نبذة مختصرة : Olanzapine, a second-generation atypical antipsychotic drug, is widely used for schizophrenia and moderate to severe mania associated with bipolar disorders. This open-label, randomized, single-dose, 2-sequence, 2-period crossover, comparative pharmacokinetic study assessed the bioequivalence of 5 mg of olanzapine administered in tablet (R) or disintegrating tablet (T) formulation in healthy Chinese volunteers under both fasting and fed conditions. Numbers of enrolled subjects were 30 and 24 for fasting and fed treatments, respectively. Blood samples were drawn and collected predose as well as up to 144 hours postdose. The plasma concentration of olanzapine was quantitated by a robust, rapid, and sensitive liquid chromatography-tandem mass spectrometry method. The R was bioequivalent to T formulation under either fasting or fed conditions. The 90%CI for ratios of the geometric means observed maximum plasma concentration, area under the curve from time 0 extrapolated to last time point, and area under the curve from time 0 extrapolated to infinity were all within the allowed limit (80.0% to 125.0%). The pharmacokinetic profiles of T and R formulations were similar under fasting and fed conditions. Both formulations were well tolerated, with a similar incidence of treatment-emergent adverse events under fasting and fed conditions.
(© 2019, The American College of Clinical Pharmacology.)
References: Callaghan JT, Bergstrom RF, Ptak LR, Beasley CM. Olanzapine. Clin Pharmacokinet. 1999;37(3):177-193.
Mauri MC, Paletta S, Di Pace C, et al. Clinical pharmacokinetics of atypical antipsychotics: an update. Clin Pharmacokinet. 2018;57(12):1493-1528.
Zhao J, Ou J, Xue H, et al. Clinical utility of orally disintegrating olanzapine in Chinese patients with schizophrenia: a review of effectiveness, patient preference, adherence, and other properties. Neuropsych Dis Treat. 2014;10:355-359.
Fulton B, Goa KL. Olanzapine. Drugs. 1997;53(2):281-298.
Lacro JP, Dunn LB, Dolder CR, Leckband SG, Jeste DV. Prevalence of and risk factors for medication nonadherence in patients with schizophrenia: a comprehensive review of recent literature. J Clin Psychiat. 2002;63(10):892-909.
Fu Y, Yang S, Jeong SH, Kimura S, Park K. Orally fast disintegrating tablets: developments, technologies, taste-masking and clinical studies. Crit Rev Ther Drug Carrier Syst. 2004;21(6):433-476.
San L, Casillas M, Ciudad A, Gilaberte I. Olanzapine orally disintegrating tablet: a review of efficacy and compliance. CNS Neurosci Ther. 2008;14(3):203-214.
Zhao J, Jiang K, Li Q, et al. Cost-effectiveness of olanzapine in the first-line treatment of schizophrenia in China. J Med Econ. 2019;22(5):439-446.
Chen J, Lou H, Jiang B, et al. Effects of food and gender on pharmacokinetics of rosuvastatin in a Chinese population based on 4 bioequivalence studies. Clin Pharmacol Drug Dev. 2020;9:235-245.
Du P, Li P, Zhao R, Liu H, Liu L. Optimized UPLC-MS/MS method for the quantitation of olanzapine in human plasma: application to a bioequivalence study. Bioanalysis. 2019;11(13):1291-1302.
Du P, Guan Y, An Z, et al. Selective and robust UPLC-MS/MS method for simultaneous quantitative determination of anlotinib, ceritinib and ibrutinib in rat plasma and its application to pharmacokinetic study. Analyst. 2019;144(18):5462-5471.
Chen J, Zhuang J, Wu J, et al. Bioequivalence of oral formulations of anastrozole in healthy Chinese male volunteers: a randomized, single-dose, two-period, two-sequence crossover study. Clin Pharmacol Drug Dev. 2019;8(2):217-222.
Bergstrom RF, Mitchell M, Witcher J, et al. Rapid onset of absorption with olanzapine orally disintegrating tablets. J Emerg Nurs. 2004;30(5):416-417.
Bonde SL, Bhadane RP, Gaikwad A, et al. Simultaneous determination of olanzapine and fluoxetine in human plasma by LC-MS/MS: its pharmacokinetic application. J Pharmaceut Biomed. 2014;90:64-71.
Processing Request
No Comments.