CN114452297B - Medicinal preparation for treating dermatitis and preparation method thereof - Google Patents
Medicinal preparation for treating dermatitis and preparation method thereof Download PDFInfo
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- CN114452297B CN114452297B CN202111681747.4A CN202111681747A CN114452297B CN 114452297 B CN114452297 B CN 114452297B CN 202111681747 A CN202111681747 A CN 202111681747A CN 114452297 B CN114452297 B CN 114452297B
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/08—Antiallergic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
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- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention belongs to the technical field of medicines, and particularly relates to a medicinal preparation for treating dermatitis and a preparation method thereof. The pharmaceutical preparation for treating dermatitis is prepared from a pharmaceutical composition and pharmaceutically acceptable auxiliary materials; the pharmaceutical composition consists of tiliroside, bletilla striata polysaccharide and glucocorticoid, wherein the weight ratio of tiliroside, bletilla striata polysaccharide and glucocorticoid is (5-15) (3-12): 1, a step of; the glucocorticoid is fluocinolone acetonide or fluocinolone acetonide. The invention combines the tiliroside, the bletilla polysaccharide and the glucocorticoid for the first time to treat dermatitis, has the anti-inflammatory, antiallergic and antipruritic effects of the glucocorticoid, can inhibit inflammatory signal paths, interfere with proinflammatory cytokine signal transduction, prevent skin wound infection, repair damaged skin, protect skin barrier, reduce the occurrence of hormone-dependent dermatitis caused by improper hormone application, and improve the treatment effect.
Description
Technical Field
The invention belongs to the technical field of medicines, and particularly relates to a medicinal preparation for treating dermatitis and a preparation method thereof.
Background
Fluocinolone acetonide has a chemical name of 11 beta, 21-dihydroxy-16 alpha, 17- [ (1-methylethylene) -bis (oxy) ] -6 alpha, 9-difluoropregna-1, 4-diene-3, 20-dione, and a CAS No. of 67-73-2; the fluocinolone acetonide has the chemical name of 11 beta-hydroxy-16 alpha, 17- [ (1-methylethylene) -bis (oxygen) ] -21- (acetoxy) -6 alpha, 9-difluoro pregna-1, 4-diene-3, 20-dione, wherein the CAS No. is 356-12-7, and the fluocinolone acetonide is fluocinolone acetonide 21-site acetate which belongs to adrenocortical hormone medicines, can shrink dermal capillary vessel, inhibit proliferation or regeneration of epidermal cells, inhibit regeneration of fibrous cells in connective tissues, stabilize intracellular lysosome membranes, prevent tissue injury caused by lysosome enzyme release, and has stronger anti-inflammatory and antiallergic effects. Can be used for treating dermatoses such as allergic dermatitis, atopic dermatitis, contact dermatitis, seborrheic dermatitis, eczema, skin pruritus, psoriasis, and neurodermatitis.
However, the long-term use of fluocinolone acetonide or fluocinolone acetonide causes a series of problems of skin barrier destruction, which are manifested by skin atrophy, telangiectasia, purpura, vellus increase and acne-like skin lesions, with various degrees of itching, burning and other symptoms, and also causes hormone-dependent dermatitis. The hormone-dependent dermatitis is a subacute inflammatory skin disease which forces a patient to take the glucocorticoid again because the original skin disease skin damage and symptoms are obviously improved after the preparation containing the glucocorticoid (such as fluocinolone acetonide, fluocinolone acetonide and the like) is externally used and the original symptoms, physical sign relapse and even aggravation are caused once the preparation is stopped. Studies have shown that hormone-dependent dermatitis is associated with long-term overdose, and out-of-range topical glucocorticoid formulations. Aiming at the problems of damage to skin barrier and occurrence of hormone-dependent dermatitis caused by long-term use of the existing external pharmaceutical preparation containing fluocinolone acetonide or fluocinolone acetonide, the pharmaceutical preparation capable of treating skin inflammatory diseases and simultaneously repairing skin is needed to be provided.
Disclosure of Invention
Aiming at the problems and the defects existing in the prior art, the invention aims at a medicinal preparation for treating dermatitis and a preparation method thereof.
