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Beta cyclodextrin clathrate of cantharidin and Chinese blister beetle extracts and method for preparing same

A clathrate and cyclodextrin technology, which is applied in the direction of active ingredients of heterocyclic compounds, medical preparations of inactive ingredients, ineffective ingredients of polymer compounds, etc., to achieve high clathrate formation rate and drug utilization rate, reduce Irritant effects on mucous membranes

Inactive Publication Date: 2010-03-17
海南美好西林生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, cantharidin has side effects such as strong mucosal irritation, so it is necessary to improve the preparation of cantharidin to improve curative effect, reduce toxic and side effects, and improve the level of clinical treatment.

Method used

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  • Beta cyclodextrin clathrate of cantharidin and Chinese blister beetle extracts and method for preparing same
  • Beta cyclodextrin clathrate of cantharidin and Chinese blister beetle extracts and method for preparing same
  • Beta cyclodextrin clathrate of cantharidin and Chinese blister beetle extracts and method for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0126] Cantharidin 0.098g β-cyclodextrin 5g

[0127] Weigh β-cyclodextrin, add distilled water and stir to make a saturated solution, keep the temperature (50°C); take cantharidin, dissolve it with 25ml of absolute ethanol, slowly drop into 37ml of β-cyclodextrin under stirring at a rotating speed of 100r / min In the dextrin saturated solution, stir at constant temperature for 2 hours, refrigerate for 24 hours, filter with suction, wash the clathrate precipitate with an appropriate amount of chloroform for 3 times, collect the precipitate, and dry at 60°C for 4 hours to obtain the product.

Embodiment 2

[0129] Cantharidin 0.15g β-cyclodextrin 5g

[0130] Weigh β-cyclodextrin, add distilled water and stir to make a saturated solution, and keep the temperature (50°C); take cantharidin, dissolve it with 25ml of absolute ethanol, and slowly drop into 56ml of β-cyclodextrin under stirring at a rotating speed of 100r / min. In the dextrin saturated solution, stir at constant temperature for 2 hours, refrigerate for 24 hours, filter with suction, wash the clathrate precipitate with an appropriate amount of chloroform for 3 times, collect the precipitate, and dry at 60°C for 3 hours to obtain the product.

Embodiment 3

[0132] Cantharidin extract 0.5g (contains cantharidin 0.085g) β-cyclodextrin 5g

[0133] Take β-cyclodextrin, add distilled water and stir to make a saturated solution, keep the temperature (40°C); take the extract of mylabris, add absolute ethanol to dilute to 25ml, slowly drop into 20ml of β-cyclodextrin under stirring at a rotating speed of 100r / min In the dextrin saturated solution, stir at constant temperature for 2 hours, refrigerate for 24 hours, filter with suction, wash the clathrate precipitate with an appropriate amount of chloroform for 3 times, collect the precipitate, and dry at 60°C for 4 hours to obtain the product.

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Abstract

The invention discloses a beta cyclodextrin clathrate of cantharidin and Chinese blister beetle extracts and a method for preparing the same. The method particularly comprises the following steps of:weighing beta cyclodextrin in a ratio, mixing the beta cyclodextrin and water to prepare a saturated solution by stirring, and keeping a constant temperature; dissolving the cantharidin in absolute ethyl alcohol, slowly adding the mixing solution in the saturated solution of the beta cyclodextrin dropwise at a stirring speed of 90 to 120r / min, stirring the mixing solution at a constant temperaturefor a given time period, and freezing the mixing solution for 20 to 30 hours; and making suction filtration of the obtained product, precipitating the clathrate, washing the precipitate by any of chloroform, ethyl acetate, methanol or acetonitrile in proper quantity for 2 to 4 times, collecting the precipitate, drying the precipitate at a temperature of 60 DEG C for 3 to 5 hours, and finally obtaining the finished product. The beta cyclodextrin clathrate of the invention can obviously lower the irritation of the cantharidin and the Chinese blister beetle extracts on the mucous membrane.

Description

Technical field: [0001] The invention provides an inclusion compound of cantharidin and a cantharidin extract and a preparation method thereof, in particular to a β-cyclodextrin inclusion compound of cantharidin and a cantharidin extract and a preparation method thereof. Background technique [0002] Mylabris is Arthropoda, the dry body of MyLabris phaLerata PaLLas or MyLabris cichorii Linnaeus, which is the insect of the family Arthropoda, first published in "Shen Nong's Materia Medica", also known as tabby cat, dragon tail, listed as Low grade. According to the records of "Shen Nong's Materia Medica", mylabris can treat diseases such as carbuncle, ulcer, ringworm sore, and has the functions of attacking poisonous erosion and forcing blood to dissipate stagnation. The main chemical components in cantharidin include cantharidin, fat, formic acid, pigment and resin, among which cantharidin, a monoterpene component, is its main component. Cantharidin is a white flaky crystal...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/34A61K47/40A61K47/69
Inventor 朱春燕安琳娜
Owner 海南美好西林生物制药有限公司
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