CN104546880A - External preparation for treating facial seborrheic dermatitis - Google Patents

External preparation for treating facial seborrheic dermatitis Download PDF

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Publication number
CN104546880A
CN104546880A CN201510006320.2A CN201510006320A CN104546880A CN 104546880 A CN104546880 A CN 104546880A CN 201510006320 A CN201510006320 A CN 201510006320A CN 104546880 A CN104546880 A CN 104546880A
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Prior art keywords
glycerol
seborrheic dermatitis
external preparation
ketoconazole
ceramide
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CN201510006320.2A
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CN104546880B (en
Inventor
安倩
高兴华
陈洪铎
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Dalian Asia Pharmaceutical Co. Ltd.
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First Hospital of China Medical University
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/164Amides, e.g. hydroxamic acids of a carboxylic acid with an aminoalcohol, e.g. ceramides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Cosmetics (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention discloses an external preparation for treating facial seborrheic dermatitis, belongs to the technical field of medical, dental or dressing preparations, and in particular relates to an external preparation for treating facial seborrheic dermatitis. The external preparation disclosed by the invention at least comprises the following medicinal components: 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 and 0.8-1.2 parts of glycyrrhizin. According to the external preparation disclosed by the invention, the staphylococcus epidermidis can be effectively killed by chlorhexidine acetate, the pityrosporum orbiculare is effectively inhibited by ketoconazole, the inflammatory reaction is inhibited by the glycyrrhizin, the natural moisturizing factors of cuticle are increased by the glycerin, and the epidermal barrier function is repaired by the ceramide. According to the comprehensive effects of the five medical components, the facial seborrheic dermatitis can be effectively treated.

