RU2124895C1 - "avermectin" antiparasitic ointment - Google Patents

Abstract

FIELD: veterinary science, pharmacology, medicine. SUBSTANCE: antiparasitic ointment has ivermectin or abamectin, or aversectin, or rustomectin as an avermectin complex and polyethylene glycol-400, polyethylene glycol-1500 and glycerol as an ointment base and methyluracil and dimethylsulfoxide also taken at the definite ratio of components. Proposed ointment provides recovery by 2-5 days earl as compared with the known analogs and it can be used for treatment of human and animals with parasitic diseases caused by ticks, nematodes, insects. EFFECT: enhanced curative effectiveness of composition proposed.

Description

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

 Known agent for the treatment and prevention of parasitic diseases of warm-blooded, including avermectin complex and a carrier. (1).

 Avermectins are known for the treatment and prevention of animal helminthiasis (2). The closest in technical essence to the claimed invention is an aversectin ointment, including an avermectin complex from Streptomyces avermitilis VNIISKHM-54 and ointment base (3). However, it slowly penetrates deeply lying tissues, has low anti-inflammatory activity, and is not very effective in demodicosis.

 The objective of the present invention is to provide an ointment with high antiparasitic, penetrating and anti-inflammatory activity, as well as expanding the spectrum of action of the ointment.

The solution to this problem is achieved by introducing ivermectin, abamectin, aversectin or rustomectin into the ointment as an ointment complex, polyethylene glycol-400, polyethylene glycol-1500 and glycerol as an ointment base, and methyluracil as a stimulator and regeneration accelerator, as well as an antimicrobial anti-inflammatory drugs - dimethyl sulfoxide, in the following ratio of components, wt.%:
avermectin complex - 0.05 - 0.2
methyluracil - 5.0 - 10.0
dimethyl sulfoxide - 5.0 -10.0
glycerin - 18.0 - 25.0
polyethylene glycol-1500 - 18.0 - 25.0
polyethylene glycol-400 - the rest
Avermectins are antiparasitic agents with exceptionally high biological activity. Obtained by fermentation of the mycelium of soil actinomycete Streptomyces avermitilis. The avermectin complex contains four closely related main components in various proportions and four minor components, each of which is a lower homologue of the corresponding main component (2). In the proposed avermectin ointment, the known avermectin complexes were used: ivermectin (4), abamectin (4), aversectin (3), rustomectin (5).

 Methyluracil-2,4-dioxi-6-methyl-1,2,3,4-tetrahydropyrimidine or 4-methyluracil. It accelerates the processes of cell reproduction and growth in various tissues and organs with resorptive and local action. The resorptive effect is manifested mainly in the stimulation of leukopoiesis (6).

Dimethyl sulfoxide (dimexide) - a colorless transparent liquid or colorless crystals, melting at a temperature of 18.5 ^o C with a specific smell. Hygroscopic. It has the ability to penetrate through biological membranes, including through skin barriers. It has analgesic and anti-inflammatory, as well as moderate antiseptic and fibrinolytic effects. It also enhances the penetration of a number of medicinal substances through the skin (7).

 Glycerin is a trihydric alcohol, a syrupy, colorless, viscous, odorless, sweet taste liquid that is widely used in the food and pharmaceutical industries, as well as in the manufacture of perfumes and cosmetics (8).

Polyethylene glycols are widely known as good solvents. (nine). The ointment is obtained by heating polyethylene glycol-1500 in glycerol at 60 - 70 ^o C and stirring to a homogeneous mass, followed by the addition of methyluracil, dimethyl sulfoxide and polyethylene glycol-400, stirring at the same temperature for 10 - 12 minutes and adding 0.05 - 0.2 wt.% avermectin complex.

 The invention is illustrated by the following examples.

 Example 1

 Table 1 shows the formulations of 1 to 4 avermectin ointments using different avermectin complexes as an active substance.

 The therapeutic effectiveness of the ointment is maintained in the intervals of values that are part of the components given on p. 1 descriptions. The following are specific examples of the use of aversectin ointment for the treatment of various parasitic diseases.

 Example 2. The therapeutic effect of 0.1% avermectin ointment for rabbit psoroptosis.

