RU102889U1 - MICROCONTAINER POLYMERIC WITH A MEDICINAL SUBSTANCE, PROVIDING A LOCAL PROLONGED COMBINED THERAPEUTIC ACTION - Google Patents

Abstract

The utility model relates to medical devices and can be used in traumatology and general surgery. The microcontainer consists of two parts: the central one, made in the form of granules with a described diameter of 0.05 to 1.5 mm, made from a copolymer of vinylpyrrolidone with butyl methacrylate, an antimicrobial substance and a substance that promotes tissue regeneration and the outer shell from a copolymer of vinyl pyrrolidone with butyl methacrylate, thickness from 0.05 to 0.2 mm. Using the utility model provides effective sorption of wound exudates, local antimicrobial action, accelerates tissue regeneration processes and also reduces the total dose of the used antimicrobial substance and a substance that promotes regeneration by 30-350 times.

Description

The utility model relates to medical devices, namely, products used in traumatology and general surgery.

Oral administration of drugs that promote tissue regeneration is known in the form of tablets, for example, potassium orotate. (M.D. Mashkovsky Medicines, 2007, M., p. 788). This method of administration has a number of disadvantages:

- funds can be administered only orally;

- the tool has low bioavailability,

- the drug substance is partially destroyed by the liver,

- it is necessary to use high total dosages per treatment course, which leads to undesirable side effects and an increase in the cost of treatment.

Injection of an antimicrobial preparation, for example gentamicin sulfate, is known by syringe. (M.D. Mashkovsky Medicines, 2007, M., S.799-800) This method of administration has the following disadvantages:

- requires repeated administration of the drug (up to 20 injections) within 5-7 days,

- not able to provide the necessary directed therapeutic effect,

- has a traumatic effect on the tissue,

- requires the introduction of large total doses of medicinal substances, which may cause unwanted adverse reactions of the body and leads to an increase in the cost of treatment

The technical task of the proposed Utility model is the creation of microcontainers from biocompatible polymers containing antimicrobial substances and substances that promote tissue regeneration, capable of absorbing postoperative exudates after application to the wound surface; capable of resolving after surgery within the body; capable of exerting a long-term local combined antimicrobial and stimulating regeneration effect in the area of damaged tissues and capable of significantly reducing the total dosage of the drugs used per treatment course ..

The technical result is achieved by the fact that the microcontainer consists of two parts: the central part in the form of granules with a described diameter of 0.05 to 1.5 mm, made from a copolymer of vinylpyrrolidone with butyl methacrylate, an antimicrobial substance and a substance that promotes regeneration, in the following ratio of components parts (% wt.):

vinylpyrrolidone copolymer with

butyl methacrylate 65.0-90.0; antimicrobial substance 1.0-30.0

promoter

tissue regeneration 2.0-34.0

and an outer shell of a copolymer of vinylpyrrolidone with butyl methacrylate, with a thickness of 0.05 to 0.2 mm.

The granule boundary size is due to the fact that granules with a size of less than 0.05 mm do not provide the necessary duration of drug release into adjacent tissues, and granules with a size of more than 1.5 mm can cause an undesirable reaction of adjacent tissues to a foreign body due to the mechanical irritating effect of large particulate matter. The thickness of the protective outer layer of less than 0.05 mm does not ensure the continuity of the protective layer, which does not allow to regulate the rate of release of the drug substance, and the thickness of more than 0.2 mm leads to an increase in the size of the microcontainer, which can cause an undesirable reaction (irritation) of surrounding tissues.

The granules and the outer shell are made of a biocompatible copolymer of vinylpyrrolidone with butyl methacrylate, which is able to completely biodegrade in the body within 14 to 60 days depending on the size of the particles and the implantation site without having a toxic effect on the surrounding tissues and the body as a whole. Medicinal substances - antimicrobial and conducive to regeneration, undergo metabolic processes and are completely eliminated from the body in terms determined by their structure and properties.

The amount of a substance that promotes regeneration is from 2.0 to 34.0%, and the antimicrobial substance is from 1.0 to 30.0%. The boundary concentrations of substances that promote regeneration are due to the fact that when the content of antimicrobial substances is less than 1.0% and substances that contribute to regeneration less than 2% do not provide the necessary local therapeutic concentrations in adjacent tissues, and at concentrations of more than 35%, as the drug is released, an increase in the porosity of the granules, which reduces the duration of the release of the drug substance and, consequently, the duration of the antimicrobial action and the action that promotes regeneration.

The use of a polymer micro-container combined drug action allows the following:

- to ensure reliable fixation of particles on the wound surface due to the high adhesion of the copolymer to soft tissues,

- provide sorption of wound exudates from the wound surface,

- eliminate the unwanted reaction of tissues to a long stay of a foreign body inside the body due to the complete biodegradation of the material,

- provide simultaneous long-term local antimicrobial action and action that promotes tissue regeneration .;

- reduce the number of doses of the drug;

- reduce the total dose of used antimicrobial substances and substances that promote tissue regeneration.

