Bora Divyakumar, Borude Priyanka, Bhise Kiran
HOD Pharmaceutics, Allana College of Pharmacy, Azam campus, Pune 411001, India.
AAPS PharmSciTech. 2008;9(4):1159-64. doi: 10.1208/s12249-008-9154-5. Epub 2008 Nov 19.
The purpose of this research was to develop the taste-masked microspheres of intensely bitter drug ondansetron hydrochloride (OSH) by spray-drying technique. The bitter taste threshold value of OSH was determined. Three different polymers viz. Chitosan, Methocel E15 LV, and Eudragit E100 were used for microsphere formation, and the effect of different polymers and drug-polymer ratios on the taste masking and release properties of microspheres was investigated. The microspheres were characterized by Fourier transform infrared spectroscopy, scanning electron microscopy, Drug loading, in vitro bitter taste evaluation, and drug-release properties. The taste masking was absent in methocel microspheres at all the drug-polymer ratios. The Eudragit microspheres depicted taste masking at 1:2 drug-polymer ratio whereas with Chitosan microspheres the taste masking was achieved at 1:1 drug-polymer ratio. The drug release was about 96.85% for eudragit microspheres and 40.07% for Chitosan microspheres in 15 min.
本研究的目的是通过喷雾干燥技术制备强苦味药物盐酸昂丹司琼(OSH)的掩味微球。测定了OSH的苦味阈值。使用了三种不同的聚合物,即壳聚糖、甲基纤维素E15 LV和丙烯酸树脂E100来制备微球,并研究了不同聚合物和药物-聚合物比例对微球掩味和释放性能的影响。通过傅里叶变换红外光谱、扫描电子显微镜、载药量、体外苦味评价和药物释放性能对微球进行了表征。在所有药物-聚合物比例下,甲基纤维素微球均无掩味效果。丙烯酸树脂微球在药物-聚合物比例为1:2时表现出掩味效果,而壳聚糖微球在药物-聚合物比例为1:1时实现了掩味。在15分钟内,丙烯酸树脂微球的药物释放率约为96.85%,壳聚糖微球的药物释放率为40.07%。