RU2089197C1 - Preparation exhibiting the prolonged effect and a method of its preparing - Google Patents

Abstract

FIELD: veterinary science. SUBSTANCE: preparation has the following components, wt.-%: preparation ASD F-2 or ASD F-3 10-12; polyethylene oxide 30-50; 1,2-propanediol 5-15; novocaine or other anesthetic agent 1-3, and dimexide up to 100. Method of preparing involves components dissolving in hot dimexide. EFFECT: improved method of preparing, enhanced effectiveness of the preparation. 3 cl, 4 tbl

Description

 The invention relates to veterinary medicine and can be used to treat animal diseases.

 Characterization of analogues of the invention.

 Tissue preparations have gained recognition in our country and are used in animal husbandry as growth stimulants, and in veterinary medicine as therapeutic agents.

 The theoretical foundations of tissue therapy were laid by M.P. Tushnov (Tushnov histolysates). The products of the splitting of tissues of various organs with parenteral administration can stimulate the activity of homologous tissues, correct metabolic disorders and eliminate pathology.

 Tissue therapy was further developed in the works of V.P. Filatov (biogenic stimulants of Filatov). In surviving tissues, specific active substances accumulate, produced by living cells, which, acting on the body as a whole, mobilizing its natural defenses and stimulating physiological and immunobiological reactions, exhibit a therapeutic effect. Biogenic stimulants, changing the activity of enzyme systems, exhibit a therapeutic effect, increasing the level of metabolic processes and resistance to various pathogenic effects.

 Along with the mentioned preparations, stilbestrol, citrate blood, the SB drug (N.G. Belenky's serum), as well as the preparations of the All-Russian Research Institute of the Meat Industry VNIIMP-2-I, VNIIMP-3, VNIIMP- were used as biostimulants of farm animals along with the mentioned drugs 4, "KGL".

 The closest in technical essence to the claimed proposal is the drug ASD.

 Among the means of tissue therapy, a special place is taken by the drug ASD (antiseptic stimulator A.V. Dorogov), proposed in 1948. It is a powerful stimulator of the vital functions of the body with internal and parenteral use, and with local, in addition, it also has an antiseptic effect. The therapeutic effect of the drug ASD has been established in a number of diseases of farm animals; it is also used in medicine (see Sources of information N 1-30).

 The drug is available in two fractions called ASD F-2 and ASD F-3. ASD F-2 volatile liquid from yellow to dark red in color, a peculiar (unpleasant) odor, soluble in water, used externally and internally. The drug ASD F-3 is a thick black liquid, a peculiar smell, almost insoluble in water. They are used for local treatment in pure form or in the form of oil solutions and ointments (sunflower, linseed oil, fish oil, petroleum jelly).

Drug ASD F-2 F-3 fluid. There are no other dosage forms of industrial manufacture. Use the drug ASD F-2 in its pure form or in the form of aqueous solutions, and the ASD F-3 in its pure form or in the form of oil solutions and ointments. Solutions and ointment are prepared on the spot. Such dosage forms have significant disadvantages:
not standard;
ASD F-3, used to treat skin diseases in humans and animals, has some undesirable properties: in its pure form, it strongly irritates the skin, delays granulation of wounds and causes some side effects associated with general intoxication of the body, especially when lubricating large surfaces of the skin (see . according to the list N 29, p. 329, paragraph 4);
for infected wounds, a dressing is applied moistened with a 15-20% aqueous solution of ASD F-2, which in most cases is practically not feasible - the animals tear off the dressing, the aqueous solution does not stay on the treated surface;
aqueous solutions of ASD F-2 have a short-term effect;
ointments and solutions on oil, fat, vaseline, lanolin bases poorly "give" the biosubstance of ASD F-3 (see N 29, p. 6.3).

 The aim of the invention is the proposal of drugs ASD FF-2 and 3 prolonged action, increasing their therapeutic efficacy due to better absorption.

 The essence of the invention lies in the fact that the drugs ASD FF-2 and 3 are made in the form of a hydrophilic-adsorption alloy using dimexide, a local anesthetic, anestesin or another anesthetic (novocaine, trimecaine, tselnovocaine, lidocaine), deodorizing, reducing volatility and viscosity-increasing ASD F-2 - 1,2-propylene glycol / 1,2-propanediol base alloys complexed with them - synthetic high molecular weight polyethylene oxide (carbovax). For these purposes, polyethylene oxide, propanediol, anesthetic, and an ASD preparation are successively dissolved in hot dimexide.

 The difference from the well-known drug.

 ASD preparations FF-2 and 3 in the form of dosage forms represent an alloy of dimexide-polyethylene oxide-propanediol base with the active component of the ASD preparation, which differs significantly from the prototype ASD preparation in the form of an aqueous, oily, fatty solution or vaseline ointment is stable and, when stored, unlike aqueous solutions of ASD F-2, convenient for external and intrauterine use, penetrating (penetrating) ability through the skin, mucous membranes, ulcer and wound surface increases, the drug enters the body tissue from solution ora of the base, and not from its melt, while the completeness of the resorption increases, due to the use of polyethylene oxide of different grades and molecular weight, as well as a different ratio of components, ointments, liniments, suppositories can be prepared, if necessary, it can be easily washed off skin, hair, and linen ( in people) without leaving a trace.

