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Pharmacokinetics and pharmacodynamics of a new transdermal delivery system for bopindolol.

机译:一种新的波平多洛尔透皮给药系统的药代动力学和药效学。

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摘要

1. In two separate studies, each with 12 healthy male volunteers, the pharmacokinetic and dynamic properties of a transdermal delivery system for bopindolol were evaluated. 2. In study I it was shown that bopindolol absorption from a 14 mg patch occurred over the whole 7-day application period. No signs of a significant skin depot were found. 3. In study II, a linear pharmacokinetic behaviour but a non-linear kinetic/dynamic relationship was established for the patches over a dose range from 7 to 21 mg. Comparable peak effects of reduction in exercise-induced tachycardia were observed after different patch doses and an i.v. injection. However, the effect was significantly prolonged with the patches compared with the injection and was maintained over 7 days. 4. The patches showed a good local and systemic tolerability in both studies over a dosing interval of up to 7 days.
机译:1.在两项分别有12名健康男性志愿者的独立研究中,评估了苯哌多洛透皮给药系统的药代动力学和动态特性。 2.在研究I中,研究表明,在整个7天的施用过程中,从14 mg贴剂中吸收出了布比多洛。没有发现明显的皮肤仓库的迹象。 3.在研究II中,在7至21 mg的剂量范围内,贴剂建立了线性药代动力学行为,但非线性动力学/动力学关系。在不同的贴剂剂量和静脉输注后,观察到了运动诱发的心动过速减少的可比峰值效应。注射。但是,与注射剂相比,贴剂的效果显着延长,并维持7天以上。 4.在两项研究中,在长达7天的给药间隔中,贴剂均显示出良好的局部和全身耐受性。

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