RU2619350C1 - Agents with diuretic activity - Google Patents

Abstract

FIELD: pharmacology.

SUBSTANCE: diuretic contains 0.5% solution of humic acids and magnesium chloride, taken in a certain ratio.

EFFECT: means allows to increase therapy effectiveness and eliminates occurrence of side effects.

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Description

The invention relates to the field of experimental medicine, namely to pharmacology, preclinical studies (on small laboratory animals). Known diuretic furosemide (1).

The disadvantage of this drug is that it is effective in sufficiently high single doses of 20-160 mg. The minimum effective (threshold) diuretic dose for this drug is a dose of 1 mg / kg. In this regard, furosemide causes a number of side effects: severe hypovolemia and hyperglycemia.

The diuretic hypothiazide is also known (2).

The disadvantage of this tool is that it is available in only one dosage form - in the form of tablets for oral administration, which makes it impossible to use it for parenteral administration.

A diuretic is also known (3).

The disadvantage of this drug is a rather high average therapeutic dose that causes a diuretic effect (5 mg / kg), which can cause a number of side effects.

The aim of the invention is to increase the effectiveness of therapeutic effects and the elimination of side effects.

This goal is achieved in that a 0.5% solution of humic acids is used as a diuretic, which additionally contains manganese (II) chloride in the following ratio of components: 0.5% solution of humic acids - 40 ml; manganese chloride - 0.1 g.

The inventive tool is prepared as follows: 0.1 g of manganese chloride is taken and dissolved in 40 ml of a 0.5% solution of humic acids at room temperature. The finished solution is sterilized with ultraviolet rays for 30 minutes, after which it is packaged in dark glass bottles with a capacity of 50 ml.

The diuretic is used as follows: administered subcutaneously (intramuscularly) at a dose of 0.1 mg / kg or 0.05 mg / kg (0.2 ml / kg or 0.1 ml / kg of animal weight) 1 time per day for 7- 14 days.

A contraindication to taking the drug is the individual intolerance of its individual components.

The drug belongs to the IV class of toxicity (low hazard substances) and is stored at a temperature of +5 to + 10 ° С.

The drug is available in dark glass bottles of 50 ml.

Preclinical example (data from experimental studies) No. 1.

When conducting chronic experiments on white outbred laboratory rats of both sexes, it was found that subcutaneous administration of a 0.5% solution of humic acids at a dose of 5 mg / kg of animal weight affects the excretory function of the kidneys, increasing the excretion of water by the kidneys from 1.22 ± 0.12 ml / day in the control up to 1.58 ± 0.12 ml / day (30%, p <0.05) in the experiment, sodium from 113.09 ± 19.51 μmol / day to 191.68 ± 24.63 μmol / day (by 69%, p <0.05), while reducing renal excretion of potassium from 92.73 ± 8.67 μmol / day to 69.30 ± 3.07 μmol / day (by 25%, p> 0.05) and creatinine from 2.38 ± 0.25 mg / day to 1.65 ± 0.19 mg / day (by 31%, p> 0.05) in 24 hours reported experiments. Therefore, humic acids in the above dose stimulate diuresis by reducing tubular reabsorption of water and sodium, however, inhibit glomerular filtration.

Note: hereinafter p <0.05 reliable data, p> 0.05 false data.

Preclinical example (data from experimental studies) No. 2.

In chronic experiments on white outbred laboratory rats of both sexes, it was found that the claimed agent at a dose of 0.1 mg / kg of the animal’s weight affects water-salt metabolism as follows: it increases the excretion of water by the kidneys in experimental animals by 34% compared to control , p <0.05, sodium - 22%, p <0.05, potassium - 30%, p <0.05, creatinine - 49%, p <0.05 for 24 hours of the experiment. Therefore, the inventive tool in a dose of 0.1 mg / kg stimulates diuresis mainly due to increased glomerular filtration, and by reducing tubular reabsorption.

Preclinical example (data from experimental studies) No. 3.

In chronic experiments on white outbred laboratory rats of both sexes, it was found that the claimed drug at a dose of 0.05 mg / kg of the animal’s weight affects water-salt metabolism as follows: it increases the excretion of water by the kidneys in experimental animals by 55% compared with the control ones , p <0.05, sodium - 71%, p <0.05, potassium - 42%, p <0.05, creatinine - 33%, p <0.05 for 24 hours of the experiment. Therefore, the claimed agent at a dose of 0.05 mg / kg significantly stimulates diuresis both by increasing glomerular filtration and by reducing tubular reabsorption of water and sodium.

The use of the proposed drug eliminates the possibility of toxic effects on a living organism and improves the effectiveness of the treatment of nephropathy of various origins, including acute renal failure.

The inventive tool can and should be used in experimental medicine, namely pharmacology and pathological physiology, when conducting complex therapy of experimental acute renal failure.

The inventive tool affects water-salt metabolism, increasing the excretion of water and ions by the kidneys, thus normalizing the excretory function of the kidneys.

Information sources

1. Mashkovsky M.D. Medicines In two volumes. T. 1. - 14th ed., Rev., Rev. and add. - M.: Publishing House New Wave LLC, Publisher SB. Divov, 2002 .-- 540 s, 8 col. silt.

2. The register of medicines of Russia. Encyclopedia of drugs. 10th issue. - M .: RLS-2003, 2003 - 1440 s.

3. Certificate for the invention of the Russian Federation No. 2456002, M.cl. A61K 31/10, A61K 33/06, A61P 7/10, 2012.

Claims (2)

Diuretic agent containing a 0.5% solution of humic acids and manganese (II) chloride in the following ratio of components:  0.5% solution of humic acids  40 ml  manganese chloride  0.1 gr