CN102119934B - Application of verbascoside in preparation of medicaments for treating chronic prostatitis - Google Patents
Application of verbascoside in preparation of medicaments for treating chronic prostatitis Download PDFInfo
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- CN102119934B CN102119934B CN2010100005083A CN201010000508A CN102119934B CN 102119934 B CN102119934 B CN 102119934B CN 2010100005083 A CN2010100005083 A CN 2010100005083A CN 201010000508 A CN201010000508 A CN 201010000508A CN 102119934 B CN102119934 B CN 102119934B
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Abstract
The invention discloses new application of verbascoside, in particular application of the verbascoside in the preparation of medicaments for treating chronic prostatitis and application of the verbascoside serving as an active ingredient in the preparation of compound preparations. Researches show that the verbascoside has an obvious suppressing effect on chronic prostatitis model rats, and the treating effect is better than that of Prostate Plus.
Description
Technical field
The present invention relates to the purposes of verbascoside in preparation treatment chronic prostatitis medicine, belong to field of medicaments.
Background technology
Chronic prostatitis is the commonly encountered diseases of adult male, and adult's sickness rate is 35%～40% more than 25 years old, and the cause of disease is complicated, is prone to recurrence, has a strong impact on male's quality of life.Because prostatic special physiological structure; Make medicine be difficult to get into body of gland inside and reach valid density; There are defectives such as therapeutic effect is poor, cure rate is low, untoward reaction is many in medicine commonly used at present such as antibiotic, anti-inflammatory agent, α receptor blocking agent, plant amedica, immunosuppressant.
Verbascoside, English Verbascoside by name, structural formula is suc as formula shown in 1.
Formula 1
CAS registration number (CAS RegistryNumber): 61276-17-3
Molecular formula: C
29H
36O
15
Molecular weight: 624.59
Verbascoside belongs to the plain glycoside of phenylpropyl alcohol; Be present in the various plants bodies such as Scrophulariaceae, Verenaceae, Orobanchaceae, Plantaginaceae; Have antibiotic, antiinflammatory, antiviral, antitumor, antioxidation, immunomodulating, hypermnesis, protect the liver, pharmacological action widely such as heart tonifying, but see the report of its treatment chronic prostatitis.
Summary of the invention
The objective of the invention is to provides a kind of good effect, new drug that toxic and side effects is little for the clinical treatment chronic prostatitis.Through research, be surprisingly found out that verbascoside has significant inhibitory effect to the chronic prostatitis rat model, curative effect is superior to QIANLIEKANG, thereby has disclosed the purposes of verbascoside in preparation treatment chronic prostatitis medicine.
Verbascoside has the commercial goods, and content can reach 98% (high-efficient liquid phase technique).Method for distilling also has many pieces of reports in the prior art, and for example one Chinese patent application 99123015.9, WO2004069218, JP2000302797, JP2191292, FR2302745.Spectroscopic datas such as its each item physical parameter and infrared, nuclear-magnetism, mass spectrum have play-by-play in Chinese patent 03114454.3.
According to document (Chinese patent 03114454.3) report, verbascoside is nontoxic basically, can be used as oral medication, injecting drug use and mucosa medication.
The inventor's pharmacodynamic experiment shows that verbascoside has remarkable inhibitory action to rat chronic prostatitis model, and embodiment 1 is seen in concrete analysis.
Therefore; With the verbascoside is active component; Add suitable pharmaceutically acceptable auxiliaries; Can be made into the pharmaceutical composition of treatment chronic prostatitis, dosage form can be peroral dosage form, injecting medicine-feeding form, cavity/canal drug administration dosage form and other pharmaceutically acceptable dosage forms, and is concrete like tablet, capsule, granule, freeze-dried powder, suppository etc.The preparation of these pharmaceutical preparatioies, those skilled in the art can select and the matched pharmaceutic adjuvant of above-mentioned dosage form according to the existing known technology of the industry, mix the back with verbascoside and prepare according to the processing method that has relevant dosage form in the known technology now.In addition, the present invention also comprises and contains the compound preparation of verbascoside as active component, is about to the medicament mixed that verbascoside and other can be used for treating chronic prostatitis and processes compound preparation.