Description

A kind of external preparation for the treatment of facial seborrheic dermatitis
Technical field
The invention belongs to the preparation technical field of medical, dental or dressing, specifically, relate to a kind of external preparation for the treatment of facial seborrheic dermatitis.
Background technology
Seborrheic dermatitis (Seborrheic Dermatitis, SD) be occur in the chronic papulosquamous of one at seborrhea position, shallow table inflammatory dermatoses, the pityriasis rubra pimple of typical rash merges the kermesinus, the yellowish red color speckle that are formed, on cover greasy scales or crust, can with pruritus in various degree.The cause of disease is not quite clear, think relevant with pityrosporum furfur field planting activity in the past, but antifungal therapy effect is not given prominence to, and its effectiveness exists academic dispute.Current facial seborrheic dermatitis Therapeutic Method comprises simple anti-inflammatory drug (as hormones external preparation, calcineurin inhibitors), assists with skin moisture-keeping skin care item, and effective percentage is lower; And symptom easily recurs after drug withdrawal.
Summary of the invention
The present invention is exactly for the above-mentioned problems in the prior art, provides a kind of therapeutic effect good and the external preparation of the treatment of not easily recurring face seborrheic dermatitis.
Research through us finds: 1) field planting of facial patients with seborrheic dermatitis staphylococcus epidermidis is increased, and (average is nearly 90cfu/cm respectively to have the significant difference of highly significant than normal population 2and 12cfu/cm 2), externally used antimicrobial treatment effectively can improve patients symptomatic's (disease severity integral mean is down to 0.3 by about 0.9), sees accompanying drawing 1, points out the staphylococcus epidermidis of high field planting to have pathogenic effects; 2) experiment in vitro finds that Malassezia furfur thalline or culture supernatant can promote that staphylococcus epidermidis is bred, and point out these two kinds of mushrooms to have collaborative pathogenic effects, and the effect of staphylococcus epidermidis may be more direct; 3) the skin barrier protective capability of seborrheic dermatitis declines, and shows as transdermal water and loses increase.The transdermal water of patients with seborrheic dermatitis cutaneous lesion loses average more than 37g/hm 2, and normal control population's average is 23g/hm 2, have significant significant difference.The destruction of this barrier is one of key factor of secondary bacterial height field planting.Based on above discovery, the present invention adopts following technical scheme, formulates a kind of externally used compound preparation of the novel facial seborrheic dermatitis of effective treatment, comprehensively gives therapeutic intervention for the pathogenesis etiology of this disease and mechanism from several angle, under the prerequisite ensureing safety, improve the effective percentage for the treatment of.
External preparation of the present invention at least comprises following ingredient: chlorhexidine acetate 0.05-0.1 part, ketoconazole 0.05-0.15 part, ceramide 0.05-0.15 part, glycerol 8-12 part, glycyrrhizic glycoside 0.8-1.2 part.
Various raw material role in formula is as follows.
Chlorhexidine acetate: effectively kill staphylococcus epidermidis.
Ketoconazole: effectively suppress pityrosporum furfur.
Ceramide: efficient moisture-retention agent, is fairly absorbed by the skin, and can promote that other nutrient substance permeates, make skin keep elasticity, smooth careful; Especially remarkable to geroderma moisturizing effectiveness.
Glycerol: increase the cuticular nature moisturizing factor of skin of face.
Glycyrrhizic glycoside: can inflammation-inhibiting reaction.
