CN113143848A - External cream for treating psoriasis and preparation method thereof - Google Patents
External cream for treating psoriasis and preparation method thereof Download PDFInfo
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- CN113143848A CN113143848A CN202110354696.8A CN202110354696A CN113143848A CN 113143848 A CN113143848 A CN 113143848A CN 202110354696 A CN202110354696 A CN 202110354696A CN 113143848 A CN113143848 A CN 113143848A
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- 201000004681 Psoriasis Diseases 0.000 title claims abstract description 38
- 238000002360 preparation method Methods 0.000 title abstract description 11
- BNPSSFBOAGDEEL-UHFFFAOYSA-N albuterol sulfate Chemical compound OS(O)(=O)=O.CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1.CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1 BNPSSFBOAGDEEL-UHFFFAOYSA-N 0.000 claims abstract description 30
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- 206010000349 Acanthosis Diseases 0.000 description 1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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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- 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
- A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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Abstract
The invention discloses an external cream for treating psoriasis and a preparation method thereof, and aims to provide an external cream which has small side effect and no irritation to human body and has good psoriasis treatment effect by transdermal administration, wherein each 100 parts of the external cream are prepared from the following raw materials in parts by weight: 0.4-0.6 part of salbutamol sulfate, 5-25 parts of stearyl alcohol, 5-25 parts of white vaseline, 1-10 parts of sodium dodecyl sulfate, 5-15 parts of propylene glycol and the balance of water; belongs to the technical field of medicine.
Description
Technical Field
The invention relates to an external cream, in particular to an external cream for treating psoriasis, and also relates to a preparation method of the external cream for treating psoriasis; belongs to the technical field of medicine.
Background
Salbutamol (Salbutamol) is a very effective adrenergic beta 2-receptor agonist with anti-inflammatory action, and has been used as a first-line medicament for clinically treating asthma for over 40 years and has always played an irreplaceable role. The anti-inflammatory effect of the salbutamol sulfate is also successfully verified through the in vivo research of ACD mice and the in vitro research of macrophages after proinflammatory. Thus, salbutamol sulfate is also used in the treatment of skin diseases such as psoriasis, eczema, contact dermatitis, and the like.
Psoriasis (Psoriasisis), which is called as rhizoma dioscoreae nipponicae in traditional Chinese medicine and is commonly called as Psoriasis. Is an autoimmune dermatosis which is regulated by genetic genes and mediated by T lymphocytes, and the worldwide morbidity is 2 to 3 percent. Its major histopathological changes are abnormal keratinocyte proliferation, parakeratosis, hyperkeratosis, angiogenesis and inflammatory cell infiltration, which are among the most common chronic inflammatory proliferative skin diseases. Psoriasis is stubborn in condition and easy to recur, can cause damage to the whole system, seriously affects the life quality and even the life cycle of patients, and is one of the diseases which are mainly concerned at home and abroad at present. The etiology and pathogenesis of the psoriasis are not completely clear at present, and no effective radical treatment method exists, but T cell mediated immune response abnormity plays an important role in the pathogenesis of the psoriasis. At present, mild to moderate psoriasis at home and abroad is treated by using glucocorticoid and vitamin D analogue in a local way. However, long-term use of corticosteroid hormones causes side effects such as loss of efficacy, skin atrophy, etc., and the therapeutic effect of vitamin D analogues is not ideal. Therefore, research, development and application of external psoriasis treatment drugs are one of the research hotspots nowadays.
According to the reports of relevant documents, the salbutamol sulfate is used for treating psoriasis, and currently, the clinical application of the salbutamol sulfate is mainly to administer the salbutamol sulfate orally or by injection, including tablets, injections and other dosage forms. However, it has been shown that chronic treatment with such systemic administration, either orally or by injection, can lead to various side effects in patients, such as diarrhea, upper respiratory tract infection, skin itch, inflammatory bowel disease, etc. Oral and injection administration are therefore not the most ideal therapeutic administration. Aiming at the requirements of patients with skin diseases, a novel external preparation medicament is developed for local administration treatment, so that the treatment effect can be improved and the side effect caused by long-term systemic administration can be avoided. The cream as a medicament form has the characteristics of simple preparation process, easy use, good biocompatibility, high bioavailability and the like, and has shown superiority in clinical application.
