De Bree H, De Boer A G
Pharm Weekbl Sci. 1987 Jun 19;9(3):179-82. doi: 10.1007/BF01967538.
Ranitidine hydrochloride solution was given rectally to six healthy volunteers by means of an osmotic pump (Osmet) at a zero-order rate for 8 h. Quite constant steady-state drug concentrations were achieved in the range of 64-123 ng/ml plasma (mean Css: 100.6 ng/ml). The mean absorption time was 0.45 h (range 0-I.02 h), indicating that absorption was not always instantaneous. It is concluded that the Osmet system together with the rectal route offer the possibility for achieving steady-state concentrations of ranitidine, enabling the determination of pharmacodynamic effects. In addition, the rectal route can be considered as an alternative to oral and intravenous administration.
通过渗透泵(Osmet)以零级速率对6名健康志愿者直肠给予盐酸雷尼替丁溶液,持续8小时。血浆中药物浓度在64 - 123 ng/ml范围内达到相当稳定的稳态(平均Css:100.6 ng/ml)。平均吸收时间为0.45小时(范围0 - 1.02小时),表明吸收并非总是瞬间完成。结论是,渗透泵系统与直肠给药途径相结合,为实现雷尼替丁的稳态浓度提供了可能性,从而能够确定药效学效应。此外,直肠给药途径可被视为口服和静脉给药的替代方法。