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Clozapine cyclodextrin inclusion compound and preparation method thereof

A clozapine cyclodextrin and cyclodextrin technology, which can be applied in the directions of non-active components of polymer compounds, pharmaceutical combinations, pharmaceutical formulations, etc., can solve the problems of limited wide application and low solubility, etc.

Inactive Publication Date: 2012-11-21
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The low solubility of natural β-cyclodextrin in water limits its wide application

Method used

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  • Clozapine cyclodextrin inclusion compound and preparation method thereof
  • Clozapine cyclodextrin inclusion compound and preparation method thereof
  • Clozapine cyclodextrin inclusion compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Weigh 14.25g of hydroxypropyl-β-cyclodextrin and 3.27g of clozapine, dissolve them in anhydrous ethanol solution, sonicate at 25°C for 30min, filter the solution through a 0.45μm microporous membrane, and rotate the filtrate at 60°C Nearly dry in the evaporator. The product was oven-dried at 40°C, crushed, and passed through an 80-mesh sieve to obtain the clozapine-hydroxypropyl-β-cyclodextrin inclusion compound. Its dissolution curve is shown in figure 1 .

Embodiment 2

[0047] Weigh 8.55g of hydroxypropyl-β-cyclodextrin and 1.96g of clozapine, dissolve in 75% (v / v) ethanol solution, ultrasonicate for 30min at 25°C, filter the solution through a 0.45μm microporous membrane, and the filtrate Place in a rotary evaporator at 60°C until nearly dry. The product was oven-dried at 40°C, crushed, and passed through an 80-mesh sieve to obtain the clozapine-hydroxypropyl-β-cyclodextrin inclusion compound. Its dissolution curve is shown in figure 2 75% of the curve.

Embodiment 3

[0049] Weigh 11.4 g of hydroxypropyl-β-cyclodextrin, 2.62 g of clozapine, dissolve in 95% (v / v) ethanol solution, ultrasonicate for 30 min at 25 ° C, filter the solution through a 0.45 μm microporous membrane, and the filtrate Place in a rotary evaporator at 60°C until nearly dry. The product was dried in an oven at 40°C, crushed, and passed through an 80-mesh sieve to obtain the clozapine-hydroxypropyl-β-cyclodextrin inclusion complex. Its dissolution curve is shown in figure 2 95% of the curves.

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Abstract

The invention belongs to the field of pharmaceutic preparations and specifically relates to a clozapine cyclodextrin inclusion compound and a preparation method thereof. The preparation method is characterized by dissolving clozapine in a solvent, performing an inclusion by cyclodextrin, and drying an inclusion compound solution to obtain the clozapine cyclodextrin inclusion compound. The clozapine cyclodextrin inclusion compound is characterized in that the cyclodextrin is hydroxypropyl-beta-cyclodextrin, the molecule molar ratio between the clozapine and the hydroxypropyl-beta-cyclodextrin is (1:1)-(1:2), the solvent utilizes ethanol of 75-100% (v / v), and an ultrasound-solvent volatilization method is utilized for the inclusion. The preparation method has the advantages of being mild incondition, simple in process, easy to control and short in production cycle.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a clozapine cyclodextrin inclusion compound and a preparation method thereof. Background technique [0002] Clozapine is a dibenzodiazepine broad-spectrum antipsychotic. It is clinically used to treat agitation and hallucinations in acute and chronic schizophrenia, mania or other psychotic disorders. Its mechanism of action is: (1) Inhibit the combination of dopamine receptors in the mesolimbic system with D1 and D2 receptors; (2) Antagonize 5-HT2 receptors, inhibit the upward activation system of the midbrain reticular structure, and have strong sedative, hypnotic and antipsychotic effects. effect. [0003] Clozapine is a class II drug in the biopharmaceutical classification system, with good biofilm permeability, but low water solubility, and the dissolution rate becomes the main limiting factor for drug absorption. The absolute bioavailability of oral clozapine or...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/551A61K47/40A61P25/18
Inventor 宗莉曾凡李燕先王硕
Owner CHINA PHARM UNIV
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