Nootropic and anxiolytic tool

 

(57) Abstract:

Usage: in medicine, in particular in the treatment of nootropic and anxiolytic funds. The inventive tool is made in the form of tablets, consisting of a nucleus containing 16,7-41.6 % of the weight. Mexidol, and polymeric membranes. The core as excipients contains white clay is 16.7 33.3 % for weight., potato starch - 16,7-33,7 % wt., calcium stearinovokisly - 0.3 to 0.5 wt%, the stearic acid is 0.3 - 0.5 wt%, talc - 0.5 to 1.0 wt%. and methylcellulose 25,0-50 % weight. with the addition of tween 80 to 8.3-25.0 % of the weight, and titanium dioxide to 8.3-25.0 % of the weight. This tool has a wide range of therapeutic action, has a pronounced anti-stress and antiamnesic effect. 7 table.

The invention relates to medicine, in particular nootropic and anxiolytic tool.

Known nootropic and anxiolytic agent is Mexidol (see M. D. Mashkovsky "Drugs", 1993, ch. II, sec. 216).

However, in clinical practice it is used only in the form of injections. The injectable form of Mexidol and provides long-lasting neuroprotective effect. In addition, when using Mexidol in the form of injections during the course of therapy the research Institute of aggressiveness, emotional reactivity, reduced anti-stress action and, therefore, not possible to assess the antiamnesic effect.

The present invention was to eliminate the above disadvantages of Mexidol inherent in its injectable dosage form.

Problem solved by creating dosage forms of Mexidol for oral administration. This dosage form is a tablet consisting of a core, active beginning which is Mexidol, and including auxiliary substances permitted for use Pharmacopoeia Committee, in particular, clay white, potato starch, stearinovokisly calcium, stearic acid, talc, methylcellulose. The core coated with a polymer, for example methylcellulose.

Tablets on the basis of Mexidol was prepared as follows.

Mexidol, clay white, potato starch, stearic acid, calcium stearinovokisly and talc sifted through sieves of appropriate sizes.

In the apparatus "Werner" load estimated number of Mexidol, white clay and starch. The mixture is thoroughly mixed, moistened with 3% solution of methylcellulose and g is mperature 50oC. the Dried granulate regranulated in the granulator to the diameter of the holes in the wall of the Cup 1.5 mm, optivault stearic acid, calcium stearinovokisly and talc and tabletirujut on a rotary press, biconvex tablets with a diameter of 9 mm and an average weight of 0.3 g

In the installation of fluidized bed pills-kernel is applied polymer shell of water-alcohol solution of methyl cellulose with the addition of Tween 80 and titanium dioxide. Research method the accelerated aging showed that the pill is valid for 5 years.

The resulting tablets were tested for "authenticity", raspadaemost and other requirements under GF XI, vol.2, S. 154. The results are shown in table.1.

The results of Mexidol release one tablet is given in table.2.

The effect of Mexidol inside and injections on the stress model Jouvet

Stress was modeled on rats according to the method Jouvet. Animals were placed in extreme conditions, putting on a small platform in a pool of water for 24 hours, which caused the deprivation of paradoxical sleep phase, limited mobility, isolation of animals and lead to stress. Feature model of stress on Jouvet is the lack of isbeginning stress on Jouvet observed violation orientation / exploratory behavior in the open field, which is characterized by a significant increase in the activity and the increase in the number of inappropriate movements.

It is established that Mexidol in a dose of 50 mg/kg orally once did not possess anti-stress effect. However, this effect appeared with long-term use of the drug (30-95 days) or with increasing doses of 125 and 250 mg/kg (once).

With the introduction of Mexidol in the injection of anti-stress effect was observed after a single dose of the drug at a dose of 50 mg/kg, However, long-term (30 day) introduction of Mexidol in the injection resulted in a decrease of this effect, associated probably with the advent of additional stress on a daily injections.

Thus, the extended 30-day and even 96-day use of Mexidol inside caused the preservation of anti-stress effect at a high level during the whole period of use of the drug, whereas injection of Mexidol this effect is not found.

Anti-stress effect of Mexidol after stress by Jouvet indicators orienting-exploratory behavior are given in table.3.

The effect of Mexidol inside and injections on the emotional status

The effect of Mexidol on an emotional one hundred is tableno, that a single injection of Mexidol orally or as injections did not cause shifts in emotional reactivity summary measures. Repeated (within 14 days) use of Mexidol in the dose of 50 mg/kg daily inside did not cause violation of the adequacy of response to the environment and did not change the emotional status. The introduction of Mexidol in the form of injections (17 days) increased the level of emotional response and animals more dramatically responded to the requirements of the test stimuli.

The effect of Mexidol inside and injections on the emotional status of mice is given in table.4.

Thus, significant differences in the effect of Mexidol in the form of injections or orally, which is that the long introduction of Mexidol in the injection violates the adequacy of the response to the situation and increase the level of emotional response, whereas Mexidol entering into such changes in emotional status is.

