CN102861116B - Method for preparing pericarpium granati polyphenol gel for treating gynecological inflammation - Google Patents
Method for preparing pericarpium granati polyphenol gel for treating gynecological inflammation Download PDFInfo
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Abstract
The invention relates to a method for preparing a pericarpium granati polyphenol gel for treating gynecological inflammation. The gel is obtained by taking a pericarpium granati polyphenol extract as raw material, and adding adjuvants such as pharmaceutically acceptable gel matrix material including Carbomer or hydroxypropyl methylcellulose or sodium carboxymethylcellulose, propylene glycol or glycerol and propylene glycol as humectant, Tween as solubilizer, methylparaben or ethylparaben as preservative, and triethanolamine as pH regulator. The pericarpium granati polyphenol gel is obtained by preparing the pericarpium granati polyphenol extract, dissolving the pericarpium granati polyphenol extract with the humectant or/and the solubilizer and then adding into the dispersed gel matrix for uniformly dispersing, adding the preservative and the balance of water, uniformly mixing, and regulating the pH value to 4.0 to 5.0. The gel obtained by the method is utilized to prevent and treat gynecological inflammation caused by the bacteria, such as vaginitis or cervicitis, and has the characteristics of being convenient to administrate, good in absorption and high in efficacy.
Description
Technical field
The present invention relates to a kind of method of pericarpium granati polyphenol gel preparing treatment gynecological inflammation, relate to specifically a kind of with pomegranate peel polyphenol be raw material prepare for gel that is scorching by bacterial gynecological inflammation medial vagina or cervicitis.
Background technology
The gynecological inflammation such as vaginitis, cervicitis, women's health in serious threat.Due to the particularity of female sex organ, gynecological inflammation has become common, the frequently-occurring disease of adult female, and its clinical manifestation is varied, and the cause of disease is complicated and normal with multiple severe complication, has a significant impact the live and work of women.Vaginitis is the general name of the multiple vaginal mucosa disease that different pathogeny causes.At normal physiological condition, vagina, due to anatomical tissue, has nature defense function to the intrusion of pathogen, and when vagina nature defense function is damaged, pathogen easily invades and causes colpitis occurs.Colpitis is the most common with bacterial vaginitis clinically, and because its state of an illness is easy repeatedly, not easily speed more.Chinese women Survey on Reproductive Health Status shows, and in the past year, once suffers from colpitic adult female and accounts for 53.86%, and wherein had people's recurrent exerbation of 9.48% to reach more than 4 times; Cervicitis is modal one in female sex organ inflammation, accounts for the more than half of married woman.The main pathogenic bacteria of cervicitis is caused to be staphylococcus, streptococcus, escherichia coli and anaerobe.
The medicine of the gynecological inflammations such as current treatment vaginitis, cervicitis is divided into oral medicine and medicine for external use.Oral medicine is based on Chinese patent medicine, and dosage form comprises capsule, drop pill etc.; Medicine for external use is then based on chemical drugs, and mostly containing the medicine such as metronidazole, clotrimazole, excessive use easily destroys the restricting relation between vaginal microbial flora, makes pathogenic bacterium produce drug resistance simultaneously, causes treatment cycle to extend, make disease can not get effective treatment.Because women dissects and physiological feature, external treatment acquires a special sense on gynecological clinic.In recent years, in the research of vaginitis, cervicitis etc., adopt external treatment of tcm, achieve good effect.Vagina local application is owing to having that local drug concentration is high, formulation dosage is low and the feature such as safe and effective, and clinical evaluation is higher.Vagina has abundant blood capillary and lymphatic vessel, and vagina does not have clear and definite teleneuron, and during administration, the pain stimulation of patient is little, is effective drug release position for the specific disease such as cervicitis, vaginitis.By medicine is placed in intravaginal, absorbed by vaginal mucosa and enter local or systemic blood circulation, avoid liver first-pass effect and gastrointestinal physiology outpost of the tax office effect, and produce good biocompatibility with human body, can adhesion be strengthened, to medicine, there is slow release, controlled-release function, the valid density of lesions position is increased, improve bioavailability, enhance curative effect of medication, thus reach the object of local or whole body therapeutic.
