Institute of Analytical Chemistry and Food Chemistry, University of Vienna, Waehringerstrasse 38, A-1090 Vienna, Austria.
J Pharm Sci. 2009 Oct;98(10):3575-81. doi: 10.1002/jps.21639.
Alendronic acid, a frequently applied compound for the treatment of different forms of diseases of bone metabolism, is a strong acid with a high solubility in water. In connection with the oral administration this exhibits a potential health risk for the upper gastrointestinal tract. The in vitro release of tablets containing alendronic acid of different brands (Stada, ratiopharm, interpharm, Fosamax) was determined by dissolution tests for the time period required for oral intake. The effect of rotation speed, temperature, and solvent volume on the release rate of alendronic acid was determined for the used dissolution apparatus. Analysis of alendronic acid was performed by a validated HPLC method. The highest rate of release was found for the original brand. The dissolution rate of the generic formulations was significantly lower in the early stage of dissolution. Over the complete range of dissolution, more than 85% of the claimed amount was dissolved within 4 min. Dissolution profiles were compared by calculation of the similarity factor f(2) showing equal products with the exception of one generic product, whose dissolution rate was lower.
阿仑膦酸钠是一种常用于治疗多种骨骼代谢疾病的药物，它是一种强酸，在水中溶解度很高。由于口服给药，它对上消化道有潜在的健康风险。通过体外溶出试验，测定了不同品牌（Stada、ratiopharm、interpharm、Fosamax）的阿仑膦酸钠片在口服摄入所需时间内的释放情况。考察了转速、温度和溶剂体积对所用溶出仪中阿仑膦酸钠释放速率的影响。采用经验证的 HPLC 方法对阿仑膦酸钠进行分析。结果表明，原研品牌的释放速率最高。仿制药在溶出初期的释放速率明显较低。在整个溶出过程中，超过 85%的宣称量在 4 分钟内溶解。通过计算相似因子 f(2)比较溶出曲线，结果表明除了一种仿制药的释放速率较低外，其余产品均具有相似性。