The effect of Mexidol inside and injections for aggressive behavior

Aggressive behavior was modeled in mice by feeding electrobalance irritation at the electrode floor (current of 0.45 mA), which were placed a pair of the setting, that a single application of Mexidol in the dose of 50 mg/kg, both internally and in the form of injections did not cause changes in aggressive behavior caused electrovalves irritation.

During long-term (21 or 36 days) introduction of Mexidol (50 mg/kg / day) orally were not recorded statistically significant changes in aggressive animals. In contrast, repeated injections of Mexidol (50 mg/kg / day) observed increased aggression and increased fights (fights) pairs of animals.

Thus, Mexidol entering into during the month does not cause increased aggressiveness, whereas injection of Mexidol aggressiveness after prolonged use increases.

The effect of Mexidol inside and injections on the aggressive behavior of a pair of mice electrode on the floor are given in table.5.

The effect of Mexidol inside and injections on the amnesia induced by scopolamine

The use of scopolamine as amazonvideo factor due to the fact that natural and especially pathological aging in humans (e.g., Alzheimer's) most clearly and accurately observed memory impairment associated with a deficit cholinergics is their memory was assessed by the standard technique of passive avoidance in the two (dark, light) camera with pain training in the dark compartment using equipment company Lafayette (USA). The safety or memory impairment was assessed by latency, time spent in light (safe) compartment of the camera when playing a reflex of passive avoidance after 24 hours of education or training and scopolamine.

Found that scopolamine causes amnesia trained, resulting in playback reflex after 24 hours, animals with short latent period came in a dark dangerous compartment.

Mexidol as in case of single oral administration and injection has expressed reliable antiamnesic action that is characterized by the increase of latency time in bright safe compartment of the camera. Long-term ingestion of Mexidol (50 mg/kg / day for 60 days) leads to increased antiamnesic effect. However, the injection of Mexidol in the same dose for 60 days or more to identify the antiamnesic effect of the drug was not possible due to the emergence and prevalence in the spectrum of pharmacological activity of heightened emotion and aggressiveness.

Antiamnesic datcyde inside and injections on memory in older animals

The study was conducted on older 18 and 24 months. white rats. Memory impairment was assessed by the method of passive avoidance in the camera Lafayette (USA) registration latency, time spent in light (safe) compartment of the camera when playing a reflex after 24 hours and 7 days after training (getting painful irritation in the dark compartment).

Control young animals after receiving painful irritation in the dark compartment of the camera (of course) well remembered trained and spent a long time in a safe, lighted compartment when playing a reflex even after 7 days after training.

The improvement under the influence of Mexidol memory impaired during aging are shown in table.7.

In animals older (18 months). and especially old age (24 months) there was a sharp deterioration of memory and they are short latent period passed in a dangerous dark compartment, where she received before painful irritation.

Mexidol (50 mg/kg / day orally) is 60 days had a distinct ability to improve memory in animals, increasing latency time of reflex. To the greatest extent antiamnesic effect was pronounced in the animals of old age, have a record of antiamnestic which enables you to assess the antiamnesic effect in connection with a change in emotional status of animals.

Thus, significant differences in the effect of Mexidol in its application by injection and orally. When using Mexidol in the form of injections during the course of treatment (more than 30 days) observed a change in the spectrum of pharmacological activity of the drug, resulting in increased aggressiveness, emotional reactivity, reducing anti-stress action and therefore cannot assess antiamnesic effect. It is likely that these effects are mediated more daily stress that animals experience when conducting daily injections.

In contrast, Mexidol entering into, as with a single and, in particular, with long-term use, has a pronounced anti-stress and antiamnesic effect which manifests itself in young and old animals. These effects not only not diminished, but even enhanced during the course of use of the drug. In addition, Mexidol with the inside does not cause negative changes in emotional status.

Thus, in comparison with Mexidol in the ampoule, which is the most indicated for acute violations, and to eliminate syndromes requiring high impact is given by injection may not be effective. TTT TTT

1. Nootropic and anxiolytic agent, containing Mexidol and the carrier, characterized in that it is a tablet consisting of a core containing a 16.7 41.6 wt. Mexidol and excipients, and a polymeric shell.

2. Nootropic and anxiolytic agent on p. 1, characterized in that the core as excipients contains clay white, potato starch, calcium stearinovokisly, stearic acid, talc and methylcellulose in the following ratio, wt.

Mexidol 16,7 41,6

Clay white 16,7 33,3

Potato starch 16,7 33,3

Calcium stearinovokisly 0,3 0,5

Stearic acid 0,3 0,5

Talc 0,5 1,00

The methylcellulose 0,3 0,5

and the shell contains methylcellulose, tween 80, and titanium dioxide in the following ratio, wt.

The methylcellulose 25,0 50,0

Tween 80 8,3 25,0

Titanium dioxide 8,3 25,0.

 

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