Periphery blood circulation improving remedy

FIELD: pharmaceuticals.

SUBSTANCE: invention provides topical blood circulation improving remedy containing simultaneously nitroglycerine and aminophylline. Remedy can be provided in the form of emulsion, gel, or ointment, which are administered 1-2 times a day.

EFFECT: strengthened blood circulation activation effect, which is prolonged to 24 hours.

5 cl, 9 ex

 

The invention relates to medicine and can be used in the treatment of peripheral circulatory disorders.

Due to the fact that human peripheral blood very frequently encountered in clinical practice, especially in chronic diseases of the heart, blood vessels of the brain and extremities, diabetes (diabetic foot), multiple sclerosis and others, there are many tools that activates peripheral blood flow. In the clinic for this purpose, widely used drugs such as nitrosorbid, nicotinic acid, Cavinton, trental, Dibazol, etc. (Medmaravis. Drugs, vol. 1, M.: Medicine 2000). However, these funds are used resorbtive and due to its pharmacokinetic they do not create needs and long-term concentrations in spastic vessels that weakens and shortens the effect.

In this regard, in our work we have set a task to create a tool for local use local activation of peripheral blood circulation.

Known means of local action Actovegin (or solcoseryl), improve peripheral circulation. However, the effect of the specified drug even under intravenous develops only after 20 minutes (the Register of medicines in Russia. Encyclopedia of drugs, 7th edition, 2000). In addition, the drug is not har is cherished on the authenticity of the chemical composition. It is obtained from the blood of healthy dairy calves. Raw materials, thus, expensive and scarce. Its production in Russia is difficult, especially in connection with the pronounced decline in the livestock population. The last time such difficulties occur and abroad in connection with the mass poisoning of cattle by vaccinia rabies. Therefore, this drug does not seem optimal for widespread clinical use.

We have shown that nitroglycerin and aminophylline in dosage forms for local action gives fast effect activation of peripheral blood circulation. The duration of this effect up to 24 hours, which will allow you to apply the emulsion (ointment, gel) only 1 - 2 times a day.

Nitroglycerin we have included this tool in connection with the fact that it is rapidly absorbed from the skin surface by expanding blood vessels in the application, which allows you to accelerate the resorption of aminophylline. The vasodilator mechanism of action of nitroglycerin is associated with the generation of cyclic GMP (guanosine monophosphate). Aminophylline blocks phosphodiesterase C-GMP and enhances the local effect of nitroglycerin (Nagatoro, Megadouche, Heteropic. Cyclic nucleotides and their analogs in medicine, 1990). When the suction in the overall flow of aminophylline (like other xanthine derivative) removes undesired hair is th effect of nitroglycerin on the cerebral blood flow, leading to the disappearance of the feeling of headache, celebrating some of the patients. (Besocial. Essays on clinical pharmacology. M.: Medicine, 1965). Due to the activation of the heart it enhances the blood circulation.

Examples of the use of funds to improve peripheral circulation.

Example 1.

The emulsion preparation.

For cooking oil solution took 186 g vaseline oil, was dissolved in 2 g of nitroglycerin. For the preparation of an aqueous solution took 542 g of distilled water and dissolved therein at 60 g of aminophylline and 90 g of ethanol. Then took 120 g of emulsion of wax and oil solution of nitroglycerin, loaded into the reactor. The resulting mixture was heated to 80C. until complete melting wax emulsion and form a homogeneous mixture.

Then the solution is poured previously prepared aqueous solution of aminophylline and ethyl alcohol. The mixture was thoroughly mixed to obtain an emulsion. The resulting emulsion is slowly cooled and added preservative.

Example 2.

The emulsion preparation.

For cooking oil solution took 100 g vaseline oil and dissolved therein 0.3 g of nitroglycerin. For the preparation of an aqueous solution took 779,7 g of distilled water and dissolved in 30 g of aminophylline and 40 g of ethyl alcohol.

Then took 50 g of emulsion of wax and oil is the solution of nitroglycerin, were loaded into the reactor. The resulting mixture was heated up to 80C until complete melting wax emulsion and form a homogeneous mixture.

Then the solution is poured previously prepared aqueous solution of aminophylline and ethyl alcohol. The mixture was thoroughly mixed to obtain an emulsion. The resulting emulsion is slowly cooled and added preservative.

