CN1491676A - Percutaneous or oral contraceptive, abortion and sterilizing composition - Google Patents

Abstract

The present invention relates to percutaneous or oral taken contraceptive, abortive and sterilizing composition comprising Chinese herbal medicine, sterilizer, penetration promoter, emulsifier, thickener and other components. It has several functions, high effect, no toxic side effect, stable performance and other advantages.

Description

Percutaneous formula (or oral formula) contraception induced abortion bactericidal composition

The present invention relates to a kind ofly, be aided with being used for contraception, induced abortion, sterilizing and preventing and treating compositions of sexually transmitted disease (STD), dermatosis and gynopathic percutaneous formula (or oral formula) administration and preparation method thereof of compositions such as disinfection sanitizer, short penetrating agent, emulsifying agent, thickening agent based on various Chinese herbal medicine.

At present, contraceptive on the market mostly is Western medicine, hormone medicine, as delalutin, megestrol, norethindrone, ethinylestradiol, estradiol valerate, estrogen, progestogen, phenylmercuric acetate, nonoxynolum, dioxygen biguanide ethane, benzalkonium bromide, gentian violet etc., these medicines all have certain side effect, as cause nausea, early pregnancy sample reactions such as headache, weight gaining, dysmenorrhea, amenorrhea, contraceptive effect is not good enough.

Some Chinese medicine composition for contraception also appear in recent years.A kind of medicinal liquor for contraception is disclosed as CN1265912A, will comprise 14 kinds of Chinese herbal medicine such as Radix Aconiti, Radix Aconiti Kusnezoffii, blood Caulis Akebiae with 50 the degree soaking in Chinese liquor, oral administration is put on the skin outward, to reach the contraception purpose.But the many batchings of this technology have certain toxicity, and are base material with high number of degrees Chinese liquor, and it is a difficult problem that the woman that can not drink is taken.CN1086140A discloses a kind of " pregnancy-proof incense ", is percutaneous formula contraceptive, is absorbed effective percentage low (92%) but the thick thing grain of its powdery is difficult for seeing through skin.CN1283498A discloses a kind of " umbilical liquid contraceptive ", and some batching is difficult for buying as summer Radix Solani Melongenae, whiteback greenbrier rhizome, Radix Rehmanniae taro, and its contraceptive prevalence rate also only has about 96%, and the coating number of times is frequent.Pure water amount by embodiment can't soak medicine.CN1207934A discloses a kind of " contraceptive and oxytocic ointment ", forms with 30 kinds of prepared from traditional Chinese medicines, and some raw material is difficult for buying, the preparation trouble.

And above-mentioned technical functionality is single, all has only the contraception function.

The object of the present invention is to provide a kind ofly, be aided with being used for contraception, induced abortion, sterilizing and preventing and treating the composition and method of making the same of sexually transmitted disease (STD), dermatosis and gynopathic percutaneous formula (or oral formula) administration of compositions such as disinfection sanitizer, short penetrating agent, emulsifying agent, thickening agent based on Chinese herbal medicine.Said composition can be made into the water base emulsifiable paste of external, water preparation washing liquid, suppository, plaster, membrane, oral liquid, orally exempts to decoct dosage forms such as electuary, have contraception, induced abortion, sterilizing, prevent and treat sexually transmitted disease (STD), dermatosis, gynaecopathia (wasting mashed, polyp, son battalion muscular tumor, uterus carcinoma, breast carcinoma, ovarian cancer, wound recovery in puerperal, dysmenorrhea, amenorrhea, menoxenia etc. as vaginitis, urethritis, battalion's neck), prolong sex time, improve multiple functions such as life quality, have no side effect, effective percentage is more than 99%, and is with low cost, easy to use.

