Blonanserin-contained oral preparation for treating schizophrenia

A technology for schizophrenia and oral preparations, which is applied in the field of pharmaceutical preparations, can solve problems such as no production, and achieve the effects of good solubility, low dosage, and simple preparation process

Active Publication Date: 2010-07-07
LIVZON PHARM GRP INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, this product is neither imported nor produced in China.

Method used

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  • Blonanserin-contained oral preparation for treating schizophrenia
  • Blonanserin-contained oral preparation for treating schizophrenia
  • Blonanserin-contained oral preparation for treating schizophrenia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Composition and preparation method of compressed tablet with active ingredient 2 mg

[0036] Mix 2.0g of active ingredients, 20.0g of microcrystalline cellulose, 15.0g of pregelatinized starch, 36.0g of lactose, 6.0g of croscarmellose sodium, and 4.0g of hydroxypropylmethylcellulose, and mix them evenly, and use 50wt % ethanol aqueous solution is the soft material made of wetting agent, granulated with a 30-mesh screen, ventilated and dried at 55°C, granulated, added with 0.5g of micro-powdered silica gel and mixed evenly, pressed into about 1000 round tablets, each containing 2mg of active ingredient, namely Have to compress the tablet.

Embodiment 2

[0038] Composition and method of preparation of compressed tablet with active ingredient 4 mg

[0039] Mix 4.0g of active ingredients, 40.0g of microcrystalline cellulose, 20.0g of pregelatinized starch, 66.0g of lactose, 8.0g of croscarmellose sodium, and 8.0g of hydroxypropylmethylcellulose, and mix them evenly, and mix them with 50wt % ethanol water solution is the soft material made of wetting agent, granulated with a 30-mesh screen, ventilated and dried at 55°C, granulated, added with 1g of magnesium stearate and 1g of micro-powdered silica gel, mixed evenly, and pressed into about 1000 round tablets, each containing Active ingredient 4mg, that is, compressed tablets.

Embodiment 3

[0041] Composition and method of preparation of compressed tablet with 8 mg active ingredient

[0042] Mix 8.0 g of active ingredients, 60.0 g of microcrystalline cellulose, 30.0 g of pregelatinized starch, 100.0 g of lactose, and 12.0 g of croscarmellose sodium, and use 3 wt % hydroxypropyl methylcellulose aqueous solution as Soft material made of wetting agent, granulated with 30-mesh screen, ventilated and dried at 55°C, granulated, added with 2g of magnesium stearate and 1g of micro-powdered silica gel, mixed evenly, pressed into about 1000 round tablets, each containing 8mg of active ingredient, A compressed tablet is obtained.

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PUM

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Abstract

Disclosed is a Blonanserin-contained oral preparation for treating schizophrenia, using a 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-cycloocta[b]pyridine as ingredient, and one or more pharmaceutically acceptable excipients. The preparation method comprises the steps of mixing the 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-cycloocta[b]pyridine and the alternative thinner, adhesive, disintegrant, abhesive and lubricant with an appropriate amount of humectants to prepare soft wood, sieving to prepare wet granules, drying the wet granules, sieving and integrating the granules to prepare oral preparation, wherein, the Blonanserin is 0.1-30 per cent of the preparation by weight. The preparation is applicable to administrate 1-2 times per day in 1-2 preparation units each time, and used for controlling the concentration of the 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-cycloocta[b]pyridine in the plasma of human body, thus enabling the 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-cycloocta[b]pyridine to play a role in treatment.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a compound containing 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro Oral formulations of aryl octa[b]pyridines and methods for their preparation. Taking this preparation makes 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydroaromatic octane in human plasma [b] Pyridine was maintained at therapeutic levels. Background technique [0002] Schizophrenia is a disorder characterized by deep cognitive and emotional dissociations that affect the most basic human behaviors, such as language, thought, perception, and self-awareness. Symptoms of the disease include a wide range, the most common being mental disorders, such as hallucinations, paranoia and delusions. [0003] According to statistics, the prevalence rate of schizophrenia in the world is 0.5% to 1.5%, and only 5% of all treated patients can finally fully recover. I...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61P25/18
Inventor 严洁黄欣
Owner LIVZON PHARM GRP INC
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