Saab M, Issa M, Samy W, El-Maradny H
Pharmazie. 2016 Dec 1;71(12):701-708. doi: 10.1691/ph.2016.5186.
The aim of this study was to formulate floating hollow tablets of salbutamol sulphate with a platform tailored drug release profile to attain a controllable drug release. Eight formulations (F1-F8) were prepared using sublimation technique. L-menthol was directly compressed as sublimable core followed by compression coating of hydroxypropylmethyl cellulose (HPMC-K15M) or polyethylene oxide (PEO-WSR301) as release retarding polymer coat. Tablets were then subjected to heat to allow sublimation of the core. The effect of polymer type and that of different drug coat/core distribution on swelling and drug release profile was studied. FTIR and DSC revealed the absence of any drug-excipients interaction. Tablets showed a hollow morphology, resulting in low density tablets that floated for over 24 hours without lag time. Moreover, different drug coat/core distribution resulted in controllable release profiles. Based on these results, an optimum drug release behavior was recorded for HPMC-based hollow tablets consisting of 2:1 drug coat/core distribution ratio (F4), revealing a zero order drug release for over 14 hours. Furthermore, F4 showed no changes in drug content, floating properties and drug release profile upon exposure to accelerated stability conditions.
本研究的目的是制备具有定制化药物释放曲线的硫酸沙丁胺醇漂浮空心片,以实现可控的药物释放。采用升华技术制备了8种制剂(F1-F8)。将L-薄荷醇直接压制成可升华的片芯,随后用羟丙基甲基纤维素(HPMC-K15M)或聚环氧乙烷(PEO-WSR301)作为缓释聚合物包衣进行压制包衣。然后对片剂进行加热以使片芯升华。研究了聚合物类型以及不同药物包衣/片芯分布对溶胀和药物释放曲线的影响。傅里叶变换红外光谱(FTIR)和差示扫描量热法(DSC)显示不存在任何药物-辅料相互作用。片剂呈现空心形态,形成低密度片剂,可漂浮超过24小时且无滞后时间。此外,不同的药物包衣/片芯分布导致了可控的释放曲线。基于这些结果,记录到由药物包衣/片芯分布比例为2:1的基于HPMC的空心片(F4)具有最佳的药物释放行为,显示出超过14小时的零级药物释放。此外,F4在加速稳定性条件下药物含量、漂浮性能和药物释放曲线均无变化。