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Pharmacokinetics and metabolism of transdermal oxybutynin: in vitro and in vivo performance of a novel delivery system.透皮奥昔布宁的药代动力学与代谢:一种新型给药系统的体外和体内性能
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Pharmacokinetics of the R- and S-enantiomers of oxybutynin and N-desethyloxybutynin following oral and transdermal administration of the racemate in healthy volunteers.消旋奥昔布宁在健康志愿者中口服和经皮给药后,其R-和S-对映体以及N-去乙基奥昔布宁的药代动力学。
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A short-term, multicenter, randomized double-blind dose titration study of the efficacy and anticholinergic side effects of transdermal compared to immediate release oral oxybutynin treatment of patients with urge urinary incontinence.一项短期、多中心、随机双盲剂量滴定研究,比较经皮与速释口服奥昔布宁治疗急迫性尿失禁患者的疗效及抗胆碱能副作用。
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Prospective randomized controlled trial of extended-release oxybutynin chloride and tolterodine tartrate in the treatment of overactive bladder: results of the OBJECT Study.氯氮卓斯汀缓释片与酒石酸托特罗定治疗膀胱过度活动症的前瞻性随机对照试验:OBJECT研究结果
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用于膀胱过度活动症的透皮给药系统:原理与实践。

Transdermal systems for overactive bladder: principles and practice.

作者信息

Staskin David R

出版信息

Rev Urol. 2003;5 Suppl 8(Suppl 8):S26-30.

PMID:16985986
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1502387/
Abstract

The transdermal system for delivery of medication to treat overactive bladder may provide an improved efficacy-to-tolerability ratio by regulating serum drug levels; avoiding gastrointestinal and hepatic metabolism, which is important when the metabolite has a lesser therapeutic index than the parent drug; and achieving clinical efficacy with a lower total drug burden. Additional advantages may include increased compliance and obviation of the need for oral drug administration, which is especially beneficial for the patient who is taking multiple oral medications or is caregiver-dependent. An efficient patch system must preserve the physical integrity of the drug layer, provide adequate adhesion, store and release the drug and permeation-enhancing agent in a predictable manner, promote consistent absorption through the skin regardless of location or skin or subcutaneous tissue differences, demonstrate dose proportionality, maintain skin integrity during product use and removal, and be cosmetically acceptable. A novel transdermal delivery system that incorporates an occlusive layer covering an acrylic adhesive containing the active agent oxybutynin and a skin permeation enhancer has been demonstrated in clinical trials to achieve these goals.

摘要

用于治疗膀胱过度活动症的透皮给药系统可通过调节血清药物水平来提高疗效与耐受性的比率;避免胃肠道和肝脏代谢,当代谢物的治疗指数低于母体药物时,这一点很重要;并以较低的总药物负担实现临床疗效。其他优点可能包括提高依从性以及无需口服给药,这对正在服用多种口服药物或依赖护理人员的患者尤其有益。一个有效的贴片系统必须保持药物层的物理完整性,提供足够的粘附力,以可预测的方式储存和释放药物及渗透促进剂,无论位置、皮肤或皮下组织差异如何,都能促进药物通过皮肤的一致吸收,显示剂量比例性,在产品使用和移除过程中保持皮肤完整性,并且在美观上是可接受的。一种新型透皮给药系统,其包含覆盖含有活性剂奥昔布宁和皮肤渗透促进剂的丙烯酸粘合剂的封闭层,已在临床试验中证明可实现这些目标。