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Method for preparing blonanserin micron drug through solvent method

A technology for blonanserin and drugs, applied in the field of chemical drug preparation, can solve the problems of easy agglomeration, uneven micron particles, irregular morphology, etc. Effect

Active Publication Date: 2015-11-04
HEBEI GUOLONG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a method for preparing blonanserin micro-medicine by solvent method, which can obtain blonanserin micro-medicine with a particle size of 1-10 μm, which overcomes the inhomogeneous micron particles in the prior art Irregular appearance, easy to reunite defect

Method used

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  • Method for preparing blonanserin micron drug through solvent method
  • Method for preparing blonanserin micron drug through solvent method
  • Method for preparing blonanserin micron drug through solvent method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Add 100ml of 1% polyethylene glycol water stabilizer to a 250ml Erlenmeyer flask, and place it in an ice-water bath at 0-4°C. Weigh 0.285 g (0.78 mmol) of blonanserin, dissolve it in 26 ml of ethanol, prepare a blonanserin ethanol solution with a concentration of 0.03 mol / l, and add it into a 50 ml constant pressure funnel. Place the constant pressure funnel on the Erlenmeyer flask filled with polyethylene glycol aqueous solution, turn on the ultrasonic cleaner, and slowly add the blonanserin ethanol solution dropwise (1ml / min) to the polyethylene glycol solution under ultrasonic conditions of 40KHZ frequency. In the ethylene glycol aqueous solution, the system became cloudy, and continued to sonicate for 30 minutes after the dropwise addition was completed. After the resulting mixed solution was left to stand for 1 h, it was subjected to high-speed centrifugation until it was completely separated, and the supernatant liquid was decanted. The obtained sample was washe...

Embodiment 2

[0025] Add 100ml of 1% polyethylene glycol water stabilizer to a 250ml Erlenmeyer flask, and place it in an ice-water bath at 0-4°C. Weigh 0.184 g (0.50 mmol) of blonanserin, dissolve it in 25 ml of ethanol, prepare a blonanserin ethanol solution with a concentration of 0.02 mol / l, and add it to a 50 ml constant pressure funnel. Place the constant pressure funnel on the Erlenmeyer flask filled with polyethylene glycol aqueous solution, turn on the ultrasonic cleaner, and slowly add the blonanserin ethanol solution dropwise (1ml / min) to the polyethylene glycol solution under the ultrasonic condition of 60KHZ frequency. In the ethylene glycol aqueous solution, the system became cloudy, and continued to sonicate for 30 minutes after the dropwise addition was completed. After the resulting mixed solution was left to stand for 2 h, it was centrifuged at 4000 r / min until it was completely separated, and the supernatant was poured off. The obtained sample was washed with distilled ...

Embodiment 3

[0027] Add 400ml of 1% polyethylene glycol water stabilizer to a 500ml Erlenmeyer flask, and place it in an ice-water bath at 15-20°C. Weigh 1.004 g (2.73 mmol) of blonanserin, dissolve it in 91 ml of ethanol, prepare a blonanserin ethanol solution with a concentration of 0.03 mol / l, and add it to a 100 ml constant pressure funnel. Place the constant pressure funnel on the Erlenmeyer flask filled with polyethylene glycol aqueous solution, turn on the ultrasonic cleaner, and slowly add the blonanserin acetone solution dropwise (1ml / min) to the polyethylene glycol solution under the ultrasonic condition of 40KHZ frequency. In the ethylene glycol aqueous solution, the system became cloudy, and continued to sonicate for 30 minutes after the dropwise addition was completed. After the resulting mixed solution was left to stand for 1 h, it was subjected to high-speed centrifugation until it was completely separated, and the supernatant liquid was decanted. The obtained sample was w...

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Abstract

The present invention discloses a method for preparing a blonanserin micron drug through solvent method. According to the method, under an ultrasonic wave condition, a certain amount of blonanserin is dissolved in an organic solvent, and the obtained solution is slowly added to a water stabilizer with a certain concentration in a dropwise manner; the affinity of the organic phase on the water is more than the affinity of the organic phase on the blonanserin, such that the blonanserin is slowly diffused into the water along with the organic phase; and the concentration of the blonanserin in the solution is increased, such that the crystal nucleus is formed and precipitated so as to obtain the blonanserin micron particles with a particle size of 1-10 [mu]m, wherein the particle size is uniform, the specific surface area is increased, and the bioavailability of the blonanserin drug is easily improved. According to the present invention, the operation is simple, other drug adjuvants are not introduced, the equipment investment is low, and the yield is high.

Description

technical field [0001] The invention relates to a method for preparing medicine, in particular to a method for preparing blonanserin micron medicine, which belongs to the technical field of chemical medicine preparation. Background technique [0002] The chemical name of Blonanserin is 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydroaromatic Octa[b]pyridine, a new generation of atypical antischizophrenia drugs, has a strong effect on dopamine D 2 and 5-HT 2 The selectivity of the two receptors of A is stronger than that of other antipsychotic drugs, the safety and tolerance are obviously better than traditional antipsychotic drugs, and the side effects are small. Its molecular structure is represented by the following formula: [0003] [0004] Blonanserin is a kind of poorly soluble drug, and the research found that the dissolution rate of conventional blonanserin drug is quite different from that of the original Japanese preparation. Because the...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/496A61P25/18
Inventor 孙京国梁冉冯玉玲焦彦辉付辉王红莉张佳王采奕张娟娟孙玲玲
Owner HEBEI GUOLONG PHARMA CO LTD
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