College of Pharmaceutical Sciences, Mohuda, Berhampur, Orissa, India.
Int Braz J Urol. 2009 Nov-Dec;35(6):716-29. doi: 10.1590/s1677-55382009000600010.
The main objective of the investigation was to develop a transdermal therapeutic system for alfuzosin hydrochloride and to study the effects of polymeric system and loading dose on the in vitro skin permeation pattern.
Principles of experimental design have been exploited to develop the dosage form. Ratio of ethyl cellulose (EC) and polyvinyl pyrrolidone (PVP) and loading dose were selected as independent variables and their influence on the cumulative amount of alfuzosin hydrochloride permeated per cm2 of human cadaver skin at 24 h (Q24), permeation flux (J) and steady state permeability coefficient (PSS) were studied using experimental design. Various physicochemical parameters of the transdermal films were also evaluated. Activation energy for in vitro transdermal permeation has been estimated.
Ratio of EC and PVP was found to be the main influential factor for all the dependent variables studied. Drug loading dose was also found to influence the dependent variables but to a lesser extent. Physicochemical parameters of the prepared films were evaluated and found satisfactory. Activation energy for alfuzosin permeation has also been estimated and reported.
The therapeutic system was found to be dermatologically non-irritant and hence, a therapeutically effective amount of alfuzosin hydrochloride can be delivered via a transdermal route.
研究的主要目的是开发盐酸阿夫唑嗪的透皮治疗系统，并研究聚合物系统和载药量对体外皮肤渗透模式的影响。
利用实验设计原理来开发剂型。乙基纤维素（EC）和聚乙烯吡咯烷酮（PVP）的比例以及载药量被选为独立变量，研究它们对 24 小时内每平方厘米人体尸体皮肤渗透的盐酸阿夫唑嗪累积量（Q24）、渗透通量（J）和稳态渗透系数（PSS）的影响，使用实验设计。还评估了透皮膜的各种物理化学参数。估计了体外透皮渗透的活化能。
发现 EC 和 PVP 的比例是所有研究的依赖变量的主要影响因素。药物载药量也被发现对依赖变量有影响，但影响较小。对制备的薄膜的物理化学参数进行了评估，结果令人满意。还估计并报告了阿夫唑嗪渗透的活化能。
该治疗系统被发现对皮肤无刺激性，因此可以通过透皮途径给予治疗有效量的盐酸阿夫唑嗪。
