Elemene nydroxy propyl-beta-cyclodextrin clathrate and preparation and preparing method thereof
A technology of cyclodextrin inclusion complex and elemene, which is applied in the directions of medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc. problems, to achieve the effect of improving bioavailability, improving stability, and convenient use
Inactive Publication Date: 2006-12-20
沈阳万嘉生物技术研究所有限公司
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- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
In the Chinese patent CN1076613A, it is described that polyoxyethylene glycerol triricinoleate 35 is used to solubilize and prepare injections. The injections prepared by using these surfactants to solubilize usually have weaknesses such as large irritation, instability, hemolysis, and sensitivity to allergies. Limit the application of elemene
It has been reported in the literature (Wang Lijun, Chinese herbal medicine 2001.4.3 14.316; Chen Xingcan, Chinese herbal medicine 1990-8 11-18), using β-cyclodextrin to carry out the inclusion of zedoary oil containing elemene, and achieved success. The curcuma oil inclusion complex is soluble in water, the stability is improved, and the bioavailability is improved, but β-cyclodextrin has a hemolytic reaction, so it is not easy to make injections
In addition, Chinese patent application 02109680.5 has also described that zedoary oil can be clathrated by hydroxypropyl-β-cyclodextrin, and the clathrate formed is very soluble in water.
These documents and patents do not indicate whether to include elemene. Searching other documents and patents at home and abroad has not found any patents and documents about elemene using hydroxypropyl-β-cyclodextrin to include elemene.
Method used
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Experimental program
Comparison scheme
Effect test
Embodiment 1
[0020] Take 0.1g of elemene, dissolve it in 0.5ml of ethanol, take 0.5g of hydroxypropyl-β-cyclodextrin, dissolve it in 20ml of water for injection, add the elemene ethanol solution dropwise into the HPCD solution, and stir magnetically at room temperature After 3 hours, it was filtered and frozen with a 0.45 μm microporous membrane to obtain a white loose powder, which was confirmed by thin-layer chromatography to form an inclusion complex of elemene and hydroxypropyl-β-cyclodextrin. As determined by gas chromatography, the inclusion rate is 95%.
Embodiment 2
[0022] The clathrate powder obtained in Example 1 was washed with ether, and the ether was evaporated to obtain a white clathrate powder.
Embodiment 3
[0024] Others are the same as Example 1, change the magnetic stirring method to the ultrasonic oscillation method, shake at room temperature for 20 minutes, filter the inclusion solution through a 0.45 μm microporous membrane, freeze-dry the filtrate, and obtain a white loose powder, which is confirmed by thin-layer chromatography. An inclusion complex was formed, and the inclusion rate was 90% as determined by gas chromatography.
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The invention relates to an elemene hydroxylpropyl-beta- cyclodextrin inclusion compound, the preparation and the preparing method. The weight ratio of elemene : hydroxylpropyl-beta- cyclodextrin =1:1-100; it adds the elemene dissolving in organic menstruum to the hydroxylpropyl-beta-cyclodextrin water solution for mixing, then freeze-dries to form water-soluble inclusion compound; and then makes ultrafiltration and 0.22mum-aperture film filtration on the water solution to freeze-dry to make freeze-dried powder injection. The inclusion compound, mixed with other assistant material, can be made into suppository, ointment, tablet and capsule.
Description
Technical field [0001] The invention relates to a hydroxypropyl-beta-cyclodextrin inclusion compound of elemene, a preparation and a preparation method. The inclusion compound can be used for injection, oral administration and external application, and has antiviral and anticancer effects. Background technique [0002] Elemene is a plant active ingredient extracted from Curcuma phaeocaulis Valeton. or Curcuma kwangsiensis S.G.Lee et C.F. or Curcuma Wenyujin Y.H.chen et C.Ling or lemongrass. The English name is Elemene, and the chemical name is 1 -Methyl-1-vinyl-2,4-diisopropenylcyclohexane, the molecular formula is C 15 h 24 , Elemene contains a variety of isomers, mainly α-elemene, β-elemene, γ-elemene, δ-elemene, as well as curcumene and caryrene. Elemene has Anti-cancer, anti-virus and other effects, milk injection made of elemene has been widely used in clinical practice, and achieved good curative effect in clinical application. There have been many literature report...
Claims
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IPC IPC(8): C08L5/16A61K31/724
Inventor 董英杰艾莉张乃先
Owner 沈阳万嘉生物技术研究所有限公司