【摘 要】
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Pharmacological studies demonstrated that paclitaxel (Zisu(R)) was very active in the inhibition of the growth of human cancer cell panel including KB cells, HC
【机 构】
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Institute of Materia Medica
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Pharmacological studies demonstrated that paclitaxel (Zisu(R)) was very active in the inhibition of the growth of human cancer cell panel including KB cells, HCT-8, A2780, and MCF-7 cells. The IC50 was as low as 0.0019, 0.0019, 0.0036 and 0.01 m g/ml respectively. Experimental therapeutic studies indicated that paclitaxel(Zisu(R)) significantly inhibited the growth of melanoma B-16, Walker carcinomsarcoma and heterotransplanted human ovarian cancer in nude mice. Biochemical pharmacological studies showed that paclitaxel (Zisu(R)) could accelerate microtubule assembly and inhibit its deassembly; population in G1 was decreased while the cell population in G2+M phase was increased significantly. In addition, a polyploid cell population appeared. Pharmacokinetic studies demonstrated that the t1/2a was 0.12 h and t1/2b was 5.02 h when it was injected intravenously at a dose of 5 mg/kg in rats. The AUC, Vc and CLs were 11.82(m g.h)/ml, 0.50L/kg and 0.42L(h.kg) respectively.
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