Mittal Ashu, Sara Udaivir S, Ali Asgar, Mohammed Aqil
ITS-Paramedical (Pharmacy) College, Muradnagar, Ghaziabad, Uttar Pradesh, India.
Pharm Dev Technol. 2009;14(4):422-34. doi: 10.1080/10837450902748388.
The matrix type transdermal drug delivery systems (patches) of Nitrendipine were prepared by film casting technique. The patches were characterized for physical, in vitro release studies and ex-vivo permeation studies (human cadaver skin). On the basis of in vitro drug release and skin permeation performance, formulation B3 was found to be better than the other formulations and it was selected as the optimized formulation. The final optimized formulation (B3) was subjected to skin irritation, pharmacokinetic, pharmacodynamic and stability studies. The maximum percentage drug release in 48 hours was 94.67 +/- 3.25 for B3 and 91.43 +/- 2.106 for A2 formulation. Again formulation B3 (0.0627 mg/cm2/h) and A2 (0.0566 mg/cm2/h) showed maximum skin flux in the respective series. Patches prepared with Plasdone S-630 were more flexible as compared to PVP K 30 containing patches. Patches prepared with PVP K 30 showed drug release and skin permeation at higher percentage as compared to those containing Plasdone S-630. The interaction studies carried out by comparing the results of ultraviolet, infrared, TLC and DSC analyses for the pure drug, medicated and placebo formulations indicated no chemical interaction between the drug and excipients. The TDDS was found to be free of any skin irritation as suggested by skin irritation score of 1.16 (< 2.00) under Draize score test.
采用流延法制备了尼群地平的基质型透皮给药系统（贴片）。对贴片进行了物理性质、体外释放研究和离体渗透研究（人尸体皮肤）。基于体外药物释放和皮肤渗透性能，发现制剂B3优于其他制剂，并将其选为优化制剂。对最终优化制剂（B3）进行了皮肤刺激性、药代动力学、药效学和稳定性研究。B3在48小时内的最大药物释放百分比为94.67±3.25，A2制剂为91.43±2.106。同样，制剂B3（0.0627mg/cm²/h）和A2（0.0566mg/cm²/h）在各自系列中显示出最大的皮肤通量。与含PVP K 30的贴片相比，用聚维酮S - 630制备的贴片更具柔韧性。与含聚维酮S - 630的贴片相比，用PVP K 30制备的贴片显示出更高百分比的药物释放和皮肤渗透。通过比较纯药物、含药和安慰剂制剂的紫外、红外、薄层色谱和差示扫描量热分析结果进行的相互作用研究表明，药物与辅料之间没有化学相互作用。根据Draize评分试验的皮肤刺激性评分为1.16（<2.00），表明透皮给药系统没有任何皮肤刺激性。
