RU2270684C1 - Medicinal preparation "vitasorb" - Google Patents

Abstract

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to a medicinal preparation used in treatment of viral diseases and prophylaxis of infectious epizootic processes. The preparation comprises an active substance prepared on the base of antimony and represents a finely crystalline sorbent consisting of structural links of the formula:

and having particles size (1 x 10^-5)-(9 x 10^-5)μm and used in the dose 100-120 mg/kg. The preparation represents suspension for intramuscular or intravenous administration or it can be included into capsules for oral intake. The prepared preparation possesses higher antiviral activity and broader spectrum of antiviral effect.

EFFECT: improved and valuable medicinal properties of preparation.

3 cl, 8 tbl, 5 ex

Description

The invention relates to medicine and can be used in veterinary medicine for the treatment and prevention of viral diseases.

The invention is known: a method for producing porous inorganic sorbents, which includes antimony compounds with a solution of monosubstituted sodium phosphate and sodium metasilicate with gel precipitation (SU 1156728 A, 1985). This sorbent is not suitable for the treatment of viral diseases.

The closest adopted for the prototype is an injection drug with antiviral properties, which is a copolymer of trivalent antimony Sb (III) and sodium tungstate, and the number of antimony atoms refers to the number of tungsten atoms as 2.5: 1 (UK patent GB 1487397, 1977). This drug, although it has antiviral activity, however, its use for the treatment of viral diseases widespread in veterinary practice, such as rabbit Aujeszky's disease, neonatal calf diarrhea (cattle rotavirus infection) and Newcastle bird disease, is not effective. In addition, a well-known drug cannot provide the removal of toxic viral products.

The objective of the invention is the expansion of the arsenal of drugs, in particular the creation of a drug for the treatment of viral diseases and the prevention of infectious epizootic processes.

The problem is solved using the proposed composition of the drug "Vitasorb", including the active substance based on antimony compounds, characterized in that it is a fine crystalline sorbent consisting of structural units of the formula obtained by the joint polycondensation of the products of the hydrolysis of antimony trioxide and sodium silicate

having a particle size of 1 × 10 ^-5 -9 × 10 ^-5 μm, in the form of a dose of 100-200 mg / kg The preparation contains antimony Sb 47-55%, bound by silicon oxide, which is an auxiliary substance; the silicon content of Si is 4-4.7%. Excipients Na, SiO ₂ , H ₂ O bonded to the polymer with SbO ₃ . The pure product may contain: sodium nitrate - less than 0.1%, sodium phosphate - traces, antimony trioxide SbO ₃ - traces, antimony pentoxide Sb ₂ O ₅ - traces, hydrogen ions.

The active substance is a white, finely dispersed crystalline powder, odorless and tasteless, containing particles 1 × 10 ^-5 -9 × 10 ^-5 microns in size. It is practically insoluble in water, in 95% alcohol, ether, benzene, acetone. With bidistilled water forms a milky white suspension. The sorbent is obtained, for example, by the method described in patent RU 2143315, 1999. The raw materials used for the manufacture of the sorbent are antimony trioxide Sb ₂ O ₃ according to GOST 14992 and GOST 1807, sodium metasilicate according to TU-2621-011-00207787-2003 and sodium phosphate GOST 245-76.

In terms of quality, the drug must meet the requirements and standards specified in the table of TU No. 9325-001-740393117-04:

N p / p Name of indicator Characteristic and norm Test method one Appearance, color Light, white, fine powder, odorless; white color. When mixed with water, forms a suspension - a milky suspension 4.1, 4.2 2 PH determination 4.3.2 3 Definition of authenticity 4.4 four Solubility in: - water Practically insoluble - alcohol 95% Also - on air Also - benzene Also - acetone Also - in sulfuric and nitric acids Soluble 5 Heavy metals,% no more 0.0001% in G.F. p.748 4.6 6 Iron,% no more 0.003% in G.F. p.748 4.7 7 Arsenic 0.001 in the preparation G.F. p.748 4.8 8 Sorption activity 4.11 9 Antimony,% no more 47.0-55% in the preparation 4.9 10 Microbiological purity Must pass the test 1.4.1 eleven Toxicity Non toxic 2.2 12 Sterility Sterile 4.12 13 Pyrogenicity Not pyrogenic 4.14

The finished antiviral preparation is obtained by grinding the sorbent to a particle size of 1 × 10 ^-5 -9 -10 × 10 ^-3 microns.

