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Nano particles of taxane cyclodextrin inclusion compound and preparation method thereof

A technology of cyclodextrin inclusion compound and taxane, which is applied in the field of taxane cyclodextrin inclusion compound nanoparticles and its preparation, can solve the problems of nanoparticles not mentioned, and achieve improved solubility and tumor inhibition The effect of increasing the rate and stabilizing the product quality

Active Publication Date: 2006-12-20
SHANGHAI ALLIST PHARM CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] As we all know, paclitaxel has great application value and economic benefits, but its wide application has obvious disadvantages: the solubility of paclitaxel in water is 0.006mg / ml, and the key technology of its intravenous infusion preparation is to solve its solubility in water
[0008] Belgian Sisen Laboratory Co., Ltd. mixed paclitaxel, acetyl-γ-cyclodextrin and hydroxypropyl-β-cyclodextrin in ethanol, and freeze-dried the resulting solid for water solubility research, and has applied for a Chinese patent (Application No. 98811010.5), but does not mention nanoparticles

Method used

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  • Nano particles of taxane cyclodextrin inclusion compound and preparation method thereof
  • Nano particles of taxane cyclodextrin inclusion compound and preparation method thereof
  • Nano particles of taxane cyclodextrin inclusion compound and preparation method thereof

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Embodiment Construction

[0045] Preparation of Paclitaxel Cyclodextrin Nanoparticles--

[0046] The prescription is as follows:

[0047] Paclitaxel 2mg

[0048] Hydroxypropyl Beta Cyclodextrin 15mg

[0049] Povidone K29 / 32 10mg

[0050]Method: Add povidone K29 / 32 to the hydroxypropyl beta-cyclodextrin solution, mix well and heat to 40°C, add paclitaxel drug solution under magnetic stirring at 900rpm, keep the temperature and stir for 3hr, freeze-dry (add nectar Alcohol, dextran and other leavening agents) or rotary evaporation to remove the organic solvent, to obtain freeze-dried powder injection.

[0051] After testing, more than 90% of the obtained paclitaxel nanoparticles have a particle diameter of 70-80 nm, a solubility of paclitaxel of 0.6 mg / ml, and can be stable for 6-8 hours at room temperature.

[0052] After dissolving the obtained freeze-dried powder injection in water, give 40 mg / kg to tumor-bearing nude mice. After 2 weeks, the tumor inhibition rate of the paclitaxel nanoparticle gro...

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Abstract

The invention relates to a Paclitaxel cyclodextrin clathrate compound nanometer grain and relative medicine agent, wherein it uses hydroxypropyl-beta-cyclodextrin as carrier and PVP as stabilizer to prepare Paclitaxel clathrate compound nanometer grain, whose diameter is 40-200nm, to improve the dissolvability of Paclitaxel as 100-50times. The animal experiment has proven that: compared with present Paclitaxel, its resistant agent is improved 2.67tims with better cancer resistant effect. The invention uses general material and simple condition, with stable quality and the application to be processed into oral agent.

Description

technical field [0001] The invention relates to taxane cyclodextrin inclusion complex nanoparticles and a preparation method thereof, in particular to the preparation of taxane inclusion complex nanoparticles by hydroxypropyl-β-cyclodextrin. Cyclodextrin inclusion can solubilize and slow-release taxanes, thereby enhancing drug efficacy, thus providing a new and feasible way for anticancer drug taxanes to be used clinically. technical background [0002] Paclitaxel (Taxol) is a natural product isolated from the bark of the Pacific Yew tree. Paclitaxel has good anticancer activity and has become the third-generation antineoplastic drug after doxorubicin and cisplatin. It is toxic to the mitotic spindle and is a strong cytostatic agent. Paclitaxel has good effects in the treatment of ovarian cancer and breast cancer, and has good effects in the treatment of prostate cancer, upper gastrointestinal cancer, small cell and non-small cell lung cancer. On February 29, 1992, the U.S...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61K47/40A61P35/00
Inventor 郭建辉朱瀛
Owner SHANGHAI ALLIST PHARM CO LTD
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