RU2146147C1 - Antiparasitic preparation of prolonged action - Google Patents

Abstract

FIELD: medicine, veterinary science, pharmacology. SUBSTANCE: invention relates to preparation used as an agent for treatment of human and animals with parasitic sicknesses caused by nematodes, mites and insects. Preparation has abamectin or ivermectin, or avertin N, or aversectin, or doramectin as the avermectin complex, cellulose derivatives as prolongator-carrier for transport of the active component to intestine compartment, methyluracil as the immunostimulating agent and lactose as the filling agent taken at the definite ratio of components. EFFECT: enhanced curative effectiveness of avermectins in capsules as compared with treatment with known analogues. 3 cl, 5 tbl, 5 ex

Description

 The invention relates to veterinary medicine, pharmacology, medicine and is intended for use as a means for the treatment of parasitic diseases of humans and animals caused by nematodes, ticks and insects.

 A means is known for the treatment and prophylaxis of warm-blooded parasitic diseases, including an avermectin complex and a carrier (1, 2).

 Avermectins are known for the treatment and prevention of animals (3, 4). The closest in technical essence to the claimed invention is an ointment comprising an aversectin complex from Streptomyces avermitilis and an immunostimulant (2). However, the ointment in this form acts for a short time, does not affect endoparasites and it must be used twice (2).

 The objective of the present invention is to provide a dosage form based on avermectins with high antiparasitic and anti-inflammatory prolonged activity, increasing the body's resistance, expanding the spectrum of action of the drug.

The solution to this problem is achieved by the composition as an avermectin complex Avertin N, abamectin, ivermectin, aversectin, doramectin; as an immunostimulant, methyluracil; cellulose derivatives as a prolongator; as a filler - lactose in the following ratio of components, wt.%:
avermectin complex - 0.1-0.3
methyluracil - 2.0 - 5.0
cellulose derivatives - 15.0 - 30.0
lactose - the rest
Avermectins are antiparasitic agents with an exceptionally high biological activity in a homeopathic dose. Obtained by fermentation of the mycelium of soil actinomycete Streptomyces avermitilis. The avermectin complex contains 4 main closely related components in various proportions and 4 minor components, each of which is a lower homologue of the corresponding main component (4). Famous avermectin complexes were used in the proposed preparation: abamectin (4), avertin N (6), ivermectin (4), aversectin (1), doramectin (7).

 Methyluracil - 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine or metacyl. It stimulates cellular and humoral defense factors, has an anti-inflammatory effect, and does not have a local irritant effect (8).

 Cellulose derivatives - cellulose acetate, methyl cellulose, ethyl cellulose, cellulose acetate phthalate, microcrystalline cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose and others are prolongation carriers (9).

 Lactose is a carbohydrate from the saccharide group, contains galactose and glucose, affects the growth of the body, promotes the absorption of calcium salts in the intestine, and increases osteogenesis (10).

 The drug is obtained by mixing and micronizing all components at room temperature for 1.5-2 hours.

 The invention is illustrated by the following examples.

 Example 1

 Table 1 shows the formulations of 1-5 avermectin powder using different avermectin complexes as an active substance.

 The therapeutic effectiveness of avertin capsules is maintained in the ranges of values included in the components given in the description on page 1.

 The following are specific examples of the use of avertin in capsules for the treatment of various parasitic diseases.

 Example 2. The therapeutic effect of avertin in capsules with nematodoses of dogs.

 Seven experimental groups were formed from dogs that isolated toxocar, toxascaride, and hookworm according to coproscopy data, and capsules made on the basis of avertin N (group 1), ivermectin (group 2), abamectin (group 3), aversectin (4) were injected once through the mouth. group), doramectin (group 5) at the rate of 0.2 mg / kg according to the animal’s DV Dogs of the 6th group received decaris tablets (levamisole), and the 7th group received placebo (untreated control). The results are shown in table 2.

 The results show that preparations based on avermectin-based prophylaxis prevent infection by nematodes for 3 months at 100%, and then the animals begin to become infected, but not significantly. Dekaris has shown weaker effectiveness and does not have a prolonged effect.

 Example 3. The therapeutic efficacy of avertin capsules for otodectosis of dogs.

 Of the patients with scabies, dogs formed 7 groups of 2 heads each. The dogs of each group were injected through the mouth once, respectively, capsules with avertin (1), ivermectin (2), abamectin (3), aversectin (4), doramectin (5), at a dose of 0.2 mg / kg DV. Animals of the 6th group were used twice with an interval of 7 days, aversectin ointment, and the 7th - placebo. The results are shown in table 3. They show a 100% effect of all therapeutic agents.

 Example 4. Therapeutic efficacy of avertin capsules in ascariasis in humans.

 Of 12 patients with ascariasis, 10 people received single capsules prepared on the basis of avermectin complexes (formulations 1-5), and 2 patients received decaris tablets once.

 The results shown in table 4 show that the recommended forms showed a 100% effect, and decaris gave only a 50% effect.

 Example 5. Therapeutic efficacy of avertin capsules in horses oxyurosis.

 Of the 21 foals infected with oxyuras, 7 equal groups were formed. The animals of the first five groups were given capsules with avertin once through the mouth (formulations 1-5), the sixth - decaris tablets, the seventh preparation was not assigned (control). The results are presented in table 5, from which it is seen that the avermectin-based preparations 100% freed the foals from oxiur and prevented new infection within 3 months; decaris freed foals by 66.6% of oxiur and did not show a preventive effect.

 Thus, the therapeutic efficacy of capsules based on avermectins is higher in comparison with the well-known decaris drug widely used both in medicine and veterinary medicine for nematodoses, and is equal to an aversectin ointment for otodectosis. The clinical condition of all patients was good, and decaris caused depression and salivation in some animals.

 The combination of these components in the proposed ratio provides high efficiency capsules based on avermectins due to the high biological effectiveness of the drug in a homeopathic dose; high anti-inflammatory effectiveness; prolonged action. Due to the manifestation of the synergistic interaction of the components, which is expressed in increasing antiparasitic activity, expanding the spectrum of action and decreasing the frequency of administration of drugs compared to existing drugs, a beneficial effect on the host organism occurs.

Claims (2)

1. An antiparasitic preparation of prolonged action, containing an avermectin complex and methyluracil, characterized in that it further contains derivatives of cellulose and lactose in the following ratio of components, wt.%:
Avermectin complex - 0.1 - 0.3
Methyluracil - 2.0 - 5.0
Cellulose derivatives - 15.0 - 30.0
Lactose - Rest
2. The antiparasitic preparation according to claim 1, characterized in that, as an avermectin complex, it contains either Avertin N, or Aversectin C, or Ivermectin, or Doramectin.  3. The antiparasitic preparation according to claim 1, characterized in that the cellulose derivatives contain either cellulose acetate or methyl cellulose or ethyl cellulose or cellulose acetate phthalate or single crystal cellulose or hydroxypropyl methyl cellulose or hydroxyethyl cellulose and the like.

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