In order to achieve the aim of the invention, the technical scheme adopted by the invention is as follows:
the first aspect of the invention provides a pharmaceutical composition, which consists of tiliroside, bletilla striata polysaccharide and glucocorticoid, wherein the weight ratio of tiliroside, bletilla striata polysaccharide and glucocorticoid is (5-15): (3-12): 1.
according to the above pharmaceutical composition, preferably, the weight ratio of tiliroside, bletilla polysaccharide and glucocorticoid is 10:8:1.
according to the above pharmaceutical composition, preferably, the glucocorticoid is fluocinolone acetonide or fluocinolone acetonide. More preferably, the glucocorticoid is fluocinolone acetonide.
In a second aspect, the present invention provides an application of the pharmaceutical composition described in the first aspect in preparing a medicament for treating dermatitis.
According to the above application, preferably, the dermatitis includes contact dermatitis, allergic dermatitis, atopic dermatitis, seborrheic dermatitis, neurodermatitis, atopic dermatitis, skin pruritus, psoriasis.
The third hair side of the present invention provides a pharmaceutical preparation for treating dermatitis, which is prepared from the pharmaceutical composition of the first aspect and pharmaceutically acceptable auxiliary materials.
The pharmaceutical preparation for treating dermatitis according to the above, preferably, the pharmaceutical preparation is a cream, a solution, a gel, a liniment or a lotion.
The pharmaceutical preparation for treating dermatitis according to the above-mentioned, preferably, the pharmaceutical preparation is a cream, and the pharmaceutical preparation comprises the following components in parts by weight: 0.01-1 part of a pharmaceutical composition, 0.5-1.6 parts of Transcutol P, 0.8-2.6 parts of Solutol HS, 6-12 parts of stearic acid, 6-15 parts of white vaseline, 5-12 parts of liquid paraffin, 2-12 parts of glycerol, 0.01-0.6 part of ethylparaben and 46-65 parts of water.
The pharmaceutical preparation for treating dermatitis according to the above-mentioned, preferably, the composition of the components of the pharmaceutical preparation is as follows in parts by weight: 0.24 part of a pharmaceutical composition, 1 part of Transcutol P, 15 parts of Solutol HS, 7 parts of stearic acid, 10 parts of white vaseline, 8 parts of liquid paraffin, 8 parts of glycerol, 0.16 part of ethylparaben and 63.6 parts of water.
The pharmaceutical preparation for treating dermatitis according to the above, preferably, the dermatitis includes contact dermatitis, allergic dermatitis, atopic dermatitis, seborrheic dermatitis, neurodermatitis, atopic dermatitis, skin pruritus, psoriasis.
In a fourth aspect, the present invention provides a method for preparing a pharmaceutical preparation for treating dermatitis according to the third aspect. The preparation method comprises the following steps:
(1) Sequentially adding Solutol HS15, glycerol and ethylparaben into water, stirring, mixing, and heating to 60-70deg.C to obtain water phase solution;
(2) Dissolving the pharmaceutical composition in Transcutol P to obtain a pharmaceutical solution;
(3) Mixing stearic acid, white vaseline and liquid paraffin, and heating to 65-75deg.C to obtain oil phase solution;
(4) Adding the oil phase solution obtained in the step (3) into the water phase solution, stirring uniformly, adding the medicinal solution prepared in the step (2), mixing uniformly, and condensing into paste to obtain the medicinal preparation for treating dermatitis.
In the pharmaceutical composition of the invention, the efficacy and effect of each component are as follows:
tilia candidum glycoside: tilia mandshurica glycoside is also called kaempferol-3-O-beta-D- (6' -O-trans-p-hydroxy cinnamoyl) glucopyranoside, tilianin, tribulus terrestris glycoside, buddleoside and the like, is a flavonoid glycoside compound, and is yellow needle crystal. Tilia candel glycoside has strong antioxidant activity, free radical scavenging activity, antibacterial and antiinflammatory activity, free radical scavenging effect, antiallergic effect, and inhibiting effect on contact dermatitis of mice caused by 2, 4-dinitrochlorobenzene.
Bletilla striata polysaccharide: the bletilla striata polysaccharide is an extract of bletilla striata (also called bletilla striata), has antibacterial, antiviral and anti-inflammatory effects, can protect mucous membrane and promote wound healing, and researches show that the action mechanism of the bletilla striata polysaccharide for promoting wound healing is possibly related to inhibiting TLR4/LPS signal paths and the expression of downstream inflammatory factors TNF-alpha and IL-6, and can interfere with proinflammatory cytokine signal transduction by inhibiting the inflammatory signal paths, so that the effects of preventing wound infection and promoting wound healing are achieved; meanwhile, the bletilla striata polysaccharide also has the effects of resisting oxidation, delaying skin aging, moisturizing skin, removing freckles, whitening skin, resisting wrinkles, protecting against sunburn and the like.
