Kawano Yayoi, Ito Akihiko, Sasatsu Masanaho, Machida Yoshiharu
Department of Drug Delivery Research, Hoshi University, Tokyo, Japan.
Yakugaku Zasshi. 2010 Jan;130(1):75-80. doi: 10.1248/yakushi.130.75.
Many orally disintegrating tablets have recently been developed to improve oral ingestion and usability and are widely administered clinically, resulting in improved quality of life for patients. Since orally disintegrating tablets rapidly disintegrate in the mouth, the masking of unpleasant taste is important. We investigated the masking of the taste of furosemide (FU) as a model drug with correctives and prepared orally disintegrating tablets. Using maltitol (MA) as a corrective, granules were prepared employing mixing, coating, and mixing/coating methods using a desktop granulator. Each preparation was subjected to tasting. The taste was masked well when granules were prepared by the mixing and mixing/coating methods. Tablets were prepared from these granules with mannitol and crystalline cellulose added as fillers. Tablets made from granules prepared by the mixing and mixing/coating methods showed appropriate strength and disintegrated rapidly. When the amount of MA was increased in the mixing method, the disintegration time was prolonged, and thus the amount should be determined considering both taste masking and disintegration property. The results showed that orally disintegrating tablets of insoluble drugs with an unpleasant taste such as FU should be prepared with the taste masked employing the methods used in this study.
近年来,人们研发出了许多口腔崩解片,以改善口服给药的便利性和实用性,并在临床上得到广泛应用,从而提高了患者的生活质量。由于口腔崩解片能在口腔中迅速崩解,因此掩盖不良味道至关重要。我们以速尿(FU)为模型药物,使用矫味剂研究了其味道的掩盖情况,并制备了口腔崩解片。以麦芽糖醇(MA)作为矫味剂,使用台式制粒机通过混合、包衣和混合/包衣方法制备颗粒。对每种制剂进行口感测试。通过混合和混合/包衣方法制备颗粒时,味道得到了很好的掩盖。用这些颗粒加入甘露醇和结晶纤维素作为填充剂制备片剂。由混合和混合/包衣方法制备的颗粒制成的片剂显示出适当的强度,并能迅速崩解。在混合法中,当MA的用量增加时,崩解时间延长,因此应综合考虑味道掩盖和崩解性能来确定其用量。结果表明,对于像FU这种具有不良味道的难溶性药物,应采用本研究中使用的方法制备掩盖味道的口腔崩解片。