Nootropic agent

 

(57) Abstract:

The invention relates to medicine, and concerns nootropic agents of broad-spectrum. The invention lies in the fact that the proposed tool is a syrup containing pantogram and excipients: glycerol, sorbitol, citric acid, aspartame, aromatic essence, sodium benzoate. The invention provides for the creation of a convenient dosage form for pediatric psychiatry and neurology, in addition, has a higher bioavailability.

The invention relates to medicine, specifically to the pharmaceutical industry, namely to the receiving means, having neuroprotective properties of mixed type with a wide range of actions affecting the gamma-aminobutyric acid (GABA).

Known nootropic drug on the basis of the GABA (eminole), which has a marked effect on the functional activity of the Central nervous system, however, poor penetration of GABA through hematoencephalic barrier makes it difficult to apply aminolink in the clinic for the treatment of Central disorders [1] .

Known nootropic drug piracetam, the first drug of this class, which when broken in various diseases [2] .

The disadvantage of the drug are some limitations in its application: the tool is not used for younger children (under 8 years), in addition, the drug has no anticonvulsant effect and, moreover, increases the risk of convulsive readiness that limits its use in practice of treating patients with a variety of paroxysmal States.

It is also known nootropic agent pantogam - calcium salt gamopetalous acid [3] . The tool used in children with mental deficiency (mental retardation and mental retardation, and delayed speech development. The product is shown in the combined therapy or in some cases alone for the treatment of children suffering from epilepsy. Adults pantogram prescribed in combination with anticonvulsant drugs for epilepsy with slow mental processes. The tool is also used for disorders of urination in children and adults (enuresis and daytime incontinence).

The disadvantage of the drug is that it only comes in the form of tablets of 0.25 and 0.5, With a daily dose for children 0,75 3 g children have to take a day from 3 to 12 tablets depending on the age is the one it is difficult to enter the desired dose children younger and sometimes older. This is further complicated by the fact that the tool itself has a bitter taste.

The present invention was the creation of dosage forms pantogama, suitable for use in child psychiatry and neurology.

The problem is solved by creating a new dosage form pantogama - 5-20% of the syrup, which in addition to pantogama include glycerin, sorbitol, citric acid, aspartame, aromatic essence, sodium benzoate, water in the following ratio, wt. %:

Pantogam - 5-20

Glycerin - 25-35

Sorbitol - 10-20

Citric acid - 0,20-0,25

Aspartame - 0,02-0,08

The essence of aromatic - 0,05-0,15

Sodium benzoate 0.05 to 0.15

Water - the Rest

Use pantogama in the form of 5-20% syrup corresponds to 0.25 to 1.0 g of the drug in 5 ml (1 teaspoon), which is determined by the ease of administration depending on the dose prescribed by the doctor. Use as excipients in the preparation of syrup sorbitol improves the taste of money, in addition, sorbitol is more indifferent substance than is usually used in syrups sugar, because the child's body does not always has from 10 to 20%, that you do not exceed the recommended for children dose of sorbitol given a daily dose of pantogama. To enhance taste the syrup enter the citric acid. When you reduce the amount of citric acid is less than 0.2% was not sufficient to improve the taste of the syrup, and when the number of 0.25% was observed precipitation of the calcium salt of citric acid. In use as a sweetener aspartame in the amount of 0.02 to 0.08%, which is traditionally used in syrups in similar concentrations. To impart a pleasant flavor and aroma in the drug being aromatic food essence, traditionally used as corrigenda. Sodium benzoate - stabilizer commonly used in the preparation of liquid forms of drugs. The choice of glycerin to prepare syrup is common and is caused in this case the experimental data of the good solubility of all the components of the drug.

The invention consists in the following.

Dissolve gradually under stirring and heated to 55-60oWith the sorbitol in purified water. To the resulting solution was added citric acid and stirred at this temperature until complete dissolution. Then pricego add the glycerin, make sodium benzoate and essence of aromatic, add the missing amount of purified water and mixed until a homogeneous mass.

To obtain the funds used pantogram corresponding FS 42-2391-99, glycerin - FS 42-2204-84; sorbitol - VFS 42-614-76 or THE 64-5-17-86, citric acid - GOST 908-79, aspartame-NF 18 USP 23, S. 2215, the essence of aromatic food - OST 18-103-84; sodium benzoate - FS 42-2458-86; purified water FS 42-2619-97.

The method of obtaining the proposed framework is illustrated by the following example.

Dissolve to 20.0 g of sorbitol in 60 ml of purified water with stirring and heated to 60oC. To the resulting solution was added 0.2 g of citric acid and stirred at this temperature until complete dissolution. To the mixture was added a solution of 5.0 g pantogama and 0.02 g of aspartame in 15 ml of purified water and mix thoroughly until a homogeneous mass. After that add on parts 25 g of glycerin, and then introduce 0.1 g of sodium benzoate and 0.1 g of aromatic essences. Add water to volume of 100 ml and stirred until a homogeneous mass.

Syrup pantogama used by a doctor from one to six to twelve teaspoons a day. With Orci taste pantogama masked auxiliary substances.

Experimental study of neuropharmacological activity of a new dosage form conducted in the laboratory of pharmacology of the State scientific research Institute of vitamins in accordance with the recommendations of the Pharmacological Committee of Ministry of health of Russia.

The obtained results of experimental study of 5-20% syrup pantogama on major tests neuropharmacological screening indicate that:

a) the drug has a pronounced deprimiruty effect characterized by a decrease in the spontaneous motor activity and fenaminovoj hyperactivity, depression indicative reactions, the prolongation of sleeping pills effects of barbiturates;

b) the drug has antiaggressive action, which leads to weakening of aggressive reactions in animals in pain irritation;

C) the drug is an anticonvulsant effect, moderate when interacting with carazolol and bicucullin and more pronounced on the test of maximal electroshock;

g) the product has a protective effect on the model gistologicheskoe hypoxia;

d) the drug has a positive effect on mental function in experimental animals, improving the processes of remembering and learning in matakishi, myorelaxation and lack of coordination of movements;

W) for tests neuropharmacological screening the effectiveness of the drug in the form of 5-20% of the syrup is almost identical to the activity of the solution pantogama made with pharmacopoeial substance.

There was also a comparative analysis of bioavailability syrup pantogama in relation to the substance and form of tablets. Using pharmacokinetic studies in animal experiments it was shown that the relative bioavailability pantogama of the syrup was 159,59% compared to tablets pantogama.

Thus, data from studies of pediatric dosage forms showed that the drug in the form of 5-20% syrup manifests expressed psychopharmacological activity and has the same properties as pantogram in tablets. The drug can be recommended for clinical trials in pediatric mental practice on the testimony previously established for pantogama.

Literature used.

1. C. M. Kopelevich. USP, 48(7), 1273-1296 (1979).

2. T. A. Voronina, S. B. Seredenin. The experts. and the wedge. pharmacology, 61(4), 3-8 (1998).

3. Pantogram. Twenty years of experience in p the substances, characterized in that it is a syrup and as excipients contains glycerin, sorbitol, citric acid, aspartame, aromatic essence, sodium benzoate in the following ratio, wt. %:

Pantogam - 5 - 20

Glycerin - 25 - 35

Sorbitol - 10 - 20

Citric acid - 0,20 - 0,25

Aspartame - 0,02 - 0,08

The essence of aromatic - 0,05 - 0,15

Sodium benzoate 0.05 to 0.15

Water - The Rest

 

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