The medicine of existing vaginal approach administration has 10 kinds of dosage forms such as flushing liquor, vagina effervescence, suppository, membrane in the market.Flushing liquor is short for action time, not easily gos deep into vagina depths; Tablet uses inconvenient, easily causes intravaginal to have foreign body sensation, and easy damaged vagina; Become liquid after suppository dissolves and easily flow out vagina, pollution clothes, such action time, short, medicine was difficult to whole release; Vaginal pellicles with polymeric membrane be carrier make membrane fill in vagina use, though prepare easy to use, medicine and mucosa contact surface little.Gel is that a class contains two or more, by solid-liquid two phase composition, the macromolecular network system with semi-solid property.By medicine dissolution or be evenly distributed in gel and be gel, there is good adhesiveness and film forming characteristics, compared with other vaginal administration, can the holdup time be extended, be easy to coating, mucosa gauffer can be infiltrated, foreign sense, nonirritant, the compliance of patient can be improved, and clean easy cleaning, being in world pharmaceutical market, showed one of most active medicine novel form in recent years, is also the class topical drug having market potential most.
The kind that Pericarpium Granati records for " Chinese Pharmacopoeia ", has the effects such as astringing intestine to stop diarrhea, hemostasis, anthelmintic, is mainly used in that chronic diarrhea is hemorrhage, chronic dysentery etc.In addition, Pericarpium Granati also has the pharmacologically active promoting ulcerated mucosa healing.The polyphenol active component contained in Pericarpium Granati, as Punicalagin, ellagic acid, gallic acid etc. all have stronger antiinflammatory bacteriostatic activity.But polyphenols is unstable, temperature is high, heated time is long oxidizable, causes that extraction ratio is low, activity decrease, therefore Pericarpium Granati is adopted extract at low temperature concentration technique, improves stability and the extraction ratio of polyphenol components; And utilize macroporous adsorption resin technology, prepare the pomegranate peel polyphenol effective site that purity is higher.The present invention and Chinese patent ZL200910113497.7 " pomegranate peel polyphenol anti-inflammation external effervescent tablet preparation method and application ", document " preparation of pomegranate peel polyphenol gel and quality control " are though be raw material with pomegranate peel polyphenol, but at different Extracting temperature, solvent concentration, under the impact of different macroreticular resins, in Pericarpium Granati extract and effective site, polyphenol components and content change to some extent.The content 60-80% of total polyphenols in the Pericarpium Granati extract that the present invention prepares, the content 2-4% of the active component ellagic acid in its total polyphenols, the content 15-20% of Punicalagin.Document " preparation of pomegranate peel polyphenol gel and quality control " the proportioning of the preparation process of undeclared extract and gel prescription, and polyphenol effective ingredient controls with gallic acid, inconsistent with effective ingredient of the present invention; On the other hand, document report pomegranate peel polyphenol gel is used for the healing of acute and chronic skin trauma, different from purposes of the present invention.
The present invention is applied to clinical with gel, because gel can produce good biocompatibility with human body, adhesion can be strengthened, to medicine, there is slow release, controlled-release function, the valid density of lesions position is increased, improves bioavailability, enhance curative effect of medication, improve the compliance of patient, and clean easy cleaning.In animal body, antiinflammatory pharmacodynamics mice caused by dimethylbenzene xylene ear swelling, carrageenan cause the research of mice toes swelling test, and result shows that pericarpium granati polyphenol gel of the present invention has good antiphlogistic effects than pomegranate peel polyphenol effervescent tablet.
Summary of the invention
Be in the object of the invention, a kind of method preparing the pericarpium granati polyphenol gel for the treatment of gynecological inflammation is provided, the method take EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL as raw material, to add adjuvant be pharmaceutically acceptable gel matrix material is carbomer or hypromellose or sodium carboxymethyl cellulose, wetting agent is propylene glycol or glycerol and propylene glycol, solubilizing agent is tween, and antiseptic is methyl hydroxybenzoate or ethyl hydroxybenzoate, and pH adjusting agent is that triethanolamine is made; Adopt and first prepare EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL, EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL wetting agent and/or solubilizing agent are first dissolved, add in the carbomer or hypromellose or carboxymethylcellulose sodium solution using aqueous dispersion, be uniformly dispersed, add antiseptic and excess water again, stir, add triethanolamine and regulate pH to 4.0-5.0, can pericarpium granati polyphenol gel be obtained.The gel obtained by the method, for the prevention and therapy by the vaginitis in bacterial gynecological inflammation or cervicitis, has convenient drug administration, good absorbing, the feature that curative effect is high.
