Article Figures & Data
Figures
- Fig. 1.
Concentration versus time curves of paclitaxel in whole blood (○) and plasma (•; A) and of CrEL (▪) in plasma (B). Pharmacokinetic data were obtained from a female patient receiving the drug formulated at 6 mg/ml in a mixture of CrEL-dehydrated ethanol USP (1:1, v/v) at an absolute dose of 256 mg.
Tables
- Table 1
Blood:plasma concentration ratio of paclitaxel in the absence and presence of various concentrations of CrEL, castor oil, and HPLC fractions of CrELa
Compound added (%) Blood:plasma ratio Percentage change vs. control (%) Pb None 1.07 ± 0.004 CrEL (0.01) 1.09 ± 0.009 +1.83 0.387 CrEL (0.05) 0.990 ± 0.015 −9.35 0.012 CrEL (0.10) 0.901 ± 0.017 −15.8 0.003 CrEL (0.50) 0.690 ± 0.005 −35.5 <0.0001 CrEL (1.0) 0.625 ± 0.008 −41.6 <0.0001 Castor oil (0.50) 1.23 ± 0.171 +13.0 0.061 CrEL fraction 1 (0.50) 1.06 ± 0.008 −0.94 0.520 CrEL fraction 2 (0.50) 0.926 ± 0.018 −13.5 0.043 CrEL fraction 3 (0.50) 0.763 ± 0.055 −28.7 0.010 CrEL fraction 4 (0.50) 0.645 ± 0.051 −39.7 0.003 CrEL fraction 5 (0.50) 0.943 ± 0.039 −11.9 0.103 -
a Paclitaxel was used at an initial concentration of 1 μg/ml and incubated in whole blood for 15 min at 37°C before fractionation and HPLC analysis. Ratio data are presented as mean values ± SD of (at least) triplicate measurements.
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b Probability value versus control (unpaired two-sided Student’s t test).
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- Table 2
Distribution of paclitaxel in artificial binary mixture systems of the main blood fractions in the absence and presence of CrELa
Binary system CrEL (%) Total:extracellular ratio Percentage change vs. control (%) Pb Erythrocytes/bufferc None 3.70 ± 0.061 0.50 0.649 ± 0.014 −82.5 <0.001 Erythrocytes/plasmac None 1.03 ± 0.021 0.50 0.664 ± 0.007 −35.5 0.002 Platelets/plasmad None 1.33 ± 0.037 0.50 1.26 ± 0.024 −5.26 0.018 -
a Paclitaxel was used at an initial concentration of 1 μg/ml and incubated in whole blood for 15 min at 37°C before fractionation and HPLC analysis. Ratio data are presented as mean values ± SD of (at least) triplicate measurements.
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b Probability value versus control (unpaired two-sided Student’s t test).
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c Hematocrit, ∼0.45.
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a Platelet count, ∼750 × 109/L.
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- Table 3
CrEL concentration-dependent blood:plasma ratio and unbound paclitaxel fraction in plasma of a patienta
Time (h)b CrEL (%) Blood:plasma ratio Unbound fraction 0.50 0.039 1.02 0.076 1.0 0.122 0.795 0.057 1.5 0.157 0.851 0.038 2.0 0.215 0.749 0.028 2.5 0.300 0.737 0.022 3.0 0.335 0.623 0.016 -
a Paclitaxel was administered as an i.v. infusion over a 3-h period at an absolute dose of 256 mg to a single female with advanced ovarian cancer.
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b Sample collection time point after the start of a 3-h i.v. infusion of paclitaxel.
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Volume 59, Issue 7
