CN103006542A - Platycodin D sperm-killing contraceptive suppository for external use and placing device thereof - Google Patents
Platycodin D sperm-killing contraceptive suppository for external use and placing device thereof Download PDFInfo
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- CN103006542A CN103006542A CN2011102900701A CN201110290070A CN103006542A CN 103006542 A CN103006542 A CN 103006542A CN 2011102900701 A CN2011102900701 A CN 2011102900701A CN 201110290070 A CN201110290070 A CN 201110290070A CN 103006542 A CN103006542 A CN 103006542A
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Abstract
The invention discloses a platycodin D sperm-killing contraceptive suppository for external use. The contraceptive suppository is characterized in that the active ingredient of the suppository is platycodin D diluent; the platycodin D diluent is different concentrations of physiological saline solution of platycodin D 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 a kind of contraceptive suppository medicine take platycodin as effective ingredient, belong to medical technical field, particularly the sub-contraceptive suppository of a kind of Platycodin D external use sperm killing and apparatus for placing.
Background technology
Radix Platycodonis is the dry root of Campanulaceae Radix Platycodonis.Radix Platycodonis is flat, bitter in the mouth, and suffering has the effect of preventing phlegm from forming and stopping coughing, relieving sore throat to recover voice, the smooth lung qi of a surname, removing pus and relieving carbuncle.In recent years, as the Chinese medicine of integration of edible and medicinal herbs, Radix Platycodonis at immunomodulating, antiinflammatory, eliminate the phlegm, protect the liver, the pharmacological action of the aspect such as blood fat reducing attracts wide attention.At present, the more monomeric compound of research is platycodin A, B, C, D, D
2, D
3With polygalic acid D, D
2
Utilize Chinese herbal medicine Radix Platycodonis extract liquid to carry out the killing sperms in vitro experiment; it is remarkable to test its spermicide effect; sperm and the adult rats sperm that can make the adult have the normal activity of fertility within 1 minute are killed; make sperm lose mobility, experimental result is embodied in the Chinese patent 200610069559.5.
Recently, saponins and other chemical compounds that we further contain Radix Platycodonis again carry out the killing sperms in vitro experiment, and our experimental result shows that Platycodin D has the external effect of killing fast sperm.Through retrieval, there is not yet the research report of relevant Platycodin D killing sperms in vitro.Especially suppository is one of the most frequently used gynaecology external-use drug species, will reach good contraceptive effect as Platycodin D is applied in the suppository class topical drug.
Summary of the invention
The invention provides the sub-contraceptive suppository of a kind of Platycodin D external use sperm killing and modes of emplacement thereof, adopt the normal saline solution of Platycodin D 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 Platycodin D external use sperm killing, solid suppository is by evenly mixing under Platycodin D diluent and the embolus substrate room temperature, described Platycodin D diluent is that the Platycodin D 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 Platycodin D diluent concentration is 0.01～1.0mg/ml.
Described Platycodin D diluent concentration is 0.01mg/ml, 0.1mg/ml and 1.0mg/ml.
Wherein the extracting method of Platycodin D extract is: accurately take by weighing Radix Platycodonis sample powder 50g, place tool plug 500mL conical flask, add 70% methanol 300mL, soaked 24 hours, supersound process 30 minutes repeats centrifugal filtration 4 times, filtrate decompression reclaims to get extractum, add the 300mL acetone precipitation, filter rear filtrate and reclaim to get extractum, add people 300mL water after, be transferred to separatory funnel, add the 300mL extracted with diethyl ether 2 times.Discard the ether layer, water layer adds 300mL water, and saturated n-butanol extraction 4 times merges the n-butanol layer reclaim under reduced pressure and gets extractum, at last with 500mL ether sedimentation decontamination, after the drying precipitate, get 280 milligrams of white powder materials.Precision takes by weighing the 50mg white powder, surely is dissolved in the 10mL volumetric flask with mobile phase, is mixed with sample solution, with its composition of hplc determination.
This Platycodin D, (English name: Platy codin-D), be white powder, molecular weight is 1224, and its molecular formula is C
57H
92O
28
The present invention also provides the apparatus for placing of the sub-contraceptive suppository of this Platycodin D 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 Platycodin D 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 90 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 platycodin extract:
Accurately take by weighing Radix Platycodonis sample powder 50g, place the 500mL conical flask, add 70% methanol 300mL, soaked 24 hours, supersound process 30 minutes repeats centrifugal filtration 4 times, filtrate decompression reclaims to get extractum, add the 300mL acetone precipitation, filter rear filtrate and reclaim to get extractum, add people 300mL water after, be transferred to separatory funnel, add the 300mL extracted with diethyl ether 2 times.Discard the ether layer, water layer adds 300mL water, and saturated n-butanol extraction 4 times merges the n-butanol layer reclaim under reduced pressure and gets extractum, at last with 500mL ether sedimentation decontamination, after the drying precipitate, get 280 milligrams of white powder materials.Precision takes by weighing the 50mg white powder, surely is dissolved in the 10mL volumetric flask with mobile phase, is mixed with sample solution, with its composition of hplc determination.
