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OBJECTIVE:To study the pharmacokinetics of oral single dose adefovir dipivoxil(ADV) tablet in Chinese healthy volunteers.METHODS:The study was a randomized,open,three-way crossover study.Twelve healthy volunteers were randomly assigned to receive single oral dose of 5 mg(Group A),10mg(Group B) or 30 mg(Group C) ADV tablets in three weeks.The plasma concentrations of ADV were determined by LC/MS/MS method.The pharmacokinetic parameters were computed.RESULTS:The main pharmacokinetic parameters in Group A,B and C were as follows:Cmax were(11.4? 3.7),(25.4? 8.2) and(76.3? 23.0) ng? mL-1;tmax were(1.69? 1.41),(0.90? 0.56) and(0.94? 0.50) h;AUC0～ t were(102.7? 51.7),(235.0? 82.3) and(715.4? 267.6) ng? h.mL-1;AUC0～ ∞ were(168.7? 30.7),(266.2? 83.7) and(741.5? 273.9) ng? h? mL-1,respectively.CONCLUSION:ADV tablets had a rapid absorption in healthy volunteers and the Cmax and AUC of adefovir tablets were directly correlated to doses.It is safe for healthy volunteers to take ADV tablets at a dose of 5～30mg.
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Objective To carry out a pharmacokinetic evaluation of oral FK506 in 13 patients after renal transplant. Methods 13 patients after renal transplantation were given prograf based immunosupressive regimen 24 hours after surgery.Blood samples to determine FK506 levels were drawn in heparinized tube at 0、20、40、60、90 min and 2、3、6、8、10 hours after the first oral dosing.The whole blood concentrations were measured by MEIA and the pharmacokinetic parameters were calculated by 3P87 program.The FK506 doses were recorded in detail for the first month. Results Cmax was (13.6259?4.1117)ng/ml;T(peak) was (1.4866?1.0725)h;t1/2 ? was (0.7749?0.7791)h,t1/2 ? was (10.7267?10.4926)h;AUC was (91.0415?40.7694)ng?ml -1 ?h -1 ,CL was (0.046?0.0036)ng?ml -1 ?h -1 and MRT was (8.1540?4.2937)h.AUC was negative correlateld with prograf dose in the first month posttransplant (r=-0.53, P =0.038). Conclusions The absorption of oral administration of FK506 was rapid in patients after renal transplantation,and can achieve Cmax in (1.5?1.1)h,the mean half life time being 10.7 h.The pharmacokinetic parameters can be the guideline for FK506 application.