Compared with the prior art, the invention has the following positive and beneficial effects:
(1) The invention combines the tiliroside, the bletilla polysaccharide and the glucocorticoid for the first time to treat dermatitis, has the anti-inflammatory, antiallergic and antipruritic effects of the glucocorticoid, can inhibit inflammatory signal paths, interfere with proinflammatory cytokine signal transduction, prevent skin wound infection, repair damaged skin, protect skin barrier, reduce the occurrence of hormone-dependent dermatitis caused by improper hormone application, and improve the treatment effect.
(2) The tiliroside and the bletilla polysaccharide in the pharmaceutical composition have antibacterial and anti-inflammatory activities, and the pharmaceutical composition can reduce the dosage of the glucocorticoid in the pharmaceutical preparation on the basis of achieving the same therapeutic effect by compounding the tiliroside, the bletilla polysaccharide and the glucocorticoid, and the prepared pharmaceutical preparation has good spreadability on the skin and good moisturizing performance.
(3) Fluorine acetate is difficult to dissolve, dimethyl sulfoxide is usually used as a solvent for dissolving, but dimethyl sulfoxide is toxic, and after contacting skin, the dimethyl sulfoxide can enter the skin to cause harm to human bodies; in addition, when dimethyl sulfoxide contacts skin, skin is easy to burn and cause skin to have stink feel, which is unfavorable for the treatment of skin inflammation and wound recovery. When the pharmaceutical preparation for treating dermatitis is prepared, the fluocinolone acetonide, the tilianin and the bletilla polysaccharide are dissolved by adopting the Transcutol P, the fluocinolone acetonide can be well dissolved in the Transcutol P, the Transcutol P has low toxicity, no stimulation to skin and safe use. In addition, the invention adopts the Solutol HS15 as the emulsifying dispersant, the Transcutol P and the Solutol HS15 can be mutually dissolved, and the interaction between the Transcutol P and the Solutol HS15 can well realize the dispersion of fluocinolone acetonide, tilioside and bletilla polysaccharide in the cream preparation, has no stimulation to skin and can improve the transdermal effect of the medicine.
Detailed Description
The present invention will be described in further detail with reference to the following examples. Unless otherwise indicated, the materials and chemical reagents used in the examples were conventional commercial products, and the technical means used were conventional means known to those skilled in the art.
Example 1:
a pharmaceutical composition comprises tilioside, bletilla striata polysaccharide and glucocorticoid, wherein the weight ratio of tilioside, bletilla striata polysaccharide and glucocorticoid in the pharmaceutical composition is 10:8:1. The glucocorticoid is fluocinolone acetonide.
Example 2:
a pharmaceutical composition comprises tilioside, bletilla striata polysaccharide and glucocorticoid, wherein the weight ratio of tilioside, bletilla striata polysaccharide and glucocorticoid in the pharmaceutical composition is 15:3:1. The glucocorticoid is fluocinolone acetonide.
Example 3:
a pharmaceutical composition comprises tilioside, bletilla striata polysaccharide and glucocorticoid, wherein the weight ratio of tilioside, bletilla striata polysaccharide and glucocorticoid in the pharmaceutical composition is 5:12:1. The glucocorticoid is fluocinolone acetonide.
Example 4:
a pharmaceutical composition comprises tilioside, bletilla striata polysaccharide and glucocorticoid, wherein the weight ratio of tilioside, bletilla striata polysaccharide and glucocorticoid in the pharmaceutical composition is 8:10:1. The glucocorticoid is fluocinolone acetonide.
Example 5:
a pharmaceutical composition comprises tilioside, bletilla striata polysaccharide and glucocorticoid, wherein the weight ratio of tilioside, bletilla striata polysaccharide and glucocorticoid in the pharmaceutical composition is 6:9:1. The glucocorticoid is fluocinolone acetonide.
Example 6:
a pharmaceutical composition comprises tilioside, bletilla striata polysaccharide and glucocorticoid, wherein the weight ratio of tilioside, bletilla striata polysaccharide and glucocorticoid in the pharmaceutical composition is 12:5:1. The glucocorticoid is fluocinolone acetonide.
Example 7:
a pharmaceutical composition comprises tilioside, bletilla striata polysaccharide and glucocorticoid, wherein the weight ratio of tilioside, bletilla striata polysaccharide and glucocorticoid in the pharmaceutical composition is 10:12:1. The glucocorticoid is fluocinolone acetonide.
