CN109700801A - A kind of pharmaceutical composition for treating psoriasis - Google Patents
A kind of pharmaceutical composition for treating psoriasis Download PDFInfo
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- CN109700801A CN109700801A CN201910139924.2A CN201910139924A CN109700801A CN 109700801 A CN109700801 A CN 109700801A CN 201910139924 A CN201910139924 A CN 201910139924A CN 109700801 A CN109700801 A CN 109700801A
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- pharmaceutical composition
- psoriasis
- aesculetin
- treating psoriasis
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Abstract
The present invention designs a kind of pharmaceutical composition for treating psoriasis, which is made of effective component and medically acceptable auxiliary material, which is characterized in that the effective component is made of the chemical component of following weight percent: aesculetin 45%-55%；Betulic acid 45%-55%.Pharmaceutical composition of the present invention can be obviously improved psoriasis model back of mice skin PASI scoring, and mitigation mouse skin thickens and weight loss, raise the ratio of regulatory T cells (Treg) in Mice Body, treat the significant effect of psoriasis.
Description
Invention field
The present invention relates to medicinal preparations, and in particular to the drug containing organic compound, the medicament can be used to treat silver
Bits disease.
Background technique
Psoriasis is otherwise known as psoriasis, is one of most common chronic inflammatory skin disease, and the state of an illness is obstinate, is easy
Recurrence, can cause whole body system to damage, main histopathology cash be keratinocyte paraplasm, parakeratosis,
Inflammatory cell infiltration and dermal tissue blood vessel hyperplasia etc..Meanwhile psoriasis is also easy to cause psoriasis arthropathica, Metabolic syndrome
The multiple complications such as disease, malignant tumour bring secondary injury to patient, seriously affect the quality of life of patient, or even existence week
Phase.However it is not yet clear at present about the exact pathogenesis of psoriasis.Studies have shown that generation and many factors of psoriasis
Related including hereditary, immune, environment influence etc., wherein immune-mediated is its universally recognized pathogenesis at present.
The drug for the treatment of psoriasis mainly includes anti-tumor drug, Calcipotriol, glucocorticoid, immunosuppressor at present
With biological agent etc..These drugs clinically can play certain therapeutic effect, but can generate secondary work after taking for a long time
With, and drug resistance and dependence are easily formed, biological agent is expensive, brings huge financial burden to patient.Therefore, it studies
Persons are actively finding a kind of new effective antipsoriatic object, to can reduce side effect, and mitigate patient and
The burden of society.
Chinese medicine has unique curative effect and advantage in terms for the treatment of many immunity diseases.In recent years, many traditional Chinese medicine monomers have been
It is successfully applied to the prevention and treatment of immunity disease, and achieves the achievement to attract people's attention, before there is development worthy of expecting
Scape.The report such as scholar Zhao Jie, Himalayan period have effects that treat psoriasis (Zhao Jie, Zhu Guizhi, Song Wenrong, Xiao Chunling happiness
Set 47 [J] Chinese journal of dermatology of alkali Ointment in Treatment psoriasis, the 2nd phase of volume 32 in April, 1999: 134-135)；Separately have
The report such as person Zhao Dan, the bark of ash bathe the treatment of joint narrow-band UVB psoriasis vulgaris definite effect (Zhao Dan, Huang Jianwei, Huang
Clinical observation on the therapeutic effect [J] tcm clinical of auspicious thunder bark of ash bath joint narrow-band UVB treatment psoriasis vulgaris is miscellaneous
Will, the 5th phase of volume 27 in May, 2015: 695-697).But camptothecine is alkaloid, it is by hydroxycamptothecin, deoxidation
The composition such as camptothecine, venoterpine, betulic acid (Betulic acid) and vincoside-lactam is good at determining any or several specific
Camptothecine have treatment psoriasis bioactivity；Coumarins, lignanoids, secoiridoid are mainly contained in the bark of ash
The chemical components such as class, benzyl carbinol glycoside, flavonoids, phenolic acid class and triterpenes (Nie Anzheng, Lin Zhijian, Zhang Bing bark of ash chemical component
With Advance on Pharmacological Activities [J] Chinese herbal medicine, in September, 2016 the 18th phase of volume 47: 3332-3341), it is good at determining any
Or several chemical components can be used for treating psoriasis.
Summary of the invention:
Technical problem to be solved by the invention is to provide a kind of pharmaceutical composition for treating psoriasis, the pharmaceutical compositions
The significant effect for treating psoriasis.
Technical proposal that the invention solves the above-mentioned problems is as described below:
A kind of pharmaceutical composition for treating psoriasis, the pharmaceutical composition is by effective component and medically acceptable auxiliary material
Composition, which is characterized in that the effective component is made of the chemical component of following weight percent: aesculetin 45%-
55%；Betulic acid 45%-55%.
