OBJECTIVE: To observe of pharmacokinetics of orally taking
ivermectin 6, 12, 18 mg and bioavailability afterpo (Per os) ivermechn
tablet 12 mg. METHODS: Three groups of volunteers (8 subjects in each group)
orally took ivermertin 6, 12, 18mg. Two kinds of
ivermectin tablet were orally administered by randomized-cross and auto-pair method within 2 weeks in the group of po 12mg. Plasma and urine concentration of ivermectin was detected by HPLC method. RESULTS: AUCo- was in proportion to dose of po ivermecitn 6-12mg (418 1 288ug.h.L-1 in 6mg group, 813 1 156ug.h.L-1 in 12 mg group), but AUCo- (980 f 474 ug.h.L-1) did not increase when dosage of po ivermectin reached 18mg compared with po 12mg. C-T curves of the 3 dosages of po ivermectin accorded with one-compent linear elimination model. t1/2ke of po ivermectin 6,12 and 18mg was 11.1 1 4.6, 21.1 1 7.0, 16.7 1 6.6 h, respectively. AUCo-72h was 791.4 1 243.ins.h.L-1 the ivermectin tablet 12mg) and 734.6 1 202.9 ug.h.L-1 (po MECTIZAN 12mg), Cmax was 31.7 1 5.6 (po ivermectin tablet 12 mg) and 31.1 1 4.7 ig.L-1(po MECTIZAN 12mg). Relative bioavailability was 102 1 19%. The two parameters were of not significant difference (P<0.05) via bioequivalence test. tmax was 3.9 1 l.6 h (po ivermectin tablet 12mg) and 4.1 1 l.2 h (Po MECTIZAN 12mg), and was significant difference (P<0.05; bioequivalence test). CONCLUSIONS: The data showed basically accordance with linear elimination pharmacoklnetics after po ivermectin 6-18mg, but the Phenomenon of absorphon saturation appeared when the dosage of po ivermectin 18mg. AUC and Cma were bioequivalent after po two sorts of ivermectin tablet. Prototype of ivermetin did not exist in urine sample following po ivermectin.