Progress in the development of alternative pharmaceutical formulations of taxanes

被引：78

作者：

Nuijen, B ^{[1
]}

Bouma, M ^{[1
]}

Schellens, JHM ^{[1
]}

Beijnen, JH ^{[1
]}

机构：

[1] Netherlands Canc Inst, Slotervaart Hosp, Dept Pharm & Pharmacol, NL-1006 BK Amsterdam, Netherlands

来源：

INVESTIGATIONAL NEW DRUGS | 2001年 / 19卷 / 02期

关键词：

taxanes; paclitaxel; docetaxel; alternative formulation; co-solvents; surfactants; emulsions; micro-encapsulation systems; liposomes; cyclodextrines; prodrugs;

D O I：

10.1023/A:1010682916808

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

The currently available taxanes paclitaxel (Taxol(R)) and docetaxel (Taxotere(R)) are clinically effective against advanced breast, ovarian and non-small cell lung cancer. Due to their low aqueous solubility, both taxanes posed difficulties to the pharmaceutical scientists with respect to the development of an intravenous dosage form. At present, paclitaxel is formulated in a mixture of 50:50% (v/v) Cremophor EL and dehydrated ethanol. However, this formulation vehicle is associated with a number of pharmacological, pharmacokinetic and pharmaceutical concerns amongst which serious hypersensitivity reactions. This review deals with the attempts made into the development of alternative dosage forms of paclitaxel devoid of the Cremophor EL/ethanol excipients and potential future taxane formulations.

引用

页码：143 / 153

页数：11

共 56 条

[1]

Adams J D, 1993, J Natl Cancer Inst Monogr, P141

[2] Preclinical in vivo efficacy of two 9-dihydrotaxane analogues against human and murine tumours [J].