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Asenapine compound

A compound, the technology of asenapine maleate, which is applied in the field of medicine, can solve the problems of asenapine maleate with many impurities, low optical purity, and high total amount of impurities

Inactive Publication Date: 2015-03-25
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0023] In the research process, repeating the method of the prior art, the number of impurities of asenapine maleate obtained is more, the total amount of impurities is higher, and the optical purity is low

Method used

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  • Asenapine compound
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] In a 400ml reaction flask equipped with stirring, a thermometer, and a condenser, add 60 grams of asenapine maleate and 180 milliliters of methanol, stir for 40 minutes, filter, and the filtrate is cooled to 8° C. for later use.

[0058] Cool 480ml of acetonitrile-acetone=5:5 mixture to 8°C, add the above standby solution under stirring, keep it warm for 15 hours, crystals precipitate out, filter, and dry to obtain 53.3 grams of white crystals. Purity 99.9% (HPLC normalization method), optical purity 99.96% ee (chiral HPLC).

[0059] This crystal was subjected to X-ray diffraction measurement. Instrument model and measurement conditions: Rigaku D / max 2500 diffractometer; CuKa 40Kv 100mA; 2θ scanning range: 0-50 ° . The result is as follows:

[0060] number of peaks 2θ angle (°) measured value d(?) Measured value I / I 0 1 10.620 15.6325 92 2 15.940 11.9140 37 3 16.560 9.5474 5 4 18.480 9.3208 4 5 19.720 7.6318 22 ...

Embodiment 2

[0062] Tablets containing the compound asenapine maleate

[0063] Prescription: 20 grams of asenapine maleate compound, 100 grams of mannitol, 140 grams of lactose, 50 grams of calcium carbonate, 5 grams of magnesium stearate, appropriate amount of 8% ethyl cellulose solution, made into 1000 capsules.

[0064] Process: Mix asenapine maleate compound, mannitol, lactose, and calcium carbonate evenly; add an appropriate amount of binder 8% ethyl cellulose solution to make a soft material, granulate with a 20-mesh screen, 40°C±2°C Dried, granulated, added externally mixed with magnesium stearate, mixed evenly, compressed into tablets, and obtained.

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Abstract

Belonging to the medical technology field, the invention in particular relates to a maleic acid asenapine compound and a preparation method thereof. The invention also relates to application of compositions containing the maleic acid asenapine compound in preparation of drugs treating antipsychotic drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a maleic acid asenapine compound and a preparation method thereof. Background technique [0002] Schizophrenia is a common mental illness with an incompletely elucidated etiology. Most of the onsets are in young adults, and there are often obstacles in perception, thinking, emotion, and behavior, and generally unconsciousness and mental retardation. At present, clinical drugs are mainly divided into two categories: first-generation antipsychotic drugs and second-generation antipsychotic drugs. The price of first-generation antipsychotic drugs is relatively low, but they cannot improve the cognitive function of patients, and cause extrapyramidal reactions and delayed onset. The proportion of dyskinesia is high, and the relief effect on positive symptoms is not good, thus reducing the compliance of patients with medication. Second-generation antipsychotic drugs, whic...

Claims

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Application Information

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IPC IPC(8): C07D491/044C07C57/145C07C51/43A61K31/407A61P25/18
CPCC07D491/044C07B2200/13C07C51/43C07C57/145
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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