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用于心律失常的控释植入剂型:综述与展望。

Controlled release implant dosage forms for cardiac arrhythmias: Review and perspectives.

机构信息

a Department of Pediatrics and Communicable Diseases, University of Michigan Medical School, Ann Arbor, Michigan, USA.

b Department of Pharmaceutics, University of Michigan College of Pharmacy, Ann Arbor, Michigan, USA.

出版信息

Drug Deliv. 1996;3(3):137-42. doi: 10.3109/10717549609029442.

DOI:10.3109/10717549609029442
PMID:26790908
Abstract

Cardiac implants using drug-polymer systems for the release of anti-arrhythmic agents directly to the myocardium have been successfully utilized in experimental studies for preventing and treating arrhythmias. This approach is hypothesized to be optimal since anti-arrhythmic agents are provided directly to the heart, and therefore the possibility of systemic side effects is reduced. Furthermore, anti-arrhythmic agents with poor oral bioavailability or with first-pass clearance characteristics following intravenous administration, such as the class III agent ibutilide, are optimally used by the direct cardiac route of administration. Cardiac controlled release implants have been demonstrated to be effective for optimizing the therapy of ventricular tachycardia, ventricular fibrillation, and atrial flutter. Monolithic matrices have been used for fixed rate release kinetics, and modulation of release has been possible through the use of iontophoretic drug delivery systems. Future implants will interface with forefront strategies in tissue engineering and molecular genetics to provide optimal therapy of the diseased arrhythmogenic myocardium.

摘要

心脏植入物使用药物-聚合物系统将抗心律失常药物直接释放到心肌中,已成功用于预防和治疗心律失常的实验研究中。这种方法被认为是最佳的,因为抗心律失常药物直接提供给心脏,因此系统副作用的可能性降低。此外,一些口服生物利用度差或静脉给药后具有首过清除特征的抗心律失常药物,如 III 类药物伊布利特,通过直接心脏给药途径得到最佳利用。心脏控制释放植入物已被证明可有效优化室性心动过速、心室颤动和心房扑动的治疗。整体基质已用于固定速率释放动力学,并且通过使用离子电渗药物递送系统可以实现释放的调节。未来的植入物将与组织工程和分子遗传学的前沿策略相接口,为病变性心律失常心肌提供最佳治疗。

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