School of Pharmacy and Biomedical Sciences, University of Portsmouth, Portsmouth, UK.
Drug Dev Ind Pharm. 2010 Aug;36(8):926-32. doi: 10.3109/03639040903585135.
The ethyl ester of captopril has been shown to exhibit enhanced permeation across human skin compared to the parent drug. A drug-in-adhesive patch formulation of a captopril ethyl ester was therefore developed for optimum drug release.
A wide range of transdermal patches were prepared using two commercially available bioadhesive polymers. Investigational screening was conducted on the patches using microscopy, texture profile analysis, and infrared spectroscopy. Drug release profiles of suitable patches were obtained using both polydimethylsiloxane (Silastic) and porcine skin in vitro.
Diffusion results across Silastic showed a gradual plateau in flux with increased drug loading that may be attributable to intramolecular interactions while flux across porcine skin was seen to increase with increasing patch thickness and attained a therapeutic level.
This study demonstrated that adhesion and drug loading are significant factors in optimizing a topical patch formulation for the delivery of a captopril prodrug.
卡托普利乙酯已被证明比母体药物具有更强的透过人体皮肤的能力。因此，为了实现最佳药物释放，开发了一种卡托普利乙酯的药物贴剂。
使用两种市售的生物粘附聚合物制备了多种透皮贴剂。使用显微镜、质地分析和红外光谱对贴剂进行了研究性筛选。使用聚二甲基硅氧烷（Silastic）和猪皮在体外获得了合适贴剂的药物释放曲线。
穿过 Silastic 的扩散结果表明，随着药物负载的增加，通量逐渐达到平台期，这可能归因于分子内相互作用，而穿过猪皮的通量则随着贴剂厚度的增加而增加，并达到治疗水平。
本研究表明，粘附和药物负载是优化卡托普利前药局部贴剂制剂以实现药物传递的重要因素。
