摘要
目的 建立帕洛诺司琼血浆中药物浓度的液-质联用检测方法，研究其在人体的药物动力学。方法 9名健康男性受试者随机自身交叉给药，分别注射高、中、低3个不同剂量帕洛诺司琼，样品经MTBE萃取，用Hypersil BDS C18柱分离，以格拉司琼为内标，采用HPLC-MS／MS检测血浆中药物浓度。结果 帕洛诺司琼在0．23～14．20ng·mL^-1呈线性关系，日内、日间变异均〈15％，1．5、0．75、0．25mg不同剂量组帕洛诺司琼药物动力学参数分别是Cmax：（7．46±1．03）、（3．27±0．76）、（1．06±0．23）ng·mL^-1。AUC0～∞：（235．68±32．06）、（108．84±35．77）、（32．44±12．69）ng·mL^-1·h，t1/2：（41．87±5．36）、（41．88±4．68）、（39．88±3．54）h，达峰时间均为0．083h。结论 本方法准确、灵敏，运用本法研究了9名健康受试者静脉注射不同剂量帕洛诺司琼后药物动力学，为临床确定给药方案提供了很好的理论基础。
Objective To establish an HPLC-MS/MS method to determine palonosetron concentration and study its pharmacokinetics in healthy chinese volunteers. Metlhods Nine subjects were given high, medium, and low dose of palonosetmn. The sample was extracted with MTBE and separated on Hypersil BDS C18 column with granisetron as the internal standard. Results Good linearity was obtained over 0. 23-14. 20 ng . mL^-1. The intra-day and inter-day precisions were both less than 15%. The Cmax of 1.5 mg, 0. 75 mg, and 0. 25 mg palonosetron was （7. 46± 1.03）, （3. 27 ± 0. 76）, and （1.06 ± 0. 23） ng . mL^-1 ; for AUC the value was （235.68 ± 32.06）, （108. 84 ± 35.77）, and （32.44 ± 12.69） ng . mL^-1. h. The half-life time was （41.87±5.36）, （41.88±4. 68）, and （39.88±3. 54） h respectively. Good lincarity was obtained over 0. 23±14.20 ng . mL^-1. The intra-day and inter-day precisions were both less than 15%. The Cmax of 1.5 mg, 0. 75 mg, and 0. 25 mg palonosetron was （7. 46±1.03）, （3.27±0. 76）, and （1.06±0. 23） ng . mL^-1; for AUC the value was （235.68± 32.06）, （108.84±35.77）, and （32.44±12.69） ng.mL^-1 .h. The half-life was（41.87±5.36）, （41.88±4.68）, and （39. 88±3. 54） h respectively. Conclusion This method is accurate and sensitive. It provided good theoretical foundation for the clinical use of palonosetron.
出处
《中南药学》
CAS
2007年第4期322-325,共4页
Central South Pharmacy
