Composition for improving brain blood circulation

 

The invention relates to medicine, namely to drugs that improve blood circulation in the brain. The essence of the invention is that the composition for improvement of brain blood circulation contains Vinpocetine and piracetam as active ingredients and put into a hard gelatin capsule, and the target additives contains sugar, milk and calcium stearate in the following ratio of components, g per 1 capsule: Vinpocetine 0,0045-0,0055, piracetam 0,3600-0,4400, sugar, milk 0,0990 - 0,1210, calcium stearate 0,0045-0,0055. The technical result is the creation of a capsulated form of a drug that has the combined effect of Vinpocetine and piracetam and expansion of the range of medicines for improvement of brain blood circulation. table 2.

The invention relates to medicine, specifically to drugs that improve blood circulation in the brain.

In recent years, widespread in medical practice has received (316th-Bornemann-14-carboxylic acid ethyl ester (Vinpocetine), used in violation of cerebral circulation of different origin [ND 42-what is it.

Known solid dosage form of Vinpocetine in the form of tablets, including Vinpocetine and excipients, M. H.: Vinpocetine -1,0, colloidal silicic acid - 0.25, starch - 19,25, lactose - 28,0, talc - 1.0, stearate and 0.5 [Pat. 0305181 EP. Ethyl-(+)-apovincaminate for treating demyelinization clinical patterns of autoimmune origin]. The drug has a low ratio of active substance to the target additives, which leads to an increase in the duration of treatment and the introduction into the organism of a large number of adverse effects on the body talc.

Well-known drug of Vinpocetine in the form of tablets containing (m h): Vinpocetine - 1,0, lactose - 22,8, microcrystalline cellulose and 2.7, stearate - 0,54 [Pat. 0689844 EP. Complexes of vinpocetine formed with cyclodextrins, process for their preparation and pharmaceutical compositions containing them]. This dosage form is characterized by a slow release of Vinpocetine (less than 20% within one hour).

Well-known drug for improvement of brain blood circulation Vinpocetine-acre tablets [U.S. Pat. 2155039 of the Russian Federation. Pharmaceutical composition for improving cerebral circulation and method thereof]. It is made in pill form and contains as active substance Vinpocetine, as well as pharmaceutically acceptable vspomogatel the ratio of ingredients, wt.h.: Vinpocetine - 1.0, Aerosil - 0,3-3,64, starch - 4,3-12,4, salt of stearic acid is 0.05 to 0.2.

Well-known drug for improvement of brain blood circulation Tablet Vinpocetine 0.005 g [VFS 42-2937-99. Tablet Vinpocetine 0.005 g]. It contains Vinpocetine 0,0050 g and auxiliary substances (sugar milk 0,1965, Aerosil - 0,0010, potato starch - 0,0400, talc - 0,0050, magnesium stearinovokisly - 0,0025).

For more than 20 drugs registered in Russia under 6 trade names, dosage form substance of Vinpocetine are tablets or perfusions [Register of medicines of Russia (RLS 2001). - M.: "radar", 2000] . They are all more or less have the characteristic tabletirovannoj forms noted deficiencies and implement only the inherent substance of Vinpocetine mechanisms of pharmacological action.

Known 2-oxo-1-pyrrolidineethanol (piracetam), which has a neuroprotective effect at very low toxicity, a positive influence on integrative brain functions [FS 42-1943-99. Piracetam].

In Russia registered more than 150 drugs piracetam with 16 trade names.

Known drug Piracetam 0.4 g capsules [VFS 42-8449-98. Piracetam 0.4 g capsules] . It contains 1 ka is

It is known that piracetam increases the effects of increased cerebral blood flow of funds [Register of medicines of Russia (RLS 2001). M:"radar", 2000].

Known compositions, including Vinpocetine and piracetam for the treatment of various manifestations of insufficiency of cerebral circulation. It usually extemporally compositions may contain other active substances, taking into account the compatibility of substances and individual manifestation of the disease.

There is a method of treatment of diseases of the vascular sclerosis Genesis by intravenous injection of diazepam, Cavinton and nootropil in one dosage form composition of the saline solution [U.S. Pat. 2126250 of the Russian Federation. The method of treatment of psychopathological syndromes edge level of vascular sclerosis Genesis] . The composition includes diazepam (5 mg), Cavinton (Vinpocetine) (2.0 ml - 0,0100 g) and nootropil (kg) (5.0 ml 1.0 g) in 200.0 ml of physiological solution N 12. Such a dosage form of the drug can be used only in a hospital environment.

The objective of the invention is the creation of a capsulated form a new, combined with the action of Vinpocetine and piracetam drug. The expansion of the range of the ith State Pharmacopoeia [State Pharmacopoeia of the USSR. XI ed: In 2 vol. - M.: Medicine, vol.1, 1987; vol.2, 1990].

The problem is solved by the creation of a capsulated form of a new pharmaceutical composition WINPATROL. This dosage form is a gelatin capsule which is placed the actual amount of the substances of Vinpocetine, piracetam and as active principle and excipients, licensed Pharmacopoeia Committee, in particular, milk sugar and magnesium walls-renovatory. Used capsules manufactured by known techniques [State Pharmacopoeia of the USSR. XI ed: In 2 vol. Vol. 2. - M. : Medicine, S. 143]. Composition one capsule, g: Vinpocetine - 0,0045-0,0055 g, pyracetam - 0,3600-0,4400 g sugar, milk 0,0990-0,1210 g calcium stearate - 0,0045-0,0055,

The proposed ratio of active substances and specific additives found experimentally and is optimal, satisfying all the requirements of the current Gosfarmakapei XI publications and regulatory documents on capsule WinPatrol.

The drug is produced in the following way: in a mixer of the type "drunken barrel" download sifted powders of Vinpocetine (FSE-42-or import LP 429175-98), piracetam (FS 42-1943-99), milk sugar (OST 4963-85) and calcium stear hard gelatin capsules of size 0. The average weight of the contents of the capsule - 0,5200, the Deviation of the mass content of each capsule of the average weight of not more than10% (from 0.47 to 0.57 g).

Capsulotomy mixture of powders has flowability of 8.70.6 g/s and bulk density 77818 kg/m³.

WinPatrol is a capsule yellow with red caps, the size of the capsules 0. Content capsules, powder white or almost white.

Studies of accelerated aging showed that WinPatrol is valid for three years (observation period 3 years 6 months).

The obtained capsules were tested for authenticity and other requirements under the global Fund XI (PL. 1, 2). Thus, uniformity of dosage was 7.5% (at the rate of 10.0%), raspadaemost - 18-23 min (at a rate of not more than 30 min), release 45 rpm 81-88% (at a rate of not less than 75%).

The drug is new, which combines the well-known tablets of Vinpocetine 0,005 grams piracetam capsules 0,4, In foreign pharmacopoeias are not described, developed on the basis of the data obtained in the analysis of pilot scale batches of the drug gained Canonpharma production" and the basis of regulations on production of the drug.

notice to improve cerebral circulation, comprising an effective amount of Vinpocetine and piracetam as active substances and additives target, characterized in that it is enclosed in a hard gelatin capsule and the target additives contains sugar, milk and calcium stearate in the following ratio of components, g per 1 capsule: Vinpocetine - 0,0045-0,0055, piracetam - 0,3600-0,4400, sugar, milk 0,0990-0,1210, calcium stearate 0,0045-0,0055.