Donbrow M, Friedman M
J Pharm Sci. 1975 Jan;64(1):76-80. doi: 10.1002/jps.2600640114.
The preparation of cast films of ethylcellulose containing caffeine and salicylic acid is described. These films exhibit timed release of drugs. Release rates were found to agree with both the classical first-order equation (log drug retained against time) and diffusion-controlled release models, as exemplified by Higuchi's equations (drug release linearly related to square root of time). Mathematical analysis of the data shows that the release behavior actually conforms with the diffusion-controlled model. Literature results, reported as first order, for the release of cetylpyridinium chloride and benzalkonium chloride from polyamide films were analyzed similarly and shown to be diffusion controlled. Recommendations are made for presentation and routine treatment of drug release data to avoid ambiguity and provide useful biopharmaceutical information.
本文描述了含咖啡因和水杨酸的乙基纤维素铸膜的制备方法。这些薄膜呈现出药物的定时释放。发现释放速率与经典的一级方程(药物残留量对时间的对数)以及扩散控制释放模型均相符,如Higuchi方程(药物释放与时间的平方根呈线性关系)所示。对数据的数学分析表明,释放行为实际上符合扩散控制模型。对文献中报道的十六烷基氯化吡啶和苯扎氯铵从聚酰胺薄膜中的释放情况(报告为一级释放)进行了类似分析,结果表明其为扩散控制释放。文中还给出了关于药物释放数据的呈现和常规处理的建议,以避免歧义并提供有用的生物药剂学信息。