Liquid pharmaceutical composition

 

(57) Abstract:

The invention relates to medicine, namely to liquid pharmaceutical compositions of a wide spectrum of action on the basis of alkaloids aberamentho stimulants and vitamins, which can be used to improve blood circulation of the brain, in particular in the treatment of the effects of traumatic brain injury, as well as for the prevention and treatment of ischemic lesions of the brain, stimulate brain activity, for the adaptation of the vestibular apparatus to the overload. As of alkaloids in the composition used Vinpocetine, vincamine, Vinburnine, their pharmaceutically acceptable salt, or a mixture thereof; vitamins - b vitamins and a-tocopherol; the solvent is water (40-96% vol.) ethyl alcohol. Effect: invention allows to eliminate the negative side effects that are more concentrated funds and products containing plant extract alkaloids, to increase the efficiency of the composition, to expand the range of its application, namely to strengthen rendered alkaloids therapeutic effect and to achieve additional therapeutic effects. 1 PL.

The present invention relates medicine, and imator in aqueous ethyl alcohol. The composition may be used as a medicine to improve blood circulation in the brain, particularly in the treatment of the effects of traumatic brain injury, for the prevention and treatment of ischemic lesions of the brain, to stimulate brain activity, for the adaptation of the vestibular apparatus to the overloads.

Alkaloids aburamanova groups were first isolated from plant materials grass Periwinkle small (family kurtovich) and used for other semi-synthetic alkaloids and drugs having vasodilator, antispasmodic, hypotensive effect, especially effective in the treatment of cerebral circulatory disorders of various etiologies.

Known drugs on the basis of alkaloids aburamanova group in the form of solid dosage forms, such as Vinpocetine (analogues Cavinton, Inex), containing a semisynthetic derivative alkaloid of vincamine contained in Periwinkle small; Vincamine (analogues Devinkan, Vinca), containing the alkaloid vincamine, Wankaner (analogues of Vinkuran, Winlaton) containing the amount of Vinca alkaloids small. These drugs used in the spasm of cerebral vessels, hypertension, neurological is e tools: a Guide to pharmacotherapy for physicians. M, LLC "New wave", so 1, 2002, S. 391].

The lack of solid dosage forms is that due to the specific technology of drug production in the form of tablets (in shell and without it) and capsules latter contains a large number of auxiliary additives, which in some cases lead to the emergence of side effects and contraindications; shell slows down the absorption rate of the active substance.

Medicines in liquid form in the form of infusions, decoctions, syrups, aqueous solutions have a high weight and rate of absorption of the drug.

Famous soft drink, stimulating brain activity, based on a combination of burninig alkaloids with compounds-derivatives of xanthine [European patent No. 0760240, a 61 K 31/52, 1997]. The drink contains alkaloids aberamentho series (vincamine, Vinpocetine or their pharmaceutically acceptable salts) or its extract in the amount of 0.5-10 mg per 100 ml of Cola drinks, cocoa, tonic, coffee, and drinks on the basis of a lemon, ginseng. Moreover, for the preparation of beverages may be used water or any non-toxic liquid that is usually used in non-alcoholic and beverage may experience side effects, due to the presence of compounds-xantina: allergies, insomnia, increased heart rates.

Most similar in essential characteristics of the claimed composition is an alcohol tincture periwinkle small, containing as the active component of the alkaloid vincamine [Lesenkina Century Century Biological features Periwinkle small in terms of Mordovia. Chemistry and computational simulation. Butlerov communications. 2001, No. 5; Amasiatsy Amirdovlat. Unnecessary for ignoramuses. M.: Nauka, 1990]. Tincture periwinkle small gain, filling 25 g dry grass ethyl alcohol concentration of 40-70% in the amount of 580 ml and insisting in a warm dark place for a week. Then the tincture strain and drink 5-7 drops 2 times a day with water. Used infusions and decoctions of malignant tumors to improve metabolism, as an astringent, hemostatic, wound healing agent, with lung tuberculosis, scurvy and sore throat.

The disadvantage of this alcohol tinctures is that in addition to vincamine tincture contains a number of other compounds, transition from vegetative mass in a solution, such as vincin, apovincamine, apovincamine, Bornemann, quebrachitol, reserpine, samidin, pirinen and others. Acetane therapeutic effect [C. Y. The Vachnadze, E. H. Jakeli, H. C. Robakidze and other Chemical composition and pharmacological activity of alkaloids cultivated in Georgia periwinkle small. Chemical and pharmaceutical journal, so 35, No. 5, 2001].

The technical result achieved during the implementation of the claimed invention, is the elimination of negative side effects, which are more concentrated funds and products containing plant extract alkaloids; improving the efficiency of funds and expanding the range of its application.

This technical result is achieved by the fact that the liquid pharmaceutical composition containing alkaloids aberamentho some water and ethyl alcohol, as alkaloids aberamentho series contains a substance selected from the group comprising Vinpocetine, vincamine, Vinburnine, their pharmaceutically acceptable salt, or a mixture of alkaloids or their salts, and optionally contains vitamin selected from the group comprising vitamin b1IN2IN3IN6b9B12and F or their mixture, in the following ratio, wt.%:

Alkaloid aberamentho series 5·10-4-0,05

Vitamin 3·10-6-0,4

Water ethyl a, because the stated upper limits are determined based on the maximum daily therapeutic and prophylactic doses of alkaloid, the necessary daily requirement of the human body vitamins, and recommended dosage.