The present invention treats the preparation method of the oil-in-water dosage form of facial seborrheic dermatitis external preparation: glycerol and triethanolamine are added in the distilled water boiled, stirring and dissolving, and temperature is also remained on 80-85 DEG C, as aqueous phase by cooling; By stearic acid, Oleum Ricini and liquid paraffin heating and melting, temperature remains on 80-85 DEG C, as oil phase; By aforementioned oil phase under slow stirring, add in aforementioned aqueous phase, complete matrix composition; When substrate is cooled to 50-60 DEG C, ingredient acid hibitane, ketoconazole, ceramide, glycerol, glycyrrhizic glycoside are together added in aforementioned substrate, stirs according to same direction, be cooled to room temperature and get final product.
The present invention treats the preparation method of the Water-In-Oil dosage form of facial seborrheic dermatitis external preparation: glycerol and triethanolamine are added in the distilled water boiled, stirring and dissolving, and temperature is also remained on 80-85 DEG C, as aqueous phase by cooling; By stearic acid, Oleum Ricini and liquid paraffin heating and melting, temperature remains on 80-85 DEG C, as oil phase; By aforementioned aqueous phase under slow stirring, add in aforementioned oil phase, complete matrix composition; When substrate is cooled to 50-60 DEG C, ingredient acid hibitane, ketoconazole, ceramide, glycerol, glycyrrhizic glycoside are together added in aforementioned substrate, stirs according to same direction, be cooled to room temperature and get final product.
The present invention treats the preparation method of the ointment dosage form of facial seborrheic dermatitis external preparation: take vaseline as substrate (addition is 8-12 weight portion), add ingredient chlorhexidine acetate 0.05-0.1 part, ketoconazole 0.05-0.15 part, ceramide 0.05-0.15 part, glycerol 8-12 part, glycyrrhizic glycoside 0.8-1.2 part, stir and get final product.
Make the oil phase of Emulsion: oil phase is the main constituent of Emulsion, and ingredient is dispersed in aqueous phase or oil phase according to the physical property of self.
Make the aqueous phase of Emulsion: aqueous phase is the main constituent of Emulsion, and ingredient is dispersed in aqueous phase or oil phase according to the physical property of self.
Make the emulsifying agent of Emulsion: emulsifying agent (being vaseline in the present invention) has significant surface activity; Interfacial film can be formed around drop; Electric screen barrier can be formed on drop surface; Dielectric viscosity can be increased; And to have good to acid, alkali, salt stable, nonirritant.
Compared with prior art beneficial effect of the present invention: external preparation of the present invention can effectively be killed staphylococcus epidermidis, ketoconazole by chlorhexidine acetate and effectively suppress that pityrosporum furfur, glycyrrhizic glycoside inflammation-inhibiting react, glycerol increases cuticular nature moisturizing factor, and ceramide repairs epidermal barrier function.By the comprehensive function of above-mentioned five kinds of ingredients, the effectively facial seborrheic dermatitis for the treatment of; In clinical experiment, patients receiving treatment is totally 75 examples, and wherein 26 examples are effective, and effectively, total effective rate reaches 94.7% to 45 examples.Utilize this Emulsion obtained by five kinds of medicines and ointment painting convenient, make expense of raw materials relative moderate.
Accompanying drawing explanation
Fig. 1 is that the embodiment of the present invention 1 and embodiment 2 treat Comparison of therapeutic figure before and after seborrheic dermatitis with existing wetting agent.# p value <0.05, the improvement degree of embodiment two treatment group is better than wetting agent treatment group.* p value <0.05, the improvement degree of embodiment one treatment group is better than wetting agent treatment group.Wherein, wetting agent is that (GlaxoSmithKline PLC Investment Co., Ltd produces the good emollient cream of Shi Taifu mist silk, and during use, in the front and back of cutaneous lesion external foregoing pharmaceutical, 2 hours planted agents avoid using the outer painting in the whole body once a day, 0.5g/ palm area.As bathing on the same day, then complete in 5 minutes after bathing, during the more moistening state of skin).
Detailed description of the invention