A kind of method preparing the pericarpium granati polyphenol gel for the treatment of gynecological inflammation of the present invention, the method is 5-30 part by EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL weight portion, adjuvant to be pharmaceutically acceptable gel matrix material be carbomer or hypromellose or sodium carboxymethyl cellulose 0.5-4 part, wetting agent is propylene glycol or glycerol and propylene glycol 5-20 part, solubilizing agent is tween 0-2 part, antiseptic is methyl hydroxybenzoate or ethyl hydroxybenzoate 0.1-0.5 part, and pH adjusting agent is that triethanolamine is made; Adopt and first prepare EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL, then be that gel prepared by raw material with extract, wherein EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL principle active component is total polyphenols, ellagic acid and Punicalagin, and concrete operations follow these steps to carry out:
The preparation of EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL:
A, get Pericarpium Granati and be ground into coarse powder, adding 5-30 times amount concentration is 35-49% ethanol warm macerating, and temperature 71-85 DEG C, extracts 1-4 time, each 1-3 hour, and filter, merging filtrate decompression recycling ethanol, is concentrated into the concentrated solution that every mL is equivalent to crude drug 0.15-0.2g;
B, the concentrated solution obtained by step a add on processed good HPD600 type macroporous adsorptive resins, absorption 3-12 hour, first with deionized water rinsing to effluent paler colour time, again with the 50-80%% ethanol elution of 2-5 times of column volume, collect containing alcohol eluen, reclaim ethanol, concentrating under reduced pressure vacuum drying becomes dry extract, pulverize, cross 80-120 mesh sieve, obtain EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL for subsequent use;
The preparation of gel:
C, step b EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL wetting agent or solubilizing agent or wetting agent and solubilizing agent first to be dissolved, add in the carbomer or hypromellose or carboxymethylcellulose sodium solution using aqueous dispersion, be uniformly dispersed, add antiseptic and excess water again, stir, add triethanolamine and regulate pH to 4.0-5.0, can pericarpium granati polyphenol gel be obtained.
The content 60-80% of total polyphenols in EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL in step b.
The active component of the total polyphenols in step b in EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL is the content 2-4% of ellagic acid, the content 15-20% of Punicalagin.
The pericarpium granati polyphenol gel exquisite quality obtained by the method for the invention is even, steady quality, and under the impact of the factors such as light, heat, low temperature, indices has no significant change.Prepare prevention and therapy by bacterial gynecological inflammation vaginitis or cervicitis in adopt novel pharmaceutical formulation to combine with Purification of traditional Chinese herbs thing means, enhancing drug effect while, add comfortableness and the adaptability of medication.
Detailed description of the invention
Embodiment 1:
The preparation of EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL:
Get Pericarpium Granati and be ground into coarse powder, adding 5 times amount concentration is 35% ethanol warm macerating, and temperature 71 DEG C is extracted 1 time, 3 hours time, filters, decompression filtrate recycling ethanol, is concentrated into the concentrated solution of every mL containing Pericarpium Granati 0.15g;
Concentrated solution is added processed good HPD600 type macroporous adsorbent resin column chromatography post, absorption 6h, when being first eluted to effluent paler colour with deionized water, be 50% ethanol elution by the concentration of 2 times of column volumes again, collect containing alcohol eluen, reclaim ethanol, concentrating under reduced pressure vacuum drying becomes extractum, pulverize, cross 80 mesh sieves, obtain EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL for subsequent use, wherein the content of extract total polyphenols is 62%, the content of ellagic acid is 3.6%, and the content of Punicalagin is 15.4%;
The preparation of gel:
Humectant propylene glycol 5 parts of going bail for grinds with Pericarpium Granati extract 10 parts and evenly first dissolves, add the carbomer 2 parts of solution with aqueous dispersion, be uniformly dispersed, add antiseptic methyl hydroxybenzoate 0.1 part, excess water is to 100g, instillation triethanolamine regulates pH 4.0, stirs, can obtain pericarpium granati polyphenol gel.
