CN103006541A - Polygalacic acid sperm-killing contraceptive suppository for external use and placing device - Google Patents
Polygalacic acid sperm-killing contraceptive suppository for external use and placing device Download PDFInfo
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- CN103006541A CN103006541A CN2011102900699A CN201110290069A CN103006541A CN 103006541 A CN103006541 A CN 103006541A CN 2011102900699 A CN2011102900699 A CN 2011102900699A CN 201110290069 A CN201110290069 A CN 201110290069A CN 103006541 A CN103006541 A CN 103006541A
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Abstract
The invention discloses a polygalacic acid sperm-killing contraceptive suppository for external use. The contraceptive suppository is characterized in that the active ingredient of the suppository is polygalacic acid diluent; the polygalacic acid diluent is different concentrations of physiological saline solution of polygalacic acid extracts; and the suppository is solid at normal temperature. When the contraceptive suppository is used, the contraceptive suppository is quickly dissolved in vaginas at body temperature, is in a semi-liquid state and can quickly kill sperms after being in contact with the sperms and deactivate the sperms, thus playing a role in contraception. The invention also discloses a matched placing device of the contraceptive suppository. The contraceptive suppository has a good contraceptive effect and can avoid unplanned pregnancy.
Description
Technical field
The present invention relates to the sub-contraceptive suppository of external use sperm killing that a kind of Polygalacic acid is made, belong to medical technical field, particularly the sub-contraceptive suppository of a kind of Polygalacic acid external use sperm killing and apparatus for placing.
Background technology
Radix Polygalae is the dry root of milk wort Radix Polygalae.Radix Polygalae is flat, bitter in the mouth, and suffering has antitussive, eliminates the phlegm, Fructus Alpiniae Oxyphyllae, stable, removing toxic substances and promoting subsidence of swelling, the strong effect of tonification.Modern pharmacological research shows that its some active component also has antibiotic, blood sugar lowering, immunostimulant isoreactivity.The applicant once utilized the Chinese herbal medicine Radix Polygalae extracting solution to carry out the killing sperms in vitro experiment, and its spermicide effect is remarkable as a result, and sperm and the adult rats sperm that can make the adult have the normal activity of fertility within 0.5 minute are killed, and make sperm lose mobility.Recently, the saponins that we further contain Radix Polygalae again, Polygalacic acid and other chemical compounds carry out the killing sperms in vitro experiment, our experimental result demonstration, and Polygalacic acid has the external effect of killing fast sperm.Through retrieval, there is not yet the research report of relevant senegenin in vitro spermicidal.
Radix Polygalae contains multiple triterpenes saponin, mainly contains polygalic acid A, B, E, F, G.In addition, the derivant etc. that still contains Radix Polygalae alkali, Polygalacic acid, polygalite, 2-acetylamino-2-deoxy-D-glucose, xanthone and cinnamic acid.
Summary of the invention
The invention provides the sub-contraceptive suppository of a kind of Polygalacic acid external use sperm killing and apparatus for placing, adopt the normal saline solution of Polygalacic acid extract as the effective ingredient of suppository, make the solid-state suppository medicine of room temperature, the spermicide function well.
The present invention realizes by following technical scheme:
The sub-contraceptive suppository of a kind of Polygalacic acid external use sperm killing, solid suppository is by evenly mixing under Polygalacic acid diluent and the embolus substrate room temperature, described Polygalacic acid diluent is that the Polygalacic acid extract is dissolved in the solution in 9% normal saline, and described embolus substrate is that volume ratio is 5: 1 cocoa butter and the mixture of instant starch.
Described Polygalacic acid diluent concentration is 0.01～1.0mg/ml.
Described Polygalacic acid diluent concentration is 0.01mg/ml, 0.1mg/ml and 1.0mg/ml.