Material component proportioning of the present invention following (weight portion): Radix Notoginseng: 5-15 (preferred 8-12), Fructus Aurantii Immaturus 5-15 (preferred 8-12), Radix Angelicae Sinensis: 5-15 (preferred 8-12), Fructus Crotonis: 5-10 (preferred 6-8), Folium Ilicis Cornutae: 5-15 (preferred 8-12), Chinese small iris seed: 5-15 (preferred 8-12), Rhizoma Chuanxiong: 5-15 (preferred 8-12), Sanguis Draxonis: 3-6 (preferred 4-5), Radix Bupleuri: 3-8 (preferred 4-6), Radix Polygalae: 3-8 (preferred 4-6), Radix Rehmanniae Preparata: 3-8 (preferred 4-6), the Radix Paeoniae Alba: 3-8 (preferred 4-6), Semen Brassicae Campestris: 3-8 (preferred 4-6), Flos Carthami: 3-8 (preferred 4-6), Herba Asari: 0.5-3 (preferred 1-2), Herba Eupatorii: 1-3 (preferred 1.5-2), Flos Caryophylli: 0.5-2 (preferred 1-1.5), Borneolum Syntheticum: 3-6 (preferred 4-5), Moschus: 0.010-0.08 (preferred 0.03-0.5), bromo geramine: 0.05-0.5 (preferred 0.1-0.4), povidone iodine: 0.01-0.5 (preferred 0.1-0.4), Polyethylene Glycol (preferred 8000): 1-3 (preferred 1.5-2.5), tween 80: 0.1-1.5 (preferred 0.8-1.2), glycerin/propylene glycol (1: 1): 3-10 (preferred 5-8).

Processing technology: (1) water base cream preparation grinds to form 100-300 purpose powder with each medicinal herb components drying, soaks 10-15 days with 10 times of water (or alcoholic solution of 50%-80%), filters to get filtrate.Filtrate is condensed into 100 parts of solution under 80-90 ℃, under stirring, add tween 80, Polyethylene Glycol (8000), glycerin/propylene glycol (1: 1) mixed liquor, Borneolum Syntheticum (alcoholic solution), Moschus (alcoholic solution), bromo geramine (saline solution), povidone iodine (aqueous solution) while hot successively, stir and promptly get water base emulsifiable paste.This emulsifiable paste can directly be applied on penis, the glans penis, or is applied to positions such as women's umbilicus, pudendum, vagina outward, and sexual life at once all can reach contraception, has an abortion, sterilizes, prevents and treats sexually transmitted disease (STD), dermatosis, gynaecopathia, prolongation sex time, improves purposes such as pleasant sensation.This emulsifiable paste also dilutable water is done the use of water preparation washing liquid.If necessary, also can to add the nitric acid organic ester in the patent in a separate paper " the percutaneous formula is used for the treatment of the compositions for the treatment of sexual impotence and female frigidity and preventing and treating sexually transmitted disease (STD) " be the tonifying YANG composition to water base emulsifiable paste.

(2) oral liquid formulations with the bromo geramine in the processing technology (1), povidone iodine, Polyethylene Glycol (8000), tween 80, the glycerin/propylene glycol mixed liquor is given up need not, get the filtrate concentrated solution and after the routine sterilization, promptly can be used as women's oral liquid, can reach contraception induced abortion purpose.

(3) orally exempt to decoct the electuary same processing technology (2) of preparing burden, raw material grinds to form 300 orders-350 order with pulverizing mill after drying, directly makes decoction, electuary.Micropowder technology can make the comprehensive cell yardstick of Chinese crude drug sporoderm-broken rate＞86.5%.After the cell wall breaking, intracellular water and oil make microparticle surfaces be half hygrometric state to external migration, make more homogenization of each effective ingredient, thereby have strengthened drug effect; Improved industrial extraction ratio, onset time is significantly shortened, acted on stronger, comprehensive; Can make the profitable strain effect faster, stronger; Because of diameter of aspirin particle is little, the adsorption of intestinal wall to be strengthened, the enteral holdup time prolongs, more favourable human body is to the absorption of medicine, reduced oral granular sense, delicate mouthfeel is satiny, can remove the decoction link from, directly bath is taken, maximally utilised the various compositions in the medicine, do not produced waste, or do not stuck with paste at the end when decocting, and can boil the full clothes in back, utilization ratio of drug is 100%; Dosage has reduced by 2 to more than 10 times (4.99 times of decreased average), has saved 81% medicine, and economical, societal benefits are very remarkable.This process also provides a kind of cooked mode for other Chinese herbal medicine processing.The same processing technology of this dosage form action function (2).

