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Hydroxypropyl-beta-cyclodextrin inclusion liposome of zedoary turmeric oil and preparation method thereof

A technology for inclusion compound of hydroxypropyl and cyclodextrin in Curcuma edulis oil is applied in the field of cyclodextrin inclusion compound lipid of Curcuma edulis and its preparation, and can solve the problem of difficulty in meeting clinical drug requirements, low concentration, limited drug-carrying effect, etc. problem, to achieve the effect of high inclusion rate, high safety performance, and high drug loading

Inactive Publication Date: 2012-05-23
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Curcuma oil can be directly made into liposomes, but the drug-loading effect is limited, and the concentration is too low to meet the needs of clinical medication

Method used

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  • Hydroxypropyl-beta-cyclodextrin inclusion liposome of zedoary turmeric oil and preparation method thereof
  • Hydroxypropyl-beta-cyclodextrin inclusion liposome of zedoary turmeric oil and preparation method thereof
  • Hydroxypropyl-beta-cyclodextrin inclusion liposome of zedoary turmeric oil and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The preparation of embodiment 1 turmeric oil hydroxypropyl-beta-cyclodextrin inclusion compound liposome

[0031] (1) First weigh 1g of zedoary oil, dissolve it in 2ml of absolute ethanol, and set aside, weigh 6g of hydroxypropyl-β-cyclodextrin, dissolve it in 12ml of distilled water, and stir the zedoary oil under constant temperature magnetic stirring at 40°C. Add the absolute ethanol solution dropwise to the aqueous solution of hydroxypropyl-β-cyclodextrin for inclusion. After the dropwise addition, continue to stir for 1 hour to make the inclusion fully, evaporate the ethanol, and filter through a 0.45 micron microporous membrane to remove the unencapsulated Combined free zedoary oil medicine, freeze-drying, obtains white powdery turmeric oil hydroxypropyl-beta-cyclodextrin inclusion compound, color method (by the 2005 edition Chinese Pharmacopoeia two recorded zedoary oil content assay methods, below The same) to determine the content of zedoary oil is 90mg / g. Dis...

Embodiment 2

[0034] The preparation of embodiment 2 zedoary oil hydroxypropyl-beta-cyclodextrin inclusion compound liposome

[0035] (1) First weigh 1g of zedoary oil, dissolve it in 2ml of absolute ethanol, and set aside, weigh 4g of hydroxypropyl-β-cyclodextrin, dissolve it in 6ml of distilled water, and stir the zedoary oil under constant temperature magnetic stirring at 40℃. Add the absolute ethanol solution dropwise to the aqueous solution of hydroxypropyl-β-cyclodextrin for inclusion, continue to stir for 1.5 hours after the dropwise addition to fully include, evaporate the ethanol, and filter through a 0.45 micron microporous membrane to remove the unencapsulated The combined free zedoary oil drug was freeze-dried to obtain a white powdery hydroxypropyl-β-cyclodextrin inclusion complex of zedoary oil, and the content of zedoary oil was 150 mg / g as determined by colorimetric method. Dissolving the prepared zedoary oil hydroxypropyl-β-cyclodextrin inclusion compound in distilled water...

Embodiment 3

[0038] The preparation of embodiment 3 zedoary oil hydroxypropyl-beta-cyclodextrin inclusion compound liposome

[0039] (1) First weigh 0.5g of turmeric oil and dissolve it in 1ml of absolute ethanol, and set aside; then weigh 10g of hydroxypropyl-β-cyclodextrin, add 5ml of water and grind it into a paste, then add turmeric oil dropwise under grinding Add the absolute ethanol solution until all the addition is complete, continue to grind for 1 hour, and dry in vacuum to obtain a white powder, then wash away the unincluded free zedoary oil drug with petroleum ether, dry at low temperature, and obtain the hydroxypropyl- β-cyclodextrin inclusion complex. The content of zedoary oil was determined to be 38 mg / g by colorimetric method. Dissolving the prepared zedoary oil hydroxypropyl-β-cyclodextrin inclusion compound in distilled water to prepare a solution with a concentration of zedoary oil of 10 mg / ml.

[0040] (2) Take by weighing 0.5g turmeric oil, 20g soybean lecithin and 2...

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Abstract

The invention discloses a hydroxypropyl-beta-cyclodextrin inclusion liposome of zedoary turmeric oil and a preparation method thereof. The liposome is prepared by the following steps of: preparing a hydroxypropyl-beta-cyclodextrin inclusion of the zedoary turmeric oil from the zedoary turmeric oil and hydroxypropyl-beta-cyclodextrin through an inclusion process; and preparing the hydroxypropyl-beta-cyclodextrin inclusion liposome of the zedoary turmeric oil from the hydroxypropyl-beta-cyclodextrin inclusion, phospholipid and cholesterol through an ethanol injection method. Experimental results show that: the hydroxypropyl-beta-cyclodextrin inclusion liposome of the zedoary turmeric oil has the advantages of good sustained release and long action, high loading rate, particularly no untoward effect such as hemolysis, and higher safety.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a cyclodextrin inclusion complex lipid of zedoary oil and a preparation method thereof. Background technique [0002] Curcuma oil is the volatile oil extracted from Curcum a phaeocaulis Val., Curcuma kwangsiensis S.G.Lee et C.F.Liang or Curcuma wenyujin Y.H.Chen et C.Ling. Curcuma oil contains The fat-soluble ingredients, represented by the anticancer active ingredient curcumol, should meet the corresponding regulations in Part I of the 2010 edition of the Chinese Pharmacopoeia. [0003] Zedoary oil is insoluble in water, so polysorbate 80 is used to solubilize clinically used Zedoary oil injection, but there are safety problems. On November 30, 2004, the State Food and Drug Administration issued the 7th "Adverse Drug Reaction Information Bulletin", requiring all localities to pay attention to the adverse reactions of zedoary oil injection. The 2010 edition o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K36/9066A61K47/48A61P35/00A61K47/61A61K47/69
Inventor 陈军陆兔林蔡宝昌毛春芹程娜娜
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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