Wherein the extracting method of Polygalacic acid extract is: pulverize after getting the Radix Polygalae sample drying, precision takes by weighing powder 5g, places tool plug 300mL conical flask, the methanol 150mL of adding 70% flooded 1 hour, and jolting in per 15 minutes once, reflux 5 hours, extracting solution evaporate to dryness, residue add 10% hydrochloric acid solution 200mL, and boiling water bath refluxed 2 hours, cooling, filter and be precipitated to neutrality with distilled water wash, with the dissolve with methanol precipitation and be settled to 200mL, namely get sample solution.Decontamination after the drying precipitate, gets white powder material 500mg.Extracting waste powdered rubber 5mg adds methanol 5mL dissolving, surely is dissolved in the 10mL volumetric flask with mobile phase.Get sample solution, sample introduction is measured under chromatographic condition.
This Polygalacic acid of gained (English name: Polygalacic Acid), be white powder, molecular weight 488.6985, its molecular formula is C
29H
44O
6
The present invention also provides the apparatus for placing of the sub-contraceptive suppository of this Polygalacic acid external use sperm killing, comprise trocar sheath, push rod, handle and front outer housing, described push rod stretches into trocar sheath inside, and handle is installed in the push rod afterbody, is installed in the head of trocar sheath with the solid contraceptive suppository of described front outer housing.
User can oneself be opened front outer housing, promotes handle and push rod, makes the solid contraceptive suppository enter the vagina deep and presses close to the cervix uteri place.Have sexual intercourse pushed in front 5 minutes, and it is semi-fluid shape that the solid contraceptive suppository melts under body temperature voluntarily, and sealing cervix uteri mouth makes seminal fluid can not directly enter cervical canal, and the Polygalacic acid composition loses activity sperm simultaneously, plays contraceptive efficacy.
Beneficial effect of the present invention is: select the diluent of variable concentrations, can reach 3 seconds of shortest time, the spermicide ability in 98 seconds of maximum duration is higher than the result of use of spermicide composition nonoxynolum commonly used; According to the spermicide effect classification that method and the standard of World Health Organization (WHO) (WHO) recommendation are revised slightly, the present invention can reach the effect of stronger spermicidal effect; The contraceptive suppository that diluent is made carries out clinical trial 618 examples and uses the suppository contraception, and success rate reaches 100%, without the unexpected gestation of 1 example.
Description of drawings
Fig. 1 is the structural representation of contraceptive suppository apparatus for placing of the present invention
The specific embodiment
Below the present invention will be further described.
1, the preparation of Polygalacic acid extract:
Pulverize after getting the Radix Polygalae sample drying, precision takes by weighing powder 5g, places tool plug 300mL conical flask, the methanol 150mL of adding 70% flooded 1 hour, and jolting in per 15 minutes once, reflux 5 hours, extracting solution evaporate to dryness, residue add 10% hydrochloric acid solution 200mL, and boiling water bath refluxed 2 hours, cooling, filter and be precipitated to neutrality with distilled water wash, with the dissolve with methanol precipitation and be settled to 200mL, namely get sample solution.Decontamination after the drying precipitate, gets white powder material 500mg.Extracting waste powdered rubber 5mg adds methanol 5mL dissolving, surely is dissolved in the 10mL volumetric flask with mobile phase.Get sample solution, sample introduction is measured under chromatographic condition.
Other gets Polygalacic acid reference standards 5mg, adds 5 milliliters of 70% methanol and makes every milliliter of solution that contains 1 milligram.Polygalacic acid standard substance (lot number A0013, purity 〉=98%) are available from Chengdu Man Site bio tech ltd.Accurate above-mentioned sample solution 20 microlitres, reference standards solution 10 microlitres drawn, the injection liquid chromatography, Agilent 1200 High Performance Liquid Chromatography posts are 4.6 millimeters mm * 150mm, and 5 microns, mobile phase is acetonitrile-0.05% phosphoric acid (volume ratio is 50: 50); Detect 210 millimicrons of wavelength; Sample size 10 microlitres; Chromatogram column temperature is 25 ℃, and flow velocity is 1 milliliter of per minute.Measurement result sample solution peak area is consistent with Polygalacic acid standard substance peak area, shows that the gained sample solution is Polygalacic acid.Remain 450 milligrams of Polygalacic acid powder and be used for the killing sperms in vitro experiment.
