Vaginal suppository eliciting with contraceptive effect

FIELD: medicine, gynecology, contraceptives, pharmaceutical chemistry.

SUBSTANCE: invention proposes vaginal suppository comprising benzalconium chloride, benzoic acid, purified water and the preparation vitespol taken in the definite content of components. Invention provides the reliable inhibition of fungal microflora being especially against fungus Candida albicans and the absence of irritation and symptoms in vagina drying. Invention can be used as an individual agent for prophylaxis of undesirable pregnancy.

EFFECT: valuable properties of suppository.

5 tbl


The invention relates to the field of pharmaceutical chemistry, namely vaginal contraceptive means, and can be used as a sole means to prevent unwanted pregnancy.

Currently widely used vaginal contraceptives with spermicidal action, including in the form of ointments, creams, gels, tablets, suppositories. For example, it is known contraceptive nonoxynol representing mono- (para-nonyl phenyl) ether of polyethylene glycol and is made in the form of vaginal suppositories or gel. However, this tool often causes irritation of the mucous membranes, and is limited to application in inflammatory diseases of the external genitalia (RLS Russia, encyclopedia of drugs, PM, No. 9, 2002, s).

Known vaginal contraceptive performed in gel form and containing as active substance Miramistin (Patent RU 2173142, 2000).

One of the widely used in gynecological practice effective contraception is benzalkonium chloride. Spermicidal effect of benzalkonium chloride, which is non-hormonal contraceptive, has allowed to create on its basis contraceptives local actions recommended for use in cases where PR is tyopoytani to the use of hormonal contraceptives or intrauterine devices, after termination of pregnancy, during lactation, as well as additional contraception when using a vaginal diaphragm or intrauterine device.

Known for vaginal suppositories, contraceptive action containing benzalkonium chloride, hydroxypropylcellulose solid and semi-synthetic glycerides at a certain content of ingredients - drug FARMATEXA, production Laboratorie Innotech International, France, registration number: candles vaginal No. 0 No. 011489/01 - 1999 (leaf-Vadis attached). Candles can cause side effects in the form of allergic reactions to components of the medication, irritation of the vagina, as well as dryness, due to the presence of hydroxypropylcellulose. In addition, these candles are expensive drug.

The set of essential characteristics specified vaginal suppositories are most similar to the proposed and adopted as a prototype.

The present invention is the creation of a domestic contraceptives local action in the form of vaginal suppositories, devoid of these shortcomings and the same time affordable.

The problem is solved in that the proposed vaginal suppositories with contraceptive effect, containing benzalkonium chloride, benzoic to the slot, the water and the Foundation, as the Foundation they contain witepsol in the following components on 1 suppository weighing 1.5 g, g:

Benzalkonium chloride - 0,015-0,020

Benzoic acid - 0,0009-0,0011

Purified water - 0,015-0,020

Witepsol - rest

The hallmark is that vaginal suppositories additionally contain benzoic acid, water and as a basis contain witepsol.

Benzalkonium chloride bactericidal effect on a whole range of bacteria, but it is less active against pathogenic fungi, in particular Candida albicans, which causes thrush.

Benzoic acid is widely used in pharmaceutical and food industries, including baby food, in dentistry, in the composition for rinsing the oral cavity, in our case it is a pH regulator, inhibits the growth of pathogenic fungi, contributes to better dissolution of the suppository into the vagina.

The basis for suppositories witepsol represents a mono -, di - and tri glycerides and glycerol esters of a mixture of saturated vegetable fatty acids derived from coconut and palm kernel oils. The basis of chemically neutral and does not contain impurities. Witepsol does not cause irritation and phenomena vaginal dryness.

The technical result in the use of the invention is expressed in a reliable suppression of fungal m is croflora, this is especially important in relation to Candida albicans, which causes thrush; benzoic acid, amplifying the effect of benzalkonium chloride on pathogenic fungi, prevents the emergence and growth of fungal microflora, in particular Candida albicans, with regular use of the suppositories, and in the absence of irritation and phenomena vaginal dryness.

Analysis of patent and scientific and technical documentation showed that the proposed vaginal suppositories, contraceptive action is “new” and meet the criterion of “inventive step”.

In accordance with the invention were produced samples of the proposed suppositories, whose formula is presented in table 1.