Disclosure of Invention
In view of the above problems, the present invention aims to provide an external cream which has low side effects on human bodies, is non-irritating, and has good psoriasis treatment effect by transdermal administration.
The second purpose of the invention is to provide a preparation method of the external cream, which is simple and easy to industrialize.
A topical cream for the treatment of psoriasis, each 100 parts of topical cream is prepared from the following raw materials by weight: 0.4-0.6 part of salbutamol sulfate, 5-25 parts of stearyl alcohol, 5-25 parts of white vaseline, 1-10 parts of sodium dodecyl sulfate, 5-15 parts of propylene glycol and the balance of water.
Further, each 100 parts of the external cream for treating psoriasis is prepared from the following raw materials in parts by weight: 0.4-0.6 part of salbutamol sulfate, 10-20 parts of stearyl alcohol, 10-20 parts of white vaseline, 3-7 parts of sodium dodecyl sulfate, 8-12 parts of propylene glycol and the balance of water.
Further, the external cream for treating psoriasis has the following structural formula:
further, in the external cream for treating psoriasis, the salbutamol sulfate is powder salbutamol sulfate.
Further, in the external cream for treating psoriasis, the stearyl alcohol is cetearyl alcohol.
The second technical scheme provided by the invention is as follows:
a method for preparing a topical cream for treating psoriasis, comprising the steps of:
1) the external cream is prepared from the following raw materials in parts by weight per 100 parts of the external cream: 0.4-0.6 part of salbutamol sulfate, 5-25 parts of stearyl alcohol, 5-25 parts of white vaseline, 1-10 parts of sodium dodecyl sulfate, 5-15 parts of propylene glycol and the balance of water by weight, and weighing each component;
2) heating stearyl alcohol and white vaseline weighed in the step 1) to 70-90 ℃, and uniformly stirring to obtain an oil phase;
3) dissolving the salbutamol sulfate obtained in the step 2) in water, stirring to fully dissolve the salbutamol sulfate, adding sodium dodecyl sulfate and propylene glycol, heating to 70-90 ℃, and uniformly stirring to obtain a water phase;
4) and (3) under the heating condition of 70-90 ℃, gradually adding the water phase into the oil phase, stirring while adding, and then complementing water to 100g until the water is condensed to obtain the water-soluble organic silicon dioxide.
Further, in the above preparation method of the external cream for treating psoriasis, the heating temperature in the step 2) is 75 ℃.
Further, in the above preparation method of the external cream for treating psoriasis, the heating temperature in step 3) is 75 ℃.
Compared with the prior art, the technical scheme provided by the invention has the following technical advantages:
1. the cream prepared by the invention has uniform and fine properties, stable system, easy storage, good compatibility, high bioavailability, no irritation reaction to skin and good safety. The cream has good anti-inflammatory effect, and has remarkable effect in treating psoriasis.
2. The technical scheme provided by the invention is simple in preparation method and easy for industrial batch production.
Drawings
FIG. 1 is a chromatogram of a cream assay provided in example 1 of the present application;
FIG. 2 is a pathological section of skin tissues of experimental animals in normal group and model group.
Detailed Description
In order to make the aforementioned objects, features and advantages of the present invention comprehensible, embodiments accompanied with examples are described in detail below.
Example 1
The invention provides an external cream for treating psoriasis, which is prepared by the following steps:
1) weighing 25g of cetostearyl alcohol and 25g of white vaseline, heating to 75 ℃, and uniformly stirring to obtain an oil phase;
2) weighing 0.5g of salbutamol sulfate, dissolving the salbutamol sulfate in 20g of ultrapure water, stirring to fully dissolve the salbutamol sulfate, weighing 10g of sodium dodecyl sulfate and 12g of 1, 3-propylene glycol, adding the sodium dodecyl sulfate and the 1, 3-propylene glycol, heating to 75 ℃, and uniformly stirring to obtain a water phase;
3) gradually adding the water phase into the oil phase under the heating condition of 75 ℃, then supplementing the water amount to 100g, stirring while adding, and then standing for condensation to obtain the external cream.
