TABLE 1.
Summary of pharmacokinetic parameters of AS, DHA, and AQ following administration of a single oral dose of the test and reference products in Chinese healthy volunteersa
| Drug and metabolite parameter | Values for indicated treatment |
|||
|---|---|---|---|---|
| T1 | T2 | R1 | R2 | |
| Artesunate | ||||
| Cmax (ng/ml) | 312 ± 161 (51.6) | 307 ± 197 (64.1) | 330 ± 189 (57.2) | 342 ± 214 (62.5) |
| Median Tmax in h (range) | 0.33 (0.17–1.5) | 0.33 (0.17–1.0) | 0.33 (0.17–1.0) | 0.33 (0.17–1.0) |
| AUC0-last (ng · h/ml) | 174 ± 54.3 (31.3) | 162 ± 65.5 (40.6) | 180 ± 59.7 (33.1) | 180 ± 73.0 (40.6) |
| AUC0-inf (ng · h/ml) | 186 ± 75.4 (40.5) | 168 ± 65.4 (39.1) | 188 ± 61.2 (32.5) | 187 ± 71.5 (38.1) |
| t1/2 (h) | 0.56 ± 0.37 (66) | 0.54 ± 0.43 (79) | 0.57 ± 0.39 (68) | 0.53 ± 0.45 (85) |
| λz (1/h) | 1.8 ± 1.1 (61) | 1.9 ± 1.2 (62) | 1.7 ± 1.1 (63) | 2.0 ± 1.2 (58) |
| Dihydroartemisinin | ||||
| Cmax (ng/ml) | 606 ± 319 (52.6) | 661 ± 304 (46.0) | 648 ± 288 (44.5) | 644 ± 265 (41.2) |
| Median Tmax in h (range) | 0.50 (0.33–1.5) | 0.50 (0.33–1.5) | 0.50 (0.33–2.0) | 0.50 (0.33–2.0) |
| AUC0-last (ng · h/ml) | 983 ± 338 (34.4) | 980 ± 272 (28.1) | 1,081 ± 275 (25.4) | 1,040 ± 277 (26.6) |
| AUC0-inf (ng · h/ml) | 993 ± 338 (34.1) | 991 ± 338 (27.5) | 1,090 ± 274 (25.1) | 1,052 ± 274 (26.0) |
| t1/2 (h) | 1.1 ± 0.3 (23) | 1.1 ± 0.5 (45) | 1.1 ± 0.3 (24) | 1.1 ± 0.3 (30) |
| λz (1/h) | 0.7 ± 0.1 (21) | 0.7 ± 0.1 (24) | 0.7 ± 0.1 (20) | 0.7 ± 0.1 (22) |
| Amodiaquine | ||||
| Cmax (ng/ml) | 41.2 ± 22.2 (53.7) | 39.1 ± 19.8 (50.6) | 45.1 ± 20.5 (45.4) | 39.7 ± 19.3 (48.6) |
| Median Tmax in h (range) | 0.50 (0.33–1.0) | 0.50 (0.17–2.0) | 0.50 (0.33–1.0) | 0.50 (0.33–0.75) |
| AUC0-last (ng · h/ml) | 331 ± 125 (37.9) | 311 ± 137 (44.1) | 327 ± 134 (40.8) | 317 ± 140 (44.1) |
| AUC0-inf (ng · h/ml) | 355 ± 126 (35.4) | 337 ± 139 (41.2) | 352 ± 134 (38.0) | 341 ± 142 (41.7) |
| t1/2 (h) | 12.2 ± 2.3 (19.0) | 12.2 ± 2.2 (17.9) | 11.6 ± 2.4 (21.0) | 12.1 ± 2.4 (20.0) |
| λz (1/h) | 0.06 ± 0.01 (21.8) | 0.06 ± 0.01 (21.1) | 0.06 ± 0.02 (24.2) | 0.06 ± 0.01 (23.1) |
a
The test and reference products were administered as 2× 100/270 mg ASAQ. Results are presented as means ± standard deviations (SD) (interindividual percent coefficient of variation [CV]) for all subjects who completed the study per protocol (n = 31) except where otherwise indicated. T1, the first time a subject received the test product; T2, the second time a subject received the test product; R1, the first time a subject received the reference product; R2, the second time a subject received the reference product.