Sasaki S, Koumi S, Sato R, Murata M, Nagasawa K, Sakurai E, Hikichi N, Hayakawa H
Department of Pharmacy, Tama-Nagayama Hospital, Tokyo, Japan.
Gen Pharmacol. 1998 Oct;31(4):589-91. doi: 10.1016/s0306-3623(98)00045-7.
Buccal absorption has an advantage when compared with other administration routes because of its rapid onset of action. We examined the pharmacokinetics of buccal-absorbed propafenone in healthy humans. 1. After a single oral administration of 150 mg of propafenone, the average peak concentration of propafenone was 27.9+/-2.5 ng/ml, and that of 5-hydroxypropafenone was 61.7+/-6.6 ng/ml (n=5). The times to reach peak serum concentrations of propafenone and 5-hydroxypropafenone were 1.8+/-0.1 hr and 1.5+/-0.2 hr, respectively. 2. After a buccal absorption of 150 mg of propafenone, the time to reach peak serum concentration of propafenone was 16.9+/-2.3 min (n=8). The average peak concentration of propafenone was 30.4+/-1.4 ng/ml (n=8), and the concentrations of 5-hydroxypropafenone were below the detection limit in all subjects. The rapid upstroke of serum concentrations of propafenone by buccal administration may cause rapid onset of pharmacological conversion.
与其他给药途径相比，颊部吸收具有起效迅速的优势。我们研究了健康人体内颊部吸收的普罗帕酮的药代动力学。1. 单次口服150毫克普罗帕酮后，普罗帕酮的平均峰浓度为27.9±2.5纳克/毫升，5-羟基普罗帕酮的平均峰浓度为61.7±6.6纳克/毫升（n = 5）。普罗帕酮和5-羟基普罗帕酮达到血清峰浓度的时间分别为1.8±0.1小时和1.5±0.2小时。2. 颊部吸收150毫克普罗帕酮后，普罗帕酮达到血清峰浓度的时间为16.9±2.3分钟（n = 8）。普罗帕酮的平均峰浓度为30.4±1.4纳克/毫升（n = 8），所有受试者中5-羟基普罗帕酮的浓度均低于检测限。颊部给药后普罗帕酮血清浓度的快速上升可能导致药理转换的快速起效。