The technical result of the invention is to expand the spectrum of antiviral action and increase the effectiveness of the drug.

The mechanism of the antiviral effect of the Vitasorb drug is that, being a highly effective sorbent, it inhibits the infectious activity of pathogens by blocking the initial stages of virus replication in target cells, neutralizes thermostable and thermolabile toxins of a protein nature, has a high adsorption rate and using pro-infectious properties, it provides fast binding and excretion of endo- and exotoxins, as well as products of incomplete protein breakdown.

The preparation may additionally contain water as a carrier and be a suspension or capsule filled with a suspension.

Pharmacological properties.

"Vitasorb" is not toxic, does not have cumulative properties, does not have embryotoxic, teratogenic and mutagenic effects. The drug is administered orally, intramuscularly and intravenously in doses of 100-200 mg / kg for therapeutic and prophylactic purposes in case of viral infections of animals.

Vitasorb, being an ion-exchange agent, has a unique effect on a viral infection in the body, with its bioavailability and ultra-small particle sizes, the average particle size of 1 × 10 ^-5 -9 -10 × 10 ^-5 microns penetrates all organs and tissues of the body. The Vitasorb surface is easily accessible to sorbed molecules of any size. It has excellent hydrophilicity, is well wetted by water, forming a suspension with it, and has a high sorption ability. With intravenous administration, the highest concentration in the blood occurs after 1 hour and lasts up to 72 hours, with oral administration after 72 hours. Vitasorb has well-balanced osmotic and hydrophilic characteristics, and therefore its virucidal effect is also manifested. It is excreted through the kidneys, liver and intestines. The Vitasorb surface is easily accessible to sorbed molecules of any size.

The drug does not have a pyrogenic reaction, does not reduce immunity, is very effective in combination with the methods of administration - oral and intravenous. It has high activity even at the peak of the above diseases in a therapeutic dose. "Vitasorb" can be perfectly used for preventive purposes in a number of infectious diseases.

"Vitasorb" - a unique drug, is indicated for the treatment of animals infected with protozoa, has an antiviral, antibacterial effect. It can be used for the prevention and treatment of animal viral infections: rabies, Aujeszky's disease of rabbits, rotavirus infection of cattle, Newcastle disease of birds, viral hepatitis of ducklings, leukemia, etc.

Studies of the drug "Vitasorb" were carried out at the All-Russian Research Institute of Animal Protection (FSI ARRIAH) and at the Research Institute of Virology named after D.I. Ivanovo RAMS.

Example 1

Rabies is an acute disease of warm-blooded animals, characterized by damage to the central nervous system. Domestic and wild animals of all species, as well as humans, are susceptible to it.

Rabies is easily reproduced on white mice. With intracerebral (intracerebral) infection, mice develop encephalitis. The diagnosis of rabies is made on the basis of epizootological data, symptoms of the disease and the results of laboratory tests, including a bioassay on white mice.

According to the data obtained, the use of the drug "Vitasorb" for the prevention of the disease was effective. With the complex administration of the drug - intravenous and intramuscular in the amount of 250 and 50 mg / kg of weight, respectively - during the period of manifestation of the clinical signs of the disease, good results were obtained - Table 1.

The death of mice with this method of administration was reduced to 10%, while the remaining animals observed the elimination of clinical signs of the disease.

Example No. 2.

Aujeszky’s disease - pseudorabies, infectious bulbar paralysis, itchy plague, rabies scabies - an acute disease of farm animals of all kinds, fur animals and rodents. It is characterized by signs of brain damage, severe itching and scratching (in all animals except pigs).

According to the data presented in table No. 2, the complex use of the drug "Vitasorb" - orally and intramuscularly - for the prevention or with the manifestation of clinical signs of the disease prevents the multiplication of the virus in the body of experimental animals, as evidenced by the results of diagnostic studies.

Example 3

Rotavirus infection in cattle (diarrhea of neonatal calves) is an acute contagious disease of newborn calves, characterized by damage to the gastrointestinal tract. The disease is widespread in all geographical regions of the globe. In practice, it was recorded everywhere where research was conducted.