Other gets 5 milligrams of Platycodin D reference standards, adds methanol and makes every milliliter of solution [Platycodin D standard substance (lot number A0321, purity 〉=98%) are available from Chengdu Man Site bio tech ltd] that contains 1 milligram.Accurate above-mentioned sample solution 20 microlitres, reference substance solution 10 microlitres drawn, the injection liquid chromatography, measure, chromatographic column is the Agilent post, 4.6 millimeters (mm) * 150mm, 5 microns, mobile phase is methanol-acetonitrile-0.2% phosphate aqueous solution (volume ratio is 3: 25: 72), detecting wavelength is 204 millimicrons, and chromatogram column temperature is 40 ℃, and flow velocity is 1 milliliter of per minute.The white powder peak area is consistent with Platycodin D standard substance peak area as a result, shows that the gained white powder is Platycodin D.The Platycodin D of 230 milligrams of extractions of other residues is configured to carry out the killing sperms in vitro experiment behind the solution.
This Platycodin D, (English name: Platycodin-D), be white powder, molecular weight is 1224, and its molecular formula is C
57H
92O
28
2, killing sperms in vitro experiment:
Take by weighing 5mg, 0.5mg and 0.05mg Platycodin D, add respectively 0.9% normal saline 5ml, shake up, be mixed with the Platycodin D diluent 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, the maneuver extracting extract is in the 25ml of clean sterilization small beaker, semen volume 2-4ml, pH 7.0-8.0, liquefying time＜30min, sperm motility 70-92%, energy a+b level 50%-80%, sperm concentration＞60 * 106/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 Platycodin D 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.Tester 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 to people's sperm in vitro killing action shortest time be 38 seconds, 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 Platycodin D suppository is that 50mg/ props up, and the 50mg Platycodin D is dissolved in sterile distilled water 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 Platycodin D loses activity sperm simultaneously, plays contraceptive efficacy.
Claims (4)
1. sub-contraceptive suppository of Platycodin D external use sperm killing, it is characterized in that solid suppository is by evenly mixing under Platycodin D diluent and the embolus substrate room temperature, described Platycodin D diluent is that the Platycodin D 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 Platycodin D external use sperm killing as claimed in claim 1 is characterized in that described Platycodin D diluent concentration is 0.01～1.0mg/ml.
3. the sub-contraceptive suppository of a kind of Platycodin D external use sperm killing as claimed in claim 1 is characterized in that described Platycodin D diluent concentration is 0.01mg/ml, 0.1mg/ml and 1.0mg/ml.
4. the apparatus for placing of the sub-contraceptive suppository of Platycodin D 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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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103385781A (en) * | 2013-07-25 | 2013-11-13 | 黄湘铭 | In vitro contraceptive for female |
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| CN2772528Y (en) * | 2005-01-27 | 2006-04-19 | 江西省康洋药业有限公司 | Suppository medicine feeder |
| CN1965881A (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 balloonflower as in-vitro spermaticide and method for preparing the medicament |
| 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 |
| CN101804094A (en) * | 2010-03-19 | 2010-08-18 | 山东省计划生育科学技术研究所 | Medicament for killing sperms in vitro |
| CN201664467U (en) * | 2010-04-21 | 2010-12-08 | 李署光 | Suppository injector |
-
2011
- 2011-09-28 CN CN2011102900701A patent/CN103006542A/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 |
| CN1965881A (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 balloonflower as in-vitro spermaticide and method for preparing the medicament |
| CN101804094A (en) * | 2010-03-19 | 2010-08-18 | 山东省计划生育科学技术研究所 | Medicament for killing sperms in vitro |
| CN201664467U (en) * | 2010-04-21 | 2010-12-08 | 李署光 | Suppository injector |
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| 许传莲等: "应用RP-HPLC法测定不同产地中秸秆皂甙D", 《吉林农业大学学报》, vol. 21, no. 4, 31 December 1999 (1999-12-31), pages 35 - 38 * |
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| CN103385781A (en) * | 2013-07-25 | 2013-11-13 | 黄湘铭 | In vitro contraceptive for female |
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Application publication date: 20130403 |