Baviskar Dheeraj T, Parik Venkatesh B, Gupta Hrishikesh N, Maniyar Ajim H, Jain Dinesh K
KVPS Institute of Pharmaceutical Education, Boradi, Tal-Shirpur.Dist-Dhule. 425428 (MH) India.
PDA J Pharm Sci Technol. 2012 Mar-Apr;66(2):126-35. doi: 10.5731/pdajpst.2012.00854.
The present work comprises the formulation and evaluation of losartan potassium with a view to developing and preparing a losartan potassium releasing system for transdermal applications. The aim of the study was to prepare the transdermal patch of drug using different blends of polymers. Transdermal patches of losartan potassium were prepared using ethyl cellulose (EC): polyvinyl pyrrolidone (PVP), Eudragit RL-100: Eudragit RS-100 and polyvinyl alcohol (PVA): polyvinyl pyrrolidone (PVP) using different ratios by the solvent casting technique. Physicochemical parameters like flexibility, thickness, smoothness, moisture content, hardness, and tensile strength were studied. The in vitro permeation study was carried out using a modified Keshery diffusion cell, and the formulation followed the Higuchi diffusion mechanism. The blood pressure lowering response of all formulations was studied using hypertension-induced rats by the chronic renal hypertension method. The formulation containing Eudragit RL-100: Eudragit RS-100 as polymers showed satisfactory drug release pattern (hydrophobic polymers) compared to combination of hydrophobic and hydrophilic polymers (EC: PVP) and PVA: PVP (hydrophilic polymers). The amount of drug release from formulations containing hydrophilic polymers and combination of both hydrophobic and hydrophilic polymers were found to be less in comparison to the patches of hydrophobic polymers.
The aim of the present study was to prepare and evaluate the transdermal patch of drug using different polymers such as hydrophobic, combination of hydrophobic: hydrophilic, and hydrophilic. Losartan potassium (hydrophilic) is the antihypertensive drug used for lowering increased blood pressure. Transdermal patches of losartan potassium were prepared using different ratios of polymers by the solvent casting technique. The prepared patches were evaluated for their flexibility, thickness, smoothness, moisture content, hardness, and tensile strength. The in vitro permeation study was carried out using a diffusion cell. The blood lowering response of all formulations was studied using hypertension-induced rats. The formulation containing hydrophobic polymers showed a satisfactory drug release pattern compared to the combination of hydrophobic: hydrophilic polymers and the hydrophilic polymers. Hence, the present study reveals that formulation of hydrophilic drug (losartan potassium) withhydrophobic polymers exhibit good release properties as compared to that of hydrophilic polymers and combination of both hydrophobic and hydrophilic polymers.
本研究工作包括氯沙坦钾的制剂研发与评估，旨在开发并制备用于透皮给药的氯沙坦钾释放系统。本研究的目的是使用不同聚合物混合物制备药物透皮贴剂。采用溶剂浇铸技术，使用不同比例的乙基纤维素（EC）：聚乙烯吡咯烷酮（PVP）、丙烯酸树脂RL - 100：丙烯酸树脂RS - 100以及聚乙烯醇（PVA）：聚乙烯吡咯烷酮（PVP）制备氯沙坦钾透皮贴剂。研究了柔韧性、厚度、光滑度、水分含量、硬度和拉伸强度等物理化学参数。使用改良的凯氏扩散池进行体外渗透研究，该制剂遵循 Higuchi 扩散机制。采用慢性肾性高血压法，在高血压诱导大鼠上研究了所有制剂的降压反应。与疏水和亲水聚合物组合（EC：PVP）以及PVA：PVP（亲水聚合物）相比，含有丙烯酸树脂RL - 100：丙烯酸树脂RS - 100作为聚合物的制剂显示出令人满意的药物释放模式（疏水聚合物）。与疏水聚合物贴剂相比，发现含有亲水聚合物以及疏水和亲水聚合物组合的制剂的药物释放量较少。
本研究的目的是使用不同聚合物（如疏水聚合物、疏水 - 亲水聚合物组合以及亲水聚合物）制备并评估药物透皮贴剂。氯沙坦钾（亲水）是用于降低血压升高的抗高血压药物。采用溶剂浇铸技术，使用不同比例的聚合物制备氯沙坦钾透皮贴剂。对制备的贴剂进行柔韧性、厚度、光滑度、水分含量、硬度和拉伸强度评估。使用扩散池进行体外渗透研究。在高血压诱导大鼠上研究了所有制剂的降压反应。与疏水 - 亲水聚合物组合和亲水聚合物相比，含有疏水聚合物的制剂显示出令人满意的药物释放模式。因此，本研究表明，与亲水聚合物以及疏水和亲水聚合物组合相比，亲水药物（氯沙坦钾）与疏水聚合物的制剂表现出良好的释放特性。