Tests of the Vitasorb preparation for rotavirus infection of cattle were carried out in June 2003 in the SEC Opole, Yuryev-Podolsky District, Vladimir Region. Infection is clinically manifested only in calves in the form of recurrent diarrhea. The incidence reaches 90%, mortality - 20-50%. Most often, the disease is recorded in late winter and early spring. Calves become infected in the first hours after birth. The causative agent of rotavirus cattle infection belongs to the family Reoviridae, the genus Rotavirus. Rotavirus virions are spherical particles with a diameter of 65-75 nm, consisting of a core, inner and outer capsid.

Intramuscular administration of the drug Vitasorb "in the amount of 10 mg per kg of live weight and oral administration in the amount of 40 mg per kg protected the calves from death and no virus was detected in fecal samples after the use of the drug. The results are presented in table 3.

To protect the Lena calf with a higher concentration of rotavirus in feces (1:40 in ELISA), 40 mg of Vitasorb oral administration was not enough.

Example 4

The test of the Vitasorb preparation for cattle leukemia was conducted on the territory of the SEC of the Starodvorsky breeding farm in the Suzdal district of the Vladimir region.

To carry out the work on September 30, 2004, blood was taken from 30 heifers of 4-6 months of age and from 10 cows 3-5 years old for hematological studies and immunodiffusion reaction (RID). The following results were obtained (see tables), in 11 animals specific antibodies to cattle leukemia virus were detected in blood serum. Three heifers have neutrophilia with a left shift of the nucleus. Cows with inv. No. 1523, 49, 40, 84 according to the results of serological and hematological studies are patients with cattle leukemia.

11/09/04, before the introduction of the drug "Vitasorb" in patients with leukemia and suspicious animals was re-selected blood.

The research results are presented in tables 4, 5 and 6.

The first injection of the drug was carried out 09.11.04, Telochki with inv. No. 6271, 7245, 8449, 8483 (average weight 100 kg), 10 cm ^{3 of a} 12% suspension of Vitasorb were administered intravenously; 15 cm ^{3 of a} 12% suspension were intravenously administered to cows with inventory numbers 1523, 49, 40, 1789, 482, 1664 (average weight 200-300 kg).

The second time the drug was administered on 10.11.04, combining intravenous and oral methods: heifers of 10 and 15 cm ³ "Vitasorba"; cows 15 and 30 cm ^{3 of the} drug, respectively.

The amount of the drug administered per 1 calf was 4.2 g (on average 42 mg / kg body weight), per 1 cow - 7.2 g (average 24-36 mg / kg body weight).

11.11.04, the selection of blood, the results in tables 4 and 6;

November 18, 04 - blood sampling, the results in tables 4 and 6;

November 24, 04 - blood sampling, the results in tables 4 and 5.

Example 5

The study of the toxicity of the drug "Vitasorb" was carried out taking into account the "Guidelines for determining the toxic properties of the drug used in veterinary medicine and animal husbandry", set out in the reference book "Veterinary preparations" edited by A.D. Tretyakov, 1988, as well as the requirements set forth in State Pharmacopoeia, XI ed. (1987).

The study of acute toxicity of the drug "Vitasorb" was carried out on 2-2.5-month-old white mice weighing 18-22 g; 3-4 month old guinea pigs weighing 450-500 g; 4-month-old rabbits weighing 2000-3000, the results are presented in table 7.

In addition to laboratory animals, 30-day-old chickens, 10-day-old ducklings, as well as newborns and 2-6-month-old calves, 3-5-year-old cows were used to study the toxicity of the Vitasorb preparation (“Vitasorb” therapeutic efficacy report for treatment of viral infections of animals ", acts from farms to test the drug" Vitasorb "). For oral administration, the Vitasorb preparation was used, packaged in 500 mg capsules (before administration, the powder was diluted in 4 cm ^{3 of} water). For intravenous and intramuscular administration, a drug was packaged in ampoules in the form of a suspension with a concentration of 120 mg / cm ³ . The results are presented in table 8.

Claims (3)

1. A drug for the treatment of viral diseases and the prevention of infectious epizootic processes, including an active substance based on antimony compounds, characterized in that it is a fine crystalline sorbent consisting of structural units of the formula obtained by the joint polycondensation of the products of the hydrolysis of antimony trioxide and sodium silicate

having a particle size of 1 × 10 ^-5 ÷ 9 × 10 ^-5 , in the form of a dose of 100-200 mg / kg 2. The drug according to claim 1, characterized in that it is a suspension based on bidistilled water for intravenous or intramuscular administration. 3. The drug according to claim 1, characterized in that it is made in the form of a capsule.