Miyazaki S, Kawasaki N, Nakamura T, Iwatsu M, Hou W M, Attwood D
Faculty of Pharmaceutical Sciences, Health Science University of Hokkaido, Ishikari-Tohbetsu, Japan.
Int J Pharm. 2000 Aug 25;204(1-2):127-32. doi: 10.1016/s0378-5173(00)00491-9.
The potential of tablets containing 1:4, 1:1 and 4:1 weight ratios of pectin and hydroxypropyl methylcellulose (HPMC) for the sustained release of diltiazem by sublingual administration has been investigated. Measurements of maximum adhesive force to rat peritoneal membrane indicated a satisfactory bioadhesive strength. An in vitro sustained release of diltiazem over 5 h was achieved with bilayer tablets composed of a drug-free ethylcellulose layer in addition to the pectin/HPMC layer containing drug. Plasma concentration-time curves obtained following sublingual administration to rabbits of single and bilayer tablets with 1:1 weight ratios of pectin and HPMC showed evidence of sustained release of diltiazem. Bioavailability of diltiazem was 2.5 times that achieved by oral administration for single layer tablets and 1.8 times for the bilayered tablets.
研究了含有果胶与羟丙基甲基纤维素（HPMC）重量比为1:4、1:1和4:1的片剂通过舌下给药实现地尔硫䓬缓释的潜力。对大鼠腹膜的最大粘附力测量表明具有令人满意的生物粘附强度。除了含有药物的果胶/HPMC层外，由无药乙基纤维素层组成的双层片剂实现了地尔硫䓬在5小时内的体外缓释。对果胶和HPMC重量比为1:1的单层和双层片剂进行兔舌下给药后获得的血浆浓度-时间曲线显示出地尔硫䓬缓释的证据。单层片剂地尔硫䓬的生物利用度是口服给药的2.5倍，双层片剂是1.8倍。
