CN102579517B - Medicament composition for preventing prostatic diseases - Google Patents

Medicament composition for preventing prostatic diseases Download PDF

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CN102579517B
CN102579517B CN201210058799.0A CN201210058799A CN102579517B CN 102579517 B CN102579517 B CN 102579517B CN 201210058799 A CN201210058799 A CN 201210058799A CN 102579517 B CN102579517 B CN 102579517B
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ilicis rotundae
extract
cortex ilicis
compositions
syringoside
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CN102579517A (en
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南敏伦
赫玉芳
赵昱玮
王莲萍
赵全成
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Jilin Academy of Traditional Chinese Medicine
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Jilin Academy of Traditional Chinese Medicine
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Abstract

The invention discloses an ilicis rotundae cortex medicament composition for preventing such diseases as prostatitis and prostatic hyperplasia. The composition is obtained through extraction from barks of llex rotunda thunb. and refinement and is characterized by being formed by pedunculoside, syringin, rotundic acid and other substances. Pharmacological tests prove that the composition has the effect of preventing prostatitis, prostatic hyperplasia and the like. The composition has new application to preparing medicaments for preventing prostatic diseases. Pharmaceutic preparations of the composition are elaborated and can be any one of tablets, capsules, pills, granules, suspensions, dripping pills, ointments and rectal administration preparations such as suppositories.

Description

A kind of pharmaceutical composition of preventing and treating prostatosis
Technical field
The invention relates to the new medical use of Cortex Ilicis Rotundae pharmaceutical composition, the application of Cortex Ilicis Rotundae pharmaceutical composition in preparing prostatosis medicine specifically, also relates to the pharmaceutical preparation of this medicine, the invention belongs to medical technical field.
Background technology
Prostatosis is because Abwehrkraft des Koepers is low, and antibacterial or other pathogenic infection prostate rapidly raised growth are bred and caused, mostly is blood circulation and infects or per urethra retrograde infection, thereby bring out prostatitis.Body of gland interstitial has slight hyperplastic tissue, and structure be take the connective tissue of hypertrophy and smooth muscle as main, and has glandular sac, the hypertrophy glandular tube epithelium of increase to be mamillary to outstanding in blister cavities, forms the Combination tuberosity of interstitial adenoid tissue, thereby has formed prostatic hyperplasia.Prostatic hyperplasia is one of common disease of male elderly patients.Along with the increase at age, male more or less has the phenomenon of prostatic hyperplasia to occur.The cardinal symptom of prostatic hyperplasia has dysuria, the lighter's urine increased frequency of getting up at night, have urine retention or urinated after also have a small amount of phenomenon of discharging; Severe patient occurs that urine rheology is thin, or the phenomenon of can not arranging; Same often with symptoms such as soreness of waist lumbago, myasthenia of limbs, seminal emissions.The necessary surgical removal of prostatic hyperplasia severe patient, general conservative treatment, comprises hand massage, effect is all not too satisfied.Prostatitis divides acute and chronic two kinds.It is cardinal symptom that acute prostatitis be take irritation sign of bladder and terminal hematuria, perineal position pain, but clinical more rare.Chronic prostatitis is urinated with delayed urination, rear the dripping of urine, or oozes white prostatic fluid, or causes that seminal emission, sexual impotence, premature ejaculation etc. are cardinal symptom.Chronic prostatitis is a kind of common and multiple urology department illness.Primary disease reason is complicated, and symptom is various, and course of disease delay is obstinate difficult, has a strong impact on the physical and mental health of adult male.At present do not have clinically a kind of antibacterials to produce good therapeutic effect to prostatosis.The one, because prostate anatomical position is special, the antibacterial being conducive in urethra enters body of gland, is unfavorable for body of gland drain, causes the easy retention of rheuminess thing and difficult discharge; The 2nd, prostata tissue structure is special, prostatic epithelium has adipose membrane to exist, antibacterials are difficult for entering prostate acinus from blood plasma disperse, and be subject to the impact of prostatic fluid pH value, reach effective sterilization, Mlc in body of gland, need have certain fat-soluble, dissociation constant is high, low with plasma protein binding rate, toxicity is low, and the medicine that can take the long period, and the antimicrobial drug using clinically at present does not still possess these features.The pathological change of prostate itself, focus is easy fibrosis around, often affects again antibacterials and spreads to focus.Therefore, treat safely and effectively medicine for prostate disease for one, chronic prostate patient is needed just.Our experimentation proof Cortex Ilicis Rotundae pharmaceutical composition has good preventive and therapeutic action to prostatosis.