Declare suppositories obtained as follows. First prepare a solution of benzalkonium chloride. To do this, load the estimated amount of benzalkonium chloride, is heated and at slow stirring enter benzoic acid, and then poured the heated water to withstand the weight until complete dissolution of the components with slow stirring.

Then carry out the preparation of a basis for this in the melter load estimated number of witepsol, where it is melted to obtain a homogeneous mass. Ready based on the heated line is passed into the reactor preparation suppozitornyj masses. In t is rotational reactor to melt witepsol with slow stirring, slowly add a solution of benzalkonium chloride, avoiding foaming.

The manufacture of suppositories perform on machines with the necessary technological modes by the method of pouring. In the preparation of suppositories mass in the reactor is continuously stirred and maintain the required temperature.

Suppositories have a yellowish color, torpedo-shaped form. Average weight suppositories 1.5 g of 5%. Shelf life 3 years.

Studies have been conducted toxicity and specific activity funds. Stated the vehicle was tested for toxicity in accordance with the methodological requirements of the health Ministry (“Guidance on experimental (preclinical) study of new pharmacological substances” M, 2000, p.7-24).

As the comparison drug were taken vaginal suppositories “FARMATEXA” “PHARMATEX” (Laboratory of Inotera, France).

Subacute experiment conducted on rabbits-females with an average body weight of 2.20 0,03 kg Compared the drugs were injected intrawaginalno for two weeks at a dose of 4.0 mg/kg, 4 times greater than therapeutic dose for rabbits.

In the process of testing revealed moderate local irritant effect of the compared drugs on the mucous membranes of the vagina animals, inherent in the benzalkonium chloride, on the background of normal rectal temperature.

The analysis of the experimental results confirmed Alstom about the lack of significant changes of the functional state of the urinary and cardiovascular systems, the cellular composition of peripheral blood and biochemical parameters. Experimentally confirmed bioequivalence steps of the proposed drug and the comparator drug in the studied dose range.

The study of specific pharmacological action.

The experiments were performed on rats population Wistar both sexes, synchronized change of biorhythm (mode day / night), weighing 250-300 g Animals were kept in standard vivarium conditions: 12-hour mode of artificial lighting, water and food ad libitum. The experiments were conducted at the same time, the corresponding night biorhythm animals. In the experiment conducted an examination of specific pharmacological activity of the dosage form claimed vaginal suppositories.

Ingredients: benzalkonium chloride to 18.9 mg, excipients - benzoic acid 1.0 mg, witepsol H 15-1461,2 mg, purified water to 18.9 mg Average weight of suppository vaginal 1.5 g, comparison conducted with vaginal suppositories Pharmatex ("Pharmatex, Inotera, France). Ingredients: benzalkonium chloride to 18.9 mg, excipients - hydroxypropylcellulose, solid, semi-synthetic glycerides in an amount necessary for one vaginal suppository weighing 1.6,

Therapeutic dose in rats was 3 mg/kg of the study drugs were injected intrawaginalno in the molten p and T 38-40° With the state in the volume of 0.06 ml and 0.2 ml, corresponding to the studied doses (3 mg/kg and 10 mg/kg, respectively). Animals of the control group was administered a placebo in the same volumes.

The experiment was conducted on 150 rats females and 15 rats male population Wistar kennel VSC BAS. The synchronized female rats was determined by the natural phases of the estrous cycle using cytological analysis of vaginal smears using light microscope (×100) and formed a group of animals that are in the phase of estrus. Each group was 35-40 animals. Selected animals intrawaginalno was administered the study medication or a placebo (control group). Immediately after injection of the drugs was performed infusion of males to the group of females (1:5) and switching the daytime running lights on twilight. Given the time of action of the drug Pharmatex (4 hours according to the Instructions for use), after 3.5 hours was carried out repeated administration of drugs and placebo in persistent mode lighting. Through the following 3.5 hours males and females territorially disconnected and conducted cytological analysis of vaginal smears. In case of detection of sperm in the number of 3 and above in the field of view of the microscope (×100) coitus was considered valid, and females were otsuzhivalis for further observation. The average of 35-40 itself is to only 7-10 in the vaginal smear was detected spermatozoa. After 10-14 days under ether anesthesia was performed removing the uterus and counting fruits. Pregnancy was considered oligopsony, if the number of fetuses in the uterus was less than the average index in the vivarium of VSC BAS (6). The efficacy was evaluated by its contraceptive (the number of pregnant animals) and spermatotsydnomu action (number oligopsony pregnancies and average number of fruits per animal in each group).

