Moriyama Y, Arimori K, Nakano M
Department of Pharmacy, Kumamoto University Hospital, Japan.
Biol Pharm Bull. 1997 Jun;20(6):701-3. doi: 10.1248/bpb.20.701.
The absorption characteristics of azasetron, a serotonin type 3 (5-HT3) receptor antagonist which is used for the treatment of chemotherapy-induced emesis and nausea, were investigated in rabbits. The serum concentrations of azasetron following rectal administration as a suppository increased rapidly and showed the mean tmax value of 0.18 h. The concentrations were greater after rectal administration than those after oral administration. The absolute bioavailability was significantly different between the rectal, 52.9% and oral doses, 21.6%. The mean Cmax and tmax values after the rectal dose were 904.8 ng/ml and 0.18 h, respectively, whereas those after the oral dose averaged 124.7 ng/ml and 0.85 h, respectively. These results indicate that azasetron is absorbed to a greater extent and more rapidly into the systemic circulation via the rectum than via the intestine in rabbits. Consequently, the suppository form of azasetron hydrochloride may be feasible for the treatment of chemotherapy-induced acute emesis and nausea.
对用于治疗化疗引起的呕吐和恶心的5-羟色胺3（5-HT3）受体拮抗剂阿扎司琼的吸收特性在兔体内进行了研究。以栓剂形式直肠给药后阿扎司琼的血清浓度迅速升高，平均达峰时间（tmax）值为0.18小时。直肠给药后的浓度高于口服给药后的浓度。直肠给药（52.9%）和口服给药（21.6%）的绝对生物利用度有显著差异。直肠给药后的平均血药峰浓度（Cmax）和达峰时间分别为904.8 ng/ml和0.18小时，而口服给药后的平均血药峰浓度和达峰时间分别为124.7 ng/ml和0.85小时。这些结果表明，在兔体内，阿扎司琼经直肠比经肠道能更大程度且更快速地吸收进入体循环。因此，盐酸阿扎司琼栓剂形式可能对治疗化疗引起的急性呕吐和恶心是可行的。
