(57) Abstract:The invention relates to the field of medicine and relates to a vaginal contraceptive. The invention lies in the fact that vaginal contraceptive contains Miramistin and gel - solution of modified cellulose, namely an aqueous solution of hydroxyethyl cellulose. The invention is a highly effective contraceptive, harmless to the body. 1 C.p. f-crystals, 2 tab. The invention relates to medicine and can be used as an individual tool for preventing unwanted pregnancy in any conditions.Known use of vaginal contraceptives with spermicidal action, in the form of gels, ointments, pills, suppositories. In particular, such as the use nonoxynol (register of medicines of Russia, Moscow, RLS-2000, 1999, S. 582), which is a derivative of polyethylene glycol. It is used in the form of vaginal suppositories or gel with a concentration of the drug is 4-5%, which is administered 10 min prior to sexual intercourse. Disadvantages: 1) often causes irritation of the vagina and/or penis, 2) requires use before each sexual act, 3) is unresolved toilet vaginal earlier than h the who solution is used as a spermicide benzalconi chloride, which is a Quaternary ammonium compound. It is used in the form of creams, suppositories, tablets (drugs "Formatex", J. "Remedium", 1998, No. 7, S. 41). The concentration of drug in the dosage form from 2 to 4%. Is introduced for 10 minutes before coitus, action candles and tablets not more than 4 h and 10 h for the cream. The disadvantage of this contraceptive is a great risk of contact dermatitis, infection of the urinary tract, Candida, candidiasis, allergic vaginitis. All this is a consequence of high concentrations of the drug due to insufficiently high spermicidal activity.The aim of the present invention is to provide a vaginal barrier contraceptive high efficiency at low concentrations the beginning of the current, which guarantees the absence of side effects in the form of irritation and vaginitis.This goal is achieved by the fact that as a spermicide used in the preparation Miramistin in the form of a gel or suppositories, when the ratio of components (% by weight):
Miramistin - 0,02 - 1,0
gel candle base 100
Miramistin approved for use as an antiseptic (FS 42-3498-98) in a 0.01% aqueous solution (VFS 42-2048-91) for the prevention of diseases, Icellulse, or methyl cellulose, or sodium carboxymethylcellulose, or polyvinyl alcohol, or polyethylene glycol.As candlestick basics use the standard formula for vaginal suppositories.Experiments in vitro.Spermicidal action Miramistin installed according to the methods recommended by who. To do this, the sperm of a man mixed with different concentrations of the drug or its dosage forms and microscope control their mobility after 15, 30, 45 and 60 C. In these experiments used the sperm of male volunteers aged 18 to 32 years. In table. 1 presents the results of experiments on determination of spermicidal activity through 15 of incubation.As can be seen from the table. 1, the concentration of Miramistin below 0.02% does not guarantee complete immobilization of spermatozoa, and 0.5% leads to complete lysis. Therefore, it is useful to consider the concentration of Miramistin from 0.02% regardless of the composition of the base.With the introduction of the drug into the vagina concentration is reduced by dilution vnutrivlagalischnye secret and ejaculate, and the degree of dilution depends on the injected volume. Therefore, it is necessary concentration Miramistin in contra, the concentration of Miramistin was considered optimal to 1.0%. In the case of the gel, depending on its type and concentrations, from 0.1 to 0.5%.Experiments in vivo.Study of the effect of 0.1% gel Miramistin (GM) on the condition of the vaginal mucosa of rats with long-term introduction of it into the vagina (30 days) did not reveal visual and histological examination of the specimens visible changes, which indicates the absence of irritants study of contraceptive. Not detected changes from other internal organs of the female, including the ovaries, which indicates no violations of oogenesis.It has also been shown that the main component of the GM - Miramistin not found to be embryotoxic action, and does not violate the morphofunctional state of the gonads and the spermatogenic epithelium and mutagenic activity.The contraceptive action of the gel Miramistin studied in female rats, which before mating intrawaginalno have introduced GM, and the control group of animals - gel basis.The obtained data (table. 2) showed that GM was caused by the contraceptive effect is 95.2% females, while the gel-based led to 16.6 percent protection from the ber is l intended clinical experiment on people-volunteers (5 couples). They used 2% of hydroxyethyl cellulose gels with a concentration of Miramistin 0.1% and 0.5% by introducing into the vagina in the amount of 5 ml, 5 min, 10 min, 30 min and 60 min prior to coitus. The experiment lasted for 2 months, the couple have had sex at least 2 times a week. All study participants (men and women) were under medical supervision of a gynecologist and dermatologist.The results of the experiment showed that in any case, the pregnancy has not occurred (100% contraceptive effect). None of the participants expressed no complaints about local irritant action of drugs, deterioration of the General condition of health or any other complaints.Not it was also noted objective changes from female genital organs during a gynecological examination. The pH of the mucus of the vagina, its cellular and microbial composition, indicators of hormonal status (estradiol+progesterone), local immunity (nst-test, phagocytic number, the index of neutrophils and macrophages) in the process of applying GM women did not change.Thus, the proposed GM has high contraceptive properties, it is harmless to the body.
is Izida contains Miramistin and as a gel base solution of modified cellulose in the following ratio of components, wt.%:
Miramistin - 0,02 - 1,0
The solution of modified cellulose 100
2. Vaginal contraceptive under item 1, characterized in that as a modified cellulose contains (1.5 to 3.0)% aqueous solution of hydroxyethyl cellulose.