Cortex Ilicis Rotundae (Ilicis rotundae cortex) derives from the dry bark of holly plant Ilex rotunda Thunb. (Ilex rotunda Thunb.).Mainly be distributed in the provinces and regions such as Guangdong, Guangxi, Fujian, Taiwan, Yunnan, Jiangsu, Zhejiang, Anhui, Jiangxi, Hunan.Bitter in the mouth, cold in nature, has heat-clearing and toxic substances removing, reducing swelling and alleviating pain, dampness removing, the effects such as expelling summer-heat of dispeling the wind, and records the record > > that gathers medicinal herbs in the < < south of the Five Ridges.The heat-clearing and toxic substances removing that is usually used among the people, reducing swelling and alleviating pain.For heat-damp in summer heating, laryngopharynx swelling and pain, damp-heat dysentery, abdominal distention, rheumatic arthralgia, eczema, furuncle, traumatic injury (2010 editions Chinese Pharmacopoeia one, 293 pages).Existing with Cortex Ilicis Rotundae or together with other medical materials at present, extracting in water or water extraction wine are heavy, make treatment gastroenteritis, the medicine of dyspepsia etc., and as Cortex Ilicis Rotundae tabellae contragasteralgiam, compound recipe Cortex Ilicis Rotundae capsule, fukean tablet, the suitable capsule of the intestines and stomach etc.Separately have pharmacological research aspect, Cortex Ilicis Rotundae mainly shows that it has vitro antibacterial activity, the effect of antiinflammatory action and cardiovascular pharmacological aspect.There is less inhibitory action at the report n-butanol extraction positions such as Zhang Rongwen to staphylococcus aureus, beta hemolytic streptococcus, Candida albicans; There is stronger inhibitory action at Cortex Ilicis Rotundae ethanol extraction position and distilled water extraction position to staphylococcus aureus, beta hemolytic streptococcus; Experimentation shows that Cortex Ilicis Rotundae ethanol extraction position can obviously suppress dimethylbenzene induced mice ear swelling, cotton balls induction rat granuloma simultaneously, and respond well.The results of study such as Zhouning County show that Cortex Ilicis Rotundae dry product and new fresh goods water extract have obvious bacteriostasis, obvious to escherichia coli, Bacillus typhi, bacillus pyocyaneus, staphylococcus aureus fungistatic effect.The researchs such as Chen little Xia show that Cortex Ilicis Rotundae n-butanol extract has arrhythmia and function of resisting myocardial ischemia.The reports such as He Bing, Cortex Ilicis Rotundae ethanol extract and water extract all can reduce isolated rat coronary flow, and are dosage one effect relation.The reports such as Dong Yanfen, Cortex Ilicis Rotundae n-butanol extract vena femoralis injection has hypotensive effect to normal rat.Liu state firewood patent of invention (CN201110008326) has been reported the ethanol of Cortex Ilicis Rotundae medical material or the extract of water, through organic reagent, process and obtain containing every gram containing the extract of syringoside 0.50~0.85g, there is the effect of clearing away heat-fire, antipyretic-antalgic, antiinflammatory.Do not have single Peltatin glucoside or syringoside or rotundicacid to there is the prostatic report for the treatment of.Research is found by experiment, and the compositions of the Cortex Ilicis Rotundae that we extract has new purposes, for the pharmacological research of this medical material is opened up new approaches.We prove experimentation, the compositions being formed by Peltatin glucoside (Pedunculoside) 30-70%, syringoside (Syringin) 6-25%, rotundicacid (rotundic acid) 1-5%, be from naturally occurring Chinese crude drug Cortex Ilicis Rotundae, to extract and obtain, there is the effect that prevents and treats prostatosis.And we have stronger pharmacologically active compared with single component Peltatin glucoside, syringoside by unexpected discovery Cortex Ilicis Rotundae pharmaceutical composition, this is just meeting compound recipe theory and multicomponent composite coordination effect of the traditional Chinese medical science, and the present invention and in the past the research tool of Cortex Ilicis Rotundae have greatly improved and novelty.For Cortex Ilicis Rotundae medical material provides a kind of new purposes, and provide a kind of new pharmaceutical composition for the treatment of prostatosis.
