Wecker M T, Graves D A, Amsel L P, Hinsvark O N, Rotenberg K S
J Pharm Sci. 1987 Jan;76(1):29-31. doi: 10.1002/jps.2600760109.
The influence of a standard meal on the extent and rate of absorption of pseudoephedrine from a controlled-release (CR) capsule formulation (Pennkinetic System) was studied in 16 normal male volunteers. Equivalent single doses of an immediate-release (IR) pseudoephedrine reference syrup and the CR capsules were each studied under both fasted and postprandial conditions. Pharmacokinetic analysis evaluated the fraction of drug absorbed over time as determined by the Wagner-Nelson method. The area under the drug concentration versus time curve (AUC) results were not influenced by food or formulation, indicating that the CR formulation was absorbed to the same extent as the IR syrup. The maximum plasma concentration (Cmax) and the time to maximum concentration (tmax) tabulations under fasted conditions indicated that the CR preparation peaked at a lower level and a later time than the IR syrup. Food minimally affected the Cmax of the IR formulation, but did not affect that of the CR formulation. Food delayed the tmax of both the IR and CR preparations by less than 1 h, but only the delay of the CR formulation was statistically significant. Neither delay was considered clinically meaningful. The results of this study strongly suggest that the pharmacokinetic profile of the CR pseudoephedrine capsules was minimally affected by the presence of food.
在16名正常男性志愿者中研究了标准餐对伪麻黄碱从控释（CR）胶囊制剂（Pennkinetic系统）的吸收程度和速率的影响。在禁食和餐后条件下分别研究了等效单剂量的速释（IR）伪麻黄碱参比糖浆和CR胶囊。药代动力学分析通过Wagner-Nelson方法评估了随时间吸收的药物分数。药物浓度-时间曲线（AUC）结果不受食物或制剂的影响，表明CR制剂与IR糖浆的吸收程度相同。禁食条件下的最大血浆浓度（Cmax）和达峰时间（tmax）列表表明，CR制剂的峰值低于IR糖浆，且出现时间较晚。食物对IR制剂的Cmax影响最小，但对CR制剂的Cmax没有影响。食物使IR和CR制剂的tmax延迟均小于1小时，但只有CR制剂的延迟具有统计学意义。两种延迟均不被认为具有临床意义。本研究结果强烈表明，食物的存在对CR伪麻黄碱胶囊的药代动力学特征影响最小。
