CN1907294A - Compound recipe copper sulfate cold cream - Google Patents

Abstract

The invention relates to the technical field of medicines, and relates to an external preparation compound copper sulfate cold cream for treating vitiligo. It consists of the drug copper sulfate, the glucocorticoid clopetasol propionate, a skin penetration enhancer and a cold cream base. Since copper sulfate and clopetasol propionate are made into a compound preparation, the local concentration is much lower than the single preparation of copper sulfate or clopetasol propionate, and the therapeutic effect is obviously improved, and the onset of effect is fast. The toxic and side effects are small.

Description

Compound Copper Sulfate Cold Cream

Technical field

The invention relates to the technical field of medicines, and relates to an external preparation compound copper sulfate cold cream for treating vitiligo.

Background technique

Vitiligo is a common skin disease with an incidence rate of about 2%. It is easy to diagnose but difficult to treat. Early studies have confirmed that the cause of vitiligo is related to the lack of trace element copper in the body and the body's autoimmunity to melanocytes, but oral administration of copper preparations can easily cause poisoning. At present, the commonly used treatment methods mainly include photochemotherapy, narrow-wave ultraviolet irradiation, autologous epidermal grafting, external application of glucocorticoid ointment or psoralen solution, etc. Prolonged application of photochemotherapy can easily damage the lens of the patient's eye, which may lead to cataracts. Narrow-wave ultraviolet radiation requires complex equipment, high treatment costs, and patients have to go to and from the hospital many times. The scope of each operation of autologous epidermis is very small, and the patient needs multiple treatments, and the total cost is very high. Glucocorticoids are commonly used immunosuppressants, and they have certain curative effect in the treatment of vitiligo, but the concentration required for external application of glucocorticoid ointment alone is relatively high, usually strong hormones such as 1% to 2% of clopetasol propionate, other Side effects are large, and local capillary hyperplasia and dilation, folliculitis, and skin atrophy often occur. If psoralen for external use is not irradiated with ultraviolet rays, the curative effect is poor, but irradiating ultraviolet rays can easily cause blisters and cause pain to patients.

Contents of invention

The invention provides an external preparation for treating vitiligo with good curative effect and few side effects----compound copper sulfate cold cream.

In the present invention, copper sulfate and glucocorticoids are made into a compound preparation, and through topical administration, trace element copper and immunosuppressants are supplemented through a transdermal route, which not only avoids the poisoning phenomenon that may be caused by oral administration of copper preparations, but also greatly reduces the The local concentration of glucocorticoids is lower, thereby avoiding many side effects that may be caused by long-term external use of high-concentration glucocorticoids.

The compound copper sulphate cold cream of the invention consists of medicine, a skin penetration enhancer and a cold cream base. The drugs were copper sulfate and the corticosteroid clopetasol propionate. Transdermal enhancers are urea and azone. The cold cream base is composed of multiple ingredients in stearic acid, stearyl alcohol, liquid paraffin, white petrolatum, glycerin, sorbic acid, Tween-80 and Span-80. The proportion of each component is: copper sulfate 0.5%-1%, urea 5%-10%, clopetasol propionate 0.05%-0.1%, azone 1%-5%, stearic acid 0-10% , stearyl alcohol 0-10%, liquid paraffin 0-10%, white petrolatum 5%-10%, glycerin 0-20%, sorbic acid 5%-10%, Tween-80 3%-6%, Span -801% -5%, dimethyl sulfoxide qs. The solvent is purified water.

The preparation method is as follows:

(1) Prepare the oil phase: put stearic acid, stearyl alcohol, liquid paraffin, white vaseline, and glycerin in a container according to the proportion, heat and melt on a water bath, keep it warm for later use, and then mix clopetasol propionate with a small amount of dimethyl After the sulfoxide is dissolved, add it to form the oil phase.

(2) Prepare the water phase: add copper sulfate, urea, azone, sorbic acid, Tween-80, and Span-80 into distilled water to dissolve according to the proportion, and then form the water phase.

(3) Preparation of cream: Slowly add the oil phase ingredients into the water phase under warm conditions, and stir in the same direction until emulsified and condensed to obtain a cream, which can be divided into packages as needed.

Through clinical trial, the compound preparation of the present invention treats vitiligo and compares with single-use 1% clopetasol propionate ointment or single-use 2% ketone sulfate solution, not only because the concentration of local clopetasol propionate and copper sulfate greatly reduces The toxic and side effects are small, and the effect is quick and the curative effect is good.

Detailed ways

Now in conjunction with embodiment, the present invention is described in detail.

Example 1 Preparation of Compound Copper Sulfate Cold Cream

Components and ratio:

Copper Sulfate 120g

Urea 1200g

Clopetasol Propionate 6 grams

Azone 240ml

Stearic acid 720g

Octadecanol 720g

Liquid paraffin 1080ml

White Vaseline 720g

Glycerin 1200g

Sorbic acid 6 grams

Tween-80 528ml

Span-80 192ml

Dimethyl Sulfoxide 5ml

Purified water 6000ml

Preparation:

(1) Prepare the oil phase: put stearic acid, stearyl alcohol, liquid paraffin, white vaseline, and glycerin in an evaporating dish according to the proportion, heat it on a water bath to 75°C and melt it, keep it warm for later use, and then add clopetasol propionate Dissolve it with dimethyl sulfoxide and add it to form an oily phase.