Had report can treat prostatosis be mainly compound Chinese medicinal preparation and chemical drugs.In its chemical drugs, antibiotic is the most frequently used, and administration time is long, and chronic prostatitis is easily recurrence after stopping using, and current multiplex antibiotic clinically and topical therapeutic are thought the way of combination, have certain curative effect, but can not effect a radical cure, and toxic and side effects is large; Compound of Chinese medicine prostatosis mainly contains pills for prostate disease, shenqi pill, suppository of wild chrysanthemum flower, Qianlie Huichun Capsules and QIANLIEKANG PIAN etc.So and have no the report that the compositions forming with Peltatin glucoside, syringoside, rotundicacid of extracting from Cortex Ilicis Rotundae is used for the treatment of prostatosis.This compositions has the circulation of anti-inflammation and sterilization, Repercusion analgesia, promotion blood, lymph fluid; Experimental results show that this compositions can effectively dwindle hypertrophy, loose prostata tissue, improve kidney function, the permeability that improves blood vessel, the hyperemia that alleviates prostata tissue and swelling, active cell active, improve body of gland immunity, eliminate focus.Thereby reach the prostatic effect for the treatment of.
Compositions of the present invention has substantial different from Cortex Ilicis Rotundae extract in the past, the patent (CN101342205) of Liu Guoqiao invention, is Cortex Ilicis Rotundae medical material, adds ethanol extraction, filter, concentrated, reclaim ethanol, after adding water and stirring evenly, leaching precipitate, wash precipitate with water, drying precipitate obtains extract, and in 1g extract dry product, containing Peltatin glucoside and rotundicacid total amount is 0.50~0.80g.The patent (CN101099753A) of Li Chaosheng invention, is also by Cortex Ilicis Rotundae medical material, adds ethanol extraction, filters, concentrated, after adding water and stirring evenly, and leaching precipitate, the dry extract that to obtain.Due to syringoside be polyhydroxy aglycon and with the glycosides compound of sugared combination, water solublity is extremely strong, Cortex Ilicis Rotundae medical material is after ethanol extraction, concentrated, after adding water filtration, syringoside is in aqueous solution, in filter cake, do not contain syringoside, main containing rotundicacid and Peltatin glucoside in filter cake, the obvious difference of patent of the present invention and above-mentioned two patents is, we utilize macroporous resin column from aqueous solution, to carry out enrichment and purification the syringoside being in the past dropped, obtained with Peltatin glucoside, syringoside, the brand-new compositions that rotundicacid forms, and syringoside and Peltatin glucoside have been carried out respectively to the comparative test of relevant pharmacodynamics to the compositions of rotundicacid, also proved independent syringoside simultaneously, the pharmacologically active of rotundicacid and Peltatin glucoside compositions is not as compositions of the present invention.Also the pharmacologically active that has further proved three kinds of compositions has coordinative role.
Usining of not finding before the present invention completes to extract from the Cortex Ilicis Rotundae compositions that Peltatin glucoside, syringoside, rotundicacid form, as the report of control prostatosis medicine, does not find that the compositions forming with Peltatin glucoside, syringoside, rotundicacid is for preventing and treating the clinicing aspect application of prostatosis yet.
Summary of the invention
Feature of the present invention is with Peltatin glucoside, syringoside, the compositions that rotundicacid forms is through extracting from Chinese medicine Cortex Ilicis Rotundae (Ilicis rotundae cortex), refine and obtain, its production technology is at patent of invention (patent No. application number: relate to 201010607538.0), it is to be noted, this patent indication with Peltatin glucoside, syringoside, the compositions that rotundicacid forms can be the product that adopts above-mentioned patent technique to obtain, also can be further to use on this basis absorption, desorbing, column chromatography, the refining goods that obtain of the technology such as recrystallization and combined method thereof.
Peltatin glucoside (Pedunculoside) structural formula
Figure BSA00000680767000051
Rotundicacid (rotundic acid) structural formula
Figure BSA00000680767000061
Syringoside (Syringin) structural formula
Figure BSA00000680767000062
The object of this invention is to provide a kind of compositions (hereinafter to be referred as Cortex Ilicis Rotundae compositions) forming with Peltatin glucoside, syringoside, rotundicacid, said composition is to obtain from holly plant Ilex rotunda Thunb.; Through further animal experiment, studies have shown that Cortex Ilicis Rotundae compositions has the effect of control prostatosis.Said composition has the new purposes in preparing the medicine of prostatosis, has obvious novelty.