Example 3.

Preparation of a gel.

Dissolved 2 g of nitroglycerin in 30 g of paraffin oil and added a solution consisting of 60 g of aminophylline, 20 g of ethanol and 868 g of distilled water, then added 20 g of polymethyl methacrylate. The resulting mixture was stirred at 80°and was stirred for 40 minutes. The obtained gel is slowly cooled and added preservative.

Example 4

The emulsion prepared as in example 2, at a dose of 10 mg was applied a uniform thin layer on the ear of the rabbit. By visual examination after 3 minutes has increased circuit vascular pattern. Blood flow velocity was determined by the volume of the blood, arising from marginal vein of the ear for 1 min Before application of the emulsion flowed 2 ml/min after 5 min after application of 4.2 ml. In the study of the ear of the rabbit on the imager was detected temperature increase of 2 C over the entire surface of the ear of the rabbit.

Example 5

Preparation of ointment.

Mixed 2 g of NITR the glycerol with 10 g of ethyl alcohol and 60 g of aminophylline with 10 g of ethyl alcohol, added 258 g of distilled water. Then added 5 g of borax, 45 g pchelinogo wax and 110 g of lanolin. Thoroughly mixed. Was heated to 80C to form a homogeneous mixture.

Example 6

The emulsion prepared as in example 1 at a dose of 10 mg was applied a uniform thin layer on the ear of the rabbit. By visual examination after 5 minutes has increased circuit vascular pattern. Blood flow velocity was determined as in example 4. Before applying the emulsion, it was 2.2 ml/min after 5 min after application of 3.1 ml/min In the study of the ear of the rabbit on the imager revealed a rise in temperature of 1 degree over the entire surface of the ear of the rabbit.

Example 7

The gel prepared as in example 1 at a dose of 10 mg was applied a uniform thin layer on the ear of the rabbit. By visual examination after 3 minutes has increased circuit vascular pattern. Blood flow velocity, defined as in example 4, was before applying the gel 2.0 ml/min, after applying the gel of 3.8 ml/min In the study of the ear of the rabbit on the imager was detected temperature increase of 2 C over the entire surface of the ear of the rabbit.

Example 8

Patient, 65 years, suffering from diabetes and trophic ulcers on the lower leg, was applied ointment on the top 1/3 of the thigh with the two parties is. After 10 min, the patient was seen to increase the body temperature up to 34-35,7C in the thigh on both sides and increased body temperature to 34C (30,1C before applying).

After 20 minutes, the patient can see the increase in zone temperature increase already from two sides. The patient continued treatment with ointment, and on the third day of treatment, it was observed the formation of a dry crust on the trophic ulcer, and on the 7th day there was the healing of venous ulcers.

Example 9

The patient And, 54 years old, suffering from diabetic angiopathy caused the emulsion in a thin layer around the wrist. Studies were conducted on the imager. Before applying the ointment reaction temperature is 28C and observed only on the back of the hand, the phalanges are not visible due to the severe pathology of the patient.

After 5 minutes after application of the emulsion, we noted an increasing temperature up to 30C in the centre of the palm and the appearance of the reaction temperature on the phalanges 26C.

After 30 min after application of the emulsion temperature increase occurred over the entire surface of the palm from 26 to 30C.

After 1 hour the entire surface of the palm from the center to the tips of the fingers was warm and noted a steady rise in temperature to 31.3C. This effect lasted for 10 hours in a single application of the emulsion.

1. Means to improve the peripheral blood circulation matnog the steps, characterized in that it contains nitroglycerin, aminophylline and special additive in the following ratio of components, g:

Nitroglycerin 0,3-2,0

Aminophylline 30,0-60,0

Targeted supplements To 1000,0

2. The tool according to claim 1, characterized in that it can be made in the form of an emulsion, gel, ointment.

3. The tool according to claim 1, made in the form of an emulsion, as the target additives contains vaseline oil, emulsive wax, distilled water and ethyl alcohol.

4. The tool according to claim 1, executed in the form of a gel, as the target additives contains vaseline oil, ethyl alcohol, distilled water, polymethylmethacrylate.

5. The tool according to claim 1, made in the form of ointments, as the target additives contains ethyl alcohol, distilled water, borax, beeswax lanolin.



 

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