Description of drawings
Fig. 1: rats in normal control group prostata tissue photo
Fig. 2: the sham operated rats rat prostate is organized photo
Fig. 3,4: the model group rat prostate is organized photo
Fig. 5: the positive controls rat prostate is organized photo
Fig. 6: verbascoside low dose group rat prostate is organized photo
Fig. 7: the dose groups rat prostate is organized photo in the verbascoside
Fig. 8: verbascoside high dose group rat prostate is organized photo
The specific embodiment:
Embodiment 1 pharmacodynamics test: verbascoside is to the influence of rat chronic prostatitis model
Summary: method: adopt male SD rat, prostate notopodium bilateral injects 25% XIAOZHILING ZHUSHEYE respectively and causes the chronic prostatitis model.Select for use QIANLIEKANG PIAN as positive control drug, establish normal control group, sham operated rats and model group simultaneously.Continuous gastric infusion is 30 days after the modeling.Through measuring the prostate weight in wet base, calculate the prostate index, measure prostate volume with drainage, carry out the curative effect that medicine is estimated in histological examination simultaneously.Result: tried thing verbascoside 30mg/kg, 60mg/kg significantly suppresses the rat chronic prostatitis model that XIAOZHILING ZHUSHEYE causes; Can significantly reduce prostatic weight in wet base, volume and prostate index; Relatively there were significant differences (P＜0.01) with model group; Histopathological examination shows that dose groups has a small amount of cell infiltration in the verbascoside, and all the other do not have obvious pathological change; High dose group rat prostate tissue is normal, and structural pipe wall is complete, does not have obvious pathological change; 15mg/kg has certain therapeutical effect to the rat prostate inflammation, and relatively there were significant differences (P＜0.05) with model group, and histopathological examination has a small amount of cell infiltration, and interstitial fibers is organized a small amount of hypertrophy, and the body of gland pleat reduces slightly, and all the other do not have obvious pathological change.Conclusion: verbascoside has the effect of remarkable inhibition chronic prostatitis.
1 experiment purpose
Observe the influence of the rat chronic prostatitis model that verbascoside causes xiaozhiling injection
2 laboratory animals
The SD rat, male, 70, body weight 200-240g provides quality certification SCXK (capital) 2007-0001 by dimension tonneau China laboratory animal technology company limited.
3 medicines and reagent
XIAOZHILING ZHUSHEYE: Shuanghe High-Tech. Natural Medicine Co., Ltd., Beijing produces, lot number: 090808;
Positive control drug: QIANLIEKANG PIAN, Kang Enbei Zhejiang Pharmaceutical Co produces, lot number: 081238;
Tried thing: verbascoside, lot number: 09080301, provide by the Tianheng Medicinal Inst., Beijing.
4 experimental techniques
70 of male SD rats; Body weight 200-240g is divided into 7 groups at random by body weight: dose groups (30mg/kg), verbascoside high dose group (60mg/kg) in normal control group, sham operated rats, model group (giving distilled water), positive controls (QIANLIEKANG PIAN 500mg/kg), verbascoside low dose group (15mg/kg), the verbascoside.The normal control group is left intact, and all the other each treated animals are applied in abdominal part with suds and shave except that the quilt hair with blade then before test, beginning modeling in the 2nd day.After 3.5% chloral hydrate anesthesia, in the about 2-3cm of aseptic condition median incision of lower abdomen, through abdominal cavity; Propose bladder and both sides seminal vesicle, expose the prostate notopodium that invests the seminal vesicle inboard, bilateral injects 25% XIAOZHILING ZHUSHEYE 0.2ml respectively; With the multiple internal organs of prompt delivery, suture muscles skin, wrapping.Sham operated rats is not injected XIAOZHILING ZHUSHEYE, injection 0.2ml sterile saline.After modeling, divided into groups in the 4th day, the beginning administration, gastric infusion is after 30 days continuously, and rat is weighed; Put to death, get prostate, carry out Anatomical Observation, take by weighing the prostate weight in wet base; Calculate the prostate index, measure prostate volume, and fix with 10% formalin solution with drainage; Embedding, section (thickness 5 μ m), histopathological examination is carried out in HE dyeing under light microscopic.
