Abstract Metformin hydrochloride (MFM) is often used as a controlled-release (CR) tablet to reduce dosing frequency. However, the MFM CR tablet contains significant amounts of excipients and the tablet size is also large. Dosing convenience and patient compliance can be increased by reducing the size of the CR tablets. The aim of this study was to prepare and evaluate the MFM controlled-release tablet (MFM-CRT) using two types of release modulators, inner and outer. The MFM-CRT was prepared by coating the MFM granules using a binder solution containing aluminum stearate (ALS) as the inner release-modulator, and polyethylene oxide (PEO) as the outer release-modulator. The dispersion stability of the binder solution was optimized by the dispersion analyzer. The MFM-CRT was evaluated for dissolution rate and tablet volume. Additionally, dissolution behavior and dissolution kinetics of the MFM-CRT were analyzed using micro-computed tomography (micro-CT). Although the optimal MFM-CRT showed no difference in the release rate as compared to the commercially available product of Glucophage® XR 500 mg (f2 value: 72), the length of the long axis was reduced by 6 mm and the weight was reduced by about 27%. We expect patient compliance to improve because of effective sustained release and volume reduction of MFM-CRT.

中文翻译：

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脂肪酸包衣颗粒剂盐酸二甲双胍控释片的制备及表征

摘要 盐酸二甲双胍 (MFM) 通常用作控释 (CR) 片剂以减少给药频率。然而，MFM CR 片剂含有大量赋形剂并且片剂尺寸也很大。通过减小 CR 片剂的尺寸，可以增加给药便利性和患者依从性。本研究的目的是使用两种类型的释放调节剂（内部和外部）制备和评估 MFM 控释片 (MFM-CRT)。MFM-CRT 是通过使用包含硬脂酸铝 (ALS) 作为内部释放调节剂和聚环氧乙烷 (PEO) 作为外部释放调节剂的粘合剂溶液涂覆 MFM 颗粒来制备的。通过分散分析仪优化粘合剂溶液的分散稳定性。评估 MFM-CRT 的溶出速率和片剂体积。此外，使用微型计算机断层扫描 (micro-CT) 分析 MFM-CRT 的溶解行为和溶解动力学。虽然最佳 MFM-CRT 与市售产品 Glucophage® XR 500 mg（f2 值：72）相比在释放速率上没有差异，但长轴长度减少了 6 mm，重量减少了约 27%。由于 MFM-CRT 的有效缓释和体积减少，我们预计患者的依从性会提高。