(2) Preparation of the water phase: add copper sulfate, urea, azone, sorbic acid, Tween-80, and Span-80 into distilled water according to the proportion and dissolve them to form the water phase, and heat to 75°C for later use.

(3) Preparation of cream: Slowly add the oil phase ingredients into the water phase under warm conditions, stir in the same direction and gradually cool until emulsified and condensed to obtain a cream, which can be divided into packages as needed.

Example 2 Preparation of Compound Copper Sulfate Cold Cream

Components and ratio:

Copper Sulfate 100g

Urea 1000g

Clopetasol Propionate 3 grams

Azone 250ml

Stearic acid 1000g

Liquid paraffin 1800ml

White Vaseline 720g

Sorbic acid 6 grams

Tween-80 528ml

Span-80 192ml

Dimethyl Sulfoxide 3ml

Purified water 6000ml

The preparation method is the same as in Example 1.

Example 3 Preparation of Compound Copper Sulfate Cold Cream

Components and ratio:

Copper Sulfate 150g

Urea 1500g

Clopetasol Propionate 10g

Azone 200ml

Octadecanol 1000g

White Vaseline 1000g

Glycerin 1500g

Sorbic acid 6 grams

Tween-80 528ml

Span-80 200ml

Dimethyl Sulfoxide 10ml

Purified water 6000ml

The preparation method is the same as in Example 1.

Clinical trials:

32 patients clinically diagnosed as localized stable vitiligo patients were randomly divided into 3 groups, respectively treated with compound copper sulfate cold cream, 1% clopetasol propionate ointment, and 2% copper sulfate solution for external use, and conducted a controlled study to observe Efficacy and adverse reactions. Medication 2 times a day, shared medicine for 2 months. Efficacy standard: recovery: all white spots subsided, and normal skin color was restored. Significantly effective: the white spot subsides or shrinks, and the normal skin color area accounts for more than 50% of the lesion area. Effective: the leukoplakia part disappears or shrinks, and the area of returning to normal skin color accounts for more than 10% and less than 50% of the skin area. Ineffective: the leukoplakia remains unchanged or shrinks, and the area of returning to normal skin color accounts for less than 10% of the lesion area. Healed, markedly effective and effective are combined to calculate the effective rate. Treatment results: Pigment skin islands appeared in 3 patients in the compound copper sulfate cold cream group in the 4th week of medication, and the pigment skin islands gradually expanded when the medication was continued, and there was no abnormality in the skin around the medication. In the 1% clopetasol propionate ointment group, local multiple miliary folliculitis and telangiectasia occurred in the 3rd week of administration, and a small amount of pigmented skin islands were seen in the 4th week. Due to the continuous aggravation of folliculitis, 2 patients could not adhere to the medication. In the 2% copper sulfate solution group, the local skin turned blue and had no pigmented skin islands after 3 weeks of medication, and only a small amount of pigmented skin islands appeared after 6 weeks of continuous medication. The specific curative effects are shown in the table below:

Comparison of clinical curative effect of 3 groups of drugs in treatment of vitiligo Number of cases get well markedly effective efficient invalid Efficient Compound copper sulfate cold cream group 10 1 3 4 2 80.00% 1% clopetasol propionate ointment group 11 0 2 5 4 63.64% 2% copper sulfate solution group 11 0 3 3 5 54.55%

The rank sum test showed that the effective rate of the compound copper sulfate cold cream group was significantly higher than that of the other two groups of drugs, and the difference was statistically significant (P<0.05).

It can be seen that, after copper sulfate and clopetasol propionate are made into compound preparations by the present invention, although the concentration of local single drug is far lower than that of single-use 1% clopetasol propionate ointment or 2% copper sulfate solution, But the effect of treating vitiligo is much better, not only quick onset, but also less side effects.

Claims (3)

1. a compound copper sulfate cold cream, is made up of medicine, transdermal accelerator and matrix, is characterized in that: medicine is copper sulfate and clopetasol propionate, and transdermal accelerator is urea and azone, and matrix is selected from Composed of stearic acid, stearyl alcohol, liquid paraffin, white petrolatum, glycerin, sorbic acid, Tween-80 and Span-80, the ratio of each component is: Copper Sulfate 0.5%-1% Urea 5%-10% Clobetasol Propionate 0.05%-0.1% Azone 1%-5% Stearic acid 0-10% Octadecanol 0-10% Liquid paraffin 0-10% White Vaseline 5%-10% Glycerin 0-20% Sorbic acid 5%-10% Tween-80 3%-6% Span-80 1%-5% Dimethyl Sulfoxide Appropriate amount The solvent is purified water. 2. by the described compound copper sulfate cold frost of claim 1, it is characterized in that component and proportioning are as follows: Copper Sulfate 120g Urea 1200g Clopetasol Propionate 6 grams Azone 240ml Stearic acid 720g Octadecanol 720g Liquid paraffin 1080ml White Vaseline 720g Glycerin 1200g Sorbic acid 6 grams Tween-80 528ml Span-80 192ml Dimethyl Sulfoxide 5ml Purified water 6000ml. 3. by the described compound copper sulfate cold frost of claim 1, it is characterized in that component and proportioning are as follows: Copper Sulfate 100g Urea 1000g Clopetasol Propionate 3 grams Azone 250ml Stearic acid 1000g Liquid paraffin 1800ml White Vaseline 720g Sorbic acid 6 grams Tween-80 528ml Span-80 192ml Dimethyl Sulfoxide 3ml Purified water 6000ml.