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Hydroxypropyl-belta-cyclodextrin inclusion compound of brucea fruit volatile oil, its preparation method and use

A technology of cyclodextrin inclusion compound and hydroxypropyl group, which is applied in the direction of non-active ingredients of polymer compounds, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of undiscovered patents and literature, poor storage stability, clinical Application of risk and other issues to achieve the effect of improving bioavailability, good stability, and no hemolytic reaction

Inactive Publication Date: 2008-11-19
HEILONGJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The volatile oil of Brucea javanica is a fat-soluble component, which is difficult to dissolve in water. It is generally used in intravenous emulsions clinically. The preparation process is usually cumbersome, the cost is high, and the storage stability is poor, which brings potential dangers to clinical application.
Retrieval of other documents and patents at home and abroad, no patents or documents related to the inclusion of volatile oil of Brucea javanica by using hydroxypropyl-β-cyclodextrin

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] The hydroxypropyl-beta-cyclodextrin clathrate of Brucea javanica volatile oil is made up of following raw material by weight ratio: Brucea javanica volatile oil: hydroxypropyl-beta-cyclodextrin=1: 1~100, it is by will The volatile oil of Brucea javanica is added to the aqueous solution containing hydroxypropyl-β-cyclodextrin, and after ultrasonic treatment at 30°C and 40KHz, it is dried to form an inclusion complex which is easily soluble in water.

[0023] Take 1g of volatile oil of Brucea javanica, 1g or 3g or 5g or 10g of hydroxypropyl-β-cyclodextrin, dissolve all of hydroxypropyl-β-cyclodextrin in 200ml, and the weight of water is hydroxypropyl-β-cyclodextrin It is 5-50 times as fine as water for injection, and it is best to use water for injection. Ultrasound at 30°C and 40KHz, add the volatile oil of Brucea javanica dropwise to the hydroxypropyl-β-cyclodextrin solution at a rate of 1-4 ml / per Minutes, after all the addition, continue to sonicate for 0.5 to 24 hour...

Embodiment 2

[0025] Dissolve hydroxypropyl-β-cyclodextrin in distilled water, the amount of distilled water added is the weight of hydroxypropyl-β-cyclodextrin: the volume of water is equal to 1:5~50; Ultrasonicate the aqueous solution of dextrin under the condition of 30°C and 40KHz, slowly add the volatile oil of Brucea javanica at a rate of 3 ml / min. μm or 0.22 μm microporous membrane, and the filtrate was freeze-dried to obtain a loose white powder, which was the inclusion compound of hydroxypropyl-β-cyclodextrin of the volatile oil of Brucea javanica. The clathrate obtained can also be washed with ether to remove the volatile oil of javanica javanica that is not clathrated.

Embodiment 3

[0027] The clathrate of the present invention in the above examples can also be prepared by other methods, such as the stirring method, that is, the aqueous solution containing hydroxypropyl-β-cyclodextrin is vigorously stirred, and the volatile oil of Brucea javanica is slowly added dropwise at a rate of 2 ml. / min, instead of the above-mentioned sonication, clathrates can also be obtained.

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PUM

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Abstract

The invention relates to a hydroxypropyl-Beta-cyclodextrin inclusion complex of khosam volatile-oil, as well as the preparation method and the application thereof. The khosam volatile-oil is a fat-soluble component and is hard to dissolve in water, and is usually used for manufacturing oil emulsion in clinics; the preparation technique is commonly complex, the cost is higher, and the storage stability is worse. The hydroxypropyl-Beta-cyclodextrin inclusion complex comprises the raw materials by weight proportion as follows: the ratio of the khosam volatile-oil to the hydroxypropyl-Beta-cyclodextrin is 1:1-100; the khosam volatile-oil is added in the water solution containing the hydroxypropyl-Beta-cyclodextrin; the mixed solution is processed at 30 DEG C by ultra audible sound of 40KHz, and then is dried to form the inclusion complex which is dissolved in water easily. The prepared drug has obvious inhibitory effects on human nasopharyngeal carcinoma cells KB, Walker-256 sarcoma and P388 lymphatic leukemia.

Description

Technical field: [0001] The invention relates to a hydroxypropyl-beta-cyclodextrin inclusion compound of javanica javanica volatile oil used for injection and oral administration and has anticancer and antitumor effects, as well as a preparation and a preparation method. Background technique: [0002] Brucea javanica is the seed of Brucea Jauanica LMerr, which was first recorded in "Compendium of Materia Medica Supplements". Kapchan et al. found that its alcohol extract had a significant inhibitory effect on human nasopharyngeal carcinoma fine KB, Walker-256 sarcoma and P388 lymphocytic leukemia. In 1978, our country began to carry out the research of javanica javanica oil intravenous emulsion. [0003] The volatile oil of Brucea javanica is a fat-soluble component and is insoluble in water. It is generally used in clinical intravenous emulsions. The preparation process is usually cumbersome, the cost is high, and the storage stability is poor, which brings potential danger...

Claims

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Application Information

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IPC IPC(8): A61K36/185A61K47/40A61K9/19A61K9/20A61K9/48A61P35/00A61K131/00
Inventor 王阳张宇
Owner HEILONGJIANG UNIV
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