Example 2
The invention provides an external cream for treating psoriasis, which is prepared by the following steps:
1) weighing 20g of cetearyl alcohol and 20g of white vaseline, heating to 75 ℃, and uniformly stirring to obtain an oil phase;
2) weighing 0.4g of salbutamol sulfate, dissolving the salbutamol sulfate in 20g of ultrapure water, stirring to fully dissolve the salbutamol sulfate, weighing 10g of sodium dodecyl sulfate and 15g of 1, 3-propylene glycol, adding the sodium dodecyl sulfate and the 1, 3-propylene glycol, heating to 75 ℃, and uniformly stirring to obtain a water phase;
3) gradually adding the water phase into the oil phase under the heating condition of 75 ℃, then supplementing the water amount to 100g, stirring while adding, and then standing for condensation to obtain the external cream.
Example 3
The invention provides an external cream for treating psoriasis, which is prepared by the following steps:
1) weighing 10g of cetearyl alcohol and 10g of white vaseline, heating to 75 ℃, and uniformly stirring to obtain an oil phase;
2) weighing 0.6g of salbutamol sulfate, dissolving the salbutamol sulfate in 20g of ultrapure water, stirring to fully dissolve the salbutamol sulfate, weighing 10g of sodium dodecyl sulfate and 15g of 1, 3-propylene glycol, adding the sodium dodecyl sulfate and the 1, 3-propylene glycol, heating to 75 ℃, and uniformly stirring to obtain a water phase;
3) gradually adding the water phase into the oil phase under the heating condition of 75 ℃, then supplementing the water amount to 100g, stirring while adding, and then standing for condensation to obtain the external cream.
Example 4
The invention provides an external cream for treating psoriasis, which is prepared by the following steps:
1) weighing 5g of cetearyl alcohol and 5g of white vaseline, heating to 75 ℃, and uniformly stirring to obtain an oil phase;
2) weighing 0.6g of levalbuterol sulfate, dissolving in 20g of ultrapure water, stirring to fully dissolve, weighing 1g of sodium dodecyl sulfate and 5g of 1, 3-propylene glycol, adding, heating to 75 ℃, and uniformly stirring to obtain a water phase;
3) gradually adding the water phase into the oil phase under the heating condition of 75 ℃, then supplementing the water amount to 100g, stirring while adding, and then standing for condensation to obtain the external cream.
In order to prove the technical scheme provided by the invention, the following provides the technical scheme property evaluation provided by the embodiment 1 of the application
1. Evaluation of cream quality criteria
And (3) performing quality standard research on the cream by adopting an HPLC method, and performing drug racemization determination on the cream.
Chromatograph: waters semi-preparative HPLC purification system
A chromatographic column: chiracel OJ-H chiral column (250X 4.6mm,5mm)
Mobile phase: n-hexane-anhydrous ethanol-trifluoroacetic acid-triethylamine (95:5:0.05:0.02) as a mobile phase
Detection wavelength: 276nm
Flow rate: 1ml/min
Sample introduction amount: 100ml of
Column temperature: at room temperature
The experimental results are shown in FIG. 1, ee ≧ 98% (R-S))/(R + S).
Experiments show that the salbutamol sulfate does not have racemization reaction in the cream mechanism system, and the anti-inflammatory drug has good stability in the system.
2. Research on drug effect of external cream
Animal modeling and histological evaluation are carried out by adopting an imiquimod induction method to research the drug effect of the external cream.
