Lam Matthew, Asare-Addo Kofi, Nokhodchi Ali
Pharmaceutics Research Laboratory, Arundel Building, School of Life Sciences, University of Sussex, Brighton, UK.
Department of Pharmacy, University of Huddersfield, Huddersfield, HD1 3DH, UK.
Iran J Basic Med Sci. 2021 Jan;24(1):108-115. doi: 10.22038/ijbms.2020.51697.11729.
Liqui-Mass technology has shown promising advantages in terms of commercial production and formulation manipulation. This study attempts to further explore the potential of enhanced drug release of effervescent Liqui-Pellet by optimizing certain parameters.
In the current study, pellets containing co-solvent, naproxen, coating and carrier materials were prepared via extrusion and spheronisation (Liqui-Pellet). Parameters investigated included polysorbate 80 concentration (as a co-solvent), water content and the presence or absence of neusilin US2 as part of the new binary carrier mixture approach.
It was found that the success of the Liqui-Pellet production was determined by the amount of polysorbate 80 and water used, where above a certain limit, agglomeration occurred, and the formulation failed. Liqui-Pellet formulation showed an excellent flow, narrow size distribution and was robust to pass friability testing. The key findings in the investigation were that the Liqui-Pellet was capable of a remarkably fast drug release, and 100% drug release achieved within 20 min at pH 1.2, wherein naproxen has been known to be practically insoluble in such pH.
Liqui-Pellets display the potential to enhance explosive dissolution where a combination of effervescent powders and binary carriers with the high surface area were used. Furthermore, X-ray microtomography revealed that the pellets were very uniform and homogenous.
液状物料技术在商业生产和制剂操作方面已显示出有前景的优势。本研究试图通过优化某些参数进一步探索泡腾液状微丸增强药物释放的潜力。
在本研究中,通过挤出滚圆法制备了含有共溶剂、萘普生、包衣材料和载体材料的微丸(液状微丸)。研究的参数包括聚山梨酯80浓度(作为共溶剂)、含水量以及作为新型二元载体混合物方法一部分的硅铝酸钠US2的有无。
发现液状微丸生产的成功取决于所用聚山梨酯80和水的量,超过一定限度会发生团聚,制剂失败。液状微丸制剂显示出优异的流动性、窄的粒度分布,并且能通过脆碎度测试。研究中的关键发现是液状微丸能够实现非常快速的药物释放,在pH 1.2时20分钟内实现100%药物释放,而萘普生在该pH下实际上是不溶的。
液状微丸在使用泡腾粉末和具有高表面积的二元载体组合时显示出增强爆发性溶解的潜力。此外,X射线显微断层扫描显示微丸非常均匀和同质。