Another object of the present invention and feature are: provide a kind of plant resources abundant, the Cortex Ilicis Rotundae compositions of can industrialization producing, not only had natural Chinese medicine chemical composition compound recipe feature, but also there is specific chemical components, the proportion of composing proper advantage of arranging in pairs or groups, said composition is comprised of saponins, triterpenes, lignans constituents.Be with previous literature report difference, we have carried out enrichment and purification by the syringoside in the aqueous solution abandoning in previous literature report, with Peltatin glucoside and rotundicacid combination, obtain natural compound chemical composition compositions, there is obvious novelty.Said composition is characterised in that: by weight percentage: Peltatin glucoside (Pedunculoside) 30-70%, syringoside (Syringin) 6-25%, rotundicacid (rotundic acid) 1-5%, experimental results show that and there is the significantly effect of antibacterial, antiinflammatory, anti-prostatic hyperplasia, without obvious toxic-side effects; Stable performance, can make various dosage form.Before completing, the present invention the compositions forming with Peltatin glucoside, syringoside, rotundicacid of not finding about extracting from Cortex Ilicis Rotundae to report the research of prostatic physiology and pharmacologically active.
Saponins, triterpenes, Phenylpropanoid Glycosides three compounds joint synergy treatment prostatosis are also a main innovate point of the present invention and significantly technological progress.
Another object of the present invention is to provide the pharmaceutical preparation of the compositions forming with Peltatin glucoside, syringoside, rotundicacid.Main drug form is tablet, capsule, pill, granule, suspensoid, drop pill, any in injection, ointment, suppository rectally preparation.
Described Cortex Ilicis Rotundae pharmaceutical composition preparation method of the present invention is as follows:
Cortex Ilicis Rotundae pulverizing medicinal materials is become to coarse powder, doubly measure alcohol reflux 1-3 time of the 50-95% of medical material weight with 5-10, each 1-3 hour, filters, and filtrate recycling ethanol filters, and obtains extract I; Filtrate is waved to without alcohol taste, and by processed good D101 or AB-8 macroporous resin column, first water is extremely colourless, then uses 30-80% ethanol elution, and concentrated ethanol, obtains extract II; Extract I and extract II are merged, be dried to obtain Cortex Ilicis Rotundae pharmaceutical composition.
Extracting method of the present invention has with short production cycle, workable, does not use inflammable and explosive chemical reagent, safety, and cost is low, can meet the needs of large suitability for industrialized production.In view of the present invention has clear and definite pharmacologically active, the Cortex Ilicis Rotundae compositions of technique gained of the present invention can be prepared in industrialization, has broad application prospects.
The present invention has carried out respectively the comparative test of relevant pharmacodynamics with syringoside and Peltatin glucoside to the compositions of rotundicacid simultaneously, result of the test shows, the more independent syringoside of compositions of the present invention, the activity of the compositions of Peltatin glucoside and rotundicacid is better, this is also an innovative point with realistic meaning of the present invention, has also embodied the synergism of natural Chinese medicine chemical composition.
The Peltatin glucoside of using in effect experiment of the present invention and the compositions of rotundicacid prepare according to following technique:
Cortex Ilicis Rotundae pulverizing medicinal materials is become to coarse powder, doubly measure alcohol reflux 1-3 time of the 50-95% of medical material weight with 5-10, each 1-3 hour, filters, and filtrate recycling ethanol filters, and filter cake washing is dry, obtains the compositions of Peltatin glucoside and rotundicacid.Wherein the content of Peltatin glucoside is 80.8%, and the content of rotundicacid is 6.7%.
The syringoside of using in pharmacodynamic experiment of the present invention is that market buys.
Peltatin glucoside, syringoside, rotundicacid high-efficient liquid phase chromatogram process measuring method:
Take octadecylsilane chemically bonded silica as filler; Take acetonitrile-0.05% phosphate aqueous solution as mobile phase; Concrete ratio sees the following form, and detection wavelength is 210nm.Number of theoretical plate calculates and is not less than 3000 by syringoside.
Figure BSA00000680767000091
The preparation precision of reference substance solution takes syringoside, Peltatin glucoside, rotundicacid reference substance, puts in volumetric flask, with dissolve with methanol, makes every ml containing syringoside 0.05mg, Peltatin glucoside 0.15mg, rotundicacid 0.008mg mixed solution.