This Polygalacic acid of gained (English name: Polygalacic Acid), be white powder, molecular weight 488.6985, its molecular formula is C
29H
44O
6
2, killing sperms in vitro experiment:
Take by weighing 5mg, 0.5mg and 0.05mg Polygalacic acid, add respectively 0.9% normal saline 5ml, shake up, be mixed with the Polygalacic acid solution of 1mg/ml (diluent-1), 0.1mg/ml (diluent-2) and 0.01mg/ml (diluent-3), 4 ℃ of Refrigerator stores are for subsequent use.
Experiment is selected from 25-35 year healthy male 38 examples with semen sample, ascetic 3-5d, and the maneuver extracting extract is in the 25ml of clean sterilization small beaker, semen volume 2-4ml, pH7.0-8.0, liquefying time＜30min, sperm motility 70-92%, energy a+b level 50%-80%, sperm concentration＞60 * 10
6/ ml, abnormal sperm rate＜20%.
Revise slightly by method and standard that World Health Organization (WHO) (WHO) is recommended.The killing sperms in vitro effect classification of this experiment regulation: from sperm contact medicine to 0.5 minute (i.e. 30 seconds) whole inactivations for having moment spermicide effect; 0.5 for having stronger spermicide effect, 3 minutes-5 minutes is faint spermicide effect between minutes-3 minutes.With people's seminal fluid 0.5ml, join respectively 1mg/ml, 0.1mg/ml and among the Polygalacic acid solution 0.5ml of 0.01mg/ml, other gets reference substance nonoxynolum (0.9% normal saline dilution, nonoxynolum concentration is for being configured to respectively 1mg/ml, 0.1mg/ml reach three kinds of variable concentrations of 0.01mg/ml) and each 0.5ml of normal saline, add same 0.5 milliliter of seminal fluid (with a seminal fluid), at once mixing, get rapidly 1 droplet on microscope slide, the lower sperm motility situation of observing of inverted microscope (37 ℃ of constant temperature), 10 high power fields of Continuous Observation all lose mobility as terminal point take sperm.Time to whole inactivations during from sperm contact medicine is the spermicide time.Each experiment is carried out 2-3 time repeatedly.
Diluent-1 (1mg/ml) was 3 seconds to people's sperm in vitro killing action shortest time, and maximum duration was 5 seconds; Diluent-2 (0.1mg/ml) was 3 seconds to people's sperm in vitro killing action shortest time, and maximum duration was 6 seconds; Diluent-3 (0.01mg/ml) was 48 seconds to people's sperm in vitro killing action shortest time, and maximum duration was 98 seconds.Nonoxynolum (NP-9) 1mg/ml was 5 seconds to people's sperm in vitro killing action shortest time, and maximum duration was 12 seconds; 0.1mg/ml liter was 38 seconds to people's sperm in vitro killing action shortest time, maximum duration was 426 seconds; 0.01mg/ml to people's sperm in vitro killing action shortest time be 19 minutes, maximum duration is 35 minutes.0.9% normal saline on sperm motility without impact, identical with former seminal fluid activity ratio.
3, contraceptive suppository apparatus for placing of the present invention and using method thereof
Such as Fig. 1, be the structural representation of contraceptive suppository apparatus for placing of the present invention, comprise trocar sheath 1, push rod 2, handle 3 and front outer housing 4, push rod 2 stretches into trocar sheath 1 inside, handle 3 is installed in push rod 2 afterbodys, is installed in the head of trocar sheath 1 with the solid contraceptive suppository of front outer housing 4.
Usually making Polygalacic acid suppository is that 50mg/ props up, and the 50mg Polygalacic acid is dissolved in glycerol 2ml, adds mixing in the embolus substrate, substrate was with cocoa butter and instant starch (5: 1, the ratio of volume) making, is solid under the room temperature, rapidly dissolving under the intravaginal body temperature, be the semi liquid state shape, contact with seminal fluid, can kill fast sperm, make sperm lose mobility, can not contact with ovum, play contraceptive efficacy.
