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Determination of concentration of granisetron in New Zealand rabbit plasma by UFLCMS/MS and its application to pharmacokinetic study after transdermal administration
Pages: 145-150
Year: Issue:  3
Journal: World Clinical Drugs

Keyword:  granisetronUFLC-MS/MSliquid-liquid extractiontransdermalpatchpharmacokinetic;
Abstract: Objective To develop an UFLC-MS/MS method for the determination of granisetron concentration in New Zealand rabbits plasma and to investigate the pharmacokinetics of self-made granisetron hydrochloride transdermal patches and Sancuso patches. Methods Using parallel design, a total of 12 New Zealand rabbits were randomly divided into the drug-exposed group and the control group with 6 rabbits in each group, which were given self-made patches and Sancuso’s patches respectively. The plasma concentration of granisetron was determained by a validated UFLC-MS/MS method. The pharmacokinetic parameters were calculated by DAS 2.1.1. Results The calibration curve of granisetron was linear within the concentration range of 1.0~500 ng/ml. The method recoveries were within 92.5%~101.4%. The RSDs of intra- and inter-day presicion were less than 5%. The mean pharmacokinetic parameters were as follows: AUC(0-t)(2106±337.0)and(2402±557.7) μg/L.h, AUC(0-∞)(2107±336.8) and(2404±558.7) μg/L.h, C max(63.03±17.53) and(82.32±34.76)μg/L, T max(3.7±2.3) and(4.8±3.2) h, T1/2(2.4±1.5) and(3.5±2.5) h, respectively for self-made patches and Sancuso’s patches. Conclusion The UFLC-MS/ms method is effective, rapid, sensitive, accurate, specifi c and suitable for granisetron therapeutic drug monitoring. The pharmacokinetics results indicated that self-made patches and Sancuso’s patches were different signifi cantly over the same administration cycle.
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