-2.5 kg as the experimental animal, and 24 hours before the test, use scissors and an electric shaver to shave an area on each side of the rabbit's back spine, with a size of about 10 cm × 5 cm. Among them, the upper part is the intact skin test area, the lower part is the damaged skin test area, and the test drug or positive control is applied on the left side (product name: compound ketoconazole ointment, batch number: 150901, manufacturer: Jiangsu Lingbao Pharmaceutical Co., Ltd. Co., Ltd.), the application amount is 1mL, and the right side is the blank control; the skin on the left and right sides of the damaged skin test area is cut with a scalpel before administration, forming a...

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Abstract

The invention belongs to the technical field of medicines and relates to compound ketoconazole cream and a preparation method thereof. Specifically, the compound ketoconazole cream is prepared from ketoconazole-paeonol lipidosome, an oil-phase matrix, a water-phase matrix and an emulsifying agent, wherein the ketoconazole-paeonol lipidosome is prepared from ketoconazole, paeonol, lecithin, cholesterol, polysorbate-80, vitamin E and phosphate buffering solution with a pH value being 6.5-7.5 by a film dispersion method. The compound ketoconazole cream has the beneficial effects that the ketoconazole and the paeonol are combined for use, so that the antibacterial activity is improved; the lipidosome has a selective effect for the skin and has penetration-enhancing and slow-release effects forthe medicines; the ketoconazole and the paeonol are encapsulated in the lipidosome simultaneously, so that the solubility and the stability of the two medicines can be improved simultaneously.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a compound ketoconazole cream and a preparation method thereof. Background technique [0002] Ketoconazole is a broad-spectrum antifungal drug that achieves therapeutic purposes by inhibiting the growth and reproduction of fungi. In order to improve the anti-inflammatory effect, it is often used in combination with clobetasol propionate. However, external application of drugs containing corticosteroid hormones can cause contact allergic reactions, and long-term use can cause adverse reactions such as telangiectasia, thinning of the epidermis, and skin atrophy. In addition, ketoconazole has low water solubility and is easily oxidized, which limits its wider application. [0003] [0004] For example, Chinese invention patent application CN 103432148 A (invention name: a preparation method of compound ketoconazole cream) discloses a compound ketoconazole cream, the raw material...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K9/06A61K9/127A61K47/24A61K47/28A61K47/26A61K47/22A61P31/10A61K31/12
CPCA61K47/22A61K47/24A61K47/26A61K47/28A61K9/06A61K9/127A61K31/12A61K31/496A61K2300/00
Inventor 浦洁王有志胡兰兰王德才
Owner JIANGSU LINGBAO PHARMA
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