Zhou Ying, Yan Peng, Zhao Xiangcheng, Zhang Hailong, Yang Yan, Ding Jinsong
Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, 410006, Hunan, China.
Changsha Jingyi Pharmaceutical Technology Co., LTD., Changsha, 410006, Hunan, China.
Drug Deliv Transl Res. 2025 Jan 16. doi: 10.1007/s13346-024-01764-x.
Dapoxetine hydrochloride tablets are the most commonly used drug for the treatment of premature ejaculation (PE). However, the tablets must be taken with water 1-3 h before sexual activity, which makes the medication intake conspicuous and inconvenient. This study aimed to develop taste-masked orodispersible films (ODFs) of dapoxetine hydrochloride using ion exchange resins. It was found that the based-Kyron T-134 resin complex achieved a high drug loading of 75.9 ± 1.4%, establishing the mass ratio of dapoxetine hydrochloride to Kyron T-134 at 2:1, and adjusting the solution pH to 5.4 ± 0.05. The effect of pH on the drug loading of the resin was initially characterized by SEM, while the binding mechanism between dapoxetine hydrochloride and the resin was investigated by XRD, DSC, and FTIR. The ODFs exhibited favorable mechanical properties and palatability. Meanwhile, the drug release in both the ODFs and commercially available tablets Priligy could reach 100.8% of the drug over 15 min in a simulated gastric fluid with pH 1.2 HCl. Furthermore, pharmacokinetic studies conducted in healthy volunteers demonstrated that the ODFs were bioequivalent to Priligy. Therefore, this ODFs, characterized by its pleasant taste and water-free administration, offer a novel and convenient oral formulation for patients with PE, thereby enhancing patient compliance.
盐酸达泊西汀片是治疗早泄（PE）最常用的药物。然而，该片剂必须在性活动前1 - 3小时用水服用，这使得药物摄入明显且不方便。本研究旨在使用离子交换树脂开发盐酸达泊西汀的掩味口腔崩解膜（ODF）。结果发现，以Kyron T - 134树脂为基础的复合物实现了75.9±1.4%的高载药量，确定盐酸达泊西汀与Kyron T - 134的质量比为2:1，并将溶液pH值调节至5.4±0.05。首先通过扫描电子显微镜（SEM）表征pH对树脂载药量的影响，同时通过X射线衍射（XRD）、差示扫描量热法（DSC）和傅里叶变换红外光谱（FTIR）研究盐酸达泊西汀与树脂之间的结合机制。该口腔崩解膜表现出良好的机械性能和适口性。同时，在pH 1.2 HCl的模拟胃液中，口腔崩解膜和市售片剂必利劲（Priligy）在15分钟内的药物释放量均可达到药物的100.8%。此外，在健康志愿者中进行的药代动力学研究表明，该口腔崩解膜与必利劲具有生物等效性。因此，这种具有宜人味道且无需用水服用的口腔崩解膜为早泄患者提供了一种新颖且方便的口服制剂，从而提高了患者的依从性。
