Pharmaceutical composition for biocorrection of sympathetic - adrenal system

 

(57) Abstract:

The invention relates to biochemical pharmacology. The essence of the invention lies in the fact that the new composition comprises dopaminereleasing tool (CSD) and corticosteroid in the following ratio of components: CSD of 0.01 to 90.0 mg, corticosteroid of 0.1 to 90.0 mg, can additionally contain water-soluble vitamin preparation or combination of such drugs. The use of the invention will allow the bio-correction of diseases associated with impaired dopamine metabolism in incurable cases. 6 C.p. f-crystals.

The invention relates to the field of biochemical pharmacology, on some aspects of the search for drugs for biocorrection violations of sympathetic-adrenal system.

Deviations activity of the sympathetic-adrenal system associated with a number of not only physiological and functional States, but also with pathological disorders neurological and physiological status of the organism.

It is now known that an important role in the regulation of the sympathetic-adrenal system play dopaminergic processes.

Dopamine is a biogenic amine formed from tyrosine. the Noah nervous system (CNS). With effect on dopaminergic processes in the brain is linked to the mechanism of action of a number of neurotropic, including psychotropic drugs (M. D. Mashkovsky, Medicines, T. 1, 1994).

Identified different subtypes of dopamine receptors: D1, D2(there may be other to D5receptors).

The functions of the D1receptors associated with the stimulating effect of dopamine on the activity of adenylate cyclase and the formation of cyclic AMP.

Dioxyphenilalanin (abbreviated DOPA or DOPA) is a nutrient substance formed in the body from tyrosine and is the precursor of dopamine, which in turn is a precursor of norepinephrine.

As the medicinal product applied synthetic levogyrate isomer of dioksifenilalanina - L-DOPA, which is much more active than programalso isomer. Levodopa is well absorbed by ingestion.

Most of levodopa is converted by decarboxylation in the tissues (liver, kidney, intestine) into dopamine, which does not penetrate the blood-brain barrier. To reduce the decarboxylation of levodopa is used with inhibitors of DOPA-decarboxylase. The together with peripheral inhibitors (extracerebral) decarboxylation of L-DOPA. One such inhibitor is carbidopa [gidrazinometildofa; 3 - (3,4-dioksifenil)-2-hydrazino-2-methylpropionate acid].

The combination of L-DOPA with carbidopa (NAKA) leads to inhibition of the decomposition of L-DOPA in the blood and peripheral tissues and enhance L-DOPA in the brain, where L-DOPA is transformed into dopamine (C. N. Vasiliev, V. S. Irons "Sympathetic-adrenal activity in different functional States person", Medicine, 1985)

The study of the biochemistry of dopaminergic processes helped to open several mechanisms of action on the sympathetic-adrenal system to suppress many pathological disorders of the nervous system. These include such as neuromuscular disease dopamine etiology of cerebral palsy (CP), multiple sclerosis (MS), the syndrome Solineu-Vasileva, parkinsonism, amyotrophic lateral sclerosis (als), Alzheimer's disease, etc., and psycho-physiological and psychosomatic abnormalities. In particular, it is known that Parkinson's disease significantly reduced the content of dopamine in the basal nuclei and decreases melanin synthesis in a black substance. There is also evidence of a role in the pathogenesis of the syndrome of acetylcholine, therefore parks is their mediator systems.

A study of the prior art showed that at the present time to address these pathologies use effects on dopaminergic neurons and dopamine, however it can be used independently, and in combination with other biologically active components.

A study of the prior art revealed the following.

The invention described in the patent US N 4771073 relates to compositions and methods rectal injection of L-DOPA in the form of ether (predecessor) together with a decarboxylase inhibitor. In the formula: a method of obtaining esters of L-DOPA for rectal administration, chemical radicals (specific formula), which is mixed with pharmaceutically acceptable amount of a decarboxylase inhibitor selected from the group consisting of carbidopa and benserazide. The composition includes the already mentioned components, i.e., the ester of L-DOPA and carboxylase inhibitor.

In the patent RU 2076700 described method of preparation of solid pharmaceutical forms on the basis of L-DOPA and carbidopa monohydrate. The active principle is mixed with lactose, powdered cellulose, add aliphatic alcohols (2-4 C), granularit, dried, pressed V described orally injected dosage form for treating conditions associated with deficiency of dopamine containing medicinal substances levodopa and carbidopa and auxiliary substances regulated as desired drug release in the initial phase of application, when this dosage form contains a mixture consisting of 100-250 wt.h. levodopa, 10-25 wt.h. carbidopa and excipients 10-200%, representing a mixture of polymers consisting of polyvinyl alcohols of various degrees of saponification, or completely saponified polyvinyl alcohol with a non-zero residual content of acetyl, or a partially saponified polyvinyl alcohol, counting the number of drugs. This dosage form designed to release drugs for a certain period of time.

In international publication WO 98/5042 described method of treating mammals by introduction of an effective amount of derivatives of corticosteroids. Including disorders of the nervous system, Alzheimer's disease, cancer, etc.

In the patent US 5929059 a method for the treatment and prevention of toxicoses in humans and animals due to the introduction of an effective amount of pharmaceutically acceptable salts of corticosteroids, in particular dexamethasone-adrenal system, the metabolism of epinephrine and norepinephrine. Individual studies are carried out using the method of attogram developed by us. New composition additionally includes a glucocorticosteroid, which is contained in the composition with dopaminereleasing means (CSD), such as dopamine, diaminopimelic, monoamine oxidase inhibitor, or a combination of these means.

