Means possessing neuroleptic activity

 

(57) Abstract:

The invention relates to the field of medicine and relates to means neuroleptic action on the basis of haloperidol. The tool contains haloperidol, potato starch, food gelatin, talc, magnesium stearic acid and sugar of milk at a certain ratio of components. The tool is made in the form of tablets by weight of 0.12 and 0.30 g when the content of haloperidol 0,0015 and 0.005 g, respectively. Neuroleptic agent satisfies the requirements of the global Fund XI, vol. 2, S. 154, has good raspadaemost due to selection of excipients. 2 C.p. f-crystals.

The invention relates to the field of medicine and for the receiving neuroleptic drugs on the basis of haloperidol.

Haloperidol is one of the most active modern neuroleptics. It has a sedative effect, potentiates the action of hypnotics, narcotics and analgesics, blocks Central noradrenergic and particularly Central dopaminergic receptors, has antiemetic action.

Haloperidol is an effective means to relieve various kinds of excitation, especially during manic States, astroballe and apathy, has an activating effect.

Haloperidol is used with schizophrenic psychoses, manic state, when agitated depression, oligophrenia, involutional, epileptiform, alcoholic psychosis and other diseases.

Haloperidol is effective for relief of pain, agitation, nausea and vomiting in acute coronary insufficiency. As an antiemetic used in vomiting of different origin.

Known dosage forms of haloperidol in the form of tablets 0.0015 and 0.005 g (M. D. Mashkovsky, Medicines, M., 1993, ch. I, sec. 76).

Closest to the technical essence and the achieved result is a solid dosage form that contains in addition to the active substance, which can be and haloperidol, a matrix material consisting of gelatin, pectin, soy protein fiber, and one or more amino acids (EN p. 2131244, a 61 K 9/14, 1999).

The aim of the present invention is to obtain on the basis of haloperidol domestic drug in pill form, corresponding to the requirements of the monograph enterprises (FSE), developed by JSC "Bryntsalov-A".

For refusesto haloperidol and excipients - potato starch, milk sugar, food gelatin, talc and magnesium stearic acid.

These ingredients are contained in a medicinal product in the following ratio, wt.%:

Haloperidol (in terms of 100% substance) - 1-2

Potato starch - 25-40

Food gelatin - 0,1-1,5

Talc - 3

Magnesium stearic acid is Not more than 1

Milk sugar - Rest

The drug is made in the form of tablets weight 0.12 g and 0.30 g Tablet weight 0.12 g contain haloperidol is 1.35%, the rest excipients. Tablets weighing 0,30 g contain haloperidol 1,67%.

Tablets are white or white with a slightly yellowish color. Time raspadaemosti - no more than 15 minutes. 45 minutes in the solution passes at least 75% of the active substance. The total content of impurities does not exceed 1.0%.

The shelf life of the tablets is 2 years.

Example 1. The reception of tablets haloperidol - 0.0015 g

Composition per tablet, g:

Haloperidol (in terms of 100% substance) is 0.0015

Potato starch - 0.04

Food gelatin is 0.0015

Talc - 0,0024

Magnesium stearic acid - 0,0012

Milk sugar - Rest

The raw materials are crushed milk and damp granulation, using as granulating liquid aqueous solution of gelatin. The obtained granulate is dried, sieved, optivault talc, magnesium stearate and tabletirujut, receiving tablets haloperidol weight of 0.12 g

Example 2. The reception of tablets haloperidol 0,005 g

Composition per tablet, g:

Haloperidol (in terms of 100% substance) - 0,005

Potato starch - 0,09923

Food gelatin - 0,00137

Talc - 0.003

Magnesium stearic acid - 0.003

Milk sugar - Rest

Proceed as described in example 1, obtaining tablets haloperidol weight 0,30,

1. The tool that has antipsychotic effect, characterized by the fact that it is made in pill form and contains the active ingredient haloperidol and excipients - potato starch, milk sugar, food gelatin, talc and magnesium stearic acid is in the following ratio, wt.%:

Haloperidol 1-2

Potato starch - 25-40

Food gelatin - 0,1-1,5

Talc - 3

Magnesium stearic acid is Not more than 1

Milk sugar - Rest

2. Means under item 1, characterized in that it is a tablet weight of 0.12 g and soda - Else

3. Means under item 1, characterized in that it is a tablet weight of 0.30 g and contains the indicated ingredients in the following ratio, g:

Haloperidol - 0,005

Excipients - the Rest

 

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