 Of the rabbits with ear scabies (psoroptosis), 6 experimental groups are formed, each of which has 3 heads. The damaged surface of the auricles of animal experimental groups is treated with an avermectin ointment made on the basis of ivermectin (group 1); abamectin (2nd group); aversectin (3rd group); rustomectin (4th group). Animals of the 5th group are treated with aversectin ointment - treated control. The rabbits of the 6th group are put on the damaged surface of the auricles of the placebo - ointment base - (untreated control). The results are shown in table 2.

 Example 3. The therapeutic efficacy of 0.2% avermectin ointment for dog demodicosis.

 Of the dogs sick with a mixed form of demodicosis, 6 experimental groups of animals were formed, 2 heads each. The damaged surface of the skin of animals of the first four groups was treated with ointment prepared analogously to example 1, but the avermectin complexes were taken at a rate of 0.2%. Dogs of the 5th group were treated with aversectin ointment (treated control). Animals of the 6th group were applied ointment base (untreated control). The ointment was applied 3-5 times with an interval of 5 days.

 The results are shown in table 3.

 Example 4. Therapeutic efficacy of 0.05% avermectin ointment for sheep wolfarthiosis.

 Of the sheep affected by wolfarthiosis, 6 experimental groups of 3 heads each were formed. The animals of the first 4 groups were treated with avermectin ointment prepared according to example 1 on the basis of ivermectin (group 1), abamectin (group 2), aversectin (group 3), rustomectin (group 4). Sheep of the fifth group was treated with 0.05% aversectin ointment. Animals of the 6th group were given a placebo (ointment base).

 The results are shown in table 4.

 Example 5. Therapeutic efficacy of 0.05% avermectin ointment for human demodicosis.

 Of the 10 demodecotic patients under observation, 8 people were treated with 0.05% prepared on the basis of avermectin complexes (formulations 1-4) with avermectin ointment, and 2 patients were treated with 0.05% aversectin ointment.

 The results are shown in table 5.

 Thus, the therapeutic effectiveness of the avermectin ointment of the proposed composition is higher compared to the known aversectin ointment and provides healing 2-5 days earlier.

 The combination of these components in the proposed ratio provides high therapeutic and prophylactic effectiveness of avermectin ointment due to good penetration into deeply lying tissues, high anti-inflammatory activity, as well as due to the synergistic effect of the components, which is expressed in an increase in the antiparasitic activity of the ointment and the expansion of its spectrum of action in comparison with the famous aversectin ointment.

Literature
1. RF patent N 2054848, 1996.

 2. Demidov IV Century Anthelmintics in veterinary medicine. - M., "Kolos", 1982, p. 349-350.

 3. Novik T. S., Golovkina L. P. In the book. "Questions of physical and chemical biology in veterinary medicine." - Sat scientific Trud Mosk. Gos. Academy of Veterinary Medicine and Biotechnology. K.I. Scriabin, 1997, p. 90-98.

 4. William C. Campbell. Ivermektin and abamectin., New York, Berlin, Heidelberg, London, Paris, Tokyo, 1989, p. 114-124.

 5. Manual on the use of rustomectin in veterinary medicine. - Approved. Veterinary Department of the Ministry of Agriculture of Russia 11/27/96. - M., Ministry of Agriculture and Food of Russia, 1996, p. 1-4.

 6. Mashkovsky M.D. Medicines T.1. - M., Medicine, 1984, p. 220.

 7. Mashkovsky M.D. Medicines T.1. - M., Medicine, 1984, p. 202-203.

 8. Brief chemical encyclopedia. T.5. - M., S.E., 1961, p. 972-973.

 9. Brief chemical encyclopedia. T.5 - M., S.E., 1961, p. 964.

Claims (1)

Antiparasitic ointment, including an avermectin complex and an ointment base, characterized in that it contains ivermectin, or abamectin, or rustomectin, or aversectin as an avermectin complex, and glycerin, polyethylene glycol-400 and polyethylene glycol-1500 as an ointment base, and additionally as regeneration stimulator - methyluracil, and as an antimicrobial and anti-inflammatory agent - dimethyl sulfoxide in the following ratio of components, wt.%:
Ivermectin, or Abamectin, or Rustomectin, or Aversectin - 0.05 - 0.2
Methyluracil - 5.0 - 10.0
Dimethyl sulfoxide - 5.0 - 10.0
Glycerin - 18.0 - 25.0
Polyethylene glycol-1500 - 18.0 - 25.0
Polyethylene Glycol-400 - The Rest

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