Example 8:
the pharmaceutical preparation for treating dermatitis is cream, and comprises the following components in parts by weight: 0.24g of a pharmaceutical composition, 1g of Transcutol P, 15g of Solutol HS, 7g of stearic acid, 10g of white vaseline, 8g of liquid paraffin, 8g of glycerol, 0.16g of ethylparaben and 63.6g of water. Wherein the pharmaceutical composition is the pharmaceutical composition of example 1.
The preparation method of the pharmaceutical preparation for treating dermatitis comprises the following specific steps:
(1) Sequentially adding Solutol HS15, glycerol and ethylparaben into water, stirring, mixing, and heating to 65deg.C to obtain water phase solution;
(2) Dissolving the pharmaceutical composition in Transcutol P to obtain a pharmaceutical solution;
(3) Mixing stearic acid, white vaseline and liquid paraffin, and heating to 70deg.C to obtain oil phase solution;
(4) Adding the oil phase solution obtained in the step (3) into the water phase solution, stirring uniformly, adding the medicinal solution prepared in the step (2), mixing uniformly, and condensing into paste to obtain the medicinal preparation for treating dermatitis.
Example 9:
the pharmaceutical preparation for treating dermatitis is cream, and comprises the following components in parts by weight: 0.5g of medicine composition, 0.8g of Transcutol P, 15.2 g of Solutol HS, 6g of stearic acid, 12g of white vaseline, 10g of liquid paraffin, 10g of glycerol, 0.5g of ethylparaben and 58g of water. Wherein the pharmaceutical composition is the pharmaceutical composition of example 1.
The preparation method of the pharmaceutical preparation for treating dermatitis comprises the following specific steps:
(1) Sequentially adding Solutol HS15, glycerol and ethylparaben into water, stirring, mixing, and heating to 60deg.C to obtain water phase solution;
(2) Dissolving the pharmaceutical composition in Transcutol P to obtain a pharmaceutical solution;
(3) Mixing stearic acid, white vaseline and liquid paraffin, and heating to 75deg.C to obtain oil phase solution;
(4) Adding the oil phase solution obtained in the step (3) into the water phase solution, stirring uniformly, adding the medicinal solution prepared in the step (2), mixing uniformly, and condensing into paste to obtain the medicinal preparation for treating dermatitis.
Example 10:
the pharmaceutical preparation for treating dermatitis is cream, and comprises the following components in parts by weight: 0.01g of a pharmaceutical composition, 0.5g of Transcutol P, 15.6 g of Solutol HS, 8g of stearic acid, 12g of white vaseline, 10g of liquid paraffin, 12g of glycerol, 0.09g of ethylparaben and 54.8g of water. Wherein the pharmaceutical composition is the pharmaceutical composition of example 1.
The preparation method of the pharmaceutical preparation for treating dermatitis comprises the following specific steps:
(1) Sequentially adding Solutol HS15, glycerol and ethylparaben into water, stirring, mixing, and heating to 70deg.C to obtain water phase solution;
(2) Dissolving the pharmaceutical composition in Transcutol P to obtain a pharmaceutical solution;
(3) Mixing stearic acid, white vaseline and liquid paraffin, and heating to 65deg.C to obtain oil phase solution;
(4) Adding the oil phase solution obtained in the step (3) into the water phase solution, stirring uniformly, adding the medicinal solution prepared in the step (2), mixing uniformly, and condensing into paste to obtain the medicinal preparation for treating dermatitis.
Example 11:
the pharmaceutical preparation for treating dermatitis is cream, and comprises the following components in parts by weight: 0.1g of a pharmaceutical composition, 0.6g of Transcutol P, 15.4 g of Solutol HS, 6g of stearic acid, 15g of white vaseline, 12g of liquid paraffin, 12g of glycerol, 0.1g of ethylparaben and 52.8g of water. Wherein the pharmaceutical composition is the pharmaceutical composition of example 1.
The preparation method of the above pharmaceutical preparation for treating dermatitis is the same as that of example 8.
Example 12:
the pharmaceutical preparation for treating dermatitis is cream, and comprises the following components in parts by weight: 0.8g of a pharmaceutical composition, 1.2g of Transcutol P, 15.0 g of Solutol HS, 12g of stearic acid, 12g of white vaseline, 5g of liquid paraffin, 2g of glycerol, 0.5g of ethylparaben and 64.5g of water. Wherein the pharmaceutical composition is the pharmaceutical composition of example 1.
