Pharmaceutics Research Laboratory, Arundel Building, School of Life Sciences, University of Sussex, Brighton, UK.
Department of Pharmacy, University of Huddersfield, Huddersfield, HD1 3DH, UK.
AAPS PharmSciTech. 2021 Mar 1;22(3):85. doi: 10.1208/s12249-021-01943-w.
In this study, an attempt was made to produce Liqui-Tablets for the first time. This was carried out through the compaction of naproxen Liqui-Pellets. The incentive to convert the novel Liqui-Pellet into Liqui-Tablet was due to the array of inherent advantages of the popular and preferred tablet dosage form. The study showed that naproxen Liqui-Tablet could be successfully produced and the rapid drug release rate (100% drug release ~ 20 min) could be achieved under pH 1.2, where naproxen is insoluble. It was observed that the different pH of the dissolution medium affected the trend of drug release from formulations with varying amounts of liquid vehicle. The order of the fastest drug-releasing formulations was different depending on the pH used. The presence of Neusilin US2 showed considerable enhancement in the drug release rate as well as improving Liqui-Tablet robustness and hardness. Furthermore, images from X-ray micro-tomography displayed a uniform distribution of components in the Liqui-Tablet. The accelerated stability studies showed acceptable stability in terms of dissolution profile.
本研究首次尝试制备液片剂。这是通过压压实萘普生液芯丸来实现的。将新型液芯丸转化为液片剂的动机是由于片剂这种受欢迎且首选的剂型具有一系列固有优势。研究表明,可成功制备萘普生液片剂,且在 pH 值为 1.2(萘普生不溶)时可实现快速药物释放率(~20 分钟内 100%药物释放)。研究还观察到,不同的溶出介质 pH 值影响不同含液量药物释放的趋势。根据所用 pH 值的不同,药物释放最快的配方的顺序也不同。Neusilin US2 的存在显著提高了药物释放率,同时提高了液片剂的稳健性和硬度。此外,X 射线微断层扫描图像显示液片剂中各成分分布均匀。加速稳定性研究表明,在溶出度方面具有可接受的稳定性。