RU2593010C1 - Antioxidant composition - Google Patents

Abstract

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to chemical-pharmaceutical industry and represents an antioxidant composition containing lithium aspartate in amount of 40-60 wt% and lithium succinate in amount of 40-60 wt%. Disclosed composition allows for long-term storage and retains activity at room temperature for six months.

EFFECT: invention provides a wider range of antioxidant agents.

1 cl, 1 tbl, 3 ex

Description

The invention relates to pharmacology, namely to agents with antioxidant activity, and can be used in medicine, veterinary medicine, pharmaceutical industry.

Lithium salts are widely used for therapeutic purposes as psychostabilizers, immunostimulants and antiseborrheic drugs (Mashkovsky MD. Medicines: in 2 volumes. T 1. M: Medicine, 1986, 624 p.). However, the spectrum of lithium salts with antioxidant properties is limited.

A known composition having antioxidant activity (RU 2372081 C1, IPC (2006.01) A61K 31/375, A61K 31/194, A61P 37/04, A61P 39/06, published 10.11.2009), including lithium ascorbate and lithium aspartate in the following the ratio of components, wt.%:

lithium ascorbate fifty lithium aspartate fifty

However, this composition is unstable when stored in solution for more than a week, oxidizes and acquires a yellowish tint.

The objective of the invention is to expand the arsenal of funds for similar purposes.

The proposed antioxidant composition, as in the prototype, contains lithium aspartate.

According to the invention, the antioxidant composition further comprises lithium succinate in the following ratio of components, wt.%:

lithium succinate 40-60 lithium aspartate 40-60

The combination of these components provides antioxidant activity, good solubility of the composition in water and stability during storage in an aqueous solution.

Studies have shown that the claimed composition can be used as an integral part in various forms: ointments, balms, solutions.

Examples characterizing the properties of the claimed composition are shown in table 1.

The antioxidant activity of the claimed composition was investigated by the method of cathodic voltammetry (RU 2224997 C1). The value of antioxidant activity was judged by the relative change in the current of oxygen electroreduction.

A three-electrode electrochemical cell was used, consisting of a working mercury-film electrode, a silver-silver electrode used as a reference electrode, and an auxiliary electrode. The electrodes were lowered into 10 cm of a background electrolyte solution. A phosphate 0.025 M buffer (pH 6.86) was used as the background electrolyte. The electrodes were connected to a TA-2 voltammetric analyzer (LLC NLP Tomanalit, Tomsk). We used the constant current mode of cathodic voltammetry, the potential sweep speed was W = 40 mV / s, the working potential range was from 0 to -1.0 V. The solution was mixed using electrode vibration for 20 sec, 10 sec - the solution was calmed down stage. Next, the first wave of cathodic reduction of oxygen dissolved in a background solvent was recorded in the indicated range of potentials. The voltammogram was repeated at least three times. Then, an aliquot of 0.5 cm ^{3 of the} sample of the studied antioxidant composition was introduced into the electrochemical cell and the voltammogram was re-recorded under the same conditions.

Based on the results obtained, we plotted the dependence of the relative current of oxygen electroreduction (I _i / I ₀ ) on the time of interaction of antioxidants with active oxygen forms. Using the tangent of the slope of the tangent to the straight section of this curve, the kinetic (k _kinet. , Μmol / l · min) criterion for antioxidant activity was calculated.

The antioxidant activity of the composition was determined by the formula:

where I _i - current electroreduction O ₂ in the presence of antioxidants in solution, μA,

I ₀ - current electroreduction O ₂ in the absence of antioxidants in solution, µA;

- исходная концентрация кислорода в растворе, мкмоль/л,

- the initial concentration of oxygen in solution, µmol / l,

t is the reaction time of the interaction of antioxidants with active oxygen forms, min.

The kinetic criterion (k _kinet. ) Reflects the number of active oxygen forms that have reacted with antioxidants (or total antioxidants) per minute of time.

Example 1

An exact sample of 400 mg of lithium succinate was mixed with 600 mg of lithium aspartate, diluted in 100 cm ^{3 of} distilled water. The resulting composition was investigated for antioxidant activity by cathodic voltammetry.

Example 2

An exact sample of 500 mg of lithium succinate was mixed with 500 mg of lithium aspartate, diluted in 100 cm ^{3 of} distilled water. The resulting composition was investigated for antioxidant activity by cathodic voltammetry.

Example 3

An exact sample of 600 mg of lithium succinate was mixed with 400 mg of lithium aspartate, diluted in 100 cm ^{3 of} distilled water. The resulting composition was investigated for antioxidant activity by cathodic voltammetry.

The antioxidant activity of the samples with respect to the oxygen reduction process is shown in table 1.

From the above data it is seen that the claimed composition exhibits antioxidant activity and can be used as an antioxidant. As a result, we can talk about the use of this composition as an integral part or as an independent drug with antioxidant activity, which prevents damage to cells by free radicals and promotes tissue regeneration.

The claimed composition allows for long-term storage and does not lose activity at room temperature for six months.

Claims (1)

Antioxidant composition containing lithium aspartate, characterized in that it further includes lithium succinate in the following ratio of components, wt.%:
lithium succinate 40-60 lithium aspartate 40-60