The proposed Utility Model operates as follows. At the end of the operation, immediately before tissue suturing, all layers of the surgical wound are uniformly sprinkled with a non-continuous layer of microcontainers, be sure to avoid the formation of a continuous layer or a heterogeneous thick layer. After applying microcontainers, the wound is sutured in layers tightly or with drainage.

Utility Model Manufacturing Examples

Example No. 1.

20 g of a copolymer of vinylpyrrolidone with butyl methacrylate grade PPB-1 (TU 2216-025-17712304-04) (65%) are dissolved in 50 g of ethyl alcohol and 0.31 g (1%) of crystalline iodine is added with stirring, stirred until it is completely dissolved and with stirring, 10.5 g (34%) of potassium orotate is added, the resulting suspension is poured onto a polypropylene substrate, dried in vacuum at 80 C for 4 hours and ground in a mill to obtain granules with a size of 1.3-1.5 mm By spraying "in a suspended layer" at a temperature of 50 ° C from a 10% acetone solution of a vinylpyrrolidone-butyl methacrylate copolymer (nitrogen content 5.7% by weight), an outer layer 0.17-0.2 mm thick is formed. Microcontainers are used for applying fascia and periosteum to the wound surface during bone osteosynthesis of tubular bones. The sorption capacity of microcontainers is 130-150%. The duration of antimicrobial action is 16-18 days. The duration of local release of orthic acid is 20 days. The time of complete destruction of the sorbent is 50 days.

Example No. 2.

20 g of a vinylpyrrolidone-butyl methacrylate copolymer (nitrogen content 4.7% by mass) (90%) are dissolved in 40 g of ethanol and, after the copolymer is completely dissolved, 1.11 g (5%) of sulfapyridazine and 1.11 g of pentaxyl (5%) are added with stirring ) The resulting suspension is poured onto a polymer substrate and dried at a temperature of 75 ° C for 8 hours. The resulting film is removed from the substrate and ground in a mill to obtain sorbent granules with a size of 0.5-0.6 mm. The granules are loaded into liquid paraffin and a 16% solution of PPB-1 copolymer is added to the suspension with stirring. The method of removing acetone while passing nitrogen and a temperature of 50 C on the surface of the granules form an outer layer with a thickness of 0.5-0.6 mm Microcontainers are used for application to the surface of the liver during its resection .. The sorption capacity of the sorbent is 100-120%. The duration of local antimicrobial action is 12-14 days. The duration of local isolation of pentoxyl in adjacent tissues is 10 days. The time of complete destruction of the sorbent is 30 days.

Example No. 3.

20 g of a copolymer of vinylpyrrolidone with butyl methacrylate grade PPB-1 (68%) and dissolved in 45 g of ethanol, 8.82 g (30%) of gentamicin sulfate and 0.59 g (2%) of orotic acid are added with stirring, the resulting suspension is poured on a polymer substrate, dried in vacuum at a temperature of 60 C. The resulting film is removed from the substrate and crushed in a mill, obtaining granules with a size of 0.05-0.07 mm The granules are placed in liquid paraffin and 4% by weight are added to the suspension with stirring. a solution of copolymer PPB-1 in ethanol. The method of removal of ethyl alcohol while passing nitrogen and a temperature of 70 C on the surface of the granules form an outer layer with a thickness of 0.05-0.07 mm Microcontainers are used for application to the surface of the intestine after the formation of intestinal anastomosis. The sorption capacity of the sorbent is 100-120%. The duration of antimicrobial action is 6-7 days. The duration of local release of the drug is 14 days. The time of complete destruction of the sorbent is 14 days.

The advantages of the proposed utility model in comparison with the prototype are shown in table No. 1.

Table number 1. Comparative results of using microcontainers according to the proposed model and the prototype. No. Parameter Name Parameter value According to the prototype According to the proposed utility model by examples one 2 3 one Dates of complete resorption in the body, day 0.15-0.25 fifty thirty fourteen 2 Sorption ability in relation to exudates,% 0 130-150 100-120 100-120 four The duration of local excretion of a substance promoting regeneration, days 0.1-0.2 twenty 10 fourteen 5 The duration of local antimicrobial activity, day 0.1-0.2 16-18 12-14 6-7 6 The total dose of a medicinal substance per course of treatment, mg: antimicrobial one hundred 10 fifty 300 conducive to regeneration 7000 340 fifty twenty

Claims (1)

A polymer microcontainer containing a medicinal substance, characterized in that it consists of two parts: a central part made in the form of granules with a diameter of the circumscribed circle of 0.05-1.5 mm, made from a copolymer of vinylpyrrolidone with butyl methacrylate, an antimicrobial substance and a substance, promoting regeneration, in the following ratio of constituent parts, wt.%: vinylpyrrolidone copolymer with butyl methacrylate 65.0-90.0 antimicrobial substance 1.0-30.0 promoter regeneration 2.0-34.0 and an outer shell of a vinylpyrrolidone copolymer with butyl methacrylate with a thickness of 0.05 to 0.2 mm.