Suber R L, Lee C, Torosian G, Edds G T
Department of Preventative Medicine and Toxicology, College of Pharmacy, University of Florida, Gainesville 32610.
J Pharm Sci. 1981 Sep;70(9):981-4. doi: 10.1002/jps.2600700903.
The pharmacokinetic profile of sulfisoxazole was studied and compared in dogs, swine, and humans. The trial was conducted over a 72-hr period after intravenous administration and a 96-hr period after oral administration in dogs and swine. In humans, the trial was conducted over an 8-hr period after oral administration. A two-compartment model system was used to define the pharmacokinetic profile. The mean half-lives for the distribution phase were 4.08, 1.30, and 0.56 hr in dogs, swine, and humans, respectively. For the elimination phase, the mean half-lives were 33.74, 46.39, and 7.40 hr in dogs, swine, and humans, respectively. The mean volume of the central compartment was approximately the same in dogs and swine, 10.6 and 10.5 liters, respectively. Humans had a smaller volume of distribution, 7.7 liters. The steady-state volumes of distribution were 17.2, 30.3, and 16.2 liters in dogs, swine, and humans, respectively. Dogs and swine excreted 42.2 and 30.7%, respectively, of the intravenous dose and 29.4 and 18.3%, respectively, of the oral dose. The bioavailability was 69.8% in dogs and 100.0% in swine. The fraction of drug bound ranged from 30 to 50% in dogs, 40 to 60% in swine, and 25 to 40% in humans.
对狗、猪和人类体内的磺胺异恶唑药代动力学特征进行了研究和比较。在狗和猪身上，静脉给药后进行了72小时的试验，口服给药后进行了96小时的试验。在人类身上，口服给药后进行了8小时的试验。采用二室模型系统来定义药代动力学特征。分布相的平均半衰期在狗、猪和人类中分别为4.08、1.30和0.56小时。消除相的平均半衰期在狗、猪和人类中分别为33.74、46.39和7.40小时。狗和猪中央室的平均容积大致相同，分别为10.6升和10.5升。人类的分布容积较小，为7.7升。狗、猪和人类的稳态分布容积分别为17.2、30.3和16.2升。狗和猪分别排泄静脉剂量的42.2%和30.7%，口服剂量的29.4%和18.3%。狗的生物利用度为69.8%，猪为100.0%。药物结合分数在狗中为30%至50%，在猪中为40%至60%，在人类中为25%至40%。