The preparation method of the above pharmaceutical preparation for treating dermatitis is the same as that of example 8.
Example 13:
the pharmaceutical preparation for treating dermatitis is cream, and comprises the following components in parts by weight: 1g of a pharmaceutical composition, 1.6g of Transcutol P, 15.8 g of Solutol HS, 8g of stearic acid, 10g of white vaseline, 8g of liquid paraffin, 12g of glycerol, 0.6g of ethylparaben and 58g of water. Wherein the pharmaceutical composition is the pharmaceutical composition of example 1.
The preparation method of the above pharmaceutical preparation for treating dermatitis is the same as that of example 8.
Example 14:
the pharmaceutical preparation for treating dermatitis is cream, and comprises the following components in parts by weight: 0.3g of a medicine composition, 1.2g of Transcutol P, 15g of Solutol HS, 12g of stearic acid, 15g of white vaseline, 12g of liquid paraffin, 12g of glycerol, 0.5g of ethylparaben and 46g of water. Wherein the pharmaceutical composition is the pharmaceutical composition of example 1.
The preparation method of the above pharmaceutical preparation for treating dermatitis is the same as that of example 8.
Example 15:
the content of example 15 is substantially the same as that of example 8, except that: the pharmaceutical composition used in the pharmaceutical preparation for treating dermatitis is the pharmaceutical composition described in example 2.
Example 16:
the content of example 16 is substantially the same as that of example 9, except that: the pharmaceutical composition used in the pharmaceutical preparation for treating dermatitis is the pharmaceutical composition described in example 3.
Example 17:
the content of example 17 is substantially the same as that of example 8, except that: the pharmaceutical composition used in the pharmaceutical preparation for treating dermatitis is the pharmaceutical composition described in example 4.
Example 18:
the content of example 18 is substantially the same as that of example 8, except that: the pharmaceutical composition used in the pharmaceutical preparation for treating dermatitis is the pharmaceutical composition described in example 5.
Example 19:
example 19 is substantially identical to example 8 except that: the pharmaceutical composition used in the pharmaceutical preparation for treating dermatitis is the pharmaceutical composition described in example 6.
Example 20:
the content of example 20 is substantially the same as that of example 9, except that: the pharmaceutical composition used in the pharmaceutical preparation for treating dermatitis is the pharmaceutical composition described in example 7.
Example 21:
the pharmaceutical preparation for treating dermatitis is a solution, and comprises the following components in parts by weight: 1g of a pharmaceutical composition, 1.0g of Transcutol P, 15.0 g of Solutol HS, 0.2g of ethylparaben and 96.8g of water. Wherein the pharmaceutical composition is the pharmaceutical composition of example 1.
Efficacy verification experiment of the pharmaceutical preparation for treating dermatitis:
efficacy verification experiments were performed by taking the pharmaceutical preparation for treating dermatitis prepared in example 8 of the present invention as an example. Meanwhile, for comparison with the pharmaceutical preparation for treating dermatitis of the present invention, the present invention also conducted a comparative test, the specific contents of which are shown in comparative examples 1 to 3.
Comparative example 1:
the pharmaceutical preparation is cream, and comprises the following components in parts by weight: tilia mandshurica glycoside 0.126g, transcutol P1 g, solutol HS15 g, stearic acid 7g, white vaseline 10g, liquid paraffin 8g, glycerol 8g, ethyl hydroxy benzoate 0.16g, and water 63.714g.
The preparation method of the pharmaceutical preparation comprises the following specific steps:
(1) Sequentially adding Solutol HS15, glycerol and ethylparaben into water, stirring, mixing, and heating to 65deg.C to obtain water phase solution;
(2) Dissolving tiliroside in Transcutol P to obtain medicinal solution;
(3) Mixing stearic acid, white vaseline and liquid paraffin, and heating to 70deg.C to obtain oil phase solution;
(4) Adding the oil phase solution obtained in the step (3) into the water phase solution, uniformly stirring, adding the medicine solution prepared in the step (2), uniformly mixing, and condensing into paste to obtain the medicine preparation.
Comparative example 2:
the pharmaceutical preparation is cream, and comprises the following components in parts by weight: bletilla striata polysaccharide 0.1g, transcutol P1 g, solutol HS15 g, stearic acid 7g, white vaseline 10g, liquid paraffin 8g, glycerol 8g, ethylparaben 0.16g, and water 63.74g.