Statistical procedures: measurement data is with X ± S, and to carrying out the t check between each group, ranked data adopt the Ridit check, adopt Sun Ruiyuan, Chen Zhiyang, and chief editors' such as professor Zheng Qingshan DAS software carries out statistical procedures to The above results.
5 experimental results
5.1 influence to rat prostate weight in wet base, index and volume
This experiment adopts XIAOZHILING ZHUSHEYE to prepare rat chronic prostatitis model.The result shows, compares with the normal control group, and the prostate weight in wet base of model group rat, volume and prostate index all significantly increase (P＜0.01); Being tried thing verbascoside 15mg/kg has certain therapeutical effect to the inflammation of rat prostate tissue, and relatively there were significant differences (P＜0.05) with model group; 30mg/kg and 60mg/kg group all can significantly reduce prostate weight in wet base, volume and prostate index, and more all there were significant differences (P＜0.01) with model group.Positive controls can significantly reduce prostate weight in wet base, volume and prostate index, and relatively there were significant differences (P＜0.05) with model group.The result sees table 1.
Table 1 verbascoside to the influence of prostate weight in wet base, index and the volume of chronic prostatitis rat (x ± s, n=10)
Annotate: compare Δ Δ P＜0.01 with the normal control group; Compare * P＜0.05, * * P＜0.01 with model group
5.2 histological examination
1, perusal:
The rats in normal control group prostata tissue is soft, ruddy, glossy, does not have adhesion with surrounding tissue.General and the surrounding tissue adhesion of model group rat prostate body of gland, body of gland is kermesinus or pale brown color, and matter is hard slightly, or tangible scleroma is arranged.Each dose groups rat prostate color of verbascoside is scarlet, and quality is softer, and elasticity is better, and is lighter with the surrounding tissue adhesion.
2, microscopic examination:
The normal control group: the prostata tissue structural integrity, the lumen of gland form differs, and pleat is many, and mostly no inflammatory cell infiltration, glandular epithelium are cube or column that lumen of gland includes a large amount of secretions, sees accompanying drawing 1.
Sham operated rats:, see accompanying drawing 2 with the normal control group.
Model group: pleat obviously reduces, the acinus atrophy, and lumen of gland secretions obviously reduces, and a large amount of cell infiltration are arranged, and interstitial fibers hamartoplasia is remarkable, sees accompanying drawing 3～4.
Positive controls: a small amount of cell infiltration is arranged, and the body of gland pleat reduces slightly, and the tube chamber endocrine has minimizing slightly, and all the other do not have obvious pathological change, sees accompanying drawing 5.
The verbascoside low dose group: a small amount of cell infiltration is arranged, and interstitial fibers is organized a small amount of hypertrophy, and the body of gland pleat reduces slightly, and all the other do not have obvious pathological change, sees accompanying drawing 6.
Dose groups in the verbascoside: a small amount of cell infiltration is arranged, and all the other do not have obvious pathological change, see accompanying drawing 7.
The verbascoside high dose group: prostata tissue is normal, and structural pipe wall is complete, does not have obvious pathological change, sees accompanying drawing 8.
The sxemiquantitative grade scale of prostata tissue lesion degree is seen table 2, and the histopathological examination result sees table 3.
