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Self-emulsifying system composition of 10-hydroxycamptothecine as well as preparation method and applications of self-emulsifying system composition

A hydroxycamptothecin and self-emulsifying technology, which can be used in pharmaceutical combinations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. Activity and other issues to achieve the effect of improving bioavailability, improving stability, and optimizing drug dissolution and release

Active Publication Date: 2016-09-07
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The pH of the intestinal microenvironment of the human body is about 6.8. Therefore, when 10-hydroxycamptothecin is in the intestinal microenvironment, the bioavailability of its effective configuration is low, which greatly affects its pharmacological activity. , which limits its application in the treatment of intestinal tumors

Method used

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  • Self-emulsifying system composition of 10-hydroxycamptothecine as well as preparation method and applications of self-emulsifying system composition
  • Self-emulsifying system composition of 10-hydroxycamptothecine as well as preparation method and applications of self-emulsifying system composition
  • Self-emulsifying system composition of 10-hydroxycamptothecine as well as preparation method and applications of self-emulsifying system composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Dissolve 2g of 10-hydroxycamptothecin in 700ml of 1,2-propanediol, and disperse evenly by ultrasonic, add 400mL of TPGS and 300mL of polyoxyethylene castor oil to mix and disperse evenly by ultrasonic, then add 500mL of ethyl oleate, and mix well Then place it in a constant temperature water-bath shaker at 37°C until a transparent uniform solution is formed to obtain a self-emulsifying system composition of 10-hydroxycamptothecin.

Embodiment 2

[0032] Dissolve 1g of 10-hydroxycamptothecin in 900mL of polyethylene glycol-400, and disperse evenly by ultrasonic; After uniformity, place in a constant temperature water bath shaker at 37°C until a transparent uniform solution is formed to obtain a self-emulsifying system composition of 10-hydroxycamptothecin.

Embodiment 3

[0034] Dissolve 2g of 10-hydroxycamptothecin in 500mL of glycerin, and disperse evenly by ultrasonic, add 500mL of TPGS and 600mL of polyoxyethylene castor oil to mix and disperse evenly by ultrasonic, then add 300mL of isopropyl myristate, and mix well Place in a constant temperature water bath shaker at 37°C until a transparent uniform solution is formed to obtain a self-emulsifying system composition of 10-hydroxycamptothecin.

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Abstract

The invention relates to a self-emulsifying system composition of 10-hydroxycamptothecine as well as a preparation method and applications of the self-emulsifying system composition. The self-emulsifying system composition is composed of an oil phase, a co-emulsifier and an emulsifier at the volume ratio of (1-10) to (2-15) to (5-20), as well as 10-hydroxycamptothecine with the concentration of 0.01-2 mg / mL in the self-emulsifying system composition, wherein the emulsifier is composed of tocopherol polyethylene glycol 1000 succinate and polyoxyethylene castor oil at the volume ratio of (1-10) to (1-10). The self-emulsifying system composition has good stability in the intestinal microenvironment, the hydrolysis of the lactone structure in 10-hydroxycamptothecine and the overturn of the effective configuration of 10-hydroxycamptothecine can be effectively prevented, the ratio of the effective configuration of 10-hydroxycamptothecine in the intestinal tract is improved, the stability of 10-hydroxycamptothecine is improved, and the application range of 10-hydroxycamptothecine is expanded.

Description

technical field [0001] The invention relates to a self-emulsifying system composition, in particular to a self-emulsifying system composition of 10-hydroxycamptothecin and a preparation method and application thereof. Background technique [0002] 10-Hydroxycamptothecin is another alkaloid extracted from camptothecin, where the hydrogen at the 10th carbon atom of camptothecin is replaced by a hydroxyl group. It is a cell cycle-specific drug that inhibits DNA replication primarily by acting on topoisomerase I, thereby inhibiting cell proliferation. The drug has a wide anti-cancer spectrum, no cross-resistance with other anti-tumor drugs, and has significant curative effect on various malignant tumors such as liver cancer and gastric cancer. It has been widely used in tumor chemotherapy regimens and is an important clinical anti-cancer drug. component. [0003] The drug stability of 10-hydroxycamptothecin depends on the pH of the environment. When pH<5.0, almost all 10-hy...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/4745A61K47/34A61K47/44A61P35/00
CPCA61K47/22A61K47/44A61K9/08A61K31/4745
Inventor 冯敏王勇
Owner SUN YAT SEN UNIV
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