Hypnotic and sedative drug

 

(57) Abstract:

The tool is used for the treatment of insomnia - difficulty falling asleep, nocturnal awakenings, early awakening, secondary sleep disorders in mental disorders. The product contains as an active ingredient zopiclone, as the target auxiliary components of microcrystalline cellulose, milk sugar, modified starch or croscarmellose, starch, Aerosil and stearic acid or its salts. The tool is made in the form of coated tablets film-coated. A new tool with a specific combination of components provides optimal physico-chemical and technological properties of the dosage form and high bioavailability of drug substances. 4 C.p. f-crystals.

The invention relates to medicine, in particular to pharmaceutical drugs used in the treatment of insomnia (difficulty falling asleep, night waking, early waking, secondary sleep disturbance and psychiatric disorders).

One of the famous drugs used in the treatment of insomnia is zopiclone. This drug is disclosed in U.S. patent 3862149, IPC 07 D 51/72, 21.01 is possible dosage forms.

In U.S. patent 5786357, IPC a 61 K 31/495, 28.07.1998, the composition prepared in the form of tablets containing 7.5 mg of zopiclone and the target auxiliary components (lactose, starch and magnesium stearate).

The disadvantage of this dosage form can be seen in the fact that the active substance is highly susceptible to moisture, temperature and light, under the influence of which may alter the physico-chemical composition of the dosage form and the education it unacceptable impurities that contribute to the loss of pharmacological activity of medicinal substance.

The problem to which the invention is directed is getting sleeping pills and sedatives, all relevant pharmacopoeial requirements, qualitative and quantitative composition which will provide a high manufacturability of the drug using available components while providing guaranteed raspadaemosti and rapid release of his medicinal substance.

The problem is solved due to the fact that hypnotic and sedative drug containing as an active ingredient zopiclone and target vspomogatelnaya auxiliary components, it also contains microcrystalline cellulose, modified starch or croscarmellose and are presented in the following ratio of components, wt.%:

Zopiclone - 2-15

Microcrystalline cellulose - 3-50

Milk sugar - 15-65

Modified starch or croscarmellose - 1-10

Starch - 15-50

Aerosil - 1-10

Stearic acid or its salts - 0,1-1,2

this granulate contains microcrystalline cellulose, milk sugar and starch, and apadravya mixture contains zopiclone, modified starch or croscarmellose, Aerosil and stearic acid or its salts.

As a modified starch product may contain sodium carboximetilkrahmal.

The preferred form of sleeping pills and sedatives is tablet, film coated liner contains in accordance with pharmacopoeial requirements 0.0075 g of zopiclone.

Selection of components for the claimed dosage form was carried out experimentally. It was found that the active substance should be put into dosage form comprising apadravya mixture after step wet granulation, during which it may be undesirable influence of temperature and moisture.

As example can be mentioned the following composition of coated tablets, sleeping pills and sedatives

Zopiclone - 0.0075 g

Microcrystalline cellulose - 0,01155 g

Milk sugar - 0,0768 g

Sodium carboximetilkrahmal - 0,00495 g

Potato starch or corn starch - 0,0576 g

Aerosil - 0,00495 g

Magnesium stearinovokisly - 0,00165 g

Oksipropilmetiltselljuloza or oxypropylation - 0,0036 g

Polyethylene glycol 4000 - 0,0006 g

Titanium dioxide - 0.0008 grams

Average weight of tablet - 0.17 g

Obtaining tablets zopiclone 0.0075 g is carried out by the following technological scheme.

Sifted and weighed ingredients - milk sugar, microcrystalline cellulose are mixed, moistened with 5% starch paste. Ready wet mass is dried to a residual moisture content of 2.0-3.0% pre and magnesium stearinovokisly. The resulting mixture tabletirujut. The obtained tablets - engine cover film cover, which includes oksipropilmetiltselljuloza or oxypropylation, polyethylene glycol 4000 and titanium dioxide.

Used in the pharmaceutical composition with the stated ratio of the components ensures optimum physico-chemical and technological properties of the dosage form and high bioavailability of the drug.

Received drug use difficulty falling asleep, nocturnal awakenings, early awakening, secondary sleep disorders in mental disorders.

1. Hypnotic and sedative drug containing as an active ingredient zopiclone and target accessories - sugar, milk, stearic acid or its salts and starch, characterized in that as the target auxiliary components, it also contains microcrystalline cellulose, modified starch or croscarmellose and are presented in the following ratio, wt.%:

Zopiclone - 2-15

Microcrystalline cellulose - 3-50

Milk sugar - 15-65

Modified starch or croscarmelose contains microcrystalline cellulose, the milk sugar and starch, and apadravya mixture contains zopiclone, modified starch or croscarmellose, Aerosil and stearic acid or its salts.

2. Hypnotic and sedative drug under item 1, characterized in that it contains as modified starch sodium carboximetilkrahmal.

3. Hypnotic and sedative drug under item 1 or 2, characterized in that it is made in the form of tablets.

4. Hypnotic and sedative drug under item 3, characterized in that the tablet is covered with a film cover.

5. Hypnotic and sedative drug according to any one of paragraphs.1-4, characterized in that it contains 0.0075 g of zopiclone.

 

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