Cheek pouch (transbuccal) pharmaceutical composition

FIELD: pharmaceutical industry.

SUBSTANCE: pharmaceutical composition exhibiting neotropical, antiepileptic, sedative, and antistress activities, normalizing metabolic processes in body, contains aminoacetic acid and pharmaceutically acceptable carrier constituted by mixture of sorbitol and crosslinked carboxymethylcellulose sodium salt at weight ratio between 1:1 and 1:3 with additive selected from vinylpyrrolidone/vinyl acetate, stearic acid, stearic acid sodium salt, and mixtures thereof.

EFFECT: increased bioavailability and active component release velocity.

2 cl, 1 tbl


The invention relates to medicine, specifically to hominids (transbukkalnye) pharmaceutical compositions comprising aminouksusnoy acid (glycine)with nootropic, anti-epileptic, anti-stress, sedative, and normalizes metabolic processes in the body by the action.

Glycine is used in pharmacology in stress conditions, emotional stress, high anxiety, emotional lability, nervousness, neurosis-like States, dystonia, the consequences of neuroinfections and traumatic brain injury, various forms of encephalopathy, including alcoholic dysfunction, sleep disorders, to improve mental health, including adolescents with deviant behaviours in acute ischemic stroke (Register of medicines of Russia. Encyclopedia of drugs. Annual collection. 10 release. 2003 Moscow. Publishing house “radar-2003”, str).

Known drug anti-stress, stress-protective, nootropic action of sublingual application, comprising the amino acid glycine or its pharmaceutically acceptable salt and a pharmaceutical carrier, described in the patent of the Russian Federation No. 2025124. In the same document describes a method for the prevention and treatment of stress conditions by sublinguales introducing an effective amount of FA is pharmaceutical drug, containing glycine, and how to improve mental performance.

Famous drug is characterized in that it contains the active ingredient glycine in an amount of 0.1-0.2 g per tablet, as a pharmaceutical carrier preferably contains methylcellulose in an amount of 0.5 to 2 wt.%.

In the patent of Russian Federation №2082398 described a method of treatment of the acute period of ischemic stroke using glycine entered during the first five days of illness sublingual tablets to 1.0 g once a day.

In the patent of Russian Federation №2171673 described pharmaceutical composition for the manufacture of tablets and prolonged action, in particular sublingual application, and how you can get it. The pharmaceutical composition contains 98,1-and 99.8 wt.% not agglomerated particles of drug substance, coated with a polymer shell microcapsules), including 97,6-99 wt.% drug and 1-2,4 wt.% film-forming, 0.1 to 1.0 wt.% lubricating and 0.1 to 0.9 wt.% water. In the song entered the Ripper, representing the medicinal substance in an amount of 0.1-10 wt.% by weight of the mixture. As a medicinal substance can be used aminouksusnoy acid. As the lubricating component can be used stearic acid, its pharmaceutically acceptable salt, or a mixture thereof. As plantours the nes apply soluble in water or in an organic solvent or a mixture of the cellulose ethers. Raspadaemost this dosage form is at least 10 and no more than 30 minutes.

However, because raspadaemost sublingual tablets glycine in the case of sublingual (from Latin sub under, lingua - language) application method is up to 30 minutes, this is not always convenient and sometimes even undesirable, especially for children and the elderly. As you know, children are mostly not differ needed patience and can swallow the sublingual tablet before it resorption, which certainly complicates the action of a medicinal product intended for sublingual(sublingual) administration.

In addition, the elderly and children have weak swallowing ability, and therefore under-tongue (sublingual) method of application known drug for them is also difficult. The same argument can be given for the use of sublingual application method paralyzed patients.

Thus, it is important to establish a drug dosage form containing glycine as an active ingredient, having a much shorter time for complete dissolution in the oral cavity of the patient, and therefore more convenient and fast.

The problem is solved by the creation of a cheek or the so-called transbukkalno applications Leka is the only drug containing aminouksusnoy acid (glycine) or its pharmaceutically acceptable salt as the active substance. (According to the “List of names dosage forms used for registration of medicinal products”, approved by the Ministry of health of Russia, there are no 27.7 tablets cheek, No. 27.8 sublingual tablets.)

The new drug has a higher rate of dissolution in the oral cavity of the patient. This technical result is achieved by the fact that the claimed preparation containing as an active substance glycine and pharmaceutically acceptable carriers, and optionally contains sorbitol and Primerose (sodium salt of cross-linked carboxymethylcellulose (croscarmellose) mass ratio of from 1:1 to 1:3.

As pharmaceutically acceptability holders can also be used variants of a copolymer of vinylpyrrolidone with vinyl acetate, stearic acid and its salts, preferably calcium and magnesium, and mixtures thereof.

To improve the organoleptic properties of the pharmaceutical composition is proposed to introduce a composition pharmaceutically suitable excipients, for example, sweeteners and flavorings. As a sweetener can be used, for example, aspartame - N - L - alpha-aspartyl - L - phenylalanine - 1 - methyl ether. As flavourings can is to be used pharmaceutically suitable flavorings, for example, lemon and menthol.

The way to obtain a new composition includes a mixture of powders of glycine and pharmaceutical carriers with an aqueous solution of a copolymer of vinylpyrrolidone with vinyl acetate, wet granulation, drying, dry granulation and dusting. To give a composition of the form of tablets obtained after dusting composition is pressed on a tablet machine.

Obtained in this way the finished dosage form has a high raspadaemost 2-3,5 minutes, taste and meets the requirements of the State Pharmacopoeia XI.

The invention is illustrated by the following examples (table 1).

Table 1
IngredientsThe content of ingredients, wt.%
Kollidon VA 642-2
Polyplasdone 630-2-
Sorbitol crystalline0,641,330,88
Stearic acid -0,95-
Magnesium stearate0,97--
Calcium stearate--0,97
The lemon flavor0,720,87-
The total number of100100100
Raspadaemost, min
Note: kollidon VA 64 and polyplasdone 630 - brand water-soluble copolymer of vinylpyrrolidone with vinyl acetate.

1. Pharmaceutical composition having nootropic, anti-epileptic, sedative, anti-stress, normalizes metabolic processes in the body effect, for hominids (transbukkalnye) form of the drug containing an effective amount aminouksusnoy acid or its pharmaceutically acceptability of salt as the active ingredient and the pharmaceutical carrier consisting of a mixture of sorbitol and sodium salt of cross-linked carboxymethyl cellulose in a weight ratio of from 1:1 to 1:3 in combination with an additive selected from the group comprising copolymers vinylpyrrole is it with vinyl acetate, stearic acid, a salt of stearic acid or mixtures thereof.

2. The pharmaceutical composition according to claim 1, characterized in that it contains aminouksusnoy acid or its pharmaceutically acceptable salt in an amount of 0.25 to 1 g in a single tablet.


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