Nilsson C G, Lukkari E, Haarala M, Kivelä A, Hakonen T, Kiilholma P
Department of Obstetrics and Gynecology, Helsinki University Central Hospital, Finland.
Neurourol Urodyn. 1997;16(6):533-42. doi: 10.1002/(sici)1520-6777(1997)16:6<533::aid-nau3>3.0.co;2-f.
Oxybutynin has long been used for the treatment of patients with detrusor overactivity and urinary urge incontinence. The short half-life of oxybutynin administered as a conventional tablet formulation or syrup requires 2-3 times daily dosage to be effective. A new controlled release (CR) tablet for once-daily administration has been developed. The efficacy and tolerability of this new controlled release tablet was compared to that of a 5-mg conventional oxybutynin tablet administered twice daily. Seventeen female incontinent patients were studied in a double-dummy crossover trial. Efficacy and tolerability were assessed by using a voiding diary, pad-weighing test, visual-analogue scale (VAS), and questionnaire. Adverse events were recorded spontaneously on a questionnaire by the patients themselves throughout the study. Serum concentrations of oxybutynin and its active metabolite N-desethyloxybutynin were studied after both a single dose and multiple dosage. There was no difference in efficacy between the two formulations. Depending on the parameters tested, the change from baseline values in a positive direction ranged from 15 to 53%. The incidence of adverse events was similar with both formulations. Oxybutynin or its metabolite showed no cumulation during the multiple dosage with a 10-mg CR tablet. The controlled release tablet formulation is as effective and as well-tolerated as the conventional one, but has the advantage of only once-a-day dosage, enhancing treatment compliance.
奥昔布宁长期以来一直用于治疗逼尿肌过度活动症和尿急失禁患者。以传统片剂或糖浆剂型给药的奥昔布宁半衰期较短，需要每日给药2 - 3次才能起效。现已开发出一种每日一次给药的新型控释（CR）片剂。将这种新型控释片剂的疗效和耐受性与每日两次给药的5毫克传统奥昔布宁片剂进行了比较。在一项双盲交叉试验中对17名女性尿失禁患者进行了研究。通过排尿日记、尿垫称重试验、视觉模拟量表（VAS）和问卷调查来评估疗效和耐受性。在整个研究过程中，患者通过问卷自行记录不良事件。在单剂量和多剂量给药后，研究了奥昔布宁及其活性代谢物N - 去乙基奥昔布宁的血清浓度。两种剂型在疗效上没有差异。根据所测试的参数，从基线值向正向的变化范围为15%至53%。两种剂型的不良事件发生率相似。在使用10毫克CR片剂进行多剂量给药期间，奥昔布宁或其代谢物未显示出蓄积现象。控释片剂剂型与传统剂型一样有效且耐受性良好，但具有每日只需给药一次的优势，提高了治疗依从性。
