CN109331032A - Application of the Hyperoside in the drug of preparation treatment pruritus dermatopathy - Google Patents
Application of the Hyperoside in the drug of preparation treatment pruritus dermatopathy Download PDFInfo
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- CN109331032A CN109331032A CN201811334060.1A CN201811334060A CN109331032A CN 109331032 A CN109331032 A CN 109331032A CN 201811334060 A CN201811334060 A CN 201811334060A CN 109331032 A CN109331032 A CN 109331032A
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- hyperoside
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- pruritus dermatopathy
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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
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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
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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
- A61P17/04—Antipruritics
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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 application of the Hyperoside in the drug of preparation treatment pruritus dermatopathy, widened the application range of Hyperoside, and provide new drug for the treatment of pruritus dermatopathy；Through pharmacological experiment it can be seen that Hyperoside has good preventive and therapeutic effect to the mouse skin itch model that dextran induces, paraxylene induced mice ear swelling has apparent anti-inflammatory effect, the increase of mouse capillary permeability is caused to significantly inhibit effect in glacial acetic acid, and it can be to the preferable antagonism of cavy itch caused by histamine phosphate, and toxicity is low, using safe, with good application prospect.
Description
Technical field
The invention belongs to field of medicaments, and in particular to Hyperoside answering in the drug of preparation treatment pruritus dermatopathy
With.
Background technique
Pruritus dermatopathy refers to one group of skin disease using pruitus as main feature, including eczema, psoriasis, papule
Property nettle rash, insect dermatitis, pityriasis rubra pilaris etc..In recent years, the disease incidence of pruritus dermatopathy is in rising trend, this and weather
Environmental change, application of a large amount of chemicals in life is nervous, and rhythm of life is accelerated, and dietary structure change is related,
The cause of disease its recurrent, intractable, pruritic and the course of disease quality of life that is touching and influencing patient, bring greatly to patient
Puzzlement.External drug currently used for treating pruritus dermatopathy is mainly sugared Corticosteroids and a little Chinese patent medicine preparation, sugar
Corticosteroids can cause that sugared Corticosteroids rely on and withdrawal is recurred just with working well, and it is obvious to continue to use its curative effect
Decline, the Exterior-applied Chinese patent medicine preparation currently used for treating pruitus is less, and curative effect is not good enough.Therefore, it actively finds and develops
It is a kind of to treat pruritus dermatopathy good effect, few side effects and the suitable external preparation of price with greatly clinical value and need
Seek potentiality.
Hyperoside (Hyperoside, Hyp) also known as Quercetin -3-O- β-D galactopyranoside, belong to flavonol glycosides
Class compound.It is widely present in various plants, such as Hypericaceae, rosaceae, Campanulaceae, Chun Xing section, little Xue section, azalea
It is a kind of important natural products in the fruit and herb of section, Malvaceae etc..Modern medicine study shows that Hyperoside has
Antibacterial, antiviral, anti-inflammatory, anti-oxidant, anticancer, it is antifatigue, decompression, reduce cholesterol, protein assimilating, part and maincenter town pain with
And to pharmacological actions such as a variety of physiological activity such as the heart, cerebrovascular protective effect, in a variety of Chinese patent drugs of clinical use at present
Containing Hyperoside, such as Yukexin capsule, tablet for coronary heart disease and hypertension, Xinan Capsule, ciwujia capsule and stilbene moon tablets of reducing blood fat.These drugs master
It is used for the adjuvant treatment of cardiovascular related diseases, such as angina pectoris, coronary heart disease, hypertension and hyperlipidemia.But related spun gold
There is not been reported for the anti-pruitus bioactivity of peach glycosides.
Summary of the invention
In view of this, the purpose of the present invention is to provide Hyperosides in the drug of preparation treatment pruritus dermatopathy
Using.For achieving the above object, the invention provides the following technical scheme:
1, application of the Hyperoside in the drug of preparation treatment pruritus dermatopathy.
Further, the pruritus dermatopathy is that eczema, psoriasis, papular urticaria, insect dermatitis or hair are red
Pityriasis.
Further, the pruritus dermatopathy is the ear swelling caused by dimethylbenzene, glacial acetic acid cause capillary permeability
The disease of itch caused by increase or dextran, histamine phosphate.
Further, single component of the Hyperoside as treatment pruritus dermatopathy drug.
