Composition with antioxidant and antibacterial activity

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and represents a composition possessing the antioxidant and antibacterial activity and containing lithium ascorbate, differing by the fact that it additionally contains lithium benzoate in the following proportions, wt %: lithium ascorbate - 50; lithium benzoate - 50.

EFFECT: invention provides extending the range of antioxidants with antibacterial activity possessing normothymic activity.

1 ex, 2 tbl

 

The invention relates to the field of medicine, biology and pharmacology, and in particular to substances with antioxidant and antibacterial activity, and can be used in medicine, veterinary medicine, pharmaceutical industry to create on its basis the complex products, including for the purpose of correction of addictive disorders (as lithium salt) and related metabolic disorders. The claimed composition can be used as an integral part in various medicinal and pharmaceutical forms: ointments, balms, solutions and tablets.

It is known that lithium salts are widely used in medical practice, because the lithium cations have normotimicheskoe (psychostabilizers) activity, and the anion determines the bioavailability, solubility, toxicity and a number of other connection options, including antioxidant and antibacterial activity. Therefore, the selection of an appropriate anion and obtaining salt from a given set of properties is an important task.

As a prototype used antioxidant composition based on lithium salts having immunostimulatory activity (patent RU №2372081 from 25.07.2008, carpenters E. C., carpenter C. M.) containing ascorbate lithium aspartate lithium in percentage ratio of 50:50.

Ascorbate lithium, which is part of this comp is the exposure, is a bioactive drug with antioxidant and immunomodulatory activity, but its antibacterial activity in combination with lithium aspartate low. This reduces the potential range of applications of lithium ascorbate in various diseases. Thus, the main disadvantage of this composition is the lack of antibacterial activity.

Technical problem on which the invention is directed, is a composition with high antibacterial and antioxidant activity, containing lithium in soluble form.

The technical result of the invention consists in the expansion of the list of low-antioxidant with antibacterial activity, with normotimicheskoe action.

The problem is solved by obtaining the composition of the lithium salts of ascorbic and benzoic acids in the ratio, wt.%:

ascorbate lithium50
benzoate of lithium50

The hallmark of the technical solution is used in the composition of lithium benzoate. Benzoate of lithium together with lithium ascorbate provides high antioxidant activity and antibacterial properties allow aemula of the invention.

The antioxidant activity of the claimed compositions in combination with the various components and the composition of the prototype was investigated using the method of cathodic voltammetry (E. I. Korotkov, Y. A. Kurbanov. Voltammetric method for determination of total activity of antioxidants. RF patent IPC G01N 33/00. No. 2002-115-232 from 06.06.02). About the size of antioxidant activity was assessed by the relative change of a current of oxygen reduction.

Determination of the antibacterial properties of the claimed compositions in combination with the various components and the composition of the prototype was carried out by assessing its minimum overwhelming concentration in relation to cultures of E. Coli and Str. Pyogenes.

Example 1.

An accurately weighed sample of 500 mg of ascorbate lithium is mixed with 500 mg of lithium benzoate, diluted in 100 cm3with distilled water. The resulting composition is examined for antioxidant activity by the cathodic voltammetry.

In the electrochemical cell was placed 10 cm3solution background electrolyte. As the background electrolyte used phosphate buffer (pH 6,86).

For collected three-electrode cell consisting of a working mercury-film electrode, the chloride of silver electrode is used as reference electrode and auxiliary electrode (HSA). The electrodes were immersed in the process the background electrolyte and connected to a voltammetric analyzer TA-2 (OOO NPP "Comunali", Tomsk). In this work, we used constant-current mode cathodic voltammetry, scanning speed capacity was W=40 mV/s, the operating range of potentials from 0 to -1,0 Century was Stirred solution using vibration electrodes 20, 10 - stage calming solution. Next shot the first wave cathodic oxygen reduction, dissolved in a background solvent, in this field potentials. Repeated shooting of voltamperometry at least three times. Later in the electrochemical cell was made an aliquot of 0.5 cm3of the sample composition and re-filmed voltamperometry under the same conditions.

According to the obtained results were building a graph of the relative current of oxygen reduction on the time of interaction of antioxidants (AO) with active oxygen forms. On the slope of the tangent to the straight-line segment of this curve was performed calculation of kinetic (kkinu(µmol/l·min)) criterion antioxidant activity. The antioxidant activity of the sample was determined by the formula:

Dimension: ámol/l·min

where Ii is the current EV O2 in the presence of AO in solution, MCA, Io is the current EV O2 in the absence of AO in solution, MCA;CO2o - initial concentration of oxygen in solution, µmol/l, t is the reaction time of interaction of antioxidants with active oxygen forms, minutes of the Kinetic criterion reflects the amount of active oxygen forms, reacted with AO (or the total content of AO) per minute of time.

Table 1
The antioxidant activity of the claimed composition
MedicationConcentration, mg/cm3Antioxidant activity, K, mmol/l·min
The claimed composition0,51,54
Song-prototype0,51,26

Determination of antibacterial properties was to determine the minimum overwhelming concentration of the composition (IPC), during which there is no growth of microorganisms. In test tubes was preparing a series of dilutions of the claimed composition and the prototype in mesopatamia broth (BCH) at concentrations of 20 mg/cm3, 10 mg/cm35 mg/cm3, 2.5 mg/cm3. Control was a test tube containing nutrient medium b is C bacterial suspension and the investigated compositions. Incubated the samples for 24 h at 37°C.

The minimum bactericidal concentration of the investigated compositions took the minimal concentration at which suppressed the growth of microorganisms. Controlling the growth of microorganisms was performed visually by the change in turbidity of the medium. To control the turbidity of the medium was used tube of bacterial suspension ("negative" control - without the analyzed compositions).

Table 2
The results of the study antibacterial activity
Studied compositionE. coliStr. pyogenes
The concentration of the composition, mg/cm3
2,5510202,551020
The claimed CompositiongrowthgrowthNo
growth
The absence of p is a hundred growthgrowthThe lack of growthThe lack of growth
The placeholdergrowthgrowthgrowthgrowthgrowthgrowthgrowthgrowth

The study results of the claimed composition are presented in tables # 1 and # 2. From the materials table. No. 1 shows that the claimed composition has a pronounced antioxidant activity, the activity of the prototype and has antibacterial activity in doses of 20.0-10.0 mg/cm3significantly surpassing the activity of the prototype table. No. 2 (dilution method).

The claimed mixture exhibits antibacterial properties. Consequently it is possible to speak about the use of this composition as an integral part or as an independent drug from the group of salts of lithium (mood stabilizers) to prevent cell damage by free radicals and possess antibacterial activity. The claimed composition can be used as an integral part in different dosage forms.

Composition of antioxida the things and antibacterial activity, including ascorbate lithium, characterized in that it further contains lithium benzoate in the following ratio, wt.%:

ascorbate lithium50
benzoate of lithium50



 

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