Zia H, Amini H, Hekmatyar F, Needham T E
Pahlavi Med J. 1977 Oct;8(4):414-58.
In vitro release of vitamin C from commercial tablets of three different manufacturers was measured by the Levy beaker, a modified USP basket and Magnetic Basket techniques and this was correlated with urinary excretion of the drug from normal, healthy, human males of 23 to 25 years of age weighing 50-72 Kg. Results showed that there was dissolution variability between the different brands of vitamin C tablets as well as between the in vitro dissolution methods used. There was also an inverse correlation between the time of in vitro release and the percent vitamin C excreted at the end of 2 hours. However, at the end of 24 hours the most rapidly dissolving tablets in vitro indicated only 66 percent excretion of the vitamin C as compared with nearly 83 percent for the slow dissolving types. It is concluded that to determine the total drug from a particular formulation, only disintegration and/or dissolution is not a good measure for an unstable and relatively rapid dissolving substance such as vitamin C. It is further suggested that perhaps if unstable rapid-dissolving substances were made more slowly released by formulation, a greater quantity of the drug would be physiologically avaiable.
采用Levy烧杯法、改良的美国药典篮法和磁篮法测定了来自三个不同厂家的市售维生素C片的体外释放情况,并将其与23至25岁、体重50 - 72千克的正常健康男性体内该药物的尿排泄情况进行了关联。结果表明,不同品牌的维生素C片之间以及所采用的体外溶出方法之间存在溶出差异。体外释放时间与2小时末维生素C排泄百分比之间也存在负相关。然而,在24小时末,体外溶出最快的片剂显示维生素C的排泄率仅为66%,而溶出慢的片剂这一比例接近83%。得出的结论是,对于像维生素C这样不稳定且相对快速溶解的物质,仅通过崩解和/或溶出来确定特定制剂中的总药物含量并非一种好的方法。进一步表明,或许通过制剂使不稳定的快速溶解物质释放得更慢一些,该药物在生理上的可利用量会更大。