The technical result - the creation of a new pharmaceutical compositions on the basis of the CSD, which contains a corticosteroid, and may additionally contain a water-soluble vitamin. New track allows you to individualize pharmacotherapy, including the hormonal metabolism of the patient.

Composition method is carried out in the individual control of dopamine metabolism by determining the level of adrenaline and noradrenaline in the urine of the patient.

A new composition based on the CSD contains the corticosteroid in the following ratio of components, mg:

CSD - 0,01 - 90,0

Corticosteroid is 0.1 to 90.0

The composition may further contain a water-soluble vitamin preparation in an amount of from 0.1 mg to 1500 mg

The claimed composition provides a different formulation, taking into account the individual sweat is este dopaminereleasing means contains a drug selected from the group of levodopa, Naka, parlodel, selegiline, sinemet, madopar, as well as the combination, i.e. the combination of these tools.

As a corticosteroid drug composition comprises a drug selected from the group of: dexamethasone, hydrocortisone, prednisolone, triamcinolone, sinaflana, flumetasone pivalate, aldosterone, hypertension acetate, and a combination of these tools.

The composition may further contain a water-soluble vitamin selected from the group of: thiamin, Riboflavin, vitamin PP, Pantothenic acid, pyridoxine, folic acid, cyanocobalamin, ascorbic acid, vitamin P, and the combination of these vitamins.

The composition may be used for biocorrection in patients with abnormalities in the activity of the sympathetic-adrenal system: with neuromuscular diseases dopamine etiology, cerebral palsy, MS, syndrome Solineu-Vasileva, parkinsonism, BASS, Alzheimer's disease and other Claimed composition can be applied in humans and animals.

Selection of the desired pharmaceutical composition is administered by adrenoliticheskoe examination of the urine.

The invention posn is a - 35

Dexamethasone - 35

Example 2:

Naka - 40

Dexamethasone - 10,0

Ascorbic acid 500

Example 3:

Parlodel - 0,1

Hydrocortisone - 10,0

Folic acid - 0,2

Thiamine - 0,1

Riboflavin - 0,3

Ascorbic acid - 200,0

Example 4:

Naka - 50

Flumetasone pivalate - 5,0

Riboflavin - 0,5

Vitamin PP - 5,0

Pantothenic acid - 1,0

Vitamin B12- 10,0

Ascorbic acid 100,0

Example 5:

Madopar - 50,0

Levodopa - 5,0

Prednisolone - 0,5

Ascorbic acid - 250,0

Vitamin P - 50,0

Thiamine - 0,5

The new composition was provided to more than 300 patients-volunteers for biocorrection of many pathologies such as Parkinson's disease, cerebral palsy, down syndrome Solineu-Vasiliev syndrome Vasiliev, Alzheimer's disease, and various neuro-physiological and other disorders associated with abnormal dopamine metabolism. A positive result was obtained in not less than 55% of cases, and when the syndrome Vasiliev in 100% of cases.

The use of the invention allows the bio-correction of various pathologies dopamine metabolism at the level of individual approaches, allows us to solve the problem with the Zeta - 5

Hydrocortisone - 10

Sinaflana - 1

Ascorbic acid - 100

Riboflavin - 0,5

Example 7:

Naka - 80

Selegiline - 5

Madopar - 5

Prednisone - 10

Sinaflana - 5

Aldosterone - 5

Ascorbic acid - 100

Vitamin P IS 0,1

Example 8:

Levodopa - 20

Sinemet - 10

Madopar - 5

Dexamethasone - 10

Flumetasone pivalate - 5

Aldosterone - 5

Pyridoxine - 5

Ascorbic acid - 50

Pantothenic acid - 0.5

Example 9:

Parlodel - 10

Madopar - 5

Triamcinolone - 10

Aldosterone - 0,2

Ascorbic acid - 100

Thiamine - 5

The ciankobalamin - 0.2 to

1. Pharmaceutical composition for biocorrection of sympathetic-adrenal system on the basis of dopaminereleasing funds (CSD), characterized in that it further comprises a corticosteroid in the following ratio of components, mg:

CSD - 0,01 - 90,0

Corticosteroid is 0.1 to 90.0

2. The pharmaceutical composition under item 1, characterized in that as the CSD contains the precursor of dopamine, diaminopimelic, monoamine oxidase inhibitor, or a combination of these tools.

3. The pharmaceutical composition under item 1, 2, clinciu these tools.

4. The pharmaceutical composition under item 1, characterized in that in contains corticosteroid dexamethasone, hydrocortisone, prednisolone, triamcinolone, sinaflana, flumetasone pivalate, aldosterone, hypertension acetate, or a combination of these tools.

5. The pharmaceutical composition according to paragraphs.1 to 4, characterized in that the composition further comprises a vitamin preparation.

6. The pharmaceutical composition according to paragraphs.1 to 5, characterized in that as a vitamin product contains a water-soluble vitamin in an amount of 0.1 - 1500 mg.

7. The pharmaceutical composition according to paragraphs.1 - 6, characterized in that it contains thiamine, Riboflavin, vitamin PP, Pantothenic acid, pyridoxine, folic acid, cyanocobalamin, ascorbic acid, vitamin P, or a combination of these vitamins.

 

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1 ex

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