In above scheme, the best weight ratio of the chemical component is aesculetin 50%, betulic acid 50%.
In above scheme, the aesculetin molecular formula is C9H6O4, molecular weight 178.14, chemical structural formula isThe betulic acid molecular formula is C30H48O3, molecular weight 456.71, chemistry knot
Structure formula is
Pharmaceutical composition of the present invention can be made into various conventional solid dosage forms, such as granule, tablet or capsule.
Above-mentioned solid dosage forms is prepared by following methods:
Aesculetin and betulic acid are weighed by recipe quantity, after mixing, corresponding auxiliary material is added by a conventional method
Granule, tablet or capsule is made.
The aesculetin and betulic acid of the composition effective component in pharmaceutical composition of the present invention have association
The significant effect of psoriasis is treated in same synergistic effect.
Effective component in pharmaceutical composition of the present invention is only by two kinds of compound groups of aesculetin and betulic acid
At being not only easy to prepare, and be conducive to quality control.
The present invention is more fully understood for the ease of the public, is come furtherly below by effect experiment and specific embodiment
Bright beneficial effects of the present invention.
One, pharmacodynamic test
1. experimental animal
SPF grades of BALB/C mices, weight: 20 ± 2g, week old: 6 weeks, being provided by Guangdong Province's Experimental Animal Center, male, from
By diet, temperature is 25 ± 3 DEG C, is raised in SPF grades of animal houses.
2. animal packet
50 BALB/C mices, are randomly divided into 7 groups, be divided into normal group, model group, experimental group A, experimental group B, experimental group C,
Control group 1-2, every group 10.
3. mouse psoriasis model is established
Each back of mice hair is shaved off using electric hair cutter, then coats depilatory cream and back of mice residue hair is taken off, exposed surface
Product is about the skin of 3cm × 2cm size.Two days later, every back of mice skin smears 5% imiquimod ointment daily
62.5mg, it is continuous to smear 7 days.Visible back of mice skin is observed apparent erythema, the scales of skin that peel off occur and thicken situation, i.e., modeling at
Function.Imiquimod ointment is not given after the depilation of Normal group back of mice.
4. test medicine and dosage
4.1 test medicine
Experimental group A: the granule of following embodiments 1；Experimental group B: the tablet of following embodiments 2；Experimental group C: Xia Shushi
Apply the capsule of example 3；
Control group 1: taking aesculetin 20g, is prepared into granule by the method for the embodiment of the present application 1；
Control group 2: taking betulic acid 20g, is prepared into granule by the method for the embodiment of the present application 1；
4.2 dosage
The test medicine of experimental group A-C and control group 1-2 are respectively with the physiological saline for containing 10% (v/v) polyethylene glycol 400
It is configured to the reagent that concentration is equivalent to every ml ingredient containing corresponding chemical 5mg, gastric infusion, dosage is by corresponding chemical ingredient
Weight is calculated as 25mg/kg, one time a day, continues 7 days.
5. experimental method
5.1 back of mice skin PASI scoring
It records back of mice skin conditions daily using digital camera, and scores according to PASI standards of grading.Scoring item
Including erythema (erythema), the scales of skin that peel off (scales) and infiltration thickened degree (thickness) at mouse skin lesion.Each is according to tight
Weight degree is divided into 0-4 point, and PASI standards of grading are as follows: 0- without；1- is slight；2- moderate；3- severe；The pole 4- severe.It is small to each group
The every item rating of mouse and three total scores are compared after being averaged.
The measurement of 5.2 mouse weights
Mouse weight is weighed using small-sized doctor's type scale daily, and is made comparisons with the mouse weight before modeling and drug treatment,
Calculate to obtain the daily situation of change of mouse weight.
The measurement of 5.3 mouse skin epidermal thicknesses
Animal is put to death with after administration 7 days, takes mouse skin, be fixed in 4% neutral formalin, soaked overnight is set by modeling
It is dehydrated in program dewaterer, paraffin wax embedding embedding, the slice after paraffin-embedded tissue is then cut into 3 μm.It is placed in 65 DEG C
Baking oven in bake piece 1-2h, to after water, indigo plant, acidified eosin stains are returned in haematoxylin dyeing 10min, tap water flushing for dewaxing
15min is dehydrated transparent, neutral gum mounting, and after drying overnight, micro- sem observation is taken pictures, and calculates skin epidermis thickness.
