Khan Kamran Ahmad, Zizzadoro Claudia, Di Cerbo Alessandro, Pugliese Nicola, Khan Gul Majid, Ghazanfar Shakira, Almusalami Eman M, Muzammal Muhammad, Alsalman Khaled J, Farid Arshad
Gomal Center of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, Pakistan.
Department of Veterinary Medicine, University of Bari, 70010 Valenzano, Italy.
Polymers (Basel). 2022 Jul 24;14(15):2993. doi: 10.3390/polym14152993.
Controlled-release formulations are essential for those drugs that require fine tuning of their activity to increase the ratio between therapeutic vs. adverse effects. Losartan potassium is among those drugs whose adverse effects may somehow impair its purported benefits. Previous investigations have been carried out to ascertain the suitability of several polymers for being associated with losartan. This study is focused on the effects of Ethocel grade 10 and Carbopol 934P NF on losartan release. Flow and physical properties were assessed according to the protocols standardized by the pharmacopeia (USP-NF 29), and the drug release in phosphate buffer (pH = 6.8) was measured for 24 h. Data evidenced good to excellent flow and physical properties according to the drug/polymer ratio and the addition of co-excipients. The release rate in 24 h was found to be 63-69% to 79-82% without or with the addition of co-excipients, respectively, following zero-order kinetics. The results also suggest a significant difference with the release profile of a traditional release losartan formulation. The results suggest the suitability of Ethocel grade 10 and Carbopol 934P NF as components of a controlled-release losartan formulation.
控释制剂对于那些需要精确调节活性以提高治疗效果与不良反应之比的药物至关重要。氯沙坦钾属于那些其不良反应可能会在某种程度上削弱其宣称益处的药物。此前已经开展了多项研究，以确定几种聚合物与氯沙坦联用的适用性。本研究聚焦于乙基纤维素10级和卡波姆934P NF对氯沙坦释放的影响。根据药典（USP-NF 29）标准化的方案评估流动性和物理性质，并在磷酸盐缓冲液（pH = 6.8）中测量药物释放24小时。数据表明，根据药物/聚合物比例和共辅料的添加情况，流动性和物理性质良好至优异。在不添加或添加共辅料的情况下，24小时内的释放率分别为63 - 69%至79 - 82%，遵循零级动力学。结果还表明，与传统释放的氯沙坦制剂的释放曲线存在显著差异。结果表明乙基纤维素10级和卡波姆934P NF适合作为氯沙坦控释制剂的成分。
