Bioequivalence study on two terazosin hydrochloride tablets / 药学实践杂志

Objective To evaluate the bioequivalence of domestic and imported terazosin hydrochloride tablets after single oral dose .Methods It was a single center ,randomized ,open ,cross-over trail design ,21 subjects were fasting oral adminis-tered of 2 mg domestic and imported terazosin hydrochloride tablets in different periods ,venous blood 4 ml were collected in different time points before and 60 h after administration ,plasma concentration of terazosin was determined by LC-MS/MS . Results The main pharmacokinetic parameters of domestic and imported terazosin hydrochloride tablets were as follows :t1/2 :(13.2± 2.39)hvs(12.5±1.93)h,tmax :(1.01±0.83)hvs(1.08±0.69)h,Cmax :(40.1±10.6)ng/mlvs(37.3± 9 .57) ng/ml;AUC0- ∞ :(428 ± 82 .1) ng · h/ml vs (426 ± 85 .2) ng · h/ml .The relative bioavailability of domestic terazosin hydrochloride tablets was (101 .2 ± 14 .7)% .90% CI of domestic and imported terazosin hydrochloride tablets AUC0-t and Cmax geometric mean ratio fell between 80% -125% .Conclusion The domestic tablets are bioequivalent to the imported tablets .

Pharmacokinetics and relative bioavailablity of domestic penicillin V dispersion tablet / 中国临床药理学与治疗学

Aim To study pharmacokinetics and bioavailablity of domestic penicillin V dispersion tablet in healthy volunteers. Methods According to the crossover design, each volunteer in two groups was orally given a single dose ( 0.75 g ) of domestic penicillin V dispersion tablet or imported penicillinV tablet alternately and the plasma concentrations were determined by RP HPLC. The pharmacokinetic parameters were obtained by using ATPK program and calculated on the basis of open single compartment model. Results After a single oral dose( 0.75 g ), the t 1/2(ke) was ( 0.75 ? 0.10 ) h and ( 0.70 ? 0.14 ) h ,the c max was( 8.44 ? 2.40 ) mg?L -1 and ( 8.75 ? 3.04 ) mg?L -1 at ( 0.56 ? 0.11 ) h and ( 0.63 ? 0.17 ) h and AUC 0～4 was( 8.44 ? 2.40 ) mg?h?L -1 and ( 8.75 ? 3.04 ) mg?h?L -1 for two formulations, respectively. Relative bioavailability of domestic penicillin V dispersion tablet was ( 90.50 ? 8.84 )%. Conclusion The result shows that the two formulations are bioequivalent.

Pharmacokinetic-pharmacodynamic modeling of irbesartan in healthy Chinese adult volunteers / 中国药理学通报

Aim To investigate the combined pharmacokinetic-pharmacodynamic(PK-PD) model of irbesartan in healthy Chinese male volunteers. Methods Eighteen healthy male volunteers received 300 mg irbesartan tablet orally. The plasma drug concentration (C_p) was determined by HPLC and pharmacologic effects, including SBP, DBP and HR, were measured simultaneously. The pharmakinetic and PK-PD model parameters were calculated. Results The pharmacokinetic profiles were best fitted a two-compartment open model. There was a hysteresis loop between effects and plasma concentrations. The relationship between effects and effect compartment concentrations of drugs could be represented by the Sigmoid-E_ max model. Conclusion We successfully eatablished the PK-PD model of irbesartan in healthy male volunteers. These findings may provide a more rational basis for patient-specific dosage individualization.