Embodiment 1: 6.2g glycerol and 10g triethanolamine are added in the 55ml distilled water boiled, stirring and dissolving, temperature is also remained on 80-85 DEG C, as aqueous phase by cooling; By 12.4g stearic acid, 12.4g Oleum Ricini and 12.4g liquid paraffin heating and melting, temperature remains on 80-85 DEG C, as oil phase; By aforementioned oil phase under slow stirring, add in aforementioned aqueous phase, complete matrix composition; When substrate is cooled to 50-60 DEG C, ingredient 0.05g chlorhexidine acetate, 0.05g ketoconazole, 0.05g ceramide, 8g glycerol, 0.8g glycyrrhizic glycoside are together added in aforementioned substrate, stirs according to same direction, be cooled to room temperature and get final product.
Embodiment 2: 6.2g glycerol and 10g triethanolamine are added in the 55ml distilled water boiled, stirring and dissolving, temperature is also remained on 80-85 DEG C, as aqueous phase by cooling; By 12.4g stearic acid, 12.4g Oleum Ricini and 12.4g liquid paraffin heating and melting, temperature remains on 80-85 DEG C, as oil phase; By aforementioned aqueous phase under slow stirring, add in aforementioned oil phase, complete matrix composition; When substrate is cooled to 50-60 DEG C, ingredient 0.08g chlorhexidine acetate, 0.1g ketoconazole, 0.1g ceramide, 10g glycerol, 1g glycyrrhizic glycoside are together added in aforementioned substrate, stirs according to same direction, be cooled to room temperature and get final product.
Embodiment 3: be that substrate chooses 10g with vaseline, add ingredient 0.1g chlorhexidine acetate, 0.15g ketoconazole, 0.15g ceramide, 12g glycerol, 1.2g glycyrrhizic glycoside, stir and get final product.
Embodiment 4: chlorhexidine acetate 0.1 part, ketoconazole 0.15 part, ceramide 0.1 part, glycerol 10 parts, glycyrrhizic glycoside 1.2 parts.
Embodiment 5: chlorhexidine acetate 0.0 part, ketoconazole 0.1 part, ceramide 0.15 part, glycerol 8 parts, glycyrrhizic glycoside 1 part.
Embodiment 6: chlorhexidine acetate part 0.08 part, ketoconazole 0.05 part, ceramide 0.05 part, glycerol 12 parts, glycyrrhizic glycoside 0.8 part.
Case 1: Lee, female 45 years old; Seborrheic dermatitis medical history half a year, be dispersed in the erythema of distribution in nasolabial fold, lower jaw part as seen, above cover greasy scales, pruritus is obvious.Right figure is the photo of application antibiotics medicinal ointment therapy after two weeks, and visible erythema, squama obviously reduce, and pruritus is alleviated, and treatment effectively.Seborrheic dermatitis area severity index SDSIA is down to 0.1 by 0.3, and pruritus index is down to 0 by 3.
Case 2: Zhao, man 56 years old; Seborrheic dermatitis medical history three months, be dispersed in the pimple of distribution as seen in two sided buccal, forehead, face goes out Chuck Steak, conscious pruritus.Right figure is the photo of antibiotics medicinal ointment therapy after two weeks.Visible pimple obviously reduces, and pruritus alleviates, and treatment effectively.Seborrheic dermatitis area severity index SDSIA is down to 0.1 by 0.6, and pruritus index is down to 0 by 3.
Case 3: Zhang, man 72 years old; Patient is HIV elderly men, HIV medical history 2 years, seborrheic dermatitis medical history 1 year.Repeatedly in Face and cheek, nasolabial fold, lower jaw part generation erythema, pimple in 1 year, conscious pruritus.Right figure is the photo of antibiotics medicinal ointment therapy after 2 weeks, and visible erythema, pimple disappear, and pruritus is alleviated, and treatment effectively.Seborrheic dermatitis area severity index SDSIA is down to 0.1 by 0.3, and pruritus index is down to 0 by 3.
Note: SDASI marking system (seborrheic dermatitis area severity index) and pruritus scoring: the classification of severity of erythema, squama: 0=is without skin lesion, and 1=is slight, 2=moderate, 3=severe.The multiplication coefficient of the different boundaries region of anatomy is as follows: frons 0.1, scalp portion 0.4, nasolabial fold 0.1, eyebrow 0.1, after ear 0.1, and ear 0.1, lower jaw part 0.1, two colpus 0.2, back 0.2.The score addition of different parts and SDASI mark (0-12.6).Pruritus grading: 0=without pruritus, 2=moderate that 1=is slight, 3=severe.

