市售阿仑膦酸钠片崩解度、溶出度和食道粘膜黏附量的研究

Comparisons on Disintegration,Dissolution and Esophageal Retention of Commercial Alendronate Tablets

阿仑膦酸钠为一新型骨质疏松症治疗和预防药物,属第三代二膦酸盐类骨再吸收抑制剂。阿仑膦酸钠生物利用度极低,个体差异大,不同品牌的产品的疗效有一定的差异,另外,阿仑膦酸钠对食道有一定的刺激性,不同品牌的产品的副作用也有较大的差异,其原因可能与不同品牌制剂的内在质量有关系。本文比较了4种不同品牌阿仑膦酸钠片的崩解性、溶出度、片剂颗粒与食道粘膜的黏附。结果显示:4种制剂的崩解、溶出、食道黏附量均有一定的差异,提示4种产品的生物利用度和对食道的副作用可能有一定的差别。该研究对于研究阿仑膦酸钠片质量标准的完善具有一定的意义。

Alendronate [ （4-amino-1-hydroxybutylidene） bisphosphonate ] is an important representative of the bisphosphonates used to treat metabolic disorders of calcium, like Paget＇s disease of bone, hypercalcemia, and osteoporosis. The oral absorption of alendronate is approximately 0.6% of the administered dose. Alendronate may cause local irritation of the upper gastrointestinal mucosa. Significant differences in bioavailabilitv and local irritation from one brand to another were observed. The present studies aimed to make comparisons of disintegration, dissolution and esophageal retention of Alendronate Tablets from different manufacturers. The results in- dicated that significant differences in disintegration, dissolution and esophageal retention could be observed. And the results could be applicable to predict or explain the differences in efficacy and adverse effects from different commercial products.