Michel-Guéroult P, Benoit I, Grellet J, Meynat Y, Merlet J P, Saux M C
Institut de Pharmacie Industrielle, Université de Bordeaux II.
Therapie. 1993 Jan-Feb;48(1):27-32.
The purpose of the study was to develop and to test a new form of rectal systemic gel for methohexitone administration in children undergoing minor surgery. Pharmacokinetics of methohexitone were determined in children following intravenous or intrarectal administration either at low or therapeutic dosage. Anaesthesic efficacy of this gel was performed in 11 patients receiving a therapeutic dosage (25 mg/kg). Pharmacokinetics of methohexitone appears independent of both dosage and route of administration in children. The bioavailability of the rectal gel appears sufficient to provide efficient clinical plasmatic concentrations. As a consequence of the rapid and good resorption of methohexitone from rectal lumen and of the low variability of plasmatic concentrations, a rapid and reliable sedation was observed in all patients. The clinical anaesthesic efficacy of the rectal hydrophilic gel associated with the absence of an apparent local intolerance and important side effects, make this new form suitable for methohexitone administration in children.
本研究的目的是开发并测试一种新型直肠全身用凝胶,用于接受小手术的儿童静脉注射美索比妥。在儿童以低剂量或治疗剂量静脉注射或直肠给药后,测定了美索比妥的药代动力学。对11名接受治疗剂量(25mg/kg)的患者进行了该凝胶的麻醉效果研究。美索比妥的药代动力学在儿童中似乎与剂量和给药途径均无关。直肠凝胶的生物利用度似乎足以提供有效的临床血浆浓度。由于美索比妥从直肠腔快速且良好地吸收,以及血浆浓度变异性低,在所有患者中均观察到快速且可靠的镇静作用。直肠亲水凝胶的临床麻醉效果,加上无明显局部不耐受和严重副作用,使得这种新剂型适用于儿童美索比妥给药。