Further, one of the compound medicine of the Hyperoside as treatment pruritus dermatopathy drug ingredient.
Further, the drug is that capsule, oral solution, particle is made in the pharmaceutically acceptable auxiliary material of Hyperoside addition
Agent, cream, ointment or spray.
Further, the capsule is to mix in proportion Hyperoside bulk pharmaceutical chemicals and carrier PEG 6000, and heating makes
It is completely dissolved, is freeze-dried, be ground into fine-powdered, cross 60-120 mesh to get Hyperoside solid dispersions；Take Hyperoside
Solid dispersions mix pelleting with microcrystalline cellulose, dry, be packed into capsule to get.
Further, the Hyperoside bulk pharmaceutical chemicals and 6000 mixed proportion of carrier PEG are 1:6.
The beneficial effects of the present invention are: present invention firstly discloses Hyperosides in preparation treatment pruritus dermatopathy
The application range of Hyperoside has been widened in application in drug, improves its market value.Hyperoside is further clarified in medicine
Usage amount range in object preparation provides reference value for actual application.
Specific embodiment
To make the objectives, technical solutions, and advantages of the present invention clearer, below to the pharmacological action of Hyperoside and
Its effect is explained in detail.
Embodiment 1, the preparation of Hyperoside capsule and assay
The preparation method of Hyperoside capsule, the specific steps are as follows: press Hyperoside bulk pharmaceutical chemicals and carrier PEG 6000
The ratio of 1:6 is uniformly mixed, until heating makes to be completely dissolved in 60 DEG C of water-baths, -20 DEG C of freeze-dryings are ground into fine-powdered, cross 80
Mesh is to get PEG solid dispersions.Hyperoside solid dispersion powder is taken to mix with microcrystalline cellulose according to mass ratio 7:8
Pelleting, it is dry, capsule is packed into get capule size 0.24g/.
The assay of Hyperoside capsule:
Chromatographic condition is using octadecylsilane chemically bonded silica as filler；With -0.1% phosphate aqueous solution of acetonitrile (20:80)
For mobile phase；Detection wavelength 360nm.Theoretical cam curve is calculated by Hyperoside peak should be not less than 2000.
The preparation of reference substance solution
Accurately weighed Hyperoside reference substance 10.1mg, is placed in 10mL volumetric flask, adds methanol to make to dissolve, and add to scale
Line constant volume, shake up to get.
The preparation of test solution
Precision weighs Hyperoside capsule 's content 30mg, finely ground, and precision measures methanol 25ml, weighs, ultrasonic 15min,
Put to room temperature, weighing is supplied weight, is shaken up, and filters, take subsequent filtrate to get.
Measuring method: accurate absorption reference substance solution and each 10ul of test solution respectively, injection liquid chromatograph, measurement,
Measurement result is that Determination of Hyperoside is 16mg/ in capsule.
Similarly Hyperoside is added pharmaceutically acceptable auxiliary material and oral solution, granule, cream, ointment, spray is made
The preparations such as mist agent.
The pharmacological action of embodiment 2, Hyperoside
1, the influence with the detection Hyperoside of capsule made of Hyperoside in embodiment 1 to mouse skin itch model
Taking weight is kunming mice 60 of 20g or so, is randomly divided into 5 groups, every group 12.High, medium and low dose of Hyperoside
Amount group distinguishes gastric infusion 100mg/kg, 50mg/kg, 25mg/kg (being 16mg/ Granule Computing by Determination of Hyperoside in capsule),
Positive controls give chaste tree anti-itching-relieving granule 10.14g/kg, (the anti-itching-relieving granule of chaste tree: Sichuan Guangda Pharmaceutical Co., Ltd of Li Zhu group,
Wind-dispelling, dehumidifying, it is clearing heat and detoxicating, antipruritic.For children's anemopyretic or damp-heat type papular urticaria.The visible impetigo of symptom) it is empty
White control group gives same volume (10ml/kg) 0.9% sodium chloride solution, qd (once a day), continuous 7d.1h after the last administration is small
Tail vein injection dextran 1 .25mg/kg.Head is scratched with mouse fore paw, right pawl scratches trunk, and mouth stings each position of whole body
As itching indication.Observe and record mouse itching latent time and itching number in 30min.Compared with blank control group, spun gold
Peach glycosides high middle dose group mouse itching latent time and itching number substantially reduce (p < 0.01).It is shown in Table 1.
