He Lei, Wang Gui-ling, Zhang Qiang
Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.
Yao Xue Xue Bao. 2003 Mar;38(3):227-30.
To evaluate the hypersensitivity reaction of the blank paclitaxel microemulsion and study the O/W paclitaxel microemulsion's pharmacokinetics in rats.
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.
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.
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.
评价空白紫杉醇微乳的过敏反应，并研究水包油型紫杉醇微乳在大鼠体内的药代动力学。
制备粒径较小的替代型紫杉醇微乳。在豚鼠中研究空白微乳的过敏反应。在药代动力学研究中，给5只大鼠静脉注射紫杉醇或紫杉醇微乳。于0、0.25、0.5、1、2、4、6、8、10、12、14小时采集血样，采用高效液相色谱法测定血浆中紫杉醇浓度。所得数据用3P87程序处理。
微乳平均粒径为17.2nm。空白微乳制剂未显示任何过敏反应，而注射市售产品则显示出明显的过敏反应。紫杉醇微乳和市售注射液（紫杉醇）的浓度 - 时间曲线符合二室模型。紫杉醇微乳的K10、K12、K21和AUC分别为0.571.h-1、1.441.h-1、3.081.h-1和34.98mg.h.L-1。市售注射液的分别为1.291.h-1、1.271.h-1、0.511.h-1和21.85mg.h.L-1。
与空白市售注射液相比，空白紫杉醇微乳制剂降低了豚鼠的过敏反应。紫杉醇微乳在大鼠体内具有相对较长的循环时间。