Experimental Material
Medicine reagent: the topical cream obtained in example 1 (homemade, 0.5% R-sal); compound dexamethasone acetate gel (jinri pharmaceutical (china) limited); imiquimod cream (Sichuan mingxin pharmaceutical industry, llc)
Experimental animals: BALB/C mouse, female, 8-11week, Guangzhou city, Happy as Biotech Co., Ltd
The results of the experiment are shown in FIG. 2. The normal group skin tissue structure is basically normal, the horny layer has no hyperkeratosis, the dermal collagen fibers are arranged regularly, and no obvious inflammatory cell infiltration is seen. The skin tissue structure of the model group is abnormal, the horny layer is hyperkeratotic and obviously thickened, and Munro micro-abscesses can be seen, partial parakeratosis is shown by black arrows, the dermis acanthosis is thickened and the cell number is increased, and the spinous processes are prolonged and fused; collagen fibers shown by yellow arrows are arranged in order; large cells, indicated by green arrows, did not increase in number. Salbutamol has basically normal skin tissue structure, parakeratosis is partially observed, and cell nuclei which are not completely keratinized are observed, as shown by black arrows; the dermis is normal and no inflammatory cell infiltration is seen. The dexamethasone group has slight abnormal skin tissue structure, hyperkeratosis of the horny layer and obvious thickening, and a Munro abscess and a large amount of necrotic neutrophils are gathered as shown by black arrows; hyphal structures were visible in the stratum corneum, as indicated by the red arrows. The spinous processes of the spinous layers of the dermis layer are elongated as indicated by the yellow arrows.
Conclusion of the experiment
The results of animal model establishment and skin tissue analysis of experimental animals show that the external cream provided by the invention has good effect and obvious anti-inflammatory effect in the treatment of psoriasis, and the external cream preparation is proved to have good efficacy.
The above-mentioned embodiments only express several embodiments of the present invention, and the description thereof is more specific and detailed, but not construed as limiting the scope of the present invention. It should be noted that, for a person skilled in the art, several variations and modifications can be made without departing from the inventive concept, which falls within the scope of the present invention. Therefore, the protection scope of the present patent shall be subject to the appended claims.
Claims (8)
1. The external cream for treating psoriasis is characterized in that each 100 parts of the external cream is prepared from the following raw materials in parts by weight: 0.4-0.6 part of salbutamol sulfate, 5-25 parts of stearyl alcohol, 5-25 parts of white vaseline, 1-10 parts of sodium dodecyl sulfate, 5-15 parts of propylene glycol and the balance of water.
2. The external cream for treating psoriasis according to claim 1, wherein each 100 parts of external cream is prepared from the following raw materials by weight: 0.4-0.6 part of salbutamol sulfate, 10-20 parts of stearyl alcohol, 10-20 parts of white vaseline, 3-7 parts of sodium dodecyl sulfate, 8-12 parts of propylene glycol and the balance of water.
3. A topical cream for the treatment of psoriasis according to claim 1 or claim 2 wherein the salbutamol sulphate has the formula:
4. an external cream for the treatment of psoriasis according to claim 1 or 2 wherein the salbutamol sulphate is powdered salbutamol sulphate.
5. The topical cream for the treatment of psoriasis according to claim 1 or 2 wherein the stearyl alcohol is cetostearyl alcohol.
6. A method of making a topical cream for the treatment of psoriasis according to claim 1 comprising the steps of:
1) weighing the components according to the weight of claim 1;
2) heating stearyl alcohol and white vaseline weighed in the step 1) to 70-90 ℃, and uniformly stirring to obtain an oil phase;
3) dissolving the salbutamol sulfate obtained in the step 2) in water, stirring to fully dissolve the salbutamol sulfate, adding sodium dodecyl sulfate and propylene glycol, heating to 70-90 ℃, and uniformly stirring to obtain a water phase;
4) and (3) under the heating condition of 70-90 ℃, gradually adding the water phase into the oil phase, stirring while adding, and then complementing water to 100g until the water is condensed to obtain the water-soluble organic silicon dioxide.
7. The method for preparing a cream for external use for treating psoriasis according to claim 6, wherein the heating temperature in the step 2) is 75 ℃.
8. The method for preparing a cream for external use for treating psoriasis according to claim 6, wherein the heating temperature in the step 3) is 75 ℃.
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Application publication date: 20210723 |