Maniruzzaman Mohammed, Douroumis Dennis
Faculty of Engineering and Science, University of Greenwich, Chatham, Kent, UK.
J Pharm Pharmacol. 2015 Jan;67(1):43-55. doi: 10.1111/jphp.12319. Epub 2014 Sep 2.
The efficiency of the Astree e-tongue and Taste Sensing system TS5000Z for the evaluation of the taste masking effect of hot melt extruded formulations was investigated in this study.
Hot melt extrusion (HME) processing was optimized using Randcastle single screw extruder (USA) to manufacture extrudates with desirable characteristics. Cationic model drug propranolol HCl (PRP) was processed with the anionic polymers - Eudragit L100 (L100) and Eudragit L100-55 (Acryl-EZE). Solid state of the drug in polymer matrices was evaluated by scanning electron microscopy (SEM), differential scanning calorimetry, particle size analysis, Fourier transform infrared (FTIR) and Nuclear magnetic resonance (NMR) analysis. In-vitro taste masking efficiency of the two polymers was performed by using two different e-tongues (Astree e-tongue and TS5000Z). The results obtained from both e-tongues were further compared and contrast to find out the sensor outputs in all formulations.
Solid state analysis of the extruded formulations revealed the presence of amorphous PRP. Both e-tongues were able to detect the taste masking variations of the extrudates and were in good agreement with the in-vivo results obtained from a panel of six healthy human volunteers (R(2) > 0.84). However, each e-tongue sensor demonstrated different sensitivity, suggesting a careful consideration of the experimental findings during melt extrusion, is necessary for the development of taste-masked formulations. Furthermore, FTIR spectroscopy and NMR studies revealed possible drug polymer intermolecular interactions as the mechanism of successful taste masking.
HME can effectively be used to manufacture taste-masked extruded formulations, while both e-tongues demonstrated satisfactory taste analysis for the development of taste-masked formulations.
本研究考察了Astree电子舌和味觉传感系统TS5000Z评估热熔挤出制剂掩味效果的效率。
使用美国Randcastle单螺杆挤出机对热熔挤出（HME）工艺进行优化，以制备具有理想特性的挤出物。将阳离子模型药物盐酸普萘洛尔（PRP）与阴离子聚合物Eudragit L100（L100）和Eudragit L100-55（Acryl-EZE）进行加工。通过扫描电子显微镜（SEM）、差示扫描量热法、粒度分析、傅里叶变换红外光谱（FTIR）和核磁共振（NMR）分析评估药物在聚合物基质中的固态情况。使用两种不同的电子舌（Astree电子舌和TS5000Z）对两种聚合物的体外掩味效率进行测定。对两种电子舌获得的结果进行进一步比较和对比，以找出所有制剂中的传感器输出情况。
对挤出制剂的固态分析表明存在无定形PRP。两种电子舌均能够检测到挤出物的掩味变化，并且与一组六名健康人类志愿者获得的体内结果高度一致（R²＞0.84）。然而，每种电子舌传感器表现出不同的灵敏度，这表明在热熔挤出过程中仔细考虑实验结果对于开发掩味制剂是必要的。此外，FTIR光谱和NMR研究表明，可能的药物-聚合物分子间相互作用是成功掩味的机制。
HME可有效地用于制造掩味挤出制剂，而两种电子舌在掩味制剂开发方面均表现出令人满意的味觉分析能力。
