RU2456991C1 - Agent for oestrus control in female cats and dogs - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention relates to veterinary science. The agent contains, wt %: 17^α- Acetoxy -3^β-butanoyloxy-6- methylpregna -4_,6-dien-20-one 0.120, ethinylestradiol 0.001, lactose 62.000, starch 36.379, tropaeolin O 0.5, calcium stearate 1.00.

EFFECT: means is highly effective for oestrus control in female cats and dogs, the use thereof enables lowering a probability of the onset and the intensity of side effects.

2 ex

Description

The invention relates to veterinary medicine and is intended to regulate sexual hunting in cats and bitches.

The proposed tool is intended to relieve excitement in females during sexual hunting, as well as to prevent unwanted pregnancies in females.

The problem of correcting the sexual function of domestic animals, in particular cats and dogs, remains extremely important in veterinary medicine. First of all, it is dictated by the need to eliminate in animals the clinical manifestations of one of the periods (libido) of the stage of the reproductive cycle - vacations in dogs and the stage of estrus in cats, indicating their readiness for mating and causing a lot of trouble to their owners. During this period, animals become aggressive, eat poorly, break into the street, emit piercing screams, often run away from home. False chastity and contact sexual diseases cause a lot of trouble. Two solutions are fundamentally possible to eliminate these problems: a hormonal correction or sterilization with castration. Both methods affect the metabolic processes of the animal organism. However, the advantage of hormonal effects is its reversibility, while castration and sterilization are irreversible, lead to an irreversible loss of reproductive function and exert constant pressure on the metabolic processes of the animal for the rest of its life.

In world veterinary practice, synthetic derivatives of 17α-hydroxyprogesterone, such as its capronate, megestrol acetate, medroxyprogesterone acetate, proligestone, are widely used to regulate the reproductive function of animals (Karpov V.A. Obstetrics and gynecology of small domestic animals. M., 1990 S. 268-270). The disadvantage of using these drugs is the increased dose of these synthetic analogues of hormones during monotherapy.

Also known is a means for regulating the sexual hunting of cats and bitches (RF patent 2295345, 03/20/2007) containing gestagen hormone from a number of pregnan alcohol esters, such as 3β-butyroxy-17α-acetoxy-6-methylpregna-4,6-diene-20 -one or 3β-acetoxy-17α-acetoxy-6-methylpregn-4,6-dien-20-one and estrogen hormone, in particular 17α-ethynyl-estratriene-1,3,5 (10) -diol-3,17β as well as gelatin, glycerin, parahydroxybenzoic acid methyl ester and refined vegetable oil, D, L-α-tocopherol and 3-methyl-6-isopropyl-cyclohexanol, and as the ester of pregnane alcohol it contains um in the following ratio, wt.%:

3β-Butyroxy-17α-acetoxy-6-methylpregna-4,6-dien-20-one or 3β-Acetoxy-17α-acetoxy-6-methylpregn-4,6-dien-20-one 0.5 17α-Ethinyl-estratriene-1,3,5 (10) -diol-3,17β 0.01 Gelatin 14.0 Glycerol 5,0 Parahydroxybenzoic acid methyl ester 0.1 D, L-α-tocopherol 0.005 3-methyl-6-isopropyl-cyclohexanol 0.01 Refined vegetable oil up to 100.0

The main disadvantage of the claimed funds is the indiscriminate nature of its action. The product is intended for complex effects on both bitches and dogs, therefore its concentration in the composition of the product is overrated. Overestimation of concentration is a necessary measure necessary for the possibility of exposure to males or cats as less sensitive to these hormones. However, an increase in concentration leads to side effects that occur in cats or dogs in response to the introduction of an increased dose of sex hormones.

In addition, the preparative form of the known funds are drops, which limits the scope of its application.

