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Hydroxypropyl-beta-cyclodextrin clathrate, preparing method and application of radix bupleuri volatile oil

A cyclodextrin inclusion compound and volatile oil technology, 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 low bioavailability, poor stability of preparations, and clinical application risks, etc. problems, to achieve the effects of improved bioavailability, easy storage, and improved utilization

Inactive Publication Date: 2008-05-14
HEILONGJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The volatile oil of Bupleurum bupleurum is a fat-soluble component, which is difficult to dissolve in water. It is usually made into tablets for clinical application, and its bioavailability is usually low, which affects the curative effect.
Bupleurum volatile oil injection is administered by intramuscular injection, which improves the bioavailability, but the stability of the preparation is poor, which brings potential danger to clinical application
Searching other domestic and foreign literatures and patents, no patents and literatures about the inclusion of Bupleurum volatile oil by using hydroxypropyl-β-cyclodextrin were found

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Take 1g of Bupleurum volatile oil and 5g of hydroxypropyl-β-cyclodextrin, dissolve all of hydroxypropyl-β-cyclodextrin in 200ml of water for injection, ultrasonicate at 30°C and 40KHz, and dissolve the bupleurum volatile oil drop by drop Add hydroxypropyl-β-cyclodextrin solution, after all the addition, continue to stir for 0.5-24 hours, use 0.45μm or 0.22μm microporous filter membrane to filter, and freeze-dry the filtrate to obtain a loose white powder. Chromatography confirmed the formation of Bupleurum volatile oil and hydroxypropyl-β-cyclodextrin inclusion complex. As determined by gas chromatography, the inclusion rate was 93%. 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 at 30°C and 40KHz, slowly add Bupleurum volatile oil dropwise, and continue to stir for 0.5 to 24 hours after all ...

Embodiment 2

[0029] The clathrate powder obtained in Example 1 was washed with ether, and the ether was evaporated to obtain a white clathrate powder.

Embodiment 3

[0031] Others are the same as in Example 1, changing the ultrasonic oscillation to strong magnetic stirring, filtering the clathrate solution through a 0.45 μm microporous membrane, and freeze-drying the filtrate to obtain a white loose powder, which was confirmed by thin-layer chromatography to form an clathrate. As determined by gas chromatography, the inclusion rate is 80%.

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PUM

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Abstract

The invention relates to a hydroxypropyl-Beta-cyclodextrin inclusion compound of bupleurum volatile oil, the preparation method and the application. The bupleurum volatile oil is a fat-soluble component, is hard to dissolve in water, and generally is made into tablet for application, which has low biological utilization degree and influences the curative efficacy. The invention comprises the materials in weight ratio as follows: bupleurum volatile oil: hydroxypropyl-Beta-cyclodextrin = 1:1 to 100; the preparation method is as follow: the bupleurum volatile oil is added into the solution of hydroxypropyl-Beta-cyclodextrin, and then is processed with ultrasonic under the condition of 30 DEG C and 40 KHz, and after cooling and drying, the easily soluble inclusion compound is formed; after inclusion, the solution is remove from the heat source, and filtered with a filtration membrane with 0.22pm micropore, and then is freezed, dried, and made into freeze-dried power injection for injection; excipients are added into the inclusion compound to be made into sublingual tablets.

Description

Technical field: [0001] The invention relates to a hydroxypropyl-beta-cyclodextrin inclusion compound of bupleurum volatile oil with antipyretic and anti-inflammation effects for injection and oral administration, a formulation and a preparation method. Background technique: [0002] Bupleurum is a traditional Chinese medicine and commonly used Chinese medicine in my country. "Chinese Pharmacopoeia" stipulates that Bupleurum chinese DC. and Bupleurum scorzonerifolium Willd., a perennial herb of Umbelliferae, are authentic Chinese medicines original plant. Its nature and taste are bitter and cool, and it has the effects of dispersing and reducing fever, soothing the liver and relieving stagnation, raising yang and elevating qi. The main active ingredients of Bupleuri are saikosaponin and volatile oil. Modern pharmacological studies have shown that Bupleurum has various physiological and biological activities such as antipyretic, anti-virus, anti-bacterial endotoxin, anti-inf...

Claims

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Application Information

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IPC IPC(8): A61K36/233A61K9/19A61K9/20A61K9/48A61K47/40A61P29/00A61P31/04A61P31/12A61P3/06A61P35/00A61P37/04
Inventor 王阳李强赵学玲龚显峰张宇
Owner HEILONGJIANG UNIV
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