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Method for preparing camptothecin medicine slow releasing microcapsule

A technology for slow-release microcapsules and camptothecin, which is applied in the directions of drug combination, drug delivery, and pharmaceutical formulation to achieve the effects of environmental friendliness, high toxicity and good reproducibility.

Inactive Publication Date: 2008-04-09
HAERBIN FENGYUAN HIGH TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The technology adopted in the present invention is all different from the technology used in the above patents, and there is no report on the preparation of camptothecin drug microcapsules by this technology so far

Method used

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  • Method for preparing camptothecin medicine slow releasing microcapsule
  • Method for preparing camptothecin medicine slow releasing microcapsule
  • Method for preparing camptothecin medicine slow releasing microcapsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] (1) Disperse the camptothecin microcrystals in deionized water, and ultrasonically disperse them for 50 minutes to obtain a suspension of the camptothecin microcrystals,

[0030] (2) Place camptothecin microcrystals in 50 mg / mL chitosan (CHI) solution for adsorption for 30 minutes, centrifuge to remove unadsorbed chitosan (CHI), and repeat washing with 1 mmol / L hydrochloric acid solution for 10 minutes times, each washing for 10 minutes,

[0031] (3) Place camptothecin microcrystals in 50 mg / mL sodium alginate (ALG) solution, adsorb for 30 minutes, centrifuge to remove unadsorbed sodium alginate (ALG), and wash repeatedly with 1 mmol / L hydrochloric acid solution 10 times, 10 minutes each wash,

[0032] (4) repeat step (2) and (3) successively, until obtaining the camptothecin microcapsules of capsule wall layer respectively 5,11,17,

[0033] (5) Place the camptothecin microcapsules coated with 5 layers of polymers under a laser confocal scanning electron microscope to...

Embodiment 2

[0040] (1) 10-hydroxycamptothecin microcrystals were dispersed in deionized water, ultrasonically dispersed for 50 minutes to obtain a suspension of 10-hydroxycamptothecin microcrystals,

[0041] (2) 10-Hydroxycamptothecin microcrystals were placed in 50mg / mL ferric chloride solution with pH=2 to absorb for 30 minutes, centrifuged to remove unadsorbed ferric chloride, and washed repeatedly with 1mmol / L hydrochloric acid solution for 10 minutes times, each washing for 10 minutes,

[0042](3) Place 10-hydroxycamptothecin microcrystals in 50 mg / mL dextran sulfate (DS) solution, and absorb for 30 minutes; centrifuge to remove unadsorbed DS, and wash repeatedly with 1 mmol / L hydrochloric acid solution for 10 times, each washing for 10 minutes,

[0043] (4) repeat step (2) and (3) successively, until obtaining the 10-hydroxycamptothecin microcapsules that capsule wall layer number is respectively 8,12,16,

[0044] (5) Dissolve the 10-hydroxycamptothecin in the microcapsules with d...

Embodiment 3

[0049] (1) 9-nitrocamptothecin microcrystals were dispersed in deionized water, and ultrasonically dispersed for 50 minutes; the suspension of 9-nitrocamptothecin microcrystals was obtained,

[0050] (2) 9-nitrocamptothecin microcrystals were placed in a 50 mg / mL pH=2 polyallyl ammonium hydrochloride (PAH) solution for 30 minutes, centrifuged to remove unadsorbed PAH, and 1 mmol / L hydrochloric acid solution was washed 10 times, each time for 10 minutes,

[0051] (3) Put the 9-nitroxime microcrystals in 50 mg / mL polystyrene sodium sulfonate (PSS) solution, adsorb for 30 minutes, centrifuge to remove unadsorbed PSS, and wash repeatedly with 1 mmol / L hydrochloric acid solution 10 times, 10 minutes each wash,

[0052] (4) Steps (2) and (3) were repeated successively until the camptothecin microcapsules with capsule wall layers of 3 and 5 were obtained.

[0053] In the present embodiment, polycation can also select chitosan, protamine, polyarginine, polydiallyldimethyl quaternar...

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Abstract

The invention relates to a preparation method of camptothecin drug slow release microcapsule. Firstly, camptothecin drug microcrystal is positioned into deionized water for ultra sonic dispersion, secondly, the dispersed camptothecin drug microcrystal is positioned into polycation solution for adsorption, centrifugation and washing, third, the camptothecin drug microcrystal adsorbing the polycation is positioned into polyanion solution for adsorption, centrifugation and washing, then the step two and the step three are repeated, and thereby the drug microcapsule with core-shell structure is obtained. The microcapsule is very stable, can realize controlled release of the drug, can be produced to be micron-nanometer drug oral liquid or injection, and also can be produced to be drug capsule, and tablets, etc. The process of the invention is simple, the reaction condition is mild, the operation is easy, the reproducibility is good, the environment is protected, the invention provides substantial foundation and technical support for the application and the research of the camptothecin and other drugs having the characteristics of high curative effect, but large toxicity and poor water solubility, and has good application prospect.

Description

technical field [0001] The invention relates to a preparation method of camptothecin sustained-release microcapsules. Background technique [0002] It is an urgent and important research content in today's medical science to find and develop anticancer active substances and develop new anticancer drug preparations with high efficiency and low toxicity. Camptothecin (CPT) is a natural compound with broad-spectrum anti-cancer activity isolated from the unique Chinese plant Camptothecus. It can selectively inhibit topoisomerase and interfere with DNA replication of tumor cells, thereby inhibiting tumor cell The discovery of the unique anti-cancer mechanism of camptothecin has aroused great interest in the field of medical research all over the world. However, due to the disadvantages of camptothecin, such as large toxic and side effects, poor water solubility, and short half-life in vivo, its application is limited to a certain extent. [0003] Microcapsule technology is a te...

Claims

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Application Information

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IPC IPC(8): A61K31/4745A61K9/52A61K47/34A61K47/38A61P35/00
Inventor 岳秀丽王洋阎秀峰
Owner HAERBIN FENGYUAN HIGH TECH DEV
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