Treg cell proportion measures in 5.4 mouse spleens and lymph node
After putting to death mouse, spleen and lymph node are taken out, ground 40 mesh screen, after cell suspension is made, supernatant is removed in centrifugation,
Splenocyte reinstates PBS washing 2 twice after splitting erythrocyte is handled, with lymph node cells one.Every sample is each after cell count
Take 106A cell is resuspended in 100 μ l PBS, and every sample is added 0.5 μ l anti-CD4-FITC room temperature and is protected from light incubation 30min.
Then fixed permeabilized cells, every sample add 0.5 μ l anti-Foxp3-APC room temperature and are protected from light incubation 30min, PBS washing one
After secondary, cell is resuspended in 300 μ l PBS, analyzes Treg cell proportion using machine on flow cytometer.
6. statistical procedures
Total data is for statistical analysis using SPSS V20 statistics software, measurement data mean ± standard deviationIt indicates.
7. experimental result
7.1 mouse skin PASI scoring
The influence (n=10) that 1 pharmaceutical composition of table scores to back of mice skin PASI
Note: compared with model group,*P < 0.05,**P < 0.01；Compared with control group 1,#P < 0.05；Compare with control group 2
Compared with+P < 0.05
After table 1 is the results show that psoriasis model mouse gives drug therapy, skin of back PASI scoring is remarkably decreased (P <
0.05 or P < 0.01).For comparing control group 1 and 2, the mouse skin PASI of experimental group A, B and C are remarkably decreased, and are illustrated opposite
For existing control drug, pharmaceutical composition has better improvement result (P < 0.05) to back of mice skin.
The variation of 7.2 mouse weights
The influence (n=10) that 2 pharmaceutical composition of table changes mouse weight
Note: compared with model group,*P < 0.05,**P < 0.01；Compared with control group 1,#P < 0.05；Compare with control group 2
Compared with+P < 0.05
After table 2 is the results show that psoriasis model mouse gives drug therapy, body weight loss obtains significant and alleviates
(P < 0.01).For comparing control group 1 and 2, the mouse weight of experimental group A, B and C, which mitigate situation, significant alleviation, shows phase
For existing control drug, pharmaceutical composition, which mitigates situation to mouse weight, better improvement result (P < 0.05).
7.3 mouse skin epidermal thicknesses
Influence (n=10) of 3 pharmaceutical composition of table to mouse skin epidermal thickness
Note: compared with model group,*P < 0.05,**P < 0.01；Compared with control group 1,##P < 0.01；Compare with control group 2
Compared with++P < 0.01
After table 3 is the results show that psoriasis model mouse gives drug therapy, epidermal thickness is significantly reduced (P <
0.01).For comparing control group 1 and 2, the mouse skin thickness of experimental group A, B and C are significantly reduced, and are shown relative to existing
For some control drugs, pharmaceutical composition, which thickens situation to mouse skin, better improvement result (P < 0.01).
7.4Treg cell proportion
Influence (n=10) of 4 pharmaceutical composition of table to Treg cell in Mice Body
Note: compared with model group,*P < 0.05,**P < 0.01；Compared with control group 1,#P < 0.05；Compare with control group 2
Compared with+P < 0.05
After table 4 is the results show that psoriasis model mouse gives drug therapy, the Treg cell proportion in spleen and lymph node
Significantly rise (P < 0.05 or P < 0.01).For comparing control group 1 and 2, the mouse spleen and lymph of experimental group A, B and C
Treg cell proportion in knot significantly rises, and shows for existing control drug, pharmaceutical composition is to Mice Body
Interior Treg cell has preferable castering action (P < 0.05).
8. conclusion
The discovery of this experimental result, comparison are used alone for aesculetin and betulic acid, pharmaceutical composition of the invention
With synergistic function.For the aesculetin and betulic acid that compare different weight proportion simultaneously, pharmaceutical composition is found
There is more preferably therapeutic effect when weight proportion is 50%:50%, illustrate that pharmaceutical composition of the invention can effectively treat silver
Bits disease.
Specific embodiment
Embodiment 1
Aesculetin 20g, betulic acid 20g are weighed by weight, is uniformly mixed, and Icing Sugar 80g, dextrin 52g, lactose is added
48g and appropriate 65% ethyl alcohol are made softwood, and particle is made in sieving, after 60 DEG C of constant pressure and dries, whole grain using packaging facilities by its
It is packaged into granule, every bag of 1g.The granule is oral, and 1 bag every time, 1 times a day, 2-3 treatment can be used continuously in 7 days as one therapeutic course
Journey.
