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Oridonin-loaded micelle preparation and preparation method thereof

A technology of oridonin A and micelles is applied in the directions of pharmaceutical formulations, medical preparations containing active ingredients, and medical preparations without active ingredients, which can solve the problems of no oridonin A pharmaceutical preparations and the like, and achieve The drug loading is easy to control, convenient for drug efficacy evaluation and standard formulation, and the effect of no toxic and side effects

Inactive Publication Date: 2010-05-19
ARMY MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In summary, there is currently no oridonin pharmaceutical preparation that can be applied clinically.

Method used

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  • Oridonin-loaded micelle preparation and preparation method thereof
  • Oridonin-loaded micelle preparation and preparation method thereof
  • Oridonin-loaded micelle preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Take 20 mg of Rubescensine A, 40 mg of phospholipids with a molecular weight distribution of 700-800, and 40 mg of bile salts, add 20 mL of absolute ethanol at 20°C and ultrasonically dissolve until clarified. Complete, after the material is constant weight, add 10 mg of 10 ℃ deionized water and carry out rotary hydration, transfer the hydrated material to a centrifuge tube, and centrifuge at 13000rpm for 5min, then discard the precipitate, take the supernatant, and obtain The supernatant was filtered through a 0.22 μm microporous membrane to obtain the oridonin A micelle preparation with a drug loading of 20%. In the present embodiment, the phospholipid is soybean phospholipid, and the bile salt is sodium deoxycholate. Of course, the phospholipid can also be egg yolk lecithin. The advantage of selecting soybean lecithin is that the purity of soybean lecithin is higher, and the bile salt can also be cholic acid Sodium, the advantage of using sodium deoxycholate is that ...

Embodiment 2

[0042] Take 10 mg of Rubescensin A, 70 mg of egg yolk lecithin with a molecular weight distribution of 700-800, and 20 mg of sodium cholate, add 30 mL of methanol at 60°C and ultrasonically dissolve until clarified, then evaporate under reduced pressure in a water bath at 35°C, and wait for the organic solvent After complete evaporation and constant weight of the material, add 50 mg of 0.05 mol / kg NaCl solution at 60°C and rotate for hydration, transfer the hydrated material to a centrifuge tube, and centrifuge at 8000 rpm for 5 min, then discard the precipitate , take the supernatant, and filter through a 0.22 μm microporous membrane to obtain the oridonin A micelle preparation, with a drug loading of 10%.

Embodiment 3

[0044] Take 10 mg of Rubescensin A, 10 mg of dipalmitate phosphatidylcholine with an average molecular weight of 734, and 80 mg of sodium deoxycholate, and add 40 mL of a mixture of methanol and chloroform at 40°C (the weight ratio of methanol to chloroform is 1:1) and ultrasonically dissolved until clarified, and then the material was subjected to reduced-pressure rotary evaporation in a water bath at 40°C. After the material was constant weight, 20 mg of pH 6.0 phosphate buffer solution at a temperature of 40°C was added and rotated for hydration. After hydration, the material was transferred into a centrifuge tube and centrifuged at 10,000rpm for 5min, discard the precipitate, and get the supernatant, which was filtered through a 0.22 μm microporous membrane, and the filtrate was freeze-dried to obtain the oridonin A micelle preparation. Freeze-dried powder with a drug loading of 10%. In this embodiment, the dipalmitate phosphatidylcholine can also be replaced by synthetic p...

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Abstract

The invention discloses an oridonin-loaded micelle preparation which comprises the raw materials of oridonin, cholate and phosphatide. An associated structure of the cholate and the phosphatide is used as a carrier of the oridonin, the water solubility of the oridonin is greatly improved through reasonably setting the proportion of the components, and the stability of the preparation is good. The micelle preparation has high drug-loading rate and easy control; the raw materials have not side and toxic effects, safety and reliability, wide source and low cost, and thus the micelle preparation is very suitable for wide clinical application. The preparation method has simple process, easy implementation, good repeatability, and suitability of large-scale production; and the liquid micelle preparation can be frozen to form frozen powder, thereby being more convenient for storage and transportation.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a micelle preparation of oridonin A and a preparation method thereof. Background technique [0002] Oridonin (ORI) is a natural organic compound of ent-kaurene diterpenoid isolated from Labtea (Labtea) plants of the genus Rabdosia, white prisms Like crystal, very slightly soluble in water and oil, its chemical formula is C 20 h 28 o 6 , the molecular weight is 364.43, and the structural formula is as follows: [0003] [0004] Pharmacological tests show that Rubescensine A has strong anti-tumor activity and can effectively inhibit the proliferation of various tumor cells. Clinical application data show that it has a good therapeutic effect on primary liver cancer and advanced esophageal cancer (Zhang Dianrui, Ren Tianchi. Progress in the pharmaceutical research of Rubescensin A. Chinese Journal of Pharmaceutical Sciences. 2003.38: 817-820). [0005] The special ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/19A61K31/352A61K47/28A61P35/00
Inventor 何凤慈陆国庆
Owner ARMY MEDICAL UNIV
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