The preparation method of the pharmaceutical preparation comprises the following specific steps:
(1) Sequentially adding Solutol HS15, glycerol and ethylparaben into water, stirring, mixing, and heating to 65deg.C to obtain water phase solution;
(2) Dissolving rhizoma bletilla polysaccharide in Transcutol P to obtain medicinal solution;
(3) Mixing stearic acid, white vaseline and liquid paraffin, and heating to 70deg.C to obtain oil phase solution;
(4) Adding the oil phase solution obtained in the step (3) into the water phase solution, uniformly stirring, adding the medicine solution prepared in the step (2), uniformly mixing, and condensing into paste to obtain the medicine preparation.
Comparative example 3:
comparative example 3 was essentially the same as example 8, except that the formulation contained no pharmaceutical composition.
1. The pharmaceutical preparation for treating dermatitis of the invention is an experiment for inhibiting the swelling of mouse auricle caused by paraxylene
(1) Experimental drugs: the pharmaceutical preparation for treating dermatitis prepared in example 8 of the present invention, the pharmaceutical preparation prepared in comparative test 1-comparative test 3, and commercially available fluocinolone acetonide cream (10 g,10g of fluocinolone acetonide cream, 2.5mg in amount).
(2) Test animals: SPF grade ICR mice, 48, male, weighing 18-22g.
(3) The test method comprises the following steps: the 48 mice were randomly divided into a blank control group, an experimental group, a control group 1, a control group 2, a control group 3 and a positive control group, 8 each. The right ear of each group of mice is smeared with the medicament corresponding to each group of mice in table 1, 0.1g of the medicament is smeared each time every day, the smeared each time in the morning and evening, and the medicament is continuously administrated for 4 days. 30 mu l of dimethylbenzene is coated on the front and back surfaces of the right auricle of the mouse 40min after the last application, the mouse is killed after cervical dislocation, round lugs are taken off from the agreeing parts of the left and right ears of the mouse respectively by using a puncher (diameter of 7 mm), the round lugs are weighed, the difference between the weights of the left and right lugs is used as an index of swelling degree, the inhibition rate of different pharmaceutical preparations on auricle swelling is calculated, and a t-test method between groups is adopted to carry out significance measurement and comparison with a model group. The specific results are shown in Table 1. Wherein, swelling = right ear weight-left ear weight; inhibition = (blank swelling degree-dosing swelling degree)/blank 100%.
Table 1 effect of each pharmaceutical formulation on xylene-induced swelling of mouse auricle
| Group of | Smearing medicament | Inhibition rate |
| Blank control group | Distilled water | -- |
| Experimental group | Pharmaceutical formulation prepared in example 8 | 73.35％ |
| Control group 1 | Pharmaceutical preparation prepared in comparative example 1 | 38.57％ |
| Control group 2 | Pharmaceutical preparation prepared in comparative example 2 | 40.05％ |
| Control group 3 | Pharmaceutical preparation prepared in comparative example 3 | 1.28％ |
| Positive control group | Commercial flomofetil acetate cream | 75.42％ |
As shown in Table 1, the pharmaceutical preparation prepared by the invention has good inhibition effect on mouse auricle swelling caused by dimethylbenzene, the inhibition effect is similar to that of commercially available fluocinolone acetonide emulsifiable paste, and the inhibition effect is obviously higher than that of a preparation which takes tilioside and bletilla polysaccharide as active medicaments alone, so that the pharmaceutical preparation has a synergistic effect by compounding the tilioside, the bletilla polysaccharide and the fluocinolone acetonide. In addition, the content of fluocinolone acetonide in the pharmaceutical preparation is obviously lower than that of commercially available fluocinolone acetonide emulsifiable paste; therefore, the pharmaceutical preparation of the invention can effectively reduce the dosage of hormone and effectively avoid symptoms such as dependency dermatitis and the like which occur in long-term use.
2. The pharmaceutical preparation for treating dermatitis of the invention is an experiment for inhibiting the increase of the abdominal capillary permeability of mice caused by paraxylene
(1) Experimental drugs: the pharmaceutical preparation for treating dermatitis prepared in example 8 of the present invention, the pharmaceutical preparation prepared in comparative test 1-comparative test 3, and commercially available fluocinolone acetonide cream (10 g,10g of fluocinolone acetonide cream, 2.5mg in amount).
(2) Test animals: SPF grade ICR mice, 48, male, weighing 18-22g.
