CN104546880B - A kind of external preparation for treating facial seborrhea - Google Patents

Abstract

A kind of external preparation for treating facial seborrhea belongs to the preparation technical field of medical, dental or dressing, is to be related to a kind of external preparation for treating facial seborrhea specifically.The external preparation of the present invention comprises at least following drug ingedient：0.05 0.1 parts of chlorhexidine acetate, 0.05 0.15 parts of ketoconazole, 0.05 0.15 parts of ceramide, 8 12 parts of glycerine, 0.8 1.2 parts of glycyrrhizin.The external preparation of the present invention can effectively be killed MRSE, ketoconazole by chlorhexidine acetate and effectively suppress pityrosporum furfur, glycyrrhizin suppression inflammatory reaction, the NMF of glycerine increase cuticula, and ceramide repairs epidermal barrier function.By the comprehensive function of above-mentioned five kinds of drug ingedients, facial seborrhea is effectively treated.

Description

A kind of external preparation for treating facial seborrheic dermatitis

technical field

The invention belongs to the technical field of preparations for medicine, dentistry or dressing, and in particular relates to an external preparation for treating facial seborrheic dermatitis.

Background technique

Seborrheic dermatitis (SD) is a chronic papulosquamous, superficial inflammatory skin disease that occurs at the seborrheic site. The typical rash is dark red and yellowish red spots formed by the fusion of follicular papules, covered with greasy Scales or scabs may be accompanied by varying degrees of itching. The etiology is unknown, but it was thought to be related to Pityrosporum colonization activities in the past, but the effect of antifungal therapy is not prominent, and its effectiveness is controversial. The current treatment methods for facial seborrheic dermatitis include simple anti-inflammatory drugs (such as hormone topical preparations, calcineurin inhibitors), supplemented with skin moisturizing and skin care products, and the effectiveness is low; and symptoms tend to recur after drug withdrawal.

Contents of the invention

The present invention aims at the above-mentioned problems existing in the prior art, and provides an external preparation for treating facial seborrheic dermatitis which has a good therapeutic effect and is not easy to relapse.

Our research found that: 1) Staphylococcus epidermidis colonization increased in patients with facial seborrheic dermatitis, which was significantly statistically different from the normal population (mean values were nearly 90cfu/cm ² and 12cfu/cm ² ), topical antibacterial treatment It can effectively improve the symptoms of patients (the average disease severity score is reduced from about 0.9 to 0.3), see Figure 1, suggesting that highly colonized Staphylococcus epidermidis has a pathogenic effect; 2) In vitro experiments found that Malassezia furfur cells or cultured The supernatant can promote the proliferation of Staphylococcus epidermidis, suggesting that the two fungi have a synergistic pathogenic effect, and the effect of Staphylococcus epidermidis may be more direct; 3) The protective ability of the skin barrier in seborrheic dermatitis is reduced, manifested as transdermal water Loss increases. The average value of transdermal water loss in the lesion of the seborrheic dermatitis patients was more than 37g/hm ² , while the average value of the normal control group was 23g/hm ² , and there was a significant statistical difference. Disruption of this barrier is one of the important factors secondary to high bacterial colonization. Based on the above findings, the present invention adopts the following technical scheme to create a new type of compound preparation for external use that effectively treats facial seborrheic dermatitis, and comprehensively targets the etiology and mechanism of the disease from several angles to give intervention treatment, while ensuring safety. Under the premise, improve the effectiveness of treatment.

The external preparation of the present invention at least includes the following pharmaceutical ingredients: 0.05-0.1 parts of chlorhexidine acetate, 0.05-0.15 parts of ketoconazole, 0.05-0.15 parts of ceramide, 8-12 parts of glycerol, and 0.8-1.2 parts of glycyrrhizin .

The role played by various raw materials in the formula is as follows.

Chlorhexidine acetate: Effectively kill Staphylococcus epidermidis.

Ketoconazole: Effectively inhibits Pityrosporum fungus.

