Montgomery P R, Sitar D S
Biopharm Drug Dispos. 1986 Jan-Feb;7(1):21-5. doi: 10.1002/bdd.2510070104.
Acetylsalicylic acid (ASA) was administered orally as a single dose to 7 healthy male volunteers as plain or enteric-coated (Entrophen) tablets using a crossover design. Blood and urine samples were collected and analysed for ASA metabolites by high performance liquid chromatography. Labile and stable glucuronide conjugates of salicylic acid (SA) were measured in urine after differential hydrolysis with glucuronidase. Plasma kinetic parameters for the ASA metabolites SA and salicyluric acid were not different for the 2 formulations, apart from the delayed appearance after the enteric-coated tablets. Total urinary recovery, and recovery of salicyluric acid and the two SA glucuronides were not different, thus confirming the equivalent bioavailability and metabolite profile of the 2 ASA formulations.
以交叉设计对7名健康男性志愿者口服单剂量的乙酰水杨酸(ASA),剂型为普通片剂或肠溶包衣(Entrophen)片剂。采集血液和尿液样本,采用高效液相色谱法分析其中ASA的代谢产物。用葡萄糖醛酸酶进行差异水解后,测定尿液中水杨酸(SA)的不稳定和稳定葡萄糖醛酸共轭物。两种剂型的ASA代谢产物SA和水杨尿酸的血浆动力学参数并无差异,只是肠溶包衣片剂后的出现时间有所延迟。两种剂型的总尿回收率、水杨尿酸回收率以及两种SA葡萄糖醛酸共轭物的回收率并无差异,从而证实了两种ASA剂型具有等效的生物利用度和代谢产物谱。