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2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-cycloocta[b]pyridine (blonanserin, blonanserin) and composition thereof

A technology of composition and crystal form, which can be used in drug combinations, organic active ingredients, nervous system diseases, etc., and can solve the problems of poor stability and low crystal form purity.

Active Publication Date: 2010-01-06
LIVZON PHARM GRP INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] The above two crystal forms have disadvantages such as low purity and poor stability.

Method used

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  • 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-cycloocta[b]pyridine (blonanserin, blonanserin) and composition thereof
  • 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-cycloocta[b]pyridine (blonanserin, blonanserin) and composition thereof
  • 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-cycloocta[b]pyridine (blonanserin, blonanserin) and composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] In a 1000ml reaction flask equipped with a stirrer, a thermometer and a condenser, add 40 grams of bonanserin and 320ml of ethanol / isopropanol (1:1) mixture, start stirring, heat up to reflux, and wait until all is dissolved. , Then slowly cool down, control the cooling rate, use 59 minutes to reduce to 52℃, 50±2℃ keep for 181 minutes; then use 118 minutes to lower to 27℃, 25±2℃ keep for 300 minutes. The crystals are precipitated, filtered, and washed with 40ml of a 1:1 ethanol / isopropanol mixture precooled to 5℃-10℃ for three times, placed indoors for 120 minutes, then moved to a vacuum drying oven, and vacuum dried (0.04- 0.05Mpa) 8 hours, 36.2 grams of white crystalline powder is obtained.

[0049] The X-ray diffraction pattern of this crystalline powder is shown in figure 1 . Instrument model and measurement conditions: Rigaku D / max2500 diffractometer; CuKa 40Kv 100mA; 2θ scanning range: 0-50°;

[0050] The infrared spectrum of this crystalline powder is shown in figu...

Embodiment 2

[0054] Granules containing the new crystal form of bonanserin

[0055] Prescription: 2 grams of branserin of new crystal form, 680 grams of lactose, 78 grams of crospovidone, 100 grams of PEG-4000, 140 grams of hydroxypropyl methylcellulose, appropriate amount of distilled water, made into 1000 bags.

[0056] Process: PEG-4000 is pulverized with the new crystal form of Bunanserin, passed through an 80-mesh sieve, mixed with other materials and then made of soft material with distilled water, granulated, dried at low temperature, and then divided into granules.

Embodiment 3

[0058] Capsules containing the new crystal form of branserin

[0059] Prescription: 4 grams of branserin of the new crystal form, 1.5 ml of propylene glycol, 150 grams of starch, made into 1000 grains.

[0060] Process: Wet the new crystal form of Brunanserin and starch with a 15% propylene glycol aqueous solution, mix well, sieving and granulating, drying at 60°C, sizing, and filling capsules.

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Abstract

The invention relates to a crystal of 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-cycloocta[b]pyridine (blonanserin, Blonanserin) and a preparation method thereof. The invention also relates to a blonanserin pharmaceutical composition containing the crystal and an application of the new crystal to the manufacture of medicines for curing schizophrenia.

Description

Technical field [0001] The present invention relates to containing 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydroaryloctano[b]pyridine (Blonanserin) a pharmaceutical composition of a new crystal form, a preparation method of the new crystal form, and application of the new crystal form in manufacturing a medicine for treating schizophrenia. Background technique [0002] Schizophrenia is a mental illness that seriously endangers the personal destiny of the patient, the public security and stability of the community, and even the society. It is extremely destructive and has become a serious public health problem. [0003] The atypical antipsychotic drugs currently on the market: clozapine, risperidone, olanzapine, piropirone, etc., their common feature is the moderate regulation of D2 receptors, which are shown to antagonize 5-HT2A receptors in vivo. The body is stronger than the antagonism of D2 receptors. Many of these drugs have been developed, but because of...

Claims

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Application Information

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IPC IPC(8): C07D221/04A61K31/496A61P25/18
Inventor 严洁卢庆勇黄欣
Owner LIVZON PHARM GRP INC
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