Embodiment 2:
The preparation of EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL:
Get Pericarpium Granati and be ground into coarse powder, adding 8 times amount concentration is 49% ethanol warm macerating, and temperature 75 DEG C is extracted 2 times, each 2 hours, filters, merging filtrate decompression recycling ethanol, is concentrated into the concentrated solution of every mL containing Pericarpium Granati 0.18g;
Added by concentrated solution on processed good HPD600 type macroporous adsorbent resin chromatography post, absorption 8h, is first eluted to effluent with deionized water closely colourless, be 60% ethanol elution by the concentration of 3 times of column volumes again, collect containing alcohol eluen, reclaim ethanol, concentrating under reduced pressure vacuum drying becomes extractum, pulverize, cross 100 mesh sieves, obtain EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL for subsequent use, wherein in EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL, the content of total polyphenols is 68%, the content of ellagic acid is 2.8%, and the content of Punicalagin is 16.2%;
The preparation of gel:
Humectant propylene glycol 5 parts of going bail for grinds with Pericarpium Granati extract 15 parts and evenly first dissolves, add the hypromellose cellulose solution 3 parts with aqueous dispersion, be uniformly dispersed, add antiseptic ethyl hydroxybenzoate 0.1 part again, excess water is to 100g, instillation triethanolamine regulates pH 4.5, stirs, can obtain pericarpium granati polyphenol gel.
Embodiment 3:
The preparation of EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL:
Get Pericarpium Granati and be ground into coarse powder, adding 15 times amount concentration is 40% ethanol warm macerating, and temperature 80 DEG C is extracted 3 times, each 1.5 hours, filters, merging filtrate decompression recycling ethanol, is concentrated into the concentrated solution of every mL containing Pericarpium Granati 0.2g;
Added by concentrated solution on processed good HPD600 type macroporous adsorbent resin chromatography post, absorption 12h, is first eluted to effluent with distilled water closely colourless, be 60% ethanol elution by the concentration of 4 times of column volumes again, collect containing alcohol eluen, reclaim ethanol, concentrating under reduced pressure vacuum drying becomes extractum, pulverize, cross 120 mesh sieves, obtain EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL for subsequent use, wherein in EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL, the content of total polyphenols is 75%, the content of ellagic acid is 2.4%, and the content of Punicalagin is 16.6%;
The preparation of gel:
Humectant glycerol 10 parts of going bail for evenly first dissolves with propylene glycol 5 parts, Pericarpium Granati extract 20 parts grinding, add the carboxymethylcellulose sodium solution 3 parts with aqueous dispersion, be uniformly dispersed, add antiseptic methyl hydroxybenzoate 0.1 part, excess water is to 100g, instillation triethanolamine regulates pH 4.8, stirs, can obtain pericarpium granati polyphenol gel.
Embodiment 4:
The preparation of EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL:
Get Pericarpium Granati and be ground into coarse powder, adding 20 times amount concentration is 45% ethanol warm macerating, and temperature 74 DEG C is extracted 2 times, each 3 hours, filters, merging filtrate decompression recycling ethanol, is concentrated into the concentrated solution of every mL containing Pericarpium Granati 0.18g;
Added by concentrated solution on processed good HPD600 type macroporous adsorbent resin chromatography post, absorption 10h, is first eluted to effluent with deionized water closely colourless, be 80% ethanol elution by the concentration of 5 times of column volumes again, collect containing alcohol eluen, reclaim ethanol, concentrating under reduced pressure vacuum drying becomes extractum, pulverize, cross 100 mesh sieves, obtain EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL for subsequent use, wherein in EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL, the content of total polyphenols is 53%, the content of ellagic acid is 3.3%, and the content of Punicalagin is 15.6%;
The preparation of gel:
Humectant glycerol 5 parts of going bail for evenly first dissolves with propylene glycol 10 parts, solubilizing agent tween 1 part, Pericarpium Granati extract 30 parts grinding, add the carbomer solution 2 parts with aqueous dispersion, be uniformly dispersed, add antiseptic ethyl hydroxybenzoate 0.3 part, excess water is to 100g, instillation triethanolamine regulates pH to be 5.0, stirs, can obtain pericarpium granati polyphenol gel.