In addition, also can be as required routinely technology make dosage forms such as various plasters, suppository, diaphragm.

Arasaponin excited uterine smooth muscle of energy and endometrium blood capillary that Radix Notoginseng of the present invention (being " Radix Stephaniae Sinicae (Radix Stephaniae Dielsianae) " again) is contained, fertilized ovum is overturned between implantation period, disturb the due peaceful condition of implantation period intrauterine environment, make blood capillary continue to shrink more than 5-7 hour, cause the endometrium anoxia and the quick inactivating fertilized ovum.

Fructus Aurantii Immaturus: picric acid is slightly cold, and dispelling the stagnated QI removes long-pending, and the painful abdominal mass that disappears of reducing phlegm is convinced hard knot by patient analysis, and it is full to control the interventral reality of umbilicus, and dispel and cut off the water, by dyspepsia, relieving constipation; There is remarkable excitation in the uterus, makes uterine contraction strong, tension force increases, and shrinks the rhythm and pace of moving things and strengthens, even straight contraction is arranged; Contain and stop pregnant substance C irantin, can suppress ovary hyaluronidase activity on every side.

Radix Angelicae Sinensis: collapsible deferent duct and cervix uteri, tool are enriched blood, the usefulness of regulating menstruation.

Fructus Crotonis: can rise and close mashed tire, fistula numbness, the tire regulating menoxenia that falls, ovum be broken excrete, suppress ovum and grow, stop its fertilization to grow implantation.

Folium Ilicis Cornutae, Chinese small iris seed: can make the ovum inactivation.

Rhizoma Chuanxiong: enrich blood, invigorate blood circulation, circulation of qi promoting, blood stasis dispelling, urge through, kill body early embryo, make that the embryo is softening to be absorbed or come off, discharge with menstruation.

Sanguis Draxonis: promoting blood circulation to remove blood stasis, detumescence.

Radix Bupleuri: bitter flat, resolving depression is soothing the liver.

Radix Polygalae: capable stagnant, the promoting blood circulation to remove blood stasis of removing food stagnancy.

Thermally: in " SIWU TANG ", play collaborative contraceptive efficacy.

The Radix Paeoniae Alba, Semen Brassicae Campestris: the yin nourishing of enriching blood, blood-activating and qi-promoting.

Flos Carthami: promoting flow of QI and blood, blood stasis dispelling, urge through, kill body early embryo.

Herba Asari: can play the slight surface anesthetic effect of the excited conduction of inhibition, the smart time of sexual intercourse time delay long shot, and antibacterial and anti-inflammation functions is arranged.

Herba Eupatorii: its fragrance has contraceptive efficacy.

Flos Caryophylli, Borneolum Syntheticum: collaborative each spice, to strengthen causing resuscitation with aromatic drugs.

Moschus: the tire of hastening parturition down, the woman hears its flavor, and menstruation shifts to an earlier date, anemia of pregnant woman's miscarriage.The abnormal smells from the patient that is distributed passes to women's maincenter, makes hypothalamus strengthen prolactin antagonist release and cause the antepituitary prolactin antagonist to be secreted and reduces, and makes the corpus luteum impaired development, and the material in excited uterus is upset endometrial growth rhythm, makes the fertilized ovum inactivation.

Bromo geramine: be the sterilizing medicine originally, and be surprised to find that it also has quick (30 seconds) 100% to kill the effect of sperm, but, also improved the safety factor that kills smart contraception, and had no side effect with this medicine both sterilizing.

Povidone iodine: be wide spectrum, efficient, non-stimulated and toxic sterilizing medicine, be surprised to find that it also has (1 minute) fast to kill the effect of sperm, can replace nonoxynolum.

Polyethylene Glycol (8000): thickening agent, and can promote medicine to dermal osmosis, and increase drug effect, shorten onset time.

Tween 80: emulsifying agent, short penetrating agent can make each component (water solublity, oil soluble material) be blended in the emulsifiable paste to stable and uniform.

Glycerin/propylene glycol (1: 1) mixed liquor: wetting agent, lubricant, short penetrating agent.

