Lukkari E, Castrèn-Kortekangas P, Juhakoski A, Löyttyniemi E, Aranko K, Neuvonen P J
Leiras Oy, Helsinki, Finland.
Eur J Clin Pharmacol. 1996;50(3):221-3. doi: 10.1007/s002280050096.
The effect of food on the bioavailability of oxybutynin was assessed in a randomised cross-over study in 23 healthy volunteers. A single oral 10 mg dose of a controlled release oxybutynin tablet was administered after a high fat breakfast and to fasting subjects. The AUC, Cmax, tmax, t1/2 and MRT of oxybutynin and its active metabolite N-desethyloxybutynin were determined.
Breakfast did not change the AUC of oxybutynin but increased the AUC of N-desethyloxybutynin by about 20%. The Cmax of oxybutynin and N-desethyloxybutynin were two-fold higher when the drug was administered after breakfast compared to the fasting state.
Breakfast significantly reduced the MRT of oxybutynin and N-desethyloxybutynin.
在一项针对23名健康志愿者的随机交叉研究中评估食物对奥昔布宁生物利用度的影响。在高脂早餐后及空腹状态下分别给予单次口服10mg控释奥昔布宁片。测定奥昔布宁及其活性代谢物N-去乙基奥昔布宁的AUC、Cmax、tmax、t1/2和MRT。
早餐未改变奥昔布宁的AUC，但使N-去乙基奥昔布宁的AUC增加约20%。与空腹状态相比，早餐后给药时奥昔布宁和N-去乙基奥昔布宁的Cmax高出两倍。
早餐显著降低了奥昔布宁和N-去乙基奥昔布宁的MRT。
