Gai M N, Thielemann A M, Arancibia A
Department of Science and Pharmaceutical Technology, Faculty of Chemical and Pharmaceutical Sciences, University of Chile, Santiago.
Int J Clin Pharmacol Ther Toxicol. 1993 Nov;31(11):547-52.
Food-induced changes on the bioavailability of a sustained-release theophylline tablet, which uses acrylic resins Eudragit as sustaining agent, were studied in 12 healthy male volunteers. The tablet was developed in our laboratory using conventional technology. It presented a good bioavailability pattern and maintained plasmatic concentrations within the therapeutic range for 12 hours under conditions of steady-state. The study design was a 4 x 4 latin square involving 12 subjects who received a single dose of the tablet while fasting or with a standardized normal, high fat or high fat/high protein meal. The results showed no differences in AUC, K, tmax, ka and MRT. Statistical differences were found in Cmax comparing the fasting condition with high fat/high protein diet. A delay was also observed in the detection of the drug in plasma when the tablet was administered with high fat and high fat/high protein food, but clinically the changes seem to be irrelevant.
在12名健康男性志愿者中研究了食物对一种以丙烯酸树脂尤特奇作为缓释剂的茶碱缓释片生物利用度的影响。该片剂是我们实验室采用传统技术研制的。它呈现出良好的生物利用度模式，在稳态条件下可将血浆浓度维持在治疗范围内达12小时。研究设计为4×4拉丁方，涉及12名受试者，他们在禁食状态下或与标准化的正常餐、高脂餐或高脂/高蛋白餐一起服用单剂量的该片剂。结果显示，曲线下面积（AUC）、消除速率常数（K）、达峰时间（tmax）、吸收速率常数（ka）和平均滞留时间（MRT）无差异。在比较禁食状态与高脂/高蛋白饮食时的血药峰浓度（Cmax）发现有统计学差异。当该片剂与高脂和高脂/高蛋白食物一起服用时，还观察到血浆中药物检测出现延迟，但临床上这些变化似乎无关紧要。