The present composition can be made into multiple dosage form, as water base emulsifiable paste, and washing liquid, spray, plaster, membrane, oral liquid, oral granule, decoction.Wherein water base emulsifiable paste dosage form is because of containing short penetrating agent, and drug effect is improved, instant effect, and can be as oil-based cream pollution clothes, make us uncomfortable; Oral granule, decoction adopt micropowder breaking cell wall technology first, have improved drug effect greatly, have improved mouthfeel, utilization ratio of drug 100%, and dose reduces by 2 to more than 10 times.

The present invention's efficient height (＞99%) of practising contraception is because the double insurance of Chinese medicine and Western medicine is arranged.The present invention not only practises contraception, and also can have an abortion, and afflux produces, induced labor is an one, the anemia of pregnant woman in much months no matter, and sending into 5-20ml this product unguentum (suppository, membrane) in the uterine cavity can be easily except that pregnant.And peroral dosage form serve on 3-5 days in menstrual phase, serve on three days puerperal, every day sooner or later each once, every day dose 10-20g, the half a year to one year of can practising contraception.And the fugitive contraception of instantaneity, consumption is that 1-5ml (g) gets final product.

The invention will be further described below in conjunction with embodiment

Embodiment 1 (water base emulsifiable paste dosage form):

With Radix Notoginseng 10g, Fructus Aurantii Immaturus 10g, Radix Angelicae Sinensis 10g, Fructus Crotonis 7g, Folium Ilicis Cornutae 10g, Chinese small iris seed 10g, Rhizoma Chuanxiong 10g, Sanguis Draxonis 4g, Radix Bupleuri 5g, Radix Polygalae 5, thermally 5g, Radix Paeoniae Alba 5g, Semen Brassicae Campestris 5g, Flos Carthami 5g, Herba Asari 1.5g, Herba Eupatorii 2g, Flos Caryophylli 1g, fully dry, grind to form 120 months powder, steeped 10 days with 10 times of water loggings, filter and remove residue gets filtrate.Filtrate is condensed into 100ml solution under 85 ℃, under the 2000R/min stirring, add 0.8g tween 80,2g Polyethylene Glycol (8000), 5g glycerol/malonic acid (1: 1) mixed liquor, 4g Borneolum Syntheticum (being dissolved in the small amount of ethanol earlier), 0.03g Moschus (being dissolved in the small amount of ethanol earlier) while hot successively, 0.1g bromo geramine (being dissolved in earlier in a small amount of saline), 0.1g povidone iodine (being dissolved in the low amounts of water earlier) stir and promptly get water base emulsifiable paste.This water base emulsifiable paste dilutable water uses as the water preparation washing liquid.

Embodiment 2 (oral liquid formulations)

With bromo geramine, povidone iodine, the Polyethylene Glycol (8000) of embodiment 1, tell wet-80, glycerin/propylene glycol mixed liquor give up need not, get filtrate concentrated solution 100ml, behind disinfection by ultraviolet light, promptly get oral liquid formulations.Can reach the purpose of contraception, induced abortion.

Embodiment 3 (oral exempt to decoct electuary):

Batching is with embodiment 2, and only the part material need not be dissolved into liquid in advance, all grinds to form 300 order smalls with pulverizing mill after drying with solid form, makes the comprehensive cell yardstick of Chinese crude drug sporoderm-broken rate:＞86.5%; Just get delicate mouthfeel, drug effect height, the electuary of exempting to decoct, decoction, full medicine utilization, utilization ratio of drug 100%.Its action function is with embodiment 2.

Of the present invention comparing Yu prior art has following You point:

1, function is many (collects contraception, induced abortion, sterilization sterilization, prevents and treats venereal disease, skin disease and gynaecology The functions such as disease, prolongation sex time, raising sexual intercourse Zhi amount are integrated);

2, drug effect remarkable (contraceptive prevalence rate＞99%, induced abortion success rate 100% is killed sperm rate 100%);

3, formulation is many, and administering mode is flexible, easy to use (water base emulsifiable paste is pollution clothes not, The strong infiltration function of You; Oral granule utilizes micro mist technology drug effect height, utilization ratio of drug 100%; Can Be applied to the positions such as penis, glans penis, wife's side navel, vagina, vaginal orifice, or oral);

4, have no side effect, safe and reliable;

5, stable performance (non-volatile, as can to preserve for a long time more than 2 years);

6, production technology is simple, and is with low cost.