Ceramide: High-efficiency moisturizer, very easy to be absorbed by the skin, and can promote the penetration of other nutrients, so that the skin maintains elasticity, smoothness and fineness; especially for aging skin, the moisturizing effect is remarkable.

Glycerol: Increases the natural moisturizing factor of the stratum corneum of the facial skin.

Glycyrrhizin: It can inhibit the inflammatory response.

The preparation method of the oil-in-water dosage form of the external preparation for treating facial seborrheic dermatitis of the present invention: add glycerin and triethanolamine into boiled distilled water, stir to dissolve, cool and keep the temperature at 80-85°C as the water phase; Stearic acid, castor oil and liquid paraffin are heated and melted, and the temperature is kept at 80-85°C as the oil phase; the aforementioned oil phase is added to the aforementioned water phase under slow stirring to complete the matrix preparation; the matrix is cooled to 50-60 At ℃, add the medicinal ingredients chlorhexidine, ketoconazole, ceramide, glycerol, and glycyrrhizin into the aforementioned matrix, stir evenly in the same direction, and cool to room temperature to obtain the product.

The preparation method of the water-in-oil dosage form of the external preparation for treating facial seborrheic dermatitis of the present invention: adding glycerin and triethanolamine into boiled distilled water, stirring to dissolve, cooling and keeping the temperature at 80-85°C, as the water phase; Stearic acid, castor oil and liquid paraffin are heated and melted, and the temperature is kept at 80-85°C as the oil phase; the aforementioned water phase is added to the aforementioned oil phase under slow stirring to complete the matrix preparation; the matrix is cooled to 50-60 At ℃, add the medicinal ingredients chlorhexidine, ketoconazole, ceramide, glycerol, and glycyrrhizin into the aforementioned matrix, stir evenly in the same direction, and cool to room temperature to obtain the product.

The preparation method of the ointment dosage form of the external preparation for treating facial seborrheic dermatitis of the present invention: take vaseline as the base (the addition amount is 8-12 parts by weight), add 0.05-0.1 parts of chlorhexidine acetate and 0.05-0.15 parts of ketoconazole 0.05-0.15 parts of ceramide, 8-12 parts of glycerol, 0.8-1.2 parts of glycyrrhizin, and stir to obtain.

Make the oil phase of the emulsion: The oil phase is the main component of the emulsion, and the drug ingredients are dispersed in the water phase or the oil phase according to their physical properties.

Make the water phase of the emulsion: the water phase is the main component of the emulsion, and the pharmaceutical ingredients are dispersed in the water phase or the oil phase according to their physical properties.

Emulsifiers for making emulsions: emulsifiers (in the present invention, vaseline) have significant surface activity; can form an interface film around the droplet; can form an electrical barrier on the surface of the droplet; can increase the viscosity of the medium; and also have a good Stable to acid, alkali and salt, non-irritating.

Compared with the prior art, the present invention has beneficial effects: the external preparation of the present invention can effectively kill Staphylococcus epidermidis through chlorhexidine acetate, ketoconazole effectively inhibits Pityrosporum, glycyrrhizin inhibits inflammatory response, and glycerol increases The natural moisturizing factor of the stratum corneum, ceramide restores the barrier function of the epidermis. Through the combined effect of the above five drug ingredients, it can effectively treat facial seborrheic dermatitis; in the clinical trial, a total of 75 patients were treated, of which 26 cases were markedly effective, 45 cases were effective, and the total effective rate was 94.7%. The emulsion and the ointment prepared by utilizing these five medicines are convenient to apply, and the cost of raw materials is relatively low.

