Tse F L, Welling P G
J Pharm Sci. 1977 Dec;66(12):1751-4. doi: 10.1002/jps.2600661225.
With a fasted dog as an animal model, the bioavailability and pharmacokinetics of prednisolone were studied following rapid intravenous injection and oral dosing of a prednisolone sodium phosphate solution and also following oral doses of prednisolone as tablets and a slurry. Hydrolysis of the phosphate ester to prednisolone in the body is extremely rapid and complete, thus permitting accurate calculation of the distribution volume of prednisolone. Enteral absorption of prednisolone from a slurry is superior to that from prednisolone tablets and from a prednisolone sodium phosphate solution. Reduced absorption from tablets, compared to the slurry, is probably due to tablet disintegration characteristics; reduced absorption from the solution is probably due to poor membrane permeability of the ionized drug. Information obtained from a single animal may indicate the need for expanded studies in humans.
以禁食犬为动物模型，在快速静脉注射和口服泼尼松龙磷酸钠溶液以及口服泼尼松龙片剂和混悬液后，研究了泼尼松龙的生物利用度和药代动力学。磷酸酯在体内水解为泼尼松龙的过程极其迅速且完全，从而能够准确计算泼尼松龙的分布容积。泼尼松龙混悬液的肠吸收优于泼尼松龙片剂和泼尼松龙磷酸钠溶液。与混悬液相比，片剂吸收减少可能归因于片剂的崩解特性；溶液吸收减少可能是由于离子化药物的膜通透性较差。从单一动物获得的信息可能表明需要在人体中开展进一步研究。