Claims (5)

1, a kind of percutaneous formula (or oral formula) contraception induced abortion bactericidal composition is characterized in that being made up of Radix Notoginseng, Fructus Aurantii Immaturus, Radix Angelicae Sinensis, Fructus Crotonis, Folium Ilicis Cornutae, Chinese small iris seed, Rhizoma Chuanxiong, Sanguis Draxonis, Radix Bupleuri, Radix Polygalae, Radix Rehmanniae Preparata, the Radix Paeoniae Alba, Semen Brassicae Campestris, Flos Carthami, Herba Asari, Herba Eupatorii, Flos Caryophylli, Borneolum Syntheticum, Moschus, bromo geramine, povidone iodine, Polyethylene Glycol (8000), tween 80, glycerin/propylene glycol (1: 1) etc.

2, by the described compositions of claim 1, it is characterized in that respectively forming proportioning and be (weight portion): Radix Notoginseng: 5-12, Fructus Aurantii Immaturus: 5-15, Radix Angelicae Sinensis: 5-15, Fructus Crotonis: 5-10, Folium Ilicis Cornutae: 5-15, Chinese small iris seed: 5-15, Rhizoma Chuanxiong: 5-15, Sanguis Draxonis: 3-6, Radix Bupleuri: 3-8, Radix Polygalae: 3-8, Radix Rehmanniae Preparata: 3-8, the Radix Paeoniae Alba: 3-8, Semen Brassicae Campestris: 3-8, Flos Carthami: 3-8, Herba Asari: 0.5-3, Herba Eupatorii: 1-3, Flos Caryophylli: 0.5-2, Borneolum Syntheticum: 3-6, Moschus 0.01-0.08, new clean that one goes out: 0.05-0.5, povidone iodine: 0.01-0.5, Polyethylene Glycol (8000): 1-3, tween 80: 0.1-0.5, glycerin/propylene glycol (1: 1): 3-10.

3,, it is characterized in that respectively making up optimum ratio and be (weight portion): Radix Notoginseng: 8-12, Fructus Aurantii Immaturus: 8-12 by the described compositions of claim 2, Radix Angelicae Sinensis: 8-12, Fructus Crotonis: 6-8, Folium Ilicis Cornutae: 8-12, Chinese small iris seed: 8-12, Rhizoma Chuanxiong: 8-12, Sanguis Draxonis: 4-5, Radix Bupleuri: 4-6, Radix Polygalae: 4-6, Radix Rehmanniae Preparata: 4-6, the Radix Paeoniae Alba: 4-6, Semen Brassicae Campestris: 4-6, Flos Carthami: 4-6, Herba Asari: 1-2, Herba Eupatorii: 1.5-2, Flos Caryophylli: 1-1.5, Borneolum Syntheticum: 4-5, Moschus: 0.03-0.05, bromo geramine: 0.1-0.4, povidone iodine: 0.1-, 0.4, Polyethylene Glycol (8000); 1.5-2.5, tween 80: 0.8-1.2, glycerin/propylene glycol (1: 1): 5-8.

4, by claim 2 or 3 described compositionss, it is characterized in that water base emulsifiable paste processing technology is with each medicinal herb components drying, grind to form 100-300 order powder, soaked 10-15 days with 10 times of water (or 50%-80 alcoholic solution), filter to get filtrate, filtrate is condensed into 100 parts of solution under 80-90 ℃, under agitation adds all the other each material, stir and promptly get water base emulsifiable paste.

5, by claim 2 or 3 described compositionss, it is characterized in that orally exempting to decoct the electuary processing technology for after drying with herbal raw material, grinding with pulverizing mill is 300-350 order smalls, make the comprehensive cell yardstick of Chinese crude drug sporoderm-broken rate＞86.5%, just must exempt to decoct electuary, decoction, making utilization ratio of drug is 100%.