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  • Title: [Studies on hypersensitivity and pharmacokinetics of paclitaxel microemulsion].
    Author: He L, Wang GL, Zhang Q.
    Journal: Yao Xue Xue Bao; 2003 Mar; 38(3):227-30. PubMed ID: 12830723.
    Abstract:
    AIM: To evaluate the hypersensitivity reaction of the blank paclitaxel microemulsion and study the O/W paclitaxel microemulsion's pharmacokinetics in rats. METHODS: An alternative paclitaxel microemulsion was prepared with small particle size. The hypersensitivity reaction of the blank microemulsion was investigated in guinea pigs. In pharmacokinetic study, 5 rats were given i.v. Taxol or paclitaxel microemulsion. Blood samples were collected at 0, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 14 h and the concentration of paclitaxel in plasma was determined by HPLC method. The data obtained were processed using 3P87 program. RESULTS: The mean size of the microemulsion is 17.2 nm. The preparation of blank microemulsion did not show any hypersensitivity, while the injection of commercial product showed significant hypersensitivity. The concentration-time curve of paclitaxel microemulsion and commercial injection (Taxol) fitted a two-compartment model. The K10, K12, K21 and AUC of paclitaxel microemulsion were 0.571.h-1, 1.441.h-1, 3.081.h-1 and 34.98 mg.h.L-1. Those of commercial injection were 1.291.h-1, 1.271.h-1, 0.511.h-1 and 21.85 mg.h.L-1. CONCLUSION: The blank paclitaxel preparation of micoemulsion reduced the hypersensitivity in guinea pigs compared with the blank commercial injection. The paclitaxel microemulsion has relatively longer circulating time in rats.
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