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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.

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。

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Pharmacokinetic characterisation of transdermal delivery systems.透皮给药系统的药代动力学特征
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The pharmacokinetics of oxybutynin in man.奥昔布宁在人体中的药代动力学。
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