Description of drawings

Fig. 1 is a comparison chart of the curative effect before and after the treatment of seborrheic dermatitis between Example 1 and Example 2 of the present invention and the existing moisturizer. # p value<0.05, the degree of improvement of the treatment group in Example 2 is better than that of the moisturizer treatment group. * p value <0.05, the degree of improvement of the treatment group in Example 1 is better than that of the moisturizer treatment group. Among them, the moisturizer is Staples Feather Moisturizing Cream (produced by GlaxoSmithKline Investment Co., Ltd.). When using it, it should be avoided within 2 hours before and after the external application of the above-mentioned medicine on the skin lesion, once a day. .If you take a bath on the same day, finish it within 5 minutes after bathing (when the skin is relatively moist).

detailed description

Example 1: Add 6.2g glycerol and 10g triethanolamine into boiled 55ml distilled water, stir to dissolve, cool and keep the temperature at 80-85°C as the water phase; add 12.4g stearic acid, 12.4g castor oil and Heat and melt 12.4g of liquid paraffin, keep the temperature at 80-85°C, as the oil phase; add the above-mentioned oil phase to the above-mentioned water phase under slow stirring to complete the matrix preparation; when the matrix is cooled to 50-60°C, add the drug Add 0.05g of chlorhexidine acetate, 0.05g of ketoconazole, 0.05g of ceramide, 8g of glycerol, and 0.8g of glycyrrhizin into the aforementioned base, stir evenly in the same direction, and cool to room temperature.

Embodiment 2: 6.2g glycerin and 10g triethanolamine are added into boiled 55ml distilled water, stir to dissolve, cool and keep the temperature at 80-85°C, as the water phase; 12.4g stearic acid, 12.4g castor oil and Heat and melt 12.4g of liquid paraffin, keep the temperature at 80-85°C, and use it as the oil phase; add the aforementioned water phase to the aforementioned oil phase under slow stirring to complete the matrix preparation; when the matrix is cooled to 50-60°C, add the drug Add 0.08g of chlorhexidine acetate, 0.1g of ketoconazole, 0.1g of ceramide, 10g of glycerol, and 1g of glycyrrhizin into the aforementioned base, stir evenly in the same direction, and cool to room temperature.

Example 3: Take 10 g of vaseline as the base, add the medicinal ingredients 0.1 g of chlorhexidine acetate, 0.15 g of ketoconazole, 0.15 g of ceramide, 12 g of glycerol, and 1.2 g of glycyrrhizin, and stir to obtain the product.

Example 4: 0.1 part of chlorhexidine acetate, 0.15 part of ketoconazole, 0.1 part of ceramide, 10 parts of glycerol, and 1.2 parts of glycyrrhizin.

Example 5: 0.0 part of chlorhexidine acetate, 0.1 part of ketoconazole, 0.15 part of ceramide, 8 parts of glycerol, and 1 part of glycyrrhizin.

Example 6: 0.08 parts of chlorhexidine acetate, 0.05 parts of ketoconazole, 0.05 parts of ceramide, 12 parts of glycerol, and 0.8 parts of glycyrrhizin.

Case 1: Li, a 45-year-old female, had a history of seborrheic dermatitis for half a year. Scattered erythema was seen on the nasolabial folds and mandible, covered with greasy scales, and itching was obvious. The photo on the right is the photo after two weeks of treatment with antibiotic ointment. It can be seen that the erythema and scales have been significantly reduced, and the itching has been relieved. The treatment is effective. Seborrheic dermatitis area severity index SDSIA decreased from 0.3 to 0.1, pruritus index decreased from 3 to 0.

Case 2: Zhao, a 56-year-old male, had a history of seborrheic dermatitis for three months. Scattered papules were seen on both cheeks and forehead. There was a lot of oil on the face, and he felt itchy. The photo on the right is after two weeks of antibiotic ointment treatment. It can be seen that the pimples are significantly reduced, the itching is relieved, and the treatment is effective. Seborrheic dermatitis area severity index SDSIA decreased from 0.6 to 0.1, pruritus index decreased from 3 to 0.