We made an attempt to develop a specialized tool for cats and dogs, taking into account their gender characteristics. In particular, a tablet form of an agent for regulating the sexual hunting of cats and bitches was developed containing 17α-acetoxy-3β-butanoyloxy-6-methylpregn-4,6-dien-20-one and ethinyl estradiol, while the agent additionally contains milk sugar, potato starch , tropeolin O, calcium stearic acid in the following recommended ratio of components, wt.%:

17α-Acetoxy-3β-butanoyloxy-6-methylpregna-4,6-dien-20-one 0,120 Ethinyl estradiol 0.001 Milk sugar 62,000 Potato starch 36,379 Tropeolin O 0.5 Calcium stearic acid 1.00

The technical result of the invention is the specificity of the action, a decrease in the concentration of active substances in the preparation, which eliminates the possibility of an overdose of the drug and, as a result, reduces the likelihood of occurrence and severity of side effects.

The distinguishing feature of this invention (namely, the dose and ratio of components) is found empirically.

The following are examples of the preparation of the proposed tool and an example of testing the proposed tool.

Example 1. Preparation of the drug in the form of tablets

Raw material preparation

Auxiliary raw materials (milk sugar, starch, calcium stearate) were sieved through a No. 32 sieve. Then, to increase the degree of solubility of the drug and the absorption area, micronization of the active substances was carried out: 17α-acetoxy-3β-butanoyloxy-6-methylpregn-4,6-dien-20-one and ethinyl estradiol (17α-ethynyl estratriene-1,3,5 (10) -diol-3.17β).

Preparation of starch paste

The components of the paste were taken in the following proportions: purified water 0.5 kg; starch 0.27 kg; hot water (90-95) ° C 5.6 kg. The components were mixed and the starch paste was stained by adding 2.5 g of tropeolin O dissolved in 0.05 kg of purified water to the paste.

Cooking trituration

Lactose 0.5 kg;

Ethinyl estradiol 0.208 g;

17α-Acetoxy-3β-butanoyloxy-6-methylpregna-4,6-dien-20-one 21.41 g;

Rubbing and mixing the powder for up to 20 min.

Loading in a granulator dryer is carried out in layers:

Lactose 6.0 kg;

Starch 3.7 kg;

Trituration mixture 0.54 kg;

Lactose 6.0 kg.

Dry mixing is carried out for 10 minutes, then starch paste is sprayed and wet granulated.

Drying at a temperature of 40-50 ° C to a residual moisture content of 1.6-2.2%.

Dry granulation includes dusting with calcium stearate - 0.145 g. Then tableting is carried out.

Example 2. The study of the action of the drug on dogs (bitches) and cats

Observations were performed on 40 cats and 25 females, both in vivarium and at home. Experiments took animals that have reached puberty. In cats, sexual hunting was manifested by piercing screams, rolling on the floor, bending the back. Cats were taken into experience when they showed manifestation of proestrus, lasting 1-2 days, swelling of the vulva, changes in behavior, frequent urination. Cats from the moment of proestrus for 1-2 days were given in isolation or with food the drug at a dose of 0.12 mg progestogen (1 tablet). Against the background of the administration of the test drug, instead of manifesting sexual hunting in most cats (92%), a stage of relatively calm behavior (diestrus) occurred. There were cases when the state of rest came after the appointment of the first pill. Observations made on 40 cats (females) showed that the duration of sexual dormancy after taking the pill was on average from 2.5 weeks to 1.5 months. Cats were well tolerated.

Observations of bitches demonstrated the need to use 1 tablet per day for every 5 kg of body weight of the claimed agent to obtain an inhibitory effect on sexual arousal. To achieve the effect, 1 tablet was administered orally for every 5 kg of body weight daily for 3-5 days. All 25 dogs had an inhibitory effect that lasted for 20-30 days

Observations of animals for several months after completing the course of taking the claimed drug showed that side effects that could be associated with taking the drugs were not detected. The reproductive function of animals was fully restored after 2-3 months after cessation of treatment.

Claims (1)

A means for regulating the sexual hunting of cats and bitches containing 17α-acetoxy-3β-butanoyloxy-6-methylpregna-4,6-dien-20-one and ethinyl estradiol, characterized in that the product further comprises milk sugar, starch, tropeolin O, calcium stearic acid in the following ratio of components, wt.%:
17α-Acetoxy-3β-butanoyloxy-6-methylpregna- 4,6-dien-20-one 0,120 Ethinyl estradiol 0.001 Milk sugar 62,000 Starch 36,379 Tropeolin O 0.5 Calcium stearic acid 1.00