(3) The test method comprises the following steps: the 48 mice were randomly divided into a blank control group, an experimental group, a control group 1, a control group 2, a control group 3 and a positive control group, 8 each. The same portion of the abdomen of each group of mice was shaved (about 2 x 2cm in area) 2 ) The skin of the abdomen dehairing part of each group of mice is smeared with the corresponding medicament of each group of mice in the table 2, 0.1g of the medicament is smeared each time, and the medicament is sequentially and continuously administrated for 4 days in the morning and evening each day. 40min after the last application, 0.5% Evan blue victory saline solution (0.1 ml/10g B.W.) was injected intravenously through the tail of the mice, 30 μl of xylene was applied to the dehaired skin of the abdomen of the mice immediately, the reagent treatment was carried out after 20min, the absorbance value was measured after 3 days, the inhibition rate of the capillary permeability of the abdomen of the mice by different pharmaceutical preparations was calculated according to the absorbance value, and the significance determination and comparison were carried out by adopting an inter-group t-test method and a model group. The specific results are shown in Table 2. Wherein inhibition ratio = (absorbance value of blank control group-absorbance value of dosing group)/blank control group × 100%.
TABLE 2 Effect of various pharmaceutical formulations on xylene-induced mouse abdominal capillary permeability
| Group of | Smearing medicament | Inhibition rate |
| Blank control group | Distilled water | -- |
| Experimental group | Pharmaceutical formulation prepared in example 8 | 72.62％ |
| Control group 1 | Pharmaceutical preparation prepared in comparative example 1 | 42.39％ |
| Control group 2 | Pharmaceutical preparation prepared in comparative example 2 | 36.07％ |
| Control group 3 | Pharmaceutical preparation prepared in comparative example 3 | 1.45％ |
| Positive control group | Commercial flomofetil acetate cream | 73.18％ |
As shown in Table 2, the inhibition effect of the pharmaceutical preparation prepared by the invention on the increase of the capillary permeability of the abdomen of the mice caused by the dimethylbenzene is similar to that of commercially available fluocinolone acetonide emulsifiable paste, and the inhibition effect is obviously higher than that of a preparation which takes tilioside and bletilla polysaccharide as active medicaments alone, which proves that the invention has a synergistic effect by compounding the tilioside, the bletilla polysaccharide and the fluocinolone acetonide.
3. The pharmaceutical preparation for treating dermatitis has the treatment effect on guinea pig itch caused by histamine phosphate
(1) Experimental drugs: the pharmaceutical preparation for treating dermatitis prepared in example 8 of the present invention, the pharmaceutical preparation prepared in comparative test 1-comparative test 3, and commercially available fluocinolone acetonide cream (10 g,10g of fluocinolone acetonide cream, 2.5mg in amount).
(2) The test method comprises the following steps: 30 guinea pigs (body weight 210-240 g) were randomly divided into a blank control group, an experimental group, a control group 1, a control group 2, a control group 3 and a positive control group, 8 each. Hairbrush of the same portion of the right hind instep of each group of guinea pigs (about 2 x 2cm in area) 2 ) The hairless parts are cleaned and wiped dry, the skin of the hairless parts of each group of guinea pigs is smeared with the medicament corresponding to each group of guinea pigs in table 3, 0.1g each time, and the hairless parts are smeared once every morning and afternoon and are continuously administrated for 4 days. 2 hours after the application of the medicine on the 4 th day, the dehairing place is scratched to redness (no bleeding) by using sand paper, then the corresponding medicine is smeared on the scratched place, and after 2 hours, the corresponding medicine is smeared again; finally, 15min after the sequential application, 0.01% of histamine phosphate (50 μl/dose) is initially applied to the wound surface, and the concentration is gradually increased by 0.02%, 0.03% and 0.04% every 3min, and the dosage is 50 μl/dose until the total amount of the histamine phosphate which is applied when the guinea pig licks the right foot back is taken as an itching threshold.