1. Contraceptive action

Pharmacological effect declared funds (vaginal suppositories) was evaluated in comparison with drug Pharmatex and placebo. With intravaginal administration of placebo in the volume of 0.06 ml and 0.2 ml in rats, selected after coitus, it was noted 100% fertilization (table 2). A similar result is obtained when using as the reference drug Pharmatex dose of 3 mg/kg (0.06 ml molten suppository), and declared suppositories, in the same dose and in the same volume. Increasing the dose of the drug Pharmatex to 10 mg/kg (0.2 ml of molten suppository) fertilization occurred only in 75% of cases. When comparing the test substance in the equivalent dose and volume of significant differences from reference drug on the number of fertilized species was not found (table 2).

2. Spermatocide action

The efficiency of ablanovo funds (vaginal suppositories) was evaluated in comparison with drug Pharmatex and placebo. With intravaginal administration of placebo in both volumes (0.06 ml, and 0.2 ml) were registered in the development of multiple pregnancy in 91-85% of cases, respectively (table 3). The number of fruits per 1 animal was 10,2-10,0 (table 2). When using the drug Pharmatex dose of 3 mg/kg (0.06 ml molten suppository) observed the development of oligopsony pregnancy in 14%, while increasing the dose to 10 mg/kg number of individuals oligopsonist reached 57%, which indicates the presence of a certain dozozavisimoe spermatocide effect. The data presented in Table 4.

When comparing spermatocidal activity funds with the reference drug according to this criterion, at a dose of 3 mg/kg (0.06 ml molten suppository) significant differences were observed. With the introduction of the drug in the dose of 10 mg/kg of 0.2 ml of molten suppository) the number of individuals with oligopsony pregnancy was 50% (table 5). When calculating the average number of fruits when using the drug Pharmatex in higher dose (10 mg/kg) showed a statistically significant trend (P<0,1) to decrease to 6.3±1,8 compared with control (placebo) (table 2). When using generic Benzalkonium chloride in the same dose, the average number of fruits was a little higher, but differences in the severity of action compare drugs on this is the indicator of statistical significance were not (table 2).

Thus, the above evidence suggests that the claimed vaginal suppositories have spermatocidal and contraceptive action, not inferior to the severity of drug comparison; at the same time declared suppositories have the price in 2 times lower foreign funds do not cause symptoms of dryness and irritation of the vagina.

Table 1

Table recipe stated suppositories.
IngredientsThe contents of the ingredients on 1 suppository
Benzalkonium chloride0,0150,0170,020
Benzoic acid0,00100,00110,0009
Purified water0,0190,0200,017
The basis for suppositories, witepsolRest

Table 2

Contraceptive and spermatocide effects of drugs Pharmatex and declared suppositories at doses of 3 mg/kg and 10 mg/kg in rats.
Rev.Placebo The farmatexaDeclared spree
Criteria0.06 ml0.2 ml3 mg/kg10 mg/kg3 mg/kg10 mg/kg
% pregnant1001001007810080
Qty fruit10,2±0,710,0±0,79,7±1,16,3±1,811,0±0,67,1±1,6

Table 3

The reproductive capacity of rats in the control group (placebo)
No.The number of fruits%
0.06 ml101113941111101210119
0.2 ml11111210810126- --0
Note: ON - oligopsony pregnancy

Table 4

The influence of the reference drug Pharmatex on the reproductive capacity of rats.
No.The number of fruits%
3 mg/kg101141311910--14
10 mg/kg10313211410057
Note: ON - oligopsony pregnancy

Table 5

The impact of the funds on the reproductive capacity of rats.
No.The number of fruits%
3 mg/kg11119121310----0
10 mg/kg259111315110050
Note: ON - oligopsony pregnancy

Vaginal suppositories with contraceptive effect, containing benzalkonium chloride and a base, characterized in that they additionally contain benzoic acid and water, and as the basis contain witepsol in the following ingredients:

Benzalkonium chloride 0,015-0,020

Benzoic acid 0,0009-0,0011

Purified water 0,015-0,020

Witepsol Else


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