Miyazaki S, Nakayama A, Oda M, Takada M, Attwood D
Faculty of Pharmaceutical Sciences, Health Science University of Hokkaido, Japan.
Biol Pharm Bull. 1994 May;17(5):745-7. doi: 10.1248/bpb.17.745.
Bioadhesive tablets for intraoral drug delivery were prepared by directly compressing the drug with a mixture of chitosan and sodium alginate in weight ratios of 4:1, 1:1 and 1:4, and the adhesion and release characteristics of the prepared systems were evaluated in vitro and in vivo. Ketoprofen was used as a model drug. The magnitudes of the adhesion force of chitosan/alginate tablets were observed to be comparable to that of Aftach, which is a typical commercial preparation of an oral mucosal adhesive tablet. Increasing the chitosan content in the tablets resulted in a decrease in the release rate of ketoprofen. When the tablets were administered to the sublingual site of rabbits, ketoprofen from the tablets with chitosan/alginate was rapidly absorbed without an initial sharp peak. Furthermore, the plasma concentration curves for the tablet with a 1:4 chitosan/alginate ratio showed a sustained release 3 h after administration. The data presented suggest that tablets prepared from chitosan and alginate are potential candidates for intraoral drug delivery.
通过将药物与壳聚糖和海藻酸钠按重量比4:1、1:1和1:4的混合物直接压片制备用于口腔内给药的生物粘附片，并在体外和体内评估所制备体系的粘附和释放特性。以酮洛芬作为模型药物。观察到壳聚糖/海藻酸片的粘附力大小与典型的口腔粘膜粘附片商业制剂Aftach相当。片剂中壳聚糖含量的增加导致酮洛芬释放速率降低。当将片剂给予兔舌下部位时，含壳聚糖/海藻酸的片剂中的酮洛芬迅速吸收，没有初始的尖峰。此外，壳聚糖/海藻酸比例为1:4的片剂的血浆浓度曲线在给药3小时后显示出持续释放。所呈现的数据表明，由壳聚糖和海藻酸钠制备的片剂是口腔内给药的潜在候选物。