 The ratio of components, wt.

Drug ASD F-2 or F-3 10 20
Polyethylene oxide 30 50
1-2-Propanediol 5 15
Novocaine or another anesthetic 1 3
Dimexidum To 100
Examples of the ratio of components are given in table 1-3.

 Example 1

 The minimum option. Dosage form liniment.

 Example 2. The best option. Dosage form ointment.

 Example 3. The maximum option. Dosage form suppository.

 Medicinal raw materials constituents must meet the requirements of the standards.

 For production purposes, dosage forms of the drug ASD FF-2 and 3 are made in a reactor with a capacity of 25, 50, 60, 100, 200 liters. The capacity of the device should be 20% more than the volume of the series planned for release. This is especially necessary when using the drug ASD F-2, which has the ability to intensive foaming, although the foam is quickly extinguished.

The amount of dimexide, polyethylene oxide, 1,2-propanediol calculated for the series is loaded into the reactor, heated to 80.90 ^° C, stirred until the polyethylene oxide is dissolved, then anesthetic is added and steam sterilized at 100 ^° C for 20 minutes. Pass cold water through the jacket of the reactor, lowering the temperature of the solution to 70.75 ^o C, add the ASD F-2 preparation in small portions at intervals until the foam disappears. The dosage form of the drug is packaged at 60.65 ^o C.

 The technology allows you to get the drug ASD F-2 or F-3 in the form of prolonged-release dosage forms: according to example 1 (minimum option) liniment, according to example 2 (optimal option) ointment, according to example 3 (maximum option) from the drug ASD F-3 ointment, from F-3 suppository.

 Example 4. The ratio of the components of example 1: the minimum option. Dosage form of the drug ASD F-2 liniment. Based on 100 l of the finished dosage form, weighed (kg): the drug ASD F-2 10, polyethylene oxide grade 2000 or 3000 30, 1,2-propanediol 5, novocaine 1, dimexide 54.

Dimexide and polyethylene oxide are charged into a reactor with a capacity of 120-150 l, heated (70. 80 ^° C) with the stirrer switched on until dissolved by flowing steam at 100 ^° C for 20 minutes. Reduce the temperature of the solution to 70 ^o C, passing through the jacket of the reactor cold water. The drug ASD F-2 is added in small portions at intervals as the foam is extinguished. Reduce the temperature to 60.65 ^o C and pack the drug.

 Example 5. The ratio of the components of example 2: the best option (ointment). Based on 10 kg of the finished dosage form, weighed, kg: drug ASD F-2 1.5, polyethylene oxide grade 3000 or 4000 4, propanediol 1, trimecaine 0.2, dimexide 3.3. The technological process is similar to example 4.

Example 6. The ratio of the components of example 3: the maximum option (suppository), based on 10 kg of the finished dosage form is weighed, kg: drug ASD F-3 2, polyethylene oxide grade 5000 or 6000 5, propanediol
1.5, tselnovokaina 0.3, dimexide 1.2. The technology is similar to examples 4 and 5. When adding the drug ASD F-3, foaming is weak.

Testing the dosage forms of the drug ASD:
a) Stability of physicochemical properties. Determined the uniformity, color, transparency, the appearance of non-breakable when shaking the sediment and decomposition into fractions (at T ^o from 20 to 50 ^o C). The criteria for assessing the physicochemical properties were compared with the initial ones after 1.6.12 months. Table 4 shows the results within the shelf life of dosage forms of the drug ASD FF stable.

B) Harmlessness / toxicity. The harmlessness and tolerability of dosage forms does not significantly differ from the drug ASD. When administered intramuscularly to white mice, the maximum tolerated dose was 1200 1300 mg / kg of weight, LD ₅₀ / death of 50% of mice /, 1500 1600 mg / kg. Therapeutic doses do not have a cumulative effect.

Claims (2)

 1. A drug of prolonged action, including ASD and an organic filler, characterized in that the preparation contains ASD-F-2 or ASD-F-3 as an ASD, synthetic high molecular weight polyethylene oxide as an organic filler and, in addition, as a solvent - 100% dimexide, as a deodorant and viscosity increasing agent, 1,2-propanediol and novocaine or another anesthetic in the following ratio of components, wt. Drug ASD F-2 or F-3 10 20
Polyethylene oxide 30 50
1,2-Propanediol 5 15
Novocaine or another anesthetic 1 3
Dimexidum To 100
2. The drug according to claim 1, characterized in that it contains polyethylene oxide with a molecular weight of 2000 and above.  3. A method of obtaining a prolonged-release preparation, including dissolving ASD in an organic filler, characterized in that the ASD F-2 or ASD F-3 is taken as an ASD, synthetic high molecular weight polyethylene oxide is used as an organic filler, and additionally 100% as a solvent dimexide, as a deodorant and viscosity increasing agent, 1,2-propanediol and novocaine or another anesthetic in the following ratio of components, wt. Drug ASD F-2 or drug ASD F-3 10 20
Polyethylene oxide 30 50
1,2-Propanediol 5 15
Novocaine or another anesthetic 1 3
Dimexidum To 100
moreover, the dissolution of the components is carried out in hot dimexide.

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