Jatav Vijay Singh, Saggu Jitender Singh, Sharma Ashish Kumar, Sharma Anil, Jat Rakesh Kumar
Department of Pharmaceutics, Gyan Vihar School of Pharmacy, SGVU, Jaipur, India.
Adv Biomed Res. 2013 Jul 30;2:62. doi: 10.4103/2277-9175.115813. eCollection 2013.
Nebivolol hydrochloride is a third generation β-blocker with highly selective β1-receptor antagonist with antihypertensive properties having plasma half life of 10 h and 12% oral bioavailability. The aim of the present investigation was to form matrix type transdermal patches containing Nebivolol hydrochloride to avoid its extensive hepatic first pass metabolism, lesser side effect and increase bioavailability of drug.
Matrix type transdermal patches containing Nebivolol hydrochloride were prepared using EudragitRS100, HPMC K100M (2:8) polymers by solvent evaporation technique. Aluminum foil was used as a backing membrane. Polyethylene glycol (PEG) 400 was used as plasticizer and Dimethyl sulfoxide (DMSO) was used as a penetration enhancer. Drug polymer interactions determined by FTIR and standard calibration curve of Nebivolol hydrochloride were determined by using UV estimation.
The systems were evaluated physicochemical parameters and drug present in the patches was determined by scanning electron microscopy. All prepared formulations indicated good physical stability. In vitro drug permeation studies of formulations were performed by using Franz diffusion cells using abdomen skin of Wistar albino rat. Result showed best in vitro skin permeation through rat skin as compared to all other formulations prepared with hydrophilic polymer containing permeation enhancer.
IT WAS OBSERVED THAT THE FORMULATION CONTAINING HPMC: EudragitRS100 (8:2) showed ideal higuchi release kinetics. On the basis of in vitro drug release through skin permeation performance, Formulation F1 was found to be better than other formulations and it was selected as the optimized formulation.
盐酸奈必洛尔是一种第三代β受体阻滞剂，是具有高度选择性的β1受体拮抗剂，具有抗高血压特性，血浆半衰期为10小时，口服生物利用度为12%。本研究的目的是制备含盐酸奈必洛尔的基质型透皮贴剂，以避免其广泛的肝脏首过代谢，减少副作用并提高药物的生物利用度。
采用溶剂蒸发技术，使用EudragitRS100、HPMC K100M（2:8）聚合物制备含盐酸奈必洛尔的基质型透皮贴剂。铝箔用作背衬膜。聚乙二醇（PEG）400用作增塑剂，二甲基亚砜（DMSO）用作渗透促进剂。通过傅里叶变换红外光谱（FTIR）确定药物与聚合物的相互作用，并使用紫外分光光度法测定盐酸奈必洛尔的标准校准曲线。
对该体系进行了理化参数评估，并通过扫描电子显微镜测定贴剂中存在的药物。所有制备的制剂均显示出良好的物理稳定性。使用Franz扩散池，以Wistar白化大鼠的腹部皮肤进行制剂的体外药物渗透研究。结果表明，与所有其他含渗透促进剂的亲水性聚合物制备的制剂相比，该制剂在大鼠皮肤中的体外皮肤渗透效果最佳。
观察到含HPMC:EudragitRS100（8:2）的制剂显示出理想的 Higuchi 释放动力学。基于体外药物透过皮肤的渗透性能，发现制剂F1优于其他制剂，并将其选为优化制剂。