The sxemiquantitative grade scale of table 2 prostata tissue lesion degree
| Classification | Pathological changes |
| - | The body of gland tube chamber is not seen obvious pathological changes, and body of gland is normal, and the body of gland tube chamber is bigger, and pleat is more; A large amount of rediance secretions are arranged in the tube chamber; Accidental or the nothing of inflammatory cell; No proliferation of fibrous tissue or accidental minute quantity proliferation of fibrous tissue. |
| + | The body of gland tube chamber diminishes slightly, and pleat reduces slightly; Pink secretions has minimizing slightly in the tube chamber; Cell infiltration is dispersed on a small quantity; Small amount of fibers hamartoplasia; Extent of disease is less than 1/3 prostata tissue. |
| ++ | The acinus atrophy, tube chamber obviously diminishes, even inaccessible, and pleat obviously reduces or disappears; Pink secretions obviously reduces in the tube chamber, and secretions is light red dyeing, even does not have secretions; A large amount of cell infiltration appear; A large amount of proliferations of fibrous tissue; Extent of disease is about 1/3～2/3 prostata tissue. |
| +++ | The acinus atrophy, tube chamber obviously diminishes, even inaccessible, and pleat obviously reduces or disappears; Pink secretions obviously reduces in the tube chamber, and secretions is light red dyeing, even does not have secretions; A large amount of cell infiltration occur, the infiltration scope surpasses 2/3 prostata tissue, and the also visible multinuclear macrophage that has forms the granulomatous pathological changes of inflammatory; A large amount of proliferations of fibrous tissue; Extent of disease is greater than 2/3 prostata tissue. |
Table 3 histopathological examination result
Annotate: compare Δ Δ P＜0.01 with the normal control group; Compare * P＜0.05, * * P＜0.01 with model group
6 conclusions and discussion
In the rat chronic prostatitis model that this experiment employing XIAOZHILING ZHUSHEYE causes, verbascoside low dosage 15mg/kg promptly has certain inhibitory action to the rat prostate inflammation; Middle dosage 30mg/kg, high dose 60mg/kg not only can significantly reduce prostate weight in wet base, volume and prostate index; And histopathology significantly improves; Curative effect is superior to positive drug, and the results suggest verbascoside has the effect of remarkable inhibition chronic prostatitis.
Embodiment 2, tablet
With verbascoside and proper auxiliary materials uniform mixing, be pressed into tablet.
Prescription:
The title recipe quantity
Verbascoside 100g
Microcrystalline Cellulose 100g
Starch 40g
Carboxymethyl starch sodium 10g
Dehydrated alcohol is an amount of
Magnesium stearate 3g
Make 1000
Preparation technology:
(1) verbascoside was pulverized 100 mesh sieves, and microcrystalline Cellulose, starch are crossed 60 mesh sieves, and is subsequent use;
(2) take by weighing verbascoside, microcrystalline Cellulose, starch, the carboxymethyl starch sodium mix homogeneously of recipe quantity;
(3) binding agent: dehydrated alcohol;
(4) add suitable amount of adhesive system soft material, 24 orders are granulated, and 40 ℃ of dryings add the recipe quantity magnesium stearate, 24 mesh sieve granulate, and mixing, subsequent use;
(5) theory of computation sheet is heavy, and tabletting promptly gets.
Embodiment 3, capsule
With verbascoside and suitable adjuvant mix homogeneously, be filled in the capsulae vacuus after directly filling or process granule, promptly get.
Prescription:
The title recipe quantity
Verbascoside 100g
Microcrystalline Cellulose 80g
Starch 40g
Carboxymethyl starch sodium 10g
Dehydrated alcohol is an amount of
Magnesium stearate 2g
Make 1000
Preparation technology:
(1) verbascoside was pulverized 100 mesh sieves, and microcrystalline Cellulose, starch are crossed 60 mesh sieves, and is subsequent use;
(2) take by weighing verbascoside, microcrystalline Cellulose, starch, the carboxymethyl starch sodium mix homogeneously of recipe quantity;
(3) binding agent: dehydrated alcohol;
(4) add suitable amount of adhesive system soft material, 24 orders are granulated, and 40 ℃ of dryings add the recipe quantity magnesium stearate, granulate, and mixing, subsequent use;
(5) theory of computation loading amount, filled capsules promptly gets.