Compositions 20mg is got in the preparation of need testing solution, accurately weighed, puts in 50ml measuring bottle, adds methanol 40ml, and ultrasonic 30min, is placed to room temperature, and methanol constant volume, to scale, shakes up, as need testing solution.
Assay method is accurate reference substance solution and each 10 μ l of need testing solution of drawing respectively, and injection liquid chromatography, measures, and obtains.
Cortex Ilicis Rotundae pharmaceutical composition (syringoside accounts for 21.3%, Peltatin glucoside accounts for 55.6%, rotundicacid account for 3.8%) has the effect of control prostatosis, and these pharmacological actions, are confirmed by following pharmacodynamics test example.
Cortex Ilicis Rotundae pharmaceutical composition claims composition I in pharmacodynamics test, and the compositions of Peltatin glucoside and rotundicacid is called composition I I in pharmacodynamics test.
1, the antiinflammatory action of Cortex Ilicis Rotundae compositions
The impact of 1.1 Cortex Ilicis Rotundae compositions xylol induced mice auricle inflammation swelling
Get 70 of mices, male, body weight (20 ± 2) g, is divided into 7 groups at random, and according to table 1 gastric infusion, every day 1 time, 7d, after last administration 1h, drips dimethylbenzene 0.3mL in mouse right ear continuously, and left ear is not coated with and contrasts.After 2h, the dislocation of mice cervical region is put to death, with the card punch of diameter 9mm, at the same position of left and right ear, lay round auricle respectively, weigh, calculate the difference of left and right auricle weight as swelling, relatively group difference.The results are shown in Table 1.
The impact of table 1 Cortex Ilicis Rotundae compositions xylol induced mice auricle inflammation swelling
**P<0.01,*P<0.05。With matched group comparison
As seen from Table 1, the swelling of the high, medium and low Three doses xylol of Cortex Ilicis Rotundae compositions induced mice auricle inflammation all has significant inhibitory action, shows that they all have significant antiinflammatory action.Equally, after positive control medicine indomethacin gavage, also there is significant antiinflammatory action.Syringoside also has very strong antiinflammatory action.But the antiphlogistic effects of the compositions of Peltatin glucoside and rotundicacid a little less than.
1.2 Cortex Ilicis Rotundae compositionss are on the swollen impact forming of rat granuloma
Get 70 of rats, by sex and body weight, be divided at random 7 groups.By cotton balls, insert method operating procedure in the sterilized cotton ball of subcutaneous each heeling-in one (30 ± 1) of groin mg.Postoperative administration on the same day, dosage is with table 2, and 7d, puts to death animal in 8d continuously, peels off and take out cotton balls granulation tissue, weighs after putting 60 ℃ of oven dried 12h, calculates swelling and suppression ratio.
Table 2, Cortex Ilicis Rotundae compositions are on the swollen impact forming of rat granuloma
Figure BSA00000680767000102
**P<0.01,*P<0.05。With matched group comparison
As seen from Table 2, Cortex Ilicis Rotundae combination object height, middle dosage, have significant inhibitory action, the significant antiinflammatory action of tool to swollen formation of rat granuloma.With the comparison of normal saline matched group, show granulation hyperplasia inflammation is had to significant antiinflammatory action.Indomethacin also has significant antiinflammatory action to granulation hyperplasia inflammation.Syringoside also has stronger antiinflammatory action.But the antiphlogistic effects of the compositions of Peltatin glucoside and rotundicacid a little less than.
2, the therapeutical effect of Cortex Ilicis Rotundae compositions to prostatic hyperplasia
2.1 Cortex Ilicis Rotundae compositionss cause the effect of castrated rats prostatic hyperplasia to androlin
Get 90 of male rats, wherein sew up as matched group cut scrotum under asepsis after for 10, another 80 are divided into 8 groups at aseptic resection bilateral testes after one week at random, by table 3 administration.Every day 1 time, gastric infusion is after 14 days (subcutaneous injection androlin 5mg/kg simultaneously) continuously, with the comparison of feminine gender simulation group, Cortex Ilicis Rotundae combination object height, in weight of prostate, the prostate index of two dosage group rats reduce to some extent (P < 0.01).It is the strongest that proscar reverses the effect of prostatic hyperplasia.The effect of high dose Cortex Ilicis Rotundae compositions is close with QIANLIEKANG effect, but is weaker than the effect of proscar.
