Lie-A-Huen L, Proost J H, Kingma J H, Meijer D K
Department of Clinical Pharmacy, St. Antonius Hospital, Nieuwegein, The Netherlands.
Eur J Clin Pharmacol. 1990;38(6):595-8. doi: 10.1007/BF00278588.
The absorption kinetics of different pharmaceutical formulations of orally and rectally administered flecainide have been assessed in a cross-over study in 7 healthy volunteers. The subjects received single doses of flecainide after a washout period of at least one week. A tablet, an oral solution, a rectal solution and a 10 min i.v. infusion during 10 min each containing 100 mg flecainide were administered to the subjects in a randomized order. The mean absolute bioavailability was 98%, 78% and 81% for the rectal and oral solutions and the tablet. The lag time after administration of the oral solution was 0.33 h and it was 0.86 h after the tablet and 0.18 h after the rectal solution. The mean time to the peak serum concentration (tmax) after the rectal solution (0.67 h) was shorter than after either the tablet (4 h) or oral solution (1 h). The maximum serum concentration (Cmax) was 0.29 mg.l-1 after the rectal solution, 0.14 mg.l-1 after the tablet and 0.17 mg.l-1 after the oral solution. All the volunteers showed significantly higher serum flecainide concentrations during the first 20 min of the absorption phase after rectal administration of 100 mg flecainide as a solution compared to its oral administration.
based on the absolute bioavailability, Cmax, tmax, and lag times, rectal administration of flecainide solution gave a better absorption profile than after oral tablet or solution.
在一项针对7名健康志愿者的交叉研究中，评估了口服和直肠给药不同剂型氟卡尼的吸收动力学。在至少一周的洗脱期后，受试者接受单剂量氟卡尼。将一片片剂、一种口服溶液、一种直肠溶液以及在10分钟内静脉输注的含100毫克氟卡尼的溶液以随机顺序给予受试者。直肠溶液、口服溶液和片剂的平均绝对生物利用度分别为98%、78%和81%。口服溶液给药后的滞后时间为0.33小时，片剂给药后为0.86小时，直肠溶液给药后为0.18小时。直肠溶液给药后达到血清峰值浓度（tmax）的平均时间（0.67小时）短于片剂（4小时）或口服溶液（1小时）。直肠溶液给药后的最大血清浓度（Cmax）为0.29毫克/升，片剂给药后为0.14毫克/升，口服溶液给药后为0.17毫克/升。与口服给药相比，所有志愿者在直肠给予100毫克氟卡尼溶液后的吸收阶段的前20分钟内血清氟卡尼浓度显著更高。
基于绝对生物利用度、Cmax、tmax和滞后时间，直肠给予氟卡尼溶液的吸收情况优于口服片剂或溶液。
