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Clathrate compound of perphenazine cyclodextrin derivative, and preparation method thereof

A technology of cyclodextrin and derivatives, which is applied in the field of medicine to achieve the effect of improving solubility and dissolution rate

Inactive Publication Date: 2012-09-26
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Hydroxypropyl-β-cyclodextrin is used to prepare inclusion complexes of perphenazine, but no relevant literature and patent reports have been seen so far

Method used

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  • Clathrate compound of perphenazine cyclodextrin derivative, and preparation method thereof
  • Clathrate compound of perphenazine cyclodextrin derivative, and preparation method thereof
  • Clathrate compound of perphenazine cyclodextrin derivative, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1: Ultrasound-solvent volatilization method prepares perphenazine hydroxypropyl-β-cyclodextrin inclusion complex (molecular ratio 1: 1)

[0050] Weigh 7.90 g of hydroxypropyl-β-cyclodextrin and 2.02 g of perphenazine, dissolve in 40% (v / v) ethanol solution, ultrasonicate for 30 min at 25°C, filter the solution through a 0.45 μm microporous membrane, and the filtrate Concentrate to nearly dryness by rotary evaporation, dry in an oven at 40°C, pulverize, and pass through an 80-mesh sieve to obtain solid perphenazine hydroxypropyl-β-cyclodextrin inclusion compound, the content of perphenazine in the inclusion compound is 20.1% .

Embodiment 2

[0051] Example 2: Preparation of perphenazine hydroxypropyl-β-cyclodextrin inclusion complex by ultrasonic-solvent evaporation method (molecular ratio 1: 2)

[0052] Weigh 7.90g of hydroxypropyl-β-cyclodextrin and 1.01g of perphenazine, dissolve in 50% (v / v) ethanol solution, ultrasonicate at 25°C for 1h, filter the solution through a 0.45μm microporous membrane, and filter the filtrate through Concentrate to nearly dryness by rotary evaporation, vacuum-dry at 40°C, pulverize, and pass through an 80-mesh sieve to obtain perphenazine hydroxypropyl-β-cyclodextrin inclusion compound, the content of perphenazine in the inclusion compound is 11.2%.

Embodiment 3

[0053] Example 3: Preparation of perphenazine hydroxypropyl-β-cyclodextrin inclusion compound by ultrasonic-solvent evaporation method (molecular ratio 1: 3)

[0054] Weigh 7.90 g of hydroxypropyl-β-cyclodextrin and 0.673 g of perphenazine, dissolve in 50% (v / v) ethanol solution, and ultrasonicate at 25°C for 1 hour to obtain a clear solution. The obtained solution is vacuum-dried, crushed, and passed through an 80-mesh sieve to obtain a perphenazine hydroxypropyl-β-cyclodextrin inclusion compound, and the perphenazine content in the inclusion compound is 7.82%.

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Abstract

The invention relates to a clathrate compound of a perphenazine cyclodextrin derivative, and a preparation method of the clathrate compound, aiming at solving the problems that perphenazine can not be dissolved in the water, and the medicine effect is low. The cyclodextrin derivative selected by the invention is hydroxypropyl-beta-cyclodextrin. The preparation method of the perphenazine hydroxypropyl-beta-cyclodextrin clathrate compound is simple in technology, easy to control, mild in clathration condition, short in production period and high in medicine content of the clathrate compound; and the clathrate compound can be mixed with pharmaceutic adjuvant to prepare any pharmaceutically acceptable oral administration preparation such as common tablets, orally disintegrating tablets, buccal tablets, etc.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an inclusion compound of a perphenazine cyclodextrin derivative and a preparation method thereof. Background technique [0002] Perphenazine is a piperazine derivative of phenothiazines, which is included in the national essential drug list of our country. Low. It is clinically used for the treatment of mania, anxiety, paranoid and organic psychosis, senile mental disorder, aggressive behavior disorder in children, simple and chronic schizophrenia, and also for the treatment of nausea, vomiting, hiccups and other symptoms. [0003] Perphenazine is a class II drug in the biopharmaceutical classification system, which has good biofilm permeability, but it is insoluble in water (the solubility in water is 28.3mg / L), and the dissolution rate of common preparations is very low. The absolute bioavailability 20-40%. The rate-limiting factor for the absorption of class II drugs in th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5415A61K47/40A61P25/18A61P1/08A61P25/22
Inventor 宗莉王玲曾凡
Owner CHINA PHARM UNIV
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