Yao T, Yamada M, Yamahara H, Yoshida M
Pharmaceutics Research Laboratory, Tanabe Seiyaku Co., Ltd., Osaka, Japan.
Chem Pharm Bull (Tokyo). 1997 Sep;45(9):1510-4. doi: 10.1248/cpb.45.1510.
Formulation of sustained release tablets containing coated particles whose coating membrane is not damaged during compression was studied and several kinds of chitosan of different particle size were evaluated as protective agents for the membrane. Comparison was made with the dissolution rate of the coated particles. Ethylcellulose or ethylcellulose/hydroxypropylcellulose was chosen as a coating agent. When the coated particles were compressed with the small particle size chitosan (Marine Chito), the coating membrane was not ruptured, and the protective effect was not influenced by the compression pressure. Both the Eudragit RS-coated particles and the tablets manufactured by compressing the coated particles with Marine Chito were orally administered to dogs, and the plasma theophylline levels of the two dosage forms were compared to determine the drug release characteristics in the gastrointestinal tract. It was found that the plasma concentration-time curve of the tablets coincided with that of the coated particles, and the compressed tablet would disintegrate instantly and redisperse into many particles in the body after oral administration.
研究了含有包衣颗粒的缓释片的制剂，这些包衣颗粒的包衣膜在压片过程中不会受损，并评估了几种不同粒径的壳聚糖作为膜保护剂的效果。将其与包衣颗粒的溶出速率进行了比较。选用乙基纤维素或乙基纤维素/羟丙基纤维素作为包衣剂。当用小粒径壳聚糖（海洋壳聚糖）对包衣颗粒进行压片时，包衣膜未破裂，且保护效果不受压片压力影响。将欧巴代RS包衣颗粒和用海洋壳聚糖对包衣颗粒进行压片制得的片剂口服给予犬，比较两种剂型的血浆茶碱水平，以确定胃肠道中的药物释放特性。结果发现，片剂的血浆浓度-时间曲线与包衣颗粒的曲线一致，口服给药后压制片会在体内立即崩解并重新分散成许多颗粒。
