Solid dosage form sedatives, hypnotics and how you can get

 

(57) Abstract:

The invention relates to medicine, and pharmacy, and can be used to obtain relief funds. The image is that of a solid dosage form contains zopiclone how active active principle and the target additives to provide the desired shape, solubility and strength tablets, as an additional component dosage form contains: milk sugar, polyvinylpyrrolidone, calcium phosphate dibasic dowolny, potato starch, refined sugar and magnesium stearate at a ratio of components. Also proposed is a method of obtaining the claimed dosage forms. The invention provides high strength and the desired raspadaemost, ease of manufacture the offered tablets. 2 S. and 2 C.p. f-crystals.

The group of inventions relates to medicine, more precisely to the pharmacy, and can be used to obtain the solid dosage forms of relief funds. These tools include the zopiclone.

Zopiclone - sedative average length shortens sleep time, reduces the number of nighttime awakenings, increases total proglib negative consequences of its use upon awakening absent or not expressed. Repeat methods are not accompanied by accumulation of the drug and its metabolites. Sleep usually comes within half an hour after ingestion, lasts 6-8 hours (see Mashkovsky M. D. Medicines. Kharkiv, Torgsin", ed. 13, 1998, T. 1, page 28).

In the patent literature there are several papers related to this tool.

We identified U.S. patent N 5786357 from 28.07.1998, which describes a method and composition using optical isomer of zopiclone for treatment of sleep disorders, seizures, epilepsy.

Known also lined with RF application N 96117003, A 61 K 9/20, with priority from 01.09.96, according to which the dosage form of zopiclone is a tablet. When this multilayer tablet contains these multiple layers of gel-forming components. According to the authors of the invention, this tablet provides dosed selection active.

This above-cited object is chosen as the closest analogue of the invention.

The disadvantages of the prototype should include the complexity of the manufacture of the dosage form, the use of expensive gelling components, unknown in the Russian market. In addition, the gelling agent is scimi doses, not creating a hypnotic effect, and provide a different therapeutic effect.

The technical result of the claimed invention is to cheapen and simplify the manufacture of the dosage form while maintaining the required consumer qualities - the dosage of the active substance, pressuemosti, strength and raspadaemosti. In addition, there is a dose increase of excretion of the active substance so that 20-30 minutes is achieved dose in the blood needed to sleep.

The technical result is achieved by the fact that the solid dosage form of sedative, hypnotic, containing zopiclone as active, and additional components that provide the desired shape, solubility and strength tablets, as additional components it contains milk sugar, polyvinylpyrrolidone, calcium phosphate dibasic dowolny, potato starch, refined sugar and magnesium stearate, in the following ratio, wt.%:

zopiclone - 3,0-6,0

polyvinylpyrrolidone - 1,5-3,0

calcium phosphate dibasic dowolny - 6,0-25,0

potato starch - 5,0-16,0

refined sugar - 1,0-7,0

magnesium stearate - 0,1-1,0

Example. Sift the components necessary for the preparation of compositions. Prepare a concentrate consisting of zopiclone and potato starch in a ratio of 1:3.

In the mixer for 5-10 min mix powder ingredients: lactose, calcium phosphate dibasic, potato starch and concentrate zopiclone. The resulting mass is moistened with a mixture of 40% sugar syrup in an amount of 10 wt.% with a 20% solution of polyvinylpyrrolidone 11,76 wt.% and mix until evenly moistened mass. Damp granulation by passing the mass through a grid g is NP-60 at a temperature of 50-60oC for 10 minutes

This is followed by a dry granulation of transmission received tablet mass through sieve granulator with holes with a diameter of 1-2 mm Obtained tabletow mass optivault mixture of potato starch with stearate. Moreover, upon receipt of a mixture of powdered ingredients use 4,50-9,18 wt.% potato starch, and when dusting of 2.5-5.0 wt.%.

Received tabletow mass tabletirujut on the press with the diameter of the punch 8 mm, weight pills, 0,17 Form biconvex tablets with a break-line. The strength of the tablets 60-100 H, raspadaemost 5-7 minutes

The resulting tablets have the following composition, wt.%: zopiclon - to 4.41; PVP - 2,35; calcium phosphate dibasic dowolny - 15,29; refined sugar 4.26 deaths; magnesium stearate is 0.65; milk sugar - 62,35, potato starch - 10,69.

Thus, the resulting new composition for the preparation of tablets with the active ingredient in the form of zopiclone, optimal conditions for production of tablets from a new composition.

1. Solid dosage form of sedative, hypnotic, containing zopiclone as active and targeted supplements that provide Fort is built form contains the milk sugar, polyvinylpyrrolidone, calcium phosphate dibasic dowolny, potato starch, refined sugar and magnesium stearate in the following ratio, wt.%:

Zopiclone - 3,0 - 6,0

Polyvinylpyrrolidone - 1,5 - 3,0

Calcium phosphate dibasic dowolny - 6,0 - 25,0

Potato starch - 5,0 - 16,0

Refined sugar - 1,0 - 7,0

Magnesium stearate - 0,1 - 1,0

Milk sugar - Rest

2. The method of obtaining the dosage form sedatives, hypnotics, including mixing zopiclone and special additives, tableting, characterized in that the mixing zopiclone powder, potato starch, calcium phosphate dibasic dowolnego milk and sugar, then moisturize with a mixture solution of polyvinylpyrrolidone and sugar syrup, carry out wet granulation, drying, dry granulation, powder.

3. The method according to p. 2, characterized in that for moistening a mixture of 2 - 22%-aqueous solution of polyvinylpyrrolidone and 30 - 50% sugar syrup in a mass ratio of 1.0 - 1,17.

4. Method p. 2, characterized in that the powder are stearate.

 

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