Table 3 Cortex Ilicis Rotundae compositions is to the treatment of castrated rats prostatic hyperplasia (n=10, X ± SD)
Figure BSA00000680767000111
**P<0.01,*P<0.05。With negative control group comparison
The therapeutical effect of 2.2 Cortex Ilicis Rotundae compositionss to mice prostatic hyperplasia
Get 90 of male mices, leave 10 and make normal control, all the other mices every days is subcutaneous injection androlin 5mg/kg successively, after 21 days, puts to death wherein 10 mices, normal control mice is also put to death equally, take body weight and prostate Chong Bingzuo pathology Histological section microscopy, confirm that prostate has after hypertrophy, remaining mice is divided into seven groups, every group 10, by the gastric infusion of dosage shown in table 4.Every day 1 time, matched group and model control group give equal-volume water, continuous 1 month.After last administration, weigh Mouse Weight, by sacrifice of animal, cut open and get prostate and weigh, Bing Zuo pathology Histological section microscopy.The results are shown in Table 4.
Table 4 Cortex Ilicis Rotundae compositions is to the therapeutical effect of Experimental Mice prostatic hyperplasia (X ± SD)
Figure BSA00000680767000121
**P<0.01,*P<0.05。With negative control group comparison
Result shows: injection androlin is after 21 days, and the prostate of mice weighs and obviously shows increase, the obvious hypertrophy of prostate body of gland.The mice with prostatic hyperplasia took this product after 1 month, its weight of prostate administration group and model control group is obvious alleviates; Prostate index is also significantly less than normal, and microscopy treatment group prostatic hyperplasia degree obviously alleviates compared with matched group, is close to normal.Body weight no significant difference to mice.The present composition is obvious compared with the composition effect of syringoside and Peltatin glucoside and rotundicacid.
3, the therapeutical effect of Cortex Ilicis Rotundae compositions to zoopery nonbacterial prostatitis
3.1 Cortex Ilicis Rotundae compositions on Carrageenan cause the prostatitic impact of mice
Get 80 of male mices, be divided at random 8 groups, by gastric infusion every day of dosage shown in table 5 once, altogether administration is 14 days, and the 15th day with 3% pentobarbital sodium intraperitoneal anesthesia, under asepsis, hypogastric region cuts, at the seminal vesicle near prostate head lobe, inject 1% carrageenin 0.1ml, Normal group injects the sodium chloride 0.1ml of injection 0.9%, after stitching, is being administered once, within 16th, put to death mice, with miniature injector, remove 10ul prostatic fluid, note leukocyte count, the results are shown in Table 5.Take out prostate and fix by 10% formalin, carry out histological examination.
Table 5 Cortex Ilicis Rotundae compositions on Carrageenan causes the prostatitic impact of mice (n=10, X ± SD)
Figure BSA00000680767000131
**P<0.01。With negative control group comparison
As can be seen from Table 5, the leukocyte of negative model group significantly increases, and each dosage group of Cortex Ilicis Rotundae compositions and the leukocyte of QIANLIEKANG group significantly reduce.Relatively there is significant difference with negative model group.The compositions of syringoside and Peltatin glucoside and rotundicacid does not all have the successful of compositions of the present invention.
3.2 Cortex Ilicis Rotundae compositions on Carrageenan cause the impact of prostatitis rat
Get 80 of male rats, be divided at random 8 groups, by gastric infusion every day of dosage shown in table 6 once, altogether administration is 14 days, and the 15th day with 3% pentobarbital sodium intraperitoneal anesthesia, under asepsis, hypogastric region cuts, at the seminal vesicle near prostate head lobe, inject 1% carrageenin 0.1ml, Normal group injects the sodium chloride 0.1ml of injection 0.9%, after stitching, is administered once again, within 16th, put to death mice, with miniature injector, get 10ul prostatic fluid, note leukocyte count, the results are shown in Table 6.Take out prostate and fix by 10% formalin, carry out histological examination.
Table 6 Cortex Ilicis Rotundae compositions on Carrageenan causes the impact (n=10, X ± SD) of prostatitis rat
Figure BSA00000680767000141
**P<0.01。With negative control group comparison
As can be seen from Table 6, the leukocyte of negative model group significantly increases, and each dosage group of Cortex Ilicis Rotundae compositions and the leukocyte of QIANLIEKANG group significantly reduce.Relatively there is significant difference with negative model group.The compositions of syringoside and Peltatin glucoside and rotundicacid does not all have the successful of compositions of the present invention.