The influence (n=12) of table 1, Hyperoside capsule to 5 groups of mouse skin itch models
P < 0.01 * * compared with blank group.
2. causing the shadow of mice auricle swelling with the detection Hyperoside paraxylene of capsule made of Hyperoside in embodiment 1
It rings
Taking weight is Kunming male mice 60 of 20g or so, is randomly divided into 5 groups, every group 12.Hyperoside is high, in,
Low dose group distinguishes gastric infusion 100mg/kg, 50mg/kg, 25mg/kg, and positive controls give chaste tree anti-itching-relieving granule 10.14g/
Kg, blank control group give same volume (10ml/kg) 0.9% sodium chloride solution, qd, continuous 7d.It is each small after last dose 30min
Mouse auris dextra smears dimethylbenzene 40ul, and left ear is as own control, and cervical dislocation puts to death mouse after applying ear 2h, cuts two along auricle base line
Ear, the punch for being 8mm with diameter are punched in two ear corresponding sites respectively, take auricle, electronic balance weighing, with left and right auricle weight
The difference of amount indicates swelling.Compared with blank control group, Hyperoside is high, middle dose group mouse auricle swelling numerical value obviously subtracts
Small (p < 0.01), the results are shown in Table 2.
The influence (n=12) of table 2, Hyperoside paraxylene induced mice auricle edema
* * P < 0.01. compared with blank control group
3. logical to glacial acetic acid induced mice capillary with the detection Hyperoside of capsule made of Hyperoside in embodiment 1
The increased influence of permeability
Taking weight is Kunming male mice 60 of 20g or so, is randomly divided into 5 groups, every group 12.Hyperoside is high, in,
Low dose group distinguishes gastric infusion 100mg/kg, 50mg/kg, 25mg/kg, and positive controls give chaste tree anti-itching-relieving granule 10.14g/
Kg, blank control group give same volume (10ml/kg) 0.9% sodium chloride solution, qd, continuous 7d.At 1 hour after the last administration,
2% Evans Blue solution of animal tail vein injection is injected by 0.1ml/10g, while in addition to control group, the equal abdomen of remaining groups of animals
Chamber injects 0.7% glacial acetic acid, injects by 0.1ml/10g, 30min execution animal after injection, and intraperitoneal injection of saline 4mL/,
Abdominal cut after rubbing abdomen, collects abdominal cavity eluate, and 1500r/min is centrifuged 15min, supernatant 1ml is taken to survey at 590nm
Determine absorbance (A).Compared with blank control group, the high, medium and low dosage group mouse capillary permeability increase of Hyperoside has
Significantly inhibit effect (p < 0.01).It the results are shown in Table 3.
Table 3, Hyperoside influence (n=12) increased on glacial acetic acid induced mice capillary permeability
* * P < 0.01. compared with blank control group
4. the influence that Hyperoside capsule induces histamine phosphate guinea pig skin itch model
Taking weight is male guinea pig 50 of 180g or so, is randomly divided into 5 groups, every group 10.Hyperoside is high, medium and low
Dosage group distinguishes gastric infusion 100mg/kg, 50mg/kg, 25mg/kg, and positive controls give chaste tree anti-itching-relieving granule 6.04g/kg,
Blank control group gives same volume (10ml/kg) 0.9% sodium chloride solution, qd, continuous 7d.In right foot after last dose 24 hours
It carries on the back and is abraded (being degree with oozing of blood) at shaving with sand paper, 10min drop incremented by successively from low concentration to high concentration at the surface of a wound after coating
Histamine phosphate's solution (0.01%, 0.02%, 0.03%0.2%), until cavy occur later licks right foot, statistics is caused
Itch concentration value, compared with blank control group, the high, medium and low dosage of Hyperoside can improve cavy caused by histamine phosphate cause to itch it is dense
Angle value shows Hyperoside to the preferable antagonism of cavy itch caused by histamine phosphate.It the results are shown in Table 4.
Table 4, Hyperoside cause the influence (n=10) of concentration value of itching to cavy
P < 0.01 * * compared with blank control group.
