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首页> 外文期刊>Life sciences >Cardiovascular effects of transdermally delivered bupranolol in rabbits: Effect of chemical penetration enhancers
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Cardiovascular effects of transdermally delivered bupranolol in rabbits: Effect of chemical penetration enhancers

机译：透皮递送的丁苯丙醇对家兔的心血管作用：化学渗透促进剂的作用

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Bupranolol is a promising candidate for transdermal drug delivery system (TDDS) development. The effect of permeation enhancers on the in vivo delivery and beta-blocking effect of reservoir type TDDS was studied in comparison with intravenous BPL in rabbits. The beta-blocking effect was quantified by measuring the inhibition of isoprenaline induced tachycardia in rabbits after BPL administration via transdermal and intravenous routes. The reservoir type TDDS containing a hydroxypropyl cellulose gel and polyethylene membrane was used as a control device. In comparison, the TDDS containing skin penetration enhancers, either 2-pyrrolidone or partially methylated beta cyclodextrin (PM beta CD) were evaluated. The control device (no enhancer) produced about 52% inhibition of isoprenaline induced tachycardia at 2 h and the effect continued over 24 h application period, however, the devices with 2-pyrolidone or PM beta CD produced about 85% inhibition of isoprenaline induced tachycardia at 3 h and the same effect continued over 24 It application period. Likewise, the AUC of these devices were significantly higher than that of control device. The intravenous bupranolol showed rapid decline in the pharmacodynamic effect with time indicating its rapid elimination. The in vivo delivery of bupranolol (as estimated by a mass balance study) from the devices made with pyrolidone or PM beta CD was 3-fold higher than that of control. The results of this study strongly suggest that the penetration enhancers in the TDDS increased the in vivo delivery of BPL, thereby increased the beta-blocking activity of BPL by 50-60% higher than control, enabling the reduction of the TDDS patch size, accordingly. (C) 2007 Elsevier Inc. All rights reserved.
机译：普萘洛尔是透皮给药系统（TDDS）开发的有希望的候选者。与静脉内BPL相比，研究了渗透增强剂对储库型TDDS的体内递送和β阻断作用的影响。通过测量经透皮和静脉内途径给予BPL后兔对异丙肾上腺素诱导的心动过速的抑制作用，可以量化β阻滞作用。包含羟丙基纤维素凝胶和聚乙烯膜的储库型TDDS用作对照装置。相比之下，评估了含有皮肤渗透促进剂（2-吡咯烷酮或部分甲基化的β-环糊精（PMβCD））的TDDS。对照装置（无增强剂）在2小时内抑制约52％的异丙肾上腺素引起的心动过速，并且效果持续了24小时，但是，带有2-吡咯烷酮或PMβCD的装置抑制了约85％的异丙肾上腺素引起的心动过速在3小时后，在24 It应用期间持续了相同的效果。同样，这些设备的AUC显着高于控制设备的AUC。静脉中的丁苯那洛尔显示随着时间的推移药效学作用迅速下降，表明其已被迅速消除。从吡咯烷酮或PMβCD制成的装置中，丁丙诺尔的体内递送量（通过质量平衡研究估算）比对照高3倍。这项研究的结果有力地表明，TDDS中的渗透增强剂增加了BPL的体内递送，从而使BPL的β阻断活性比对照提高了50-60％，从而使TDDS贴片的尺寸减小了。 。 （C）2007 Elsevier Inc.保留所有权利。

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