Ye Genyang, Wang Qun, Shang Yibo, Li Yibo, Yang Rui, Jing Boyu, Fu Qiang
Wuya College of Innovation, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China.
Clinical Pharmacology Laboratory, The Second Affiliated Hospital, Liaoning University of Traditional Chinese Medicine, Shenyang, 110034, China.
AAPS PharmSciTech. 2025 Jun 3;26(5):158. doi: 10.1208/s12249-025-03138-z.
The taste of a drug impacts the compliance of patients for oral administration. In this study, the bitter taste of diclofenac sodium (DS) was masked with purolite A430MR through ion exchange. The DS-A430MR complexes (DACs) were prepared at a 1:1 (w/w) drug to resin through a simple aqueous binding process. The key factors affecting release behaviors were identified by optimized experiments. The taste masking effect of the DACs was evaluated by human taste panel studies and simulated saliva release. The physical characterization proved successful preparation of DACs. The released experiments demonstrated that the pH values, types, and strengths of counter ions were important factors affecting the DS release from the DACs. The simulated saliva release profiles demonstrated that the DS concentration in oral cavity was lower than its bitterness threshold. The bitter taste of DS was almost completely masked by the IERs, which provided guidance for the development of palatable oral preparations using IERs.
药物的味道会影响患者口服给药的依从性。在本研究中，通过离子交换，用普立特A430MR掩盖双氯芬酸钠（DS）的苦味。通过简单的水相结合过程，以1:1（w/w）的药物与树脂比例制备DS - A430MR复合物（DACs）。通过优化实验确定了影响释放行为的关键因素。通过人体味觉小组研究和模拟唾液释放评估了DACs的掩味效果。物理表征证明成功制备了DACs。释放实验表明，抗衡离子的pH值、类型和强度是影响DS从DACs中释放的重要因素。模拟唾液释放曲线表明，口腔中DS的浓度低于其苦味阈值。IERs几乎完全掩盖了DS的苦味，这为使用IERs开发可口的口服制剂提供了指导。