Embodiment 4, granule
With verbascoside and suitable auxiliary materials and mixing, granulate, drying, granulate, packing promptly gets.
Prescription:
The title recipe quantity
Verbascoside 100g
Dextrin 1000g
Sucrose 1000g
90% alcoholic solution is an amount of
Make 1000 bags
Preparation technology:
(1) verbascoside was pulverized 100 mesh sieves, and dextrin, Fructus Citri tangerinae XIANGFEN were pulverized 80 mesh sieves, and be subsequent use;
(2) take by weighing verbascoside, sucrose, the dextrin mix homogeneously of recipe quantity;
(3) binding agent: 90% alcoholic solution;
(4) add suitable amount of adhesive system soft material, 18 orders are granulated, 40 ℃ of dryings, and 18 mesh sieve granulate, subsequent use;
(5) theory of computation loading amount, pack promptly gets.
Embodiment 5, freeze-dried powder
Prescription:
The title recipe quantity
Verbascoside 100g
Potassium dihydrogen phosphate 13.60g
Sodium hydroxide 1.88g
Mannitol 200g
Make 1000
Preparation technology:
(1) measure 4000ml water for injection, add potassium dihydrogen phosphate, sodium hydroxide, the mannitol of recipe quantity, dissolving, subsequent use;
(2) the verbascoside extract of adding recipe quantity, stirring and dissolving adds the injection water and is settled to 5000ml;
(3) filtration sterilization, fill;
(4) nitrogen is filled in lyophilization, and gland promptly gets.
Embodiment 6, suppository
Prescription:
The title recipe quantity
Verbascoside 100g
Macrogol 4000 2000g
Make 1000 pieces
Preparation technology:
(1) take by weighing the Macrogol 4000 heat fused, verbascoside was pulverized 200 mesh sieves, added mix homogeneously in the above-mentioned molten matrix, and was subsequent use;
(2) mould is irritated in insulation;
(3) put coldly, after treating to solidify fully, remove and overflow part, die sinking is taken out, and promptly gets.
Claims (3)
1. verbascoside is treated the purposes in the chronic prostatitis medicine in preparation.
2. according to the purposes of claim 1, wherein said medicine is peroral dosage form, injecting medicine-feeding form or cavity/canal drug administration dosage form.
3. according to the purposes of claim 1, wherein said medicine is tablet, capsule, granule, freeze-dried powder or suppository.
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| Application Number | Priority Date | Filing Date | Title |
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| CN2010100005083A CN102119934B (en) | 2010-01-11 | 2010-01-11 | Application of verbascoside in preparation of medicaments for treating chronic prostatitis |
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|---|---|---|---|
| CN2010100005083A CN102119934B (en) | 2010-01-11 | 2010-01-11 | Application of verbascoside in preparation of medicaments for treating chronic prostatitis |
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| CN102119934B true CN102119934B (en) | 2012-07-11 |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1569008A (en) * | 2004-05-14 | 2005-01-26 | 兰州大学 | Medicine for preventing and treating cerebral infarction |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1569008A (en) * | 2004-05-14 | 2005-01-26 | 兰州大学 | Medicine for preventing and treating cerebral infarction |
Non-Patent Citations (1)
| Title |
|---|
| 朱小薇等.马缨丹化学成分与生物活性.《国外医药植物药分册》.2002,第17卷(第3期), * |
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Address after: 014400 Inner Mongolia Tianheng Pharmaceutical Co., Ltd., Chengbei small and medium-sized business park, wulatqianqi, Bayannur City, Inner Mongolia Autonomous Region Patentee after: Inner Mongolia Tianheng Hospital Management Co., Ltd Address before: 100070, room 25, building 188, No. eighteen, 407 West Fourth Ring Road, Fengtai District, Beijing Patentee before: Beijing Tianheng Hospital Management Co. Ltd. |