Embodiment 2
Aesculetin 22g, betulic acid 18g are weighed by weight, is uniformly mixed, and Icing Sugar 80g, dextrin 52g, lactose is added
Softwood is made in 48g and appropriate 65% ethyl alcohol, and particle is made in sieving, and 3% that grain amount is added after 60 DEG C of constant pressure and dries, whole grain is hard
Fatty acid magnesium 6.6g mixes, particle is then pressed into 440 tablets with stamping device.The tablet is oral, and 2 tablets once, and one day 1
Secondary, the 2-3 course for the treatment of can be used continuously in 7 days as one therapeutic course.
Embodiment 3
Aesculetin 18g, betulic acid 22g are weighed by weight, is uniformly mixed, and Icing Sugar 80g, dextrin 52g, lactose is added
Softwood is made in 48g and appropriate 65% ethyl alcohol, and sieving is made particle, No. 3 capsulae vacuus are loaded on after 60 DEG C of constant pressure and dries, whole grain
In, every capsule average content weight 500mg.The capsule is oral, and 2 every time, 1 times a day, 7 days as one therapeutic course can be continuous
Use the 2-3 course for the treatment of.
Claims (4)
1. a kind of pharmaceutical composition for treating psoriasis, the pharmaceutical composition is by effective component and medically acceptable auxiliary material group
At, which is characterized in that the effective component is made of the chemical component of following weight percent: aesculetin 45%-55%,
Betulic acid 45%-55%.
2. a kind of pharmaceutical composition for treating psoriasis according to claim 1, which is characterized in that the effective component
It is made of the chemical component of following weight percent: aesculetin 50%, betulic acid 50%.
3. a kind of pharmaceutical composition for treating psoriasis according to claim 1 or 2, which is characterized in that the drug
Composition is granule, tablet or capsule.
4. a kind of pharmaceutical composition for treating psoriasis according to claim 3, which is characterized in that the pharmaceutical composition
Object is prepared by following methods:
Aesculetin and betulic acid are weighed by recipe quantity, after mixing, corresponding auxiliary material is added and is made by a conventional method
Granule, tablet or capsule.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910139924.2A CN109700801B (en) | 2019-02-26 | 2019-02-26 | A pharmaceutical composition for the treatment of psoriasis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910139924.2A CN109700801B (en) | 2019-02-26 | 2019-02-26 | A pharmaceutical composition for the treatment of psoriasis |
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| Publication Number | Publication Date |
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| CN109700801A true CN109700801A (en) | 2019-05-03 |
| CN109700801B CN109700801B (en) | 2021-04-06 |
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| CN201910139924.2A Active CN109700801B (en) | 2019-02-26 | 2019-02-26 | A pharmaceutical composition for the treatment of psoriasis |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110604098A (en) * | 2019-09-23 | 2019-12-24 | 广东省中医院（广州中医药大学第二附属医院、广州中医药大学第二临床医学院、广东省中医药科学院） | Method for constructing animal model of rheumatoid arthritis combined with interstitial lung disease |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105982970A (en) * | 2015-02-15 | 2016-10-05 | 北京振东光明药物研究院有限公司 | Traditional Chinese medicinal composition for treating psoriasis and preparation method of traditional Chinese medicinal composition |
| CN109078134A (en) * | 2018-11-05 | 2018-12-25 | 王立强 | It is a kind of that not only there is Chinese medicine composition and preparation method thereof that is anti-oxidant but also can reduce gout patients serum Uric Acid Concentration |
-
2019
- 2019-02-26 CN CN201910139924.2A patent/CN109700801B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105982970A (en) * | 2015-02-15 | 2016-10-05 | 北京振东光明药物研究院有限公司 | Traditional Chinese medicinal composition for treating psoriasis and preparation method of traditional Chinese medicinal composition |
| CN109078134A (en) * | 2018-11-05 | 2018-12-25 | 王立强 | It is a kind of that not only there is Chinese medicine composition and preparation method thereof that is anti-oxidant but also can reduce gout patients serum Uric Acid Concentration |
Non-Patent Citations (2)
| Title |
|---|
| MAICON ROBERTO KVIECINSKI等: "Healing effect of Dillenia indica fruit extracts standardized to betulinic acid on ultraviolet radiation-induced psoriasis-like wounds in rats", 《PHARMACEUTICAL BIOLOGY》 * |
| YUCHAO CHEN等: "Esculetin ameliorates psoriasis-like skin disease in mice by inducing CD4+Foxp3+ regulatory T cells", 《FRONTIERS IN IMMUNOLOGY》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110604098A (en) * | 2019-09-23 | 2019-12-24 | 广东省中医院（广州中医药大学第二附属医院、广州中医药大学第二临床医学院、广东省中医药科学院） | Method for constructing animal model of rheumatoid arthritis combined with interstitial lung disease |
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| CN109700801B (en) | 2021-04-06 |
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