TABLE 3 influence of the pharmaceutical formulations on the itching response of histamine phosphate
| Group of | Smearing medicament | Itching threshold (mug) |
| Blank control group | Distilled water | 0.18±0.14 |
| Experimental group | Pharmaceutical formulation prepared in example 8 | 0.86±0.23 |
| Control group 1 | Pharmaceutical preparation prepared in comparative example 1 | 0.37±0.09 |
| Control group 2 | Pharmaceutical preparation prepared in comparative example 2 | 0.46±0.32 |
| Control group 3 | Pharmaceutical preparation prepared in comparative example 3 | 0.19±0.19 |
| Positive control group | Commercial flomofetil acetate cream | 0.91±0.16 |
As can be seen from Table 3, the medicinal preparation prepared by the invention has an itching threshold close to that of commercially available fluocinolone acetonide emulsifiable paste, and the itching threshold is obviously higher than that of a preparation taking tilioside and bletilla polysaccharide as active medicaments.
The above description is merely illustrative of the preferred embodiments of the present invention and is not intended to limit the invention to the particular embodiments disclosed, but on the contrary, the intention is to cover all modifications, equivalents, and alternatives falling within the spirit and scope of the invention.
Claims (8)
1. A pharmaceutical composition is characterized in that the pharmaceutical composition consists of tilioside, bletilla striata polysaccharide and glucocorticoid, wherein the weight ratio of tilioside, bletilla striata polysaccharide and glucocorticoid is (5-15): 1 (3-12); the glucocorticoid is fluocinolone acetonide or fluocinolone acetonide.
2. The pharmaceutical composition according to claim 1, wherein the weight ratio of tiliroside, bletilla polysaccharide to glucocorticoid is 10:8:1.
3. use of a pharmaceutical composition according to claim 1 or 2 for the preparation of a medicament for the treatment of dermatitis.
4. A pharmaceutical formulation for treating dermatitis, characterized in that it is prepared from the pharmaceutical composition of claim 1 or 2 and pharmaceutically acceptable excipients.
5. The pharmaceutical formulation for treating dermatitis according to claim 4, wherein said pharmaceutical formulation is a cream, a gel, a liniment or a lotion.
6. The pharmaceutical preparation for treating dermatitis according to claim 5, wherein said pharmaceutical preparation is a cream, and comprises the following components in parts by weight: 0.01-1 part of a pharmaceutical composition, 0.5-1.6 parts of Transcutol P, 0.8-2.6 parts of Solutol HS, 6-12 parts of stearic acid, 6-15 parts of white vaseline, 5-12 parts of liquid paraffin, 2-12 parts of glycerol, 0.01-0.6 part of ethylparaben and 46-65 parts of water.
7. The dermatitis therapeutic preparation as claimed in claim 6, wherein the pharmaceutical preparation comprises the following components in parts by weight: 0.24 part of a pharmaceutical composition, 1 part of Transcutol P, 15 parts of Solutol HS, 7 parts of stearic acid, 10 parts of white vaseline, 8 parts of liquid paraffin, 8 parts of glycerol, 0.16 part of ethylparaben and 63.6 parts of water.
8. A method of preparing a pharmaceutical formulation for treating dermatitis according to claim 6 or 7, comprising the steps of:
(1) Sequentially adding Solutol HS15, glycerol and ethylparaben into water, stirring, mixing, and heating to 60-70deg.C to obtain water phase solution;
(2) Dissolving the pharmaceutical composition in Transcutol P to obtain a pharmaceutical solution;
(3) Mixing stearic acid, white vaseline and liquid paraffin, and heating to 65-75deg.C to obtain oil phase solution;
(4) Adding the oil phase solution obtained in the step (3) into the water phase solution, stirring uniformly, adding the medicinal solution prepared in the step (2), mixing uniformly, and condensing into paste to obtain the medicinal preparation for treating dermatitis.
Priority Applications (1)
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| CN101795733A (en) * | 2007-08-13 | 2010-08-04 | 默克专利股份有限公司 | tyrosinase inhibitors |
| CN102379878A (en) * | 2011-07-15 | 2012-03-21 | 吉林敖东集团大连药业股份有限公司 | Pharmaceutical composition for treating dermatitis and eczema and preparation method thereof |
| WO2013138744A1 (en) * | 2012-03-16 | 2013-09-19 | M. Alphabet 1, Llc | Compositions for the treatment of skin disorders |
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| CN101795733A (en) * | 2007-08-13 | 2010-08-04 | 默克专利股份有限公司 | tyrosinase inhibitors |
| CN102379878A (en) * | 2011-07-15 | 2012-03-21 | 吉林敖东集团大连药业股份有限公司 | Pharmaceutical composition for treating dermatitis and eczema and preparation method thereof |
| WO2013138744A1 (en) * | 2012-03-16 | 2013-09-19 | M. Alphabet 1, Llc | Compositions for the treatment of skin disorders |
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