RU2410094C1 - Pharmaceutical agent - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention concerns a pharmaceutical agent in the form of a solution for injections containing Mexidol, sodium metabisulphite as a preserving agent which can be used for treating an acute myocardial infarction, vegetovascular dystonia, psychosomatic and some other diseases. The pharmaceutical agent exhibits high storage stability provided a pH value of the solution is maintained at 4.2-4.4. Preferentially, the pharmaceutical agent is packed in dark glass ampoules of nominal volume 2 ml or 5 ml.

EFFECT: improved properties of the pharmaceutical agent.

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Description

The invention relates to medicine, specifically to injectable preparations based on Mexidol, and can be used to treat acute myocardial infarction, vegetovascular dystonia, psychosomatic and some other diseases.

Mexidol (2-ethyl-6-methyl-3-hydroxypyridine succinate) has a wide spectrum of pharmacological activity. It is known for its use as an antibacterial and anti-inflammatory agent (RF patent No. 2157686, 1999); as a means for the correction of insulin resistance (RF patent No. 2158590, 1999); for the treatment of opium addiction (RF patent No. 2159615, 1999); for the treatment of reactive arthritis (RF patent No. 2168992, 2000), as well as for the prevention and treatment of a number of other diseases.

Mexidol is used in the form of various pharmaceutical dosage forms, in particular in the form of a solution for injection. The dosage form of Mexidol in the form of a 5% aqueous solution is described in the publication Mashkovsky M.D. Medicines 1997, v. 2, p. 197). The disadvantage of this dosage form is the low stability of the solution of Mexidol during storage, which under the influence of light and temperature changes its color.

Known pharmaceutical composition for injection containing Mexidol, in which to increase stability added succinic acid and Trilon B (RF patent No. 2205640, 2003). However, the amount of stabilizers added practically coincides with the amount of mexidol itself and may not always make the desired correction in the therapeutic effect of the drug.

The proposed pharmaceutical agent in the form of a solution for injection based on Mexidol can significantly increase the stability of the solution (shelf life) with a small amount of stabilizer added, which is sodium metabisulfite (sodium pyrosulphate, Na ₂ S ₂ O ₅ ).

The pharmaceutical agent according to the invention contains components in the following ratio, wt.%:

Mexidol 4.0-6.0 Sodium metabisulfite 0.08-0.15 Water for injections Up to 100

The injected solution is preferably enclosed in glass ampoules with a nominal volume of 2 or 5 ml. The actual volume of the solution may exceed the nominal by 0.15 ml for 2 ml ampoules and 0.3 ml for 5 ml ampoules.

The ampoule can be made of colorless or light-shielding (dark) glass of the 1st hydrolytic class or HC-3 glass with a break point. Dark glass is more preferred as it provides the pharmaceutical agent with additional protection against exposure to light.

The invention is illustrated by examples of the preparation and analysis of a pharmaceutical agent.

Example 1

48.0 g of Mexidol and 0.9 g of sodium metabisulfite were introduced into the reactor with a magnetic stirrer. 0.8 L of water for injection was added to the reactor. The contents of the reactor were heated to 30 ° C with continuous stirring, which was continued until complete dissolution of the solid components. The resulting solution was brought to a volume of 1.0 L with water for injection, filtered and packaged in ampoules with a nominal volume of 5 ml of colorless glass.

Example 2

Analogously to the example, an injection solution was prepared with a total volume of 0.5 l, containing 26.0 g of Mexidol, 0.6 g of sodium metabisulfite, the rest was water for injection. During the preparation, the temperature was maintained at 32-33 ° C. The resulting solution was filtered and packaged in ampoules with a nominal volume of 2 ml of dark glass.

Example 3

The resulting solutions of examples 1 and 2 were a colorless transparent liquid. Ultraviolet absorption spectra had an absorption maximum in the wavelength range of 240-340 nm. A qualitative reaction with succinic acid gave an orange color on the chromatogram of the solution with intense green fluorescence; The pH of the solution was 4.2-4.4, the bacterial endotoxins determined by the OFS 42-0002-00 method were not more than 0.76 EU per 1 mg of ethyl methylhydroxypyridine succinate (mexidol).

The pharmaceutical product can be stored according to list B in a dry, dark place at a temperature of not 25 ° C for at least 3 years.

Mexidol has minor side effects and low toxicity, is well tolerated by patients and causes only a few side effects. The maximum daily dose of Mexidol should not exceed 800 mg, a single - 250 mg.

Claims (3)

1. The pharmaceutical agent in the form of a solution for injection, containing components in the following ratio, wt.%:
Mexidol 4.0-5.0 Sodium metabisulfite 0.08-0.15 Water for injections up to 100
provided that the pH of the solution is 4.2-4.4. 2. The pharmaceutical agent according to claim 1, characterized in that it is enclosed in glass ampoules with a nominal volume of 2 ml or 5 ml. 3. The pharmaceutical agent according to claim 2, characterized in that the glass ampoules are made of dark glass.