尼索地平口腔黏附片的制备及影响因素考察

目的：考察尼索地平口腔黏附片处方工艺对体外释放度和生物黏附力的影响。方法：测定各处方工艺条件下黏附片的释放度及黏附力。结果：保护层用量〉41．66％时，可保证药物的单向释放；含药层中卡波姆比例增加、乳糖比例减少及硬度的增大会使释药速度减慢；黏附力随卡波姆比例增加而增大，随乳糖增加而减少，硬度为5kg时黏附力较大。结论：处方中卡波姆比例、乳糖用量、黏附片硬度对体外释药速度和黏附力有显著影响。

Assessment of factors impacting the preparation of nisoldipine buccoadhesive tablets

Objective:To assess the factors that impact the dissolution in vitro and bioadhesive capacity of nisoldipine buccal adhesive tablets.Methods:The formulation of nisoldipine buccal adhesive tablets was optimized.The dissolution in vitro and bioadhesive capacity of the nisoldipine buccal adhesive tablets were evaluated by modified apparatus.Results:A monodirectional release towards the mucosa were achieved when the ratio of the protective layer(%)was greater than 41.66% (w/w).The dissolu- tion rate of nisoldipine from the buccal adhesive tablets was inversely proportioned to the amount of car- bopol(CP) and chitosan(CS) used as excipients and the hardness of the tablets and positively to the a- mount of lactose used.The bioadhesive capacity increased in a positive CP (%)-dependent and negative lactose (%)-dependent manner.The maximal bioadhesive capacity was reachable at the hardness index of 5 kilograms.Conclusion:The dissolution rate and adhesive capacity of the nisoldipine buccal adhesive tab- lets were significantly dependent on the proportions of CP/CS and lactose used as excipients and the hard- ness of the tablets.