RESUMO
OBJECTIVE: To study the pharmacokinetics of blonanserin and its main metabolite in Chinese healthy volunteers after multiple-dose administration. METHODS: Twenty Chinese healthy volunteers were randomly divided to two groups and given 4 mg blonanserin twice daily (bid) and 8 mg blonanserin once daily (qd) for 7 d, respectively. HPLC-MS/MS was used to determine the plasma concentrations of blonanserin and its metabolite N-desethyl blonanserin. The pharmacokinetic parameters were calculated by DAS software. RESULTS: The main pharmacokinetic parameters of blonanserin and its metabolite after multiple-dose administration of 4 mg bid were as follows; pav were (327.75±83.83) and (200.38±67.75) ng · L-1; tmax were(1.48±0.69) and (4.15±2.16) h; t1/2 were(12.98±3.35) and(18.68±4.90) h; AUCSS were (3933.00±1005.96) and(2404.56±813.03) ng · h · L-1; AUC0-∞ were (8160.18±2173.64) and (7730.84±1732.06) ng · h · L-1. CONCLUSION: The inter-individual variation of the pharmacokinetic parameters of blonanserin is very large and therapeutic drug monitoring of blonanserin will be needed during clinical therapy.