Yousuf M, Ahmad M, Usman M, Ali I
Department of Pharmacy, Faculty of Pharmacy and Alternative Medicine, The Islamia University of Bahawalpur, Bahawalpur-63100, Pakistan.
Indian J Pharm Sci. 2013 Sep;75(5):569-77.
The present work was performed to develop and evaluate transdermal patches of combined antiasthmatic drugs (salbutamol sulphate and ketotifen fumarate). Polyvinyl alcohol membrane was used as backing membrane and eudragit RL-100 was used as matrix material to suspend the drugs in the continuous thickness of the patch. Methanol was solvent and propylene glycol was used as plasticizer. Tween 20, isopropyl myristate, eucalyptus oil, castor oil and span-20 were used as permeability enhancers. Thickness, weight variation and drug uniformity were investigated. The patch formulations were also subjected to drug release in dissolution media and permeation through rabbit skin. Effects of different enhancers were evaluated on release and permeation of drugs. F3 formulations having isopropyl myristate as permeation enhancer, showed maximum amounts of drugs release (88.11% of salbutamol sulphate and 88.33% of ketotifen fumarate) at the end of 24 h dissolution study. F3 also showed maximum permeation of both drugs (4.235 mg salbutamol sulphate and 1.057 mg ketotifen fumarate) after 24 h permeation study through rabbit skin mounted in Franz cell. The patches having no enhancer in the formulation also showed some drug release and permeation due to the presence of plasticizer. The results of the study suggested that new controlled release transdermal formulations of combined antiasthmatic drugs can be suitably developed as an alternate to conventional dosage forms.
本研究旨在开发和评估联合抗哮喘药物（硫酸沙丁胺醇和富马酸酮替芬）的透皮贴剂。使用聚乙烯醇膜作为背衬膜，用尤特奇RL - 100作为基质材料将药物悬浮在贴剂的连续厚度中。甲醇为溶剂，丙二醇用作增塑剂。吐温20、肉豆蔻酸异丙酯、桉叶油、蓖麻油和司盘 - 20用作渗透促进剂。研究了厚度、重量差异和药物均匀性。贴剂制剂还在溶出介质中进行药物释放研究，并通过兔皮进行渗透研究。评估了不同促进剂对药物释放和渗透的影响。以肉豆蔻酸异丙酯作为渗透促进剂的F3制剂在24小时溶出研究结束时显示出最大量的药物释放（硫酸沙丁胺醇为88.11%，富马酸酮替芬为88.33%）。在通过安装在弗兰兹扩散池中的兔皮进行24小时渗透研究后，F3制剂还显示出两种药物的最大渗透量（硫酸沙丁胺醇为4.235毫克，富马酸酮替芬为1.057毫克）。制剂中没有促进剂的贴剂由于增塑剂的存在也显示出一定的药物释放和渗透。研究结果表明，联合抗哮喘药物的新型控释透皮制剂可作为传统剂型的替代品进行适当开发。