Vitamins are preferably used at a concentration (wt.%): b1IN2IN65·10-4-0,04;3and E 0,05-0,4;9and B123·10-6-0,007.

The combination of vitamins selected from the group b and E, alkaloids aberamentho series allows you to boost provided by the alkaloids therapeutic effect and to achieve additional therapeutic effects. Selected vitamins have a positive effect on the nervous system, hematopoiesis, cell renewal, strengthen capillaries and stimulate muscle activity.

Because plant material is grass periwinkle small - contains not more than 0.06% vincamine (usually 0.03 to 0.04%), and the process for selection is quite complex, for the preparation of compositions proposed to use the substance of vincamine and/or other alkaloids obtained by synthetic or semi-synthetic, including from other more accessible alkaloids.

For the preparation of the composition is (Switzerland), and ethyl alcohol GOST R 51652-2000. As a mixture of alkaloids aberamentho series used a mixture of substances synthetic or purified alkaloids extract alkaloids of plant origin firm Kovacs” (Spain).

The invention is illustrated by examples.

Example 1.

In 1000 g of ethanol concentration of 70% vol. at room temperature, was dissolved 0.1 g of vincamine, 0,012 g vitamin b1and 0,012 g of vitamin b2. Then to the resulting solution was added 0.05 g of a solution of vitamin B12in ethanol, prepared by mixing 0.0011 g of vitamin b12and 50.0 g of ethyl alcohol 70%. The resulting solution was well mixed. The composition is a clear solution of lemon-yellow color.

The estimated dose funds for an adult is 10 ml 3-4 times daily rate up to 1 month, with a single dose funds diluted in half a glass of water.

The effectiveness of the compositions was tested on rats with experimental pathological conditions of the Central nervous system. Evaluated several groups of indicators: morphometric, biochemical, and functional. First of all observed cliniche, retardation, lethargy, ataxia. Some animals during the day were observed lateral position. In this group by the end of the observation period, the mortality rate was 3 out of 10 animals.

The application of the proposed composition resulted in no mortality. The objective condition of the animals was better, as evidenced by the test results.

Application of funds warned violation of microcirculation and phenomena of chromatolysis in neurons of the cerebral cortex and the basal ganglia; in addition, the normalized energy metabolism of the brain, as evidenced by indicators of metabolic and oxidative processes in the brain. The use of normalized energy metabolism of the brain.

In acute traumatic brain injury suffered all the functions of the Central nervous system of experimental animals that were apparent violations of the processes of learning, memory, arousal, inhibition. Introduction means is completely eliminated disorders of the nervous system: it was not observed any significant increase muscle tone, and the magnitude of the response to mechanical stimulation was back to normal.

Efficiency is eljnosti restore the ability to rectilinear movement after rotation. The test was conducted in mice. The result shows that the use of tools significantly reduces the recovery period after rotation, i.e., improves the ability of the vestibular apparatus to adapt to the radial acceleration.

Resistance to hypoxia was determined by reaspiration mice. Recorded using a stopwatch maximum life expectancy and symptoms of teratogenesis. It turned out that the inventive tool significantly increases the lifetime of mice (from 33.6 to 50.8 min). This stabilized the indices of lipid peroxidation and restored the antioxidant (catalase) activity, indicating that the increase in the reserve antioxidant activity of the brain.

In addition, evaluated the effectiveness of the tools in ischaemic brain damage. The disease was modelled on the rats male compression of the common carotid arteries. Reperfusion-induced changes in the brain were observed in the dynamics after 24 and 72 hours after removal of the clamps.

It was found that the tool has a positive effect on the energy metabolism of the ischemic brain; it effectively reduces the intensity of oxidation of lipids and advance the ha

Research shows that the means of the indicated composition has a high efficiency and helps to restore disturbed functions for post-traumatic encephalopathy, ischemic lesions of the brain, increases resistance of brain structures to hypoxia and adaptation of the vestibular apparatus to the overloads.

Example 2.

In 1000 g of ethanol concentration 96% vol. at room temperature, dissolved 0.005 g of vincamine and 0.4 g of vitamin b6. The resulting solution was well mixed. The composition is a clear solution of lemon-yellow color with the smell of ethyl alcohol.

Examples 3, 4, 6, 7.

The composition is prepared as described in example 2.

Example 5.

The composition is prepared analogously to Example 1. The composition is a clear solution yellow with the smell of ethyl alcohol.

The composition of example 1 and subsequent examples 2-7 and their properties are shown in the table.

As follows from the description, the liquid pharmaceutical composition based alkaloids aberamentho stimulants, vitamins and ethyl alcohol may be used as therapeutic and preventive tool Shiro is a high equipment.

Liquid pharmaceutical composition comprising alkaloids aberamentho some water and ethyl alcohol, characterized in that as alkaloids aberamentho number it contains a substance selected from the group comprising Vinpocetine, vincamine, Vinburnine, their pharmaceutically acceptable salt, or a mixture thereof, and further comprises a vitamin selected from the group comprising B1B2IN3IN6IN9B12and-tocopherol or a mixture as water-ethanol - 40-96% vol. ethyl alcohol in the following ratio, wt.%:

Alkaloid aberamentho series 5·10-4-0,05

Vitamin 3·10-6-0,4

Water ethyl alcohol 40-96% vol. The Rest



 

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