Adopt contraceptive suppository apparatus for placing shown in Figure 1, user can oneself be opened front outer housing, promotes handle and push rod, makes contraceptive suppository enter the vagina deep and presses close to the cervix uteri place.Have sexual intercourse pushed in front 5 minutes, and it is semi-fluid shape that contraceptive suppository melts under body temperature voluntarily, and sealing cervix uteri mouth makes seminal fluid can not directly enter cervical canal, and Polygalacic acid loses activity sperm simultaneously, plays contraceptive efficacy.
Claims (4)
1. sub-contraceptive suppository of Polygalacic acid external use sperm killing, it is characterized in that solid suppository is by evenly mixing under Polygalacic acid diluent and the embolus substrate room temperature, described Polygalacic acid diluent is that the Polygalacic acid extract is dissolved in the solution in 9% normal saline, and the volume ratio of described embolus substrate is 5: 1 cocoa butter and the mixture of instant starch.
2. the sub-contraceptive suppository of a kind of Polygalacic acid external use sperm killing as claimed in claim 1 is characterized in that described Polygalacic acid diluent concentration is 0.01～1.0mg/ml.
3. the sub-contraceptive suppository of a kind of Polygalacic acid external use sperm killing as claimed in claim 1 is characterized in that described Polygalacic acid diluent concentration is 0.01mg/ml, 0.1mg/ml and 1.0mg/ml.
4. the apparatus for placing of the sub-contraceptive suppository of Polygalacic acid external use sperm killing, comprise trocar sheath, push rod, handle and front outer housing, it is characterized in that described push rod stretches into trocar sheath inside, handle is installed in the push rod afterbody, is installed in the head of trocar sheath with the solid contraceptive suppository of described front outer housing.
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| CN2011102900699A CN103006541A (en) | 2011-09-28 | 2011-09-28 | Polygalacic acid sperm-killing contraceptive suppository for external use and placing device |
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Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN2772528Y (en) * | 2005-01-27 | 2006-04-19 | 江西省康洋药业有限公司 | Suppository medicine feeder |
| CN1965912A (en) * | 2006-11-01 | 2007-05-23 | 山东省计划生育科学技术研究所 | Application of Chinese medicine polygala root as in-vitro spermaticide and method for preparing the medicament thereof |
| CN101069686A (en) * | 2006-05-12 | 2007-11-14 | 南京圣和药业有限公司 | Laevo-ornidazole vagina administration preparation, its preparing method and use |
| CN101804109A (en) * | 2010-03-19 | 2010-08-18 | 山东省计划生育科学技术研究所 | Compound senegenin in vitro spermicidal drug |
| CN201664467U (en) * | 2010-04-21 | 2010-12-08 | 李署光 | Suppository injector |
-
2011
- 2011-09-28 CN CN2011102900699A patent/CN103006541A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN2772528Y (en) * | 2005-01-27 | 2006-04-19 | 江西省康洋药业有限公司 | Suppository medicine feeder |
| CN101069686A (en) * | 2006-05-12 | 2007-11-14 | 南京圣和药业有限公司 | Laevo-ornidazole vagina administration preparation, its preparing method and use |
| CN1965912A (en) * | 2006-11-01 | 2007-05-23 | 山东省计划生育科学技术研究所 | Application of Chinese medicine polygala root as in-vitro spermaticide and method for preparing the medicament thereof |
| CN101804109A (en) * | 2010-03-19 | 2010-08-18 | 山东省计划生育科学技术研究所 | Compound senegenin in vitro spermicidal drug |
| CN201664467U (en) * | 2010-04-21 | 2010-12-08 | 李署光 | Suppository injector |
Non-Patent Citations (2)
| Title |
|---|
| 赵云生等: "远志中远志酸含量影响因素初探", 《天然产物研究与开发》, vol. 22, 31 December 2010 (2010-12-31), pages 634 - 638 * |
| 邱毅等: "中药远志提取物体外杀精子效果与机制研究", 《中国计划生育学杂志》, no. 11, 31 December 2010 (2010-12-31), pages 652 - 655 * |
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Application publication date: 20130403 |