Claims (9)

1. treat an external preparation for facial seborrheic dermatitis, it is characterized in that: at least comprise following ingredient: chlorhexidine acetate 0.05-0.1 part, ketoconazole 0.05-0.15 part, ceramide 0.05-0.15 part, glycerol 8-12 part, glycyrrhizic glycoside 0.8-1.2 part.
2. the external preparation of the facial seborrheic dermatitis for the treatment of as claimed in claim 1, is characterized in that: chlorhexidine acetate 0.1 part, ketoconazole 0.15 part, ceramide 0.1 part, glycerol 10 parts, glycyrrhizic glycoside 1.2 parts.
3. the external preparation of the facial seborrheic dermatitis for the treatment of as claimed in claim 2, is characterized in that: chlorhexidine acetate 0.0 part, ketoconazole 0.1 part, ceramide 0.15 part, glycerol 8 parts, glycyrrhizic glycoside 1 part.
4. the external preparation of the facial seborrheic dermatitis for the treatment of as claimed in claim 3, is characterized in that: chlorhexidine acetate part 0.08 part, ketoconazole 0.05 part, ceramide 0.05 part, glycerol 12 parts, glycyrrhizic glycoside 8 parts.
5. the preparation method of the external preparation of the treatment face seborrheic dermatitis as described in claim 1-4, it is characterized in that: glycerol and triethanolamine are added in the distilled water boiled, stirring and dissolving, temperature is also remained on 80-85, as aqueous phase by cooling; By stearic acid, Oleum Ricini and liquid paraffin heating and melting, temperature remains on 80-85 DEG C, as oil phase; By aforementioned aqueous phase under slow stirring, add in aforementioned oil phase, complete matrix composition; When substrate is cooled to 50-60 DEG C, ingredient acid hibitane, ketoconazole, ceramide, glycerol, glycyrrhizic glycoside are together added in aforementioned substrate, stirs according to same direction, be cooled to room temperature and namely obtain the present invention.
6. the preparation method of the external preparation of the treatment face seborrheic dermatitis as described in claim 1-4, it is characterized in that: glycerol and triethanolamine are added in the distilled water boiled, stirring and dissolving, temperature is also remained on 80-85 DEG C, as aqueous phase by cooling; By stearic acid, Oleum Ricini and liquid paraffin heating and melting, temperature remains on 80-85 DEG C, as oil phase; By aforementioned oil phase under slow stirring, add in aforementioned aqueous phase, complete matrix composition; When substrate is cooled to 50-60 DEG C, ingredient acid hibitane, ketoconazole, ceramide, glycerol, glycyrrhizic glycoside are together added in aforementioned substrate, stirs according to same direction, be cooled to room temperature and namely obtain the present invention.
7. the external preparation of the treatment face seborrheic dermatitis as described in claim 1-4, it is characterized in that: take vaseline as substrate (addition is 8-12 weight portion), add ingredient chlorhexidine acetate 0.05-0.1 part, ketoconazole 0.05-0.15 part, ceramide 0.05-0.15 part, glycerol 8-12 part, glycyrrhizic glycoside 0.8-1.2 part, stir and obtain the present invention.
8. the external preparation of the facial seborrheic dermatitis for the treatment of as claimed in claim 6, is characterized in that: 6.2g glycerol and 10g triethanolamine are added in the 55ml distilled water boiled, stirring and dissolving, and temperature is also remained on 80-85 DEG C, as aqueous phase by cooling; By 12.4g stearic acid, 12.4g Oleum Ricini and 12.4g liquid paraffin heating and melting, temperature remains on 80-85 DEG C, as oil phase; By aforementioned oil phase under slow stirring, add in aforementioned aqueous phase, complete matrix composition; When substrate is cooled to 50-60 DEG C, ingredient 0.05g chlorhexidine acetate, 0.05g ketoconazole, 0.05g ceramide, 8g glycerol, 0.8g glycyrrhizic glycoside are together added in aforementioned substrate, stirs according to same direction, be cooled to room temperature and get final product.
9. the external preparation of the facial seborrheic dermatitis for the treatment of as claimed in claim 6, is characterized in that: 6.2g glycerol and 10g triethanolamine are added in the 55ml distilled water boiled, stirring and dissolving, and temperature is also remained on 80-85 DEG C, as aqueous phase by cooling; By 12.4g stearic acid, 12.4g Oleum Ricini and 12.4g liquid paraffin heating and melting, temperature remains on 80-85 DEG C, as oil phase; By aforementioned aqueous phase under slow stirring, add in aforementioned oil phase, complete matrix composition; When substrate is cooled to 50-60 DEG C, ingredient 0.08g chlorhexidine acetate, 0.1g ketoconazole, 0.1g ceramide, 10g glycerol, 1g glycyrrhizic glycoside are together added in aforementioned substrate, stirs according to same direction, be cooled to room temperature and get final product.
CN201510006320.2A 2015-01-07 2015-01-07 A kind of external preparation for treating facial seborrhea Active CN104546880B (en)

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* Cited by examiner, † Cited by third party
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WO2017129643A1 (en) * 2016-01-26 2017-08-03 Nestec S.A. Composition for preventing or reducing transepidermal water loss
CN107157993A (en) * 2017-04-28 2017-09-15 广西信业生物技术有限公司 It is a kind of to treat pharmaceutical composition of dry skin and preparation method thereof

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WO2017129643A1 (en) * 2016-01-26 2017-08-03 Nestec S.A. Composition for preventing or reducing transepidermal water loss
CN108472274A (en) * 2016-01-26 2018-08-31 雀巢产品技术援助有限公司 Composition for preventing or reducing percutaneous water loss
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CN107157993A (en) * 2017-04-28 2017-09-15 广西信业生物技术有限公司 It is a kind of to treat pharmaceutical composition of dry skin and preparation method thereof

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Inventor after: An Qian

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