Costa P, Sousa Lobo J M
Serviço de Tecnologia Farmacêutica, Faculdade de Farmácia da Universidade do Porto Rua Aníbal Cunha, 164, 4050-047, Porto, Portugal.
Eur J Pharm Sci. 2001 May;13(2):123-33. doi: 10.1016/s0928-0987(01)00095-1.
Over recent years, drug release/dissolution from solid pharmaceutical dosage forms has been the subject of intense and profitable scientific developments. Whenever a new solid dosage form is developed or produced, it is necessary to ensure that drug dissolution occurs in an appropriate manner. The pharmaceutical industry and the registration authorities do focus, nowadays, on drug dissolution studies. The quantitative analysis of the values obtained in dissolution/release tests is easier when mathematical formulas that express the dissolution results as a function of some of the dosage forms characteristics are used. In some cases, these mathematic models are derived from the theoretical analysis of the occurring process. In most of the cases the theoretical concept does not exist and some empirical equations have proved to be more appropriate. Drug dissolution from solid dosage forms has been described by kinetic models in which the dissolved amount of drug (Q) is a function of the test time, t or Q=f(t). Some analytical definitions of the Q(t) function are commonly used, such as zero order, first order, Hixson-Crowell, Weibull, Higuchi, Baker-Lonsdale, Korsmeyer-Peppas and Hopfenberg models. Other release parameters, such as dissolution time (tx%), assay time (tx min), dissolution efficacy (