含苯磺酸氨氯地平普鲁兰基口腔崩解膜的研制与表征

采用溶剂铸造法制备含苯磺酸氨氯地平的pululan基口腔崩解膜。为此，采用不同的增塑剂(甘油、山梨糖醇、丙二醇)和不同的超级崩解剂(交联淀粉钠、淀粉乙醇酸钠、氯吡酮)制备了9种不同的ODF配方(F1-F9)。

突出了

高血压是世界各国普遍存在的公共卫生问题。

口服给药是最可取的给药途径。

滴法测定普鲁兰基苯磺酸氨氯地平ODF的崩解时间为28.8 s，培养皿法测定其崩解时间为51.3 s。

普鲁兰是一种用于口腔崩解膜的聚合物成膜剂。

氨氯地平酸盐口服崩解薄膜尚未商购。

FD＆C绿色和aspartame分别用作着色剂和甜味剂。According to the results of preformulation studies, the optimum ODF (F9) was determined and various characterization studies such as uniformity of mass, film thickness, surface pH of films, and mechanical properties (such as elongation at break, tensile strength, Young’s modulus, and folding endurance), moisture content, disintegration time, uniformity of content and dissolution test, X-ray, DSC, SEM and short term stability analysis were performed on this formulation. Cytotoxicity and permeability studies for the F9 formulation were performed on the human epithelial colorectal adenocarcinoma (Caco-2) cell line. The formulation F9 had appropriate morphological and mechanical properties and disintegrated within 51.3 s according to the petri dish method, and 28.8 s according to the drop method. Dissolution studies revealed that 78.1 % of amlodipine besylate was dissolved in 20 min from F9 formulation. Cell culture studies showed that the formulation had no significant toxic effect on the Caco-2 cells. Also, there was no significant difference between the Caco-2 permeabilities of amlodipine besylate powder and amlodipine besylate ODFs. As a result of all these studies, we suggest to use the pullulan based amlodipine besylate ODFs to enhance ease of administration and patient compliance.含苯磺酸氨氯地平普鲁兰基口腔崩解膜的研制与表征

关键字苯磺酸氨氯地平体外溶出度口腔崩解膜透性pululan甘油山梨醇丙二醇，crospovidone，croscarmellose钠、乙醇酸淀粉钠、阿斯巴甜。