摘要
目的建立高效液相色谱法测定大鼠血浆中甲磺酸伊马替尼浓度,并研究其在大鼠体内的药物动力学。方法色谱柱为Dikma Diamonsil C18;流动相为甲醇-1%三乙醇胺溶液=55：45（pH=6）;流速为1.0 mL min-1;柱温为30℃;检测波长285 nm;并用该液相方法测定伊马替尼在SD大鼠体内的药动学参数。结果伊马替尼血药浓度在20~2 000 ng mL-1线性关系良好（r=0.999 3）,最低检测限为20 ng mL-1;日内、日间RSD均〈15%,提取回收率在82.1%~87.5%。6只SD大鼠单剂量静脉给予伊马替尼（10 mg kg-1）后药动学参数分别为：Cmax（1 567.4±127.5）ng mL-1;t1/2（15.6±3.5）h;MRT（17.9±4.6）h;Vd（27.3±6.9）L;AUC0~24 h（2 267.4±109.6）ng h mL-1;AUC0~∞（3 308.2±208.2）ng h mL-1。结论本方法简便、准确、灵敏、专属性强,可作为伊马替尼临床用药时的药动学数据补充。
Objective To develop a simple and sensitive HPLC-UV method to quantify imatinib in rat plasma. Methods The chromatographic separation was carried out on a Dikma Diamonsil C 18 column with a mobile phase consisting of methanol-1% TEA（55 ：45, v/v, pH = 6） at 1.0 mL min- 1. The column temperature was 30 ℃. UV wavelength mode was used, with imatinib monitored at 285 nm. Results The calibration was linear at 20- 2 000 ng mL- 1for imatinib. Inter-day and intra-day imprecision was 15% for imatinib. The pharmacokinetic parameters were： C max（1 567.4±127.5） ng mL- 1;t 1/2（15.6±3.5） h;MRT（17.9±4.6） h;Vd（27.3±6.9） L;AUC0 ~ 24h（2 267.4±109.6） ng h mL- 1;AUC 0 ~ ∞（3 308.2±208.2） ng h mL- 1. Conclusion This simple, sensitive, accurate and cost-effective method can be used in routine clinical practice to monitor imatinib concentrations in the plasma.
出处
《中南药学》
CAS
2013年第11期818-820,共3页
Central South Pharmacy
