苯磺酸左旋氨氯地平口崩片的制备及质量控制

Preparation and Quality Control of Levamlodipine Besylate Orally Disintegrating Tablets

美国辉瑞公司的氨氯地平（1）于1993年在我国上市，主要用作抗高血压药物。1左旋体[（-）-1]的钙拮抗活性是右旋体的1000倍，是消旋体[（±）-1]的2倍。苯磺酸（-）-1可用作抗心绞痛药，对冠脉痉挛性心绞痛也有效。消旋体片剂通常口服起始剂量为5mg，每日一次；瘦小及体质虚弱者、老年患者或肝功能受损者的起始剂量为2．5mg。由于制剂规格较小，且无嗅无味、微溶于水，适宜开发成口腔崩解片。

The orally disintegrating tablets of micronized levamlodipine besylate were prepared by direct powder compression with lactose and mannitol as fillers and polyplasdone as disintegrant. The formulation was optimized by orthogonal design. The uniformity of dosage units was good. The mean disintegrating time of the tablets in vitro and in oral cavity of six volunteers were both within 30 s. The in vitro dissolution of the tablets was above 90% in 5 min.