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Preparation method of menthol inclusion compound

A technology of menthol and clathrates, applied in the field of clathrates, can solve the problems of poor solubility of menthol and clathrates, long cladding time of preparation methods, low bioavailability, etc., shorten clathrate time and reduce drug particle size , Improve the effect of inclusion rate

Active Publication Date: 2016-06-15
宁夏金太阳药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, although the stability of the existing menthol inclusion compound has been improved, it is still relatively poor, the bioavailability is not high, and the preparation method has a long inclusion time, a low inclusion rate, poor solubility of menthol and the inclusion agent, and production high cost

Method used

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  • Preparation method of menthol inclusion compound
  • Preparation method of menthol inclusion compound
  • Preparation method of menthol inclusion compound

Examples

Experimental program
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Effect test

Embodiment 1

[0050](1) Weigh hydroxypropyl-β-cyclodextrin with 6 times the weight of menthol, add water with 5 times the weight of hydroxypropyl-β-cyclodextrin, put it in an ultrasonic cleaner, mix evenly, and make hydroxypropyl-β-cyclodextrin A saturated aqueous solution of β-cyclodextrin. Weigh 5g of menthol ultrafine powder (ultrafinely pulverized to a particle size of 5 μm, accounting for more than 90%), slowly add it to the above saturated aqueous solution, start timing after all the addition, ultrasonic inclusion compound and cyclopaste after 20min The refined mixed solution was placed at 4°C for 24 hours, poured into a Buchner funnel, and filtered with suction. When there were no more drops, pour the clathrate and filter paper into an evaporating dish, and place it at 40°C. Vacuum-dry to dryness to obtain menthol hydroxypropyl-β-cyclodextrin inclusion compound, the inclusion rate of menthol is 67.88%.

[0051] (2) Weigh 2.0 g of the menthol inclusion compound prepared above, weigh ...

Embodiment 2

[0053] (1) Weigh hydroxypropyl-β-cyclodextrin with 8 times the weight of menthol, add water with 5 times the weight of hydroxypropyl-β-cyclodextrin, put it in an ultrasonic cleaner, mix evenly, and make hydroxypropyl-β-cyclodextrin For the saturated aqueous solution of propyl-β-cyclodextrin, weigh 5g of menthol superfine powder (the particle size is 5 μm and account for more than 90%), slowly add it to the above saturated aqueous solution, start timing after all the addition, and ultrasonically clathrate for 60 minutes Finally, put the mixed solution of inclusion compound and cyclodextrin at 4°C for 24 hours, pour it into a Buchner funnel, and filter it with suction. When there are no more drops, pour the inclusion compound and filter paper together. In an evaporating dish, vacuum-dry to dryness at 40° C. to obtain a menthol hydroxypropyl-β-cyclodextrin inclusion compound, and the inclusion rate of menthol is 82.88%.

[0054] (2) Weigh 2.0 g of the menthol inclusion compound p...

Embodiment 3

[0056] (1) Weigh hydroxypropyl-β-cyclodextrin with 6 times the weight of menthol, add water with 5 times the weight of hydroxypropyl-β-cyclodextrin, put it in an ultrasonic cleaner, mix evenly, and make hydroxypropyl-β-cyclodextrin Based on the saturated aqueous solution of β-cyclodextrin, weigh 5g of menthol superfine powder (the particle size is 5 μm and account for more than 90%), slowly add it to the above saturated aqueous solution, start timing after all the addition, and ultrasonic inclusion after 40min Put the mixed solution of clathrate and cyclodextrin at 4°C for 24 hours, pour it into a Buchner funnel, and filter it with suction. When there are no more drops, pour clathrate and filter paper together. In an evaporating dish, vacuum-dry to dryness at 40° C. to obtain menthol hydroxypropyl-β-cyclodextrin inclusion compound, and the inclusion rate of menthol is 71.69%.

[0057] (2) Weigh 2.0 g of the menthol inclusion compound prepared above, weigh it accurately, wash w...

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Abstract

The invention belongs to the field of pharmaceutical technology, and discloses a preparation method of a menthol inclusion compound. Superfine grinding is carried out for menthol into menthol ultrafine powder; ultrasonic mixing is carried out for (2-hydroxypropyl)-beta-cyclodextrin and water for uniformly mixing, and a saturated aqueous solution of (2-hydroxypropyl)-beta-cyclodextrin is prepared; finally, the menthol ultrafine powder is slowly added into the saturated aqueous solution of (2-hydroxypropyl)-beta-cyclodextrin, continuously ultrasonic inclusion is carried out, mixed liquor is permitted to stand, pumping filtration is carried out, vacuum drying is carried out till the liquor is dry, and the inclusion compound of menthol with (2-hydroxypropyl)-beta-cyclodextrin is obtained. The menthol inclusion compound prepared by the method has the advantages of short inclusion time of the menthol inclusion compound, high inclusion rate, good dissolvability between menthol and the inclusion agent, and substantially improved utilization rate of menthol.

Description

technical field [0001] The invention belongs to the field of clathrate technology, and in particular relates to a preparation method of menthol clathrate. Background technique [0002] Menthol is a saturated cyclic alcohol obtained by steam distillation, freezing and recrystallization from the fresh stems and leaves of the mint of the Labiatae plant. It is the main ingredient in peppermint and peppermint essential oils. Menthol is a traditional Chinese medicine, pungent in taste and cool in nature. It has the functions of dispelling wind, clearing heat and detoxifying. It is mainly used in traditional Chinese medicine preparations for its cooling, aroma, seasoning, and functions of expelling wind and relieving pain. In addition, the toxic and side effects of menthol are very rare, and it can be taken internally or externally, so it is widely used in food processing, spices, beverages, pharmaceutical industry, daily chemical industry, cosmetics, light chemical industry and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/045A61P11/04A61K47/69
CPCA61K31/045
Inventor 张军龙张启文马少平
Owner 宁夏金太阳药业有限公司
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