Embodiment 5:
The preparation of EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL:
Get Pericarpium Granati and be ground into coarse powder, adding 10 times amount concentration is 40% ethanol warm macerating, and temperature is 80 DEG C, extracts 3 times, each 2 hours, filters, merging filtrate decompression recycling ethanol, is concentrated into the concentrated solution of every mL containing Pericarpium Granati 0.16g;
Added by concentrated solution on processed good HPD600 type macroporous resin chromatography, absorption 6h, is first eluted to effluent with distilled water closely colourless, be 70% ethanol elution by the concentration of 4 times of column volumes again, collect containing alcohol eluen, reclaim ethanol, concentrating under reduced pressure vacuum drying becomes extractum, pulverize, cross 120 mesh sieves, obtain EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL for subsequent use, wherein in EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL, the content of total polyphenols is 71%, the content of ellagic acid is 2.5%, and the content of Punicalagin is 17.6%;
The preparation of gel:
Go bail for humectant propylene glycol 15 parts, solubilizing agent tween 2 parts, Pericarpium Granati extract 25 parts grinding evenly first dissolve, add the carboxymethylcellulose sodium solution 4 parts with aqueous dispersion, be uniformly dispersed, add antiseptic methyl hydroxybenzoate 0.5 part, excess water is to 100g, instillation triethanolamine regulates pH to be 4.3, stirs, can obtain pericarpium granati polyphenol gel.
Embodiment 6:
The preparation of EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL:
Get Pericarpium Granati and be ground into coarse powder, adding 20 times amount concentration is 45% ethanol warm macerating, and temperature 85 DEG C is extracted 4 times, each 1 hour, filters, merging filtrate decompression recycling ethanol, is concentrated into the concentrated solution of every mL containing Pericarpium Granati 0.15g;
Added by concentrated solution on processed good HPD600 type macroporous resin chromatography, absorption 12h, is first eluted to effluent with distilled water closely colourless, be 60% ethanol elution by the concentration of 3 times of column volumes again, collect containing alcohol eluen, reclaim ethanol, concentrating under reduced pressure vacuum drying becomes extractum, pulverize, cross 80 mesh sieves, obtain EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL for subsequent use, wherein in EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL, the content of total polyphenols is 66%, the content of ellagic acid is 3.2%, and the content of Punicalagin is 15.8%;
The preparation of gel:
Go bail for humectant propylene glycol 5 parts, Pericarpium Granati extract 15 parts grinding evenly first dissolve, add the carbomer solution 1 part with aqueous dispersion, be uniformly dispersed, add antiseptic ethyl hydroxybenzoate 0.2 part again, excess water is to 100g, instillation triethanolamine is 4.5 to pH, stirs, can obtain pericarpium granati polyphenol gel.
Embodiment 7
Pericarpium granati polyphenol gel is preparing prevention and therapy by bacterial gynecological inflammation vaginitis or cervicitis.Pharmacodynamic experiment:
(1) toxicology test research
Tests For Irritating Effects
The female White Rabbit of New Zealand, 6, body weight 1.8-2.0kg, tested material is the solution of the highest application liquid of sample 5 times of concentration, matched group adopts normal saline, slowly inject 2ml to laboratory animal to contaminate to vagina by test solution, control animals normal saline does same process, after contamination 24h, aeroembolism method is adopted to put to death animal, cut open the belly and take out complete vagina, longitudinally cut, whether perusal has hyperemia, the performances such as edema, then vagina is put into 10% formalin solution and fix more than 24h, choose three the position film-makings in two ends and central authorities of vagina, HE dyes, carry out histopathological examination, by " disinfection technology standard " (version in 2002) vaginal mucosa irritant reaction standards of grading table and strength grading table, scoring is stimulated to vaginal mucosa, intensity is evaluated, result of the test is in table 1:
From the result of the test of table 1, the difference that the average integral of tested treated animal vaginal mucosa irritant reaction and matched group average product divide is 0, according to " disinfection technology standard " (version in 2002) vaginal mucosa stimulus intensity hierarchical table, belongs to nonirritant;
(2) pharmacodynamics test research in body:
Mice caused by dimethylbenzene xylene ear swelling is tested:
Get Kunming mouse 50, body weight 18-22g, be divided into 5 groups at random, often organize 10, be respectively matched group, basic, normal, high three the dosage groups of pericarpium granati polyphenol gel (0.14 g/kg, 0.28 g/kg, 0.56 g/kg), pomegranate peel polyphenol effervescent tablet (0.30 g/kg); Each administration group gavage gives relative medicine, matched group gives isopyknic 0.5% CMC-Na, once a day, continuous 7 days, after last administration 1h, evenly dimethylbenzene 1ml/10g is coated with outside every mouse right ear, left ear is contrast, after 1h, mice is taken off neck to put to death, sweep away auricle in the sclerotic ring of left and right ear same position diameter 9mm, divide another name auricle weight with electronic balance, with the difference of two auricle weight for swelling, calculate each group of mice ear degree average and standard deviation, and calculate swelling suppression ratio, the results are shown in Table 2;
Suppression ratio=(matched group average ear swelling degree-administration group average ear swelling degree)/matched group average ear swelling degree x100%;
Remarks: compare with matched group,
﹡p<0.05,
﹡ ﹡p < 0.01
Table 2 data show: pericarpium granati polyphenol gel high dose group (0.56 g/kg) has the effect significantly suppressing mice ear, and pomegranate peel polyphenol effervescent tablet also has same purpose;
Carrageenan causes the impact of mice pedal swelling:
Get Kunming mouse 50, body weight 18-22g, be divided into 5 groups at random, often organize 10, be respectively Vehicle controls group, basic, normal, high three the dosage groups of pericarpium granati polyphenol gel (0.14 g/kg, 0.28 g/kg, 0.56 g/kg), pomegranate peel polyphenol effervescent tablet (0.30 g/kg); Each administration group gavage gives relative medicine, and Vehicle controls group gives isopyknic 0.5% CMC-Na, once a day, and continuous 7 days.After last administration 1h, every mice electronic digital display micrometer measures left back sufficient sole of the foot thickness, then the 0.1ml carrageenan suspension of subcutaneous injection 1% causes inflammation, and causing the left back sufficient sole of the foot thickness of scorching rear 0.5h, 1h, 2h, 6h electronic digital display micrometer mensuration respectively, so that the difference of sufficient sole of the foot thickness is as swelling before and after scorching, calculate each group of mice swelling degree of the paw average and standard deviation, and calculate swelling degree of the paw suppression ratio, the results are shown in Table 3 tables 4;
Suppression ratio=(matched group average ear swelling degree-administration group average ear swelling degree)/matched group average ear swelling degree x100%;
Remarks: compare with matched group,
﹡p<0.05,
﹡ ﹡p < 0.01
Table 3 table 4 data show: pericarpium granati polyphenol gel high dose group (0.56 g/kg) has the effect of significantly suppression mice ear causing scorching rear 0.5h, pomegranate peel polyphenol effervescent tablet also has same purpose.
Claims (1)
1. prepare the method for the pericarpium granati polyphenol gel for the treatment of gynecological inflammation for one kind, it is characterized in that this gel is is 5-30 part by EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL weight portion, adjuvant to be pharmaceutically acceptable gel matrix material be carbomer or hypromellose or sodium carboxymethyl cellulose 0.5-4 part, wetting agent is propylene glycol or glycerol and propylene glycol 5-20 part, solubilizing agent tween 0-2 part, antiseptic is methyl hydroxybenzoate or ethyl hydroxybenzoate 0.1-0.5 part, and pH adjusting agent is that triethanolamine is made; Wherein the principle active component of EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL is total polyphenols, ellagic acid and Punicalagin, and concrete operations follow these steps to carry out:
The preparation of EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL:
A, get Pericarpium Granati and be ground into coarse powder, adding 5-30 times amount concentration is 35-49% ethanol warm macerating, and temperature 71-85 DEG C, extracts 1-4 time, each 1-3 hour, and filter, merging filtrate decompression recycling ethanol, is concentrated into the concentrated solution that every mL is equivalent to crude drug 0.15-0.2g;
B, the concentrated solution obtained by step a adds on processed good HPD600 type macroporous adsorptive resins, absorption 3-12 hour, first with deionized water rinsing to effluent paler colour time, again with the 50-80%% ethanol elution of 2-5 times of column volume, collect containing alcohol eluen, reclaim ethanol, concentrating under reduced pressure vacuum drying becomes dry extract, pulverize, cross 80-120 mesh sieve, obtain EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL for subsequent use, the wherein content 60-80% of total polyphenols in EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL, the active component of the total polyphenols in EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL is the content 2-4% of ellagic acid, the content 15-20% of Punicalagin,
The preparation of gel:
C, step b EFFECT OF POLYPHENOLIC EXTRACT FROM POMEGRANATE PEEL wetting agent or solubilizing agent or wetting agent and solubilizing agent first to be dissolved, add in the carbomer or hypromellose or carboxymethylcellulose sodium solution using aqueous dispersion, be uniformly dispersed, add antiseptic and excess water again, stir, add triethanolamine and regulate pH to 4.0-5.0, can pericarpium granati polyphenol gel be obtained.