Embodiment 3, Hyperoside acute toxicity
Mouse 40 of 20 ± 2g of weight are taken, half male and half female, every mouse gives gold according to the dosage of 5.0g/kg (weight)
Silk peach glycosides, oral gastric infusion 3 times daily, successive administration 7 days, whether there is or not acute toxic reactions for observation mouse.
The results show that giving mouse (mouse middle dosage medication 50mg/kg) oral and being equivalent to 100 times of human administration's dosage
Hyperoside when, have no dead mouse, do not measure LD50.The above results show that the safety of Hyperoside is good, are equivalent to people
Dead mouse is had no at 100 times of body dosage.
Finally, it is stated that preferred embodiment above is only used to illustrate the technical scheme of the present invention and not to limit it, although logical
It crosses above preferred embodiment the present invention is described in detail, however, those skilled in the art should understand that, can be
Various changes are made to it in form and in details, without departing from claims of the present invention limited range.
Claims (8)
1. application of the Hyperoside in the drug of preparation treatment pruritus dermatopathy.
2. application according to claim 1, which is characterized in that the pruritus dermatopathy is eczema, psoriasis, papule
Property nettle rash, insect dermatitis or pityriasis rubra pilaris.
3. application according to claim 1, it is characterised in that: the pruritus dermatopathy is that the ear caused by dimethylbenzene swells
Swollen, glacial acetic acid causes the disease of itch caused by capillary permeability increase or dextran, histamine phosphate.
4. application according to claim 1, it is characterised in that: the Hyperoside is as treatment pruritus dermatopathy drug
Single component.
5. application according to claim 1, it is characterised in that: the Hyperoside is as treatment pruritus dermatopathy drug
One of compound medicine ingredient.
6. described in any item applications according to claim 1~5, it is characterised in that: the drug is that medicine is added in Hyperoside
Capsule, oral solution, granule, cream, ointment or spray is made in acceptable auxiliary material on.
7. application according to claim 6, it is characterised in that: the capsule is by Hyperoside bulk pharmaceutical chemicals and carrier PEG
6000 mix in proportion, and heating makes to be completely dissolved, and are freeze-dried, and are ground into fine-powdered, cross 60-120 mesh to get spun gold
Peach glycosides solid dispersions；Take Hyperoside solid dispersions to mix pelleting with microcrystalline cellulose, it is dry, be packed into capsule to get.
8. application according to claim 7, it is characterised in that: the Hyperoside bulk pharmaceutical chemicals and carrier PEG 6000 are mixed
Ratio is 1:6.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811334060.1A CN109331032A (en) | 2018-11-09 | 2018-11-09 | Application of the Hyperoside in the drug of preparation treatment pruritus dermatopathy |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811334060.1A CN109331032A (en) | 2018-11-09 | 2018-11-09 | Application of the Hyperoside in the drug of preparation treatment pruritus dermatopathy |
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| Publication Number | Publication Date |
|---|---|
| CN109331032A true CN109331032A (en) | 2019-02-15 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201811334060.1A Pending CN109331032A (en) | 2018-11-09 | 2018-11-09 | Application of the Hyperoside in the drug of preparation treatment pruritus dermatopathy |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116808086A (en) * | 2023-07-13 | 2023-09-29 | 首都医科大学附属北京中医医院 | Application of flos Abelmoschi Manihot in preparing medicine for treating psoriasis |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104324094A (en) * | 2014-11-25 | 2015-02-04 | 中国人民解放军第三军医大学第一附属医院 | Application of globeflower flavonoids in preparation of medicine for treating itch dermatoses |
-
2018
- 2018-11-09 CN CN201811334060.1A patent/CN109331032A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104324094A (en) * | 2014-11-25 | 2015-02-04 | 中国人民解放军第三军医大学第一附属医院 | Application of globeflower flavonoids in preparation of medicine for treating itch dermatoses |
Non-Patent Citations (2)
| Title |
|---|
| 史宁等: "金丝桃苷对急性炎症疼痛模型小鼠的抗炎镇痛作用研究", 《药物评价研究》 * |
| 贾媛: "金丝桃苷胶囊的药学研究", 《中国优秀硕士学位论文全文数据库 医药卫生科技辑》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116808086A (en) * | 2023-07-13 | 2023-09-29 | 首都医科大学附属北京中医医院 | Application of flos Abelmoschi Manihot in preparing medicine for treating psoriasis |
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Application publication date: 20190215 |
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