Bi Y, Sunada H, Yonezawa Y, Danjo K, Otsuka A, Iida K
Faculty of Pharmacy, Meijo University, Nagoya, Japan.
Chem Pharm Bull (Tokyo). 1996 Nov;44(11):2121-7. doi: 10.1248/cpb.44.2121.
In order to make a compressed tablet which can rapidly disintegrate in the oral cavity, microcrystalline cellulose and low-substituted hydroxypropylcellulose were used as disintegrants, and ethenzamide and ascorbic acid were chosen as poorly and easily water soluble model drugs, respectively. The mixture of microcrystalline cellulose and low-substituted hydroxypropylcellulose was compressed at 100--500 kgf in the absence of an active ingredient. The properties of these tablets, such as hardness, porosity, the time required for complete wetting of a tested tablet (wetting time), water uptake and disintegration time determined by a new disintegration apparatus, were investigated to elucidate the wetting and disintegration characteristics of these tablets, When the MCC/L-HPC ratio was in the range of 8:2 to 9:1, the shortest disintegration time was observed. The disintegration of tablets containing ethenzamide or ascorbic acid was examined next. Tablet disintegration time in the oral cavity was also tested, and good correlation between the disintegration behaviors in vitro and in the oral cavity was recognized.
为了制备一种能在口腔中快速崩解的压制片，使用微晶纤维素和低取代羟丙基纤维素作为崩解剂，并分别选择乙水杨胺和抗坏血酸作为难溶性和易溶性模型药物。在没有活性成分的情况下，将微晶纤维素和低取代羟丙基纤维素的混合物在100 - 500千克力下压制。研究了这些片剂的性质，如硬度、孔隙率、受试片剂完全润湿所需的时间（润湿时间）、吸水性以及通过新型崩解仪测定的崩解时间，以阐明这些片剂的润湿和崩解特性。当微晶纤维素/低取代羟丙基纤维素比例在8:2至9:1范围内时，观察到最短的崩解时间。接下来检查了含有乙水杨胺或抗坏血酸的片剂的崩解情况。还测试了片剂在口腔中的崩解时间，并且认识到体外和口腔中的崩解行为之间具有良好的相关性。