Case 3: Zhang, a 72-year-old male; the patient is an elderly male infected with HIV, with a 2-year history of HIV infection and a 1-year history of seborrheic dermatitis. During the year, erythema and papules occurred repeatedly on the cheeks, nasolabial folds, and mandibles, and itching was felt consciously. The photo on the right is the photo of antibiotic ointment after 2 weeks of treatment. It can be seen that the erythema and papules disappeared, and the itching was relieved. The treatment is effective. Seborrheic dermatitis area severity index SDSIA decreased from 0.3 to 0.1, pruritus index decreased from 3 to 0.

Note: SDASI scoring system (Seborrheic Dermatitis Area Severity Index) and pruritus scoring: grading of severity of erythema and scales: 0=no skin lesions, 1=mild, 2=moderate, 3=severe. The multiplication coefficients of different anatomical parts are as follows: forehead 0.1, scalp 0.4, nasolabial fold 0.1, eyebrows 0.1, behind the ear 0.1, ear 0.1, mandible 0.1, between breasts 0.2, back 0.2. SDASI scores (0-12.6) are obtained by adding the scores of different parts. Grading of itching degree: 0=no itching, 1=mild, 2=moderate, 3=severe.

Claims (6)

1. An external preparation for treating facial seborrheic dermatitis, characterized in that: at least comprising the following pharmaceutical ingredients in parts by weight: 0.05-0.1 part of chlorhexidine acetate, 0.05-0.15 part of ketoconazole, 0.05-0.15 part of ceramide 8-12 parts of glycerin, 0.8-1.2 parts of glycyrrhizin. 2. the external preparation for the treatment of facial seborrheic dermatitis as claimed in claim 1, is characterized in that: at least comprises the following pharmaceutical composition of weight parts: 0.1 part of chlorhexidine acetate, 0.15 part of ketoconazole, 0.1 part of ceramide , 10 parts of glycerin, 1.2 parts of glycyrrhizin. 3. The external preparation for the treatment of facial seborrheic dermatitis as claimed in claim 1, characterized in that: at least comprise the following pharmaceutical ingredients in parts by weight: 0.08 part of chlorhexidine acetate, 0.05 part of ketoconazole, 0.05 part of ceramide part, 12 parts of glycerin, and 0.8 part of glycyrrhizin. 4. as the preparation method of the external preparation of the arbitrary described treatment facial seborrheic dermatitis of claim 1-3, it is characterized in that: glycerol and triethanolamine are added in the distilled water that has boiled, stirring and dissolving, cooling and keeping temperature At 80-85°C, as the water phase; heat and melt stearic acid, castor oil and liquid paraffin, and keep the temperature at 80-85°C, as the oil phase; add the water phase to the oil phase under slow stirring to complete the matrix Preparation: when the base is cooled to 50-60°C, add the drug ingredients chlorhexidine, ketoconazole, ceramide, glycerol, and glycyrrhizin into the base, stir evenly in the same direction, and cool to room temperature to obtain . 5. the preparation method of the external preparation for the treatment of facial seborrheic dermatitis as claimed in claim 4 is characterized in that: 6.2g glycerol and 10g triethanolamine are added in the 55ml distilled water that has boiled, stirring and dissolving, cooling and temperature maintenance At 80-85°C, as the water phase; heat and melt 12.4g stearic acid, 12.4g castor oil and 12.4g liquid paraffin, keep the temperature at 80-85°C, as the oil phase; slowly stir the water phase, add In the oil phase, the preparation of the matrix is completed; when the matrix is cooled to 50-60°C, add the drug ingredients 0.08g chlorhexidine acetate, 0.1g ketoconazole, 0.1g ceramide, 10g glycerol, and 1g glycyrrhizin In the matrix, stir evenly in the same direction, and cool to room temperature. 6. The external preparation for the treatment of facial seborrheic dermatitis as claimed in claim 1, characterized in that: taking 8-12 parts by weight of vaseline as a base, adding 0.05-0.1 part of chlorhexidine acetate and 0.05 part of ketoconazole -0.15 parts, 0.05-0.15 parts of ceramide, 8-12 parts of glycerin, 0.8-1.2 parts of glycyrrhizin, and stir to obtain.