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
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| CN201210396920.0A CN102861116B (en) | 2012-10-18 | 2012-10-18 | Method for preparing pericarpium granati polyphenol gel for treating gynecological inflammation |
| PCT/CN2013/084674 WO2014059880A1 (en) | 2012-10-18 | 2013-09-30 | Method for preparation of pomegranate-peel polyphenol gel used to treat gynecological inflammation |
| EA201590591A EA029649B1 (en) | 2012-10-18 | 2013-09-30 | Pomegranate-peel polyphenol gel used to treat gynecological inflammation diseases and method for preparation thereof |
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| CN201210396920.0A CN102861116B (en) | 2012-10-18 | 2012-10-18 | Method for preparing pericarpium granati polyphenol gel for treating gynecological inflammation |
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| CN102861116B (en) * | 2012-10-18 | 2015-02-25 | 中国科学院新疆理化技术研究所 | Method for preparing pericarpium granati polyphenol gel for treating gynecological inflammation |
| CN103585321B (en) * | 2013-11-16 | 2015-05-13 | 李伟丽 | Externally used traditional Chinese medicine composition for treating trichomonas vaginitis |
| CN106822714A (en) * | 2017-03-22 | 2017-06-13 | 内蒙古医科大学 | A kind of gynaecological gel and preparation method thereof |
| CN107007778A (en) * | 2017-05-03 | 2017-08-04 | 沈阳恒泽医药技术有限公司 | Treat traditional Chinese medicine gel of gynaecological imflammation and preparation method thereof |
| CN107773607A (en) * | 2017-10-31 | 2018-03-09 | 桂林纽泰生物科技有限公司 | The method that litchi rind polyphenol is extracted from litchi rind |
| CN109288997A (en) * | 2018-12-06 | 2019-02-01 | 新疆维吾尔自治区维吾尔医药研究所 | A kind of compound medicine and its preparation method and application for treating rhinitis |
| CN113694093B (en) * | 2021-09-06 | 2023-03-21 | 成都大学 | Antibacterial and anti-inflammatory quillajasaponins gel and preparation method thereof |
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| CN101700257A (en) * | 2009-10-26 | 2010-05-05 | 中国科学院新疆理化技术研究所 | Pomegranate peel polyphenol antibiosis and antiphlogosis effervescent tablet as well as preparation method and application thereof |
| CN102453039A (en) * | 2010-11-03 | 2012-05-16 | 张守力 | Method for extracting ellagic acid from pomegranate rind by enzymolysis method |
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| US5536743A (en) * | 1988-01-15 | 1996-07-16 | Curatek Pharmaceuticals Limited Partnership | Intravaginal treatment of vaginal infections with buffered metronidazole compositions |
| CN100384447C (en) * | 2006-03-15 | 2008-04-30 | 常学军 | Medicine for treating gynecopathy and its preparing method |
| CN102293972B (en) * | 2011-08-25 | 2013-06-19 | 宁夏医科大学 | Extract for adjusting female vaginal microecology |
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| CN101700257A (en) * | 2009-10-26 | 2010-05-05 | 中国科学院新疆理化技术研究所 | Pomegranate peel polyphenol antibiosis and antiphlogosis effervescent tablet as well as preparation method and application thereof |
| CN102453039A (en) * | 2010-11-03 | 2012-05-16 | 张守力 | Method for extracting ellagic acid from pomegranate rind by enzymolysis method |
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| Publication number | Publication date |
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| EA201590591A1 (en) | 2016-01-29 |
| EA029649B1 (en) | 2018-04-30 |
| WO2014059880A1 (en) | 2014-04-24 |
| CN102861116A (en) | 2013-01-09 |
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