STUDY ON PHARMACOKINETICS AND BIOAVAILABILITY OF DOMESTIC SULTAMICILLIN CAPSULE AND GRANULE

The pharmacokinetics and bioavailability of sultamicillin capsule and sultamicillin granule were compared with those of imported product Unasyn tablet . A single oral dose of 750 mg sultamicillin was given to 9 male volunteers in an open randomized cross over study . Plasma levels of ampicillin were detected by HPLC-FL method and sulbactam were determined by HPLC-UV . The concentration time curves of ampicillin and sulbactam were fitted to one compartment model estimated by 3P87 program. The pharmacokinetic parameters of three formulations for ampicillin were T1/2:1.04±0.22 h,1.19±0.44 h,0.89±0.12 h (P0.05); TPK: 0.83±0.45 h,1.24±0.27 h,0.59±0.16 h(P0.05); Cmax:12.35±3.13 mg·L-1,10.94±2.41mg·L-1,15.42±2.33 mg·L-1 (P0.05) respectively, for sulbactam were T1/2:1.17±0.26 h, 1.23±0.28 h, 1.18±0.23 h (P0.05); TPK:0.75 ±0.46 h, 1.58±0.41 h, 0.71±0.25 h (P0.05); Cmax: 4.49±2.44 mg·L-1, 4.27±1.66 mg·L-1,5.03 ±2.05 mg·L-1 (P0.05).The relative bioavailability of ampicillin were capsule=103.05±14.78%,Granule=102.39±10.81% , and sulbactam were capsule=103.99±13.39%, Granule =103.29±11.56%, respectively. The results demonstrated that the three preparations were bioequivalent by t-test,two one sided tests and analysis of variance.