Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, D. I. Khan 29050, Pakistan.
Department of Veterinary Medicine, University of Bari, 70010 Valenzano, Italy.
Molecules. 2022 May 18;27(10):3242. doi: 10.3390/molecules27103242.
Controlled-release effervescent floating bilayer tablets reduce dosage frequency and improve patient compliance with enhanced therapeutic outcomes. Generally, two different tablets of clarithromycin and esomeprazole, respectively, are given for the treatment of Helicobacter pylori infection and it might be worth incorporating both in a single tablet. In the current study, controlled-release floating bilayer tablets of clarithromycin and esomeprazole (F1−F4) were developed with different rates of polymeric materials by a direct compression method. During the formulation, Fourier-transform infrared spectroscopy (FTIR) analysis was performed for possible interactions between drugs and excipients. No interactions between drugs and excipients were noted. Moreover, the bilayer tablets’ thickness, diameter, friability, hardness, weight variation, dissolution, and percent purity were found within the acceptable limits. The floating lag time and total floating time of all formulations were found to be < 25 s and 24 h, respectively. The release of both the clarithromycin and esomeprazole started at the same time from the controlled-release floating bilayer tablets by anomalous non-Fickian diffusion, and the polymeric materials extended the drug release rate up to 24 h. In the case of F1, the results approached ideal zero-order kinetics. The dissolution profiles of the tested and reference tablet formulations were compared, but no significant differences were observed. It can be concluded that such controlled-release effervescent floating bilayer tablets can be efficiently used in clinical practice to reduce dosage frequency and increase patient compliance with continuous drug release for 24 h, which ultimately might enhance therapeutic efficacy.
控释型双层起泡漂浮片可减少给药频率，提高患者顺应性，改善治疗效果。通常，治疗幽门螺杆菌感染需要分别使用两种不同的克拉霉素片和埃索美拉唑片，但将两者合并到一片双层片中或许更有意义。在本研究中，我们采用直接压片法，使用不同比例的聚合物材料制备了克拉霉素和埃索美拉唑的控释型双层起泡漂浮片（F1-F4）。在配方过程中，我们进行了傅里叶变换红外光谱（FTIR）分析，以检测药物与辅料之间是否存在相互作用。结果未发现药物与辅料之间存在相互作用。此外，双层片的厚度、直径、脆碎度、硬度、重量差异、溶出度和纯度均在可接受范围内。所有配方的漂浮滞后时间和总漂浮时间均小于 25 s 和 24 h。两种药物均从控释型双层起泡漂浮片中同时以异常非 Fickian 扩散方式释放，聚合物材料将药物释放速率延长至 24 h。对于 F1，结果接近理想的零级动力学。我们比较了测试和参比片剂配方的溶出曲线，但未观察到显著差异。由此可以得出结论，这种控释型双层起泡漂浮片可以在临床实践中有效应用，减少给药频率，提高患者顺应性，实现 24 h 持续药物释放，从而提高治疗效果。
