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Paclitaxel Derivative (paclitaxel + derivative)

Distribution by Scientific Domains
Chemistry100%

Selected Abstracts

Determination of a hydrophilic paclitaxel derivative, 7-xylosyl-10-deacetylpaclitaxel in rat plasma by LC,MS/MS

BIOMEDICAL CHROMATOGRAPHY, Issue 5 2009
Shou Gang Jiang
Abstract A LC-MS/MS method for the determination of a hydrophilic paclitaxel derivative 7-xylosyl-10-deacetylpaclitaxel in rat plasma was developed to evaluate the pharmacokinetics of 7-xylosyl-10-deacetylpaclitaxel in the rats. 7-Xylosyl-10-deacetylpaclitaxel and docetaxel (IS for 7-xylosyl-10-deacetylpaclitaxel) were extracted from rat plasma with acetic ether and analyzed on a Hypersil C18 column (4.6 × 150 mm i.d., particle size 5 µm) with the mobile phase of ACN/0.05% formic acid (50:50, v/v). The analytes were detected using an ESI MS/MS in the multiple reaction monitoring mode. The standard curves for 7-xylosyl-10-deacetylpaclitaxel in plasma were linear (r >0.999) over the concentration range of 2.0,1000 ng/mL with a weighting of 1/concentration2. The method showed a satisfactory sensitivity (2.0 ng/mL using 50 µL plasma), precision (CV , 10.1%), accuracy (relative error ,12.4 to 12.0%), and selectivity. This method was successfully applied to the pharmacokinetic study of 7-xylosyl-10-deacetylpaclitaxel in rat plasma after intravenous administration of 7-xylosyl-10-deacetylpaclitaxel to female Wistar rats. Copyright © 2008 John Wiley & Sons, Ltd. [source]

Determination of a novel paclitaxel derivative (NPD-103) in human plasma by ultra-performance liquid chromatography,tandem mass spectrometry

BIOMEDICAL CHROMATOGRAPHY, Issue 5 2009
Shuang-Qing Zhang
Abstract A sensitive and specific ultra-performance liquid chromatography,tandem mass spectrometry (UPLC-MS-MS) method for quantification of a newly developed anticancer agent NPD-103 has been established. An aliquot of human plasma sample (200 µL) was spiked with 13C-labeled paclitaxel (internal standard) and extracted with 1.3 mL of tert -butyl methyl ether. NPD-103 was quantitated on a C18 column with methanol,0.1% formic acid (75:25, v/v) as mobile phase using UPLC-MS-MS operating in positive electrospray ionization mode with a total run time of 3.0 min. For NPD-103 at the concentrations of 1.0, 5.0 and 10.0 µg/mL in human plasma, the absolute extraction recoveries were 95.58, 102.43 and 97.77%, respectively. The linear quantification range of the method was 0.1,20.0 µg/mL in human plasma with linear correlation coefficients greater than 0.999. The intra- and inter-day accuracy for NPD-103 at 1.0, 5.0 and 10.0 µg/mL levels in human plasma fell into the ranges of 95.29,100.00% and 91.04,94.21%, and the intra- and inter-day precisions were in the ranges of 8.96,11.79% and 7.25,10.63%, respectively. This assay is applied to determination of half-life of NPD-103 in human plasma. Copyright © 2008 John Wiley & Sons, Ltd. [source]

A New and Simply Available Class of Hydrosoluble Bioconjugates by Coupling Paclitaxel to Hyaluronic Acid through a 4-Hydroxybutanoic Acid Derived Linker

HELVETICA CHIMICA ACTA, Issue 1 2005
Francesca Leonelli
A simple preparation of a new hydrosoluble paclitaxel bioconjugate 8, representing a new class of paclitaxel derivatives, is described. Bioconjugate 8 was obtained by coupling hyaluronic acid (2) to paclitaxel (1) by means of a 4-hydroxybutanoic acid derived linker (Scheme,2). [source]