From above pharmacodynamic experiment, Cortex Ilicis Rotundae compositions has treatment prostatic hyperplasia and/or prostatitic effect, and with matched group comparison, its therapeutic effect is better than QIANLIEKANG, suitable with proscar.And long-term taking is free from side effects.
The present invention executes example by following experiment to be achieved (confirmation)
example 1, (preparation of compositions)
Cortex Ilicis Rotundae medical material 2kg is ground into coarse powder, with 70% alcohol reflux of 8 times of amount medical material weight 3 times, each 2 hours, filter, merging filtrate, reclaims ethanol, to 2500ml, filters, and gets filter cake and obtains extract I; Filtrate is waved to without alcohol taste, by processed good D101 or AB-8 macroporous resin column, first washes with water to colourless, then uses 50% ethanol elution 4BV, collects ethanol elution, reclaims ethanol, concentrated, obtains extract II; Extract I and extract II are merged, dry, obtain Cortex Ilicis Rotundae pharmaceutical composition 155.3g.Utilize high effective liquid chromatography for measuring, calculate, syringoside accounts for 21.3%, Peltatin glucoside accounts for 55.6%, rotundicacid accounts for 3.8%.
embodiment 2, (capsule)
Composition material 200g, medical starch is appropriate, and mix homogeneously is granulated, and dry, granulate, packs capsule into No. 1, makes 1000, obtains.Each 2, every day 2 times.
embodiment 3, (tablet)
Composition material 200g, medical starch is appropriate, and dextrin is appropriate, and mix homogeneously is granulated, dry, and granulate is dry, adds lubricant appropriate, and tabletting, makes 1000, obtains.Each 2, every day 2 times.
embodiment 4, (drop pill)
Take 30g Macrogol 4000, in water-bath, melt, add composition material 20g, stir, in impouring insulating tube, regulating thermostatic device, makes medicinal liquid at 80-90 ℃, splash in the liquid paraffin of cooling mistake, after dripping off, by blotting paraffin oil on pill impouring filter paper, make 1000, obtain.Each 20, every day 2 times.
embodiment 5, (granule)
Composition material 200g, Icing Sugar 300g, mix homogeneously, uses appropriate alcohol granulation, and dry, granulate, subpackage, make 500 bags, obtains.Each 1 bag, every day 2 times.

Claims (2)

1. the application of Cortex Ilicis Rotundae extract in the medicine of preparing prostatosis control, it is characterized in that Cortex Ilicis Rotundae extract is mainly comprised of Peltatin glucoside, syringoside, rotundicacid, wherein Peltatin glucoside accounts for 30-70%, and syringoside accounts for 6-25%, and rotundicacid accounts for 1-5%; The preparation method of described extract is: Cortex Ilicis Rotundae pulverizing medicinal materials is become to coarse powder, doubly measure alcohol reflux 1-3 time of the 50-95% of medical material weight with 5-10, each 1-3 hour, filters, and filtrate recycling ethanol filters, and obtains extract I; Filtrate is waved to without alcohol taste, by processed good D101 or AB-8 macroporous resin column, first washes with water to colourless, then uses 30-80% ethanol elution, and concentrated ethanol, obtains extract II; Extract I and extract II are merged, be drying to obtain Cortex Ilicis Rotundae extract.
2. the application of Cortex Ilicis Rotundae extract according to claim 1 in the medicine of preparing prostatosis control, is characterized in that said prostatosis comprises prostatitis and prostatic hyperplasia.
CN201210058799.0A 2012-03-08 2012-03-08 Medicament composition for preventing prostatic diseases Expired - Fee Related CN102579517B (en)

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CN102078344A (en) * 2010-12-28 2011-06-01 赵全成 Ilicis routundae cortex pharmaceutical composition and application thereof
CN102233105A (en) * 2010-04-28 2011-11-09 苏州福龙生物科技有限公司 Traditional Chinese medicine for treating prostate disease

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Publication number Priority date Publication date Assignee Title
CN102233105A (en) * 2010-04-28 2011-11-09 苏州福龙生物科技有限公司 Traditional Chinese medicine for treating prostate disease
CN102058632A (en) * 2010-12-28 2011-05-18 赵全成 Application of medicinal composition to preparation of medicament for preventing and treating alcoholic liver damage and fatty liver and lowering blood fat
CN102078344A (en) * 2010-12-28 2011-06-01 赵全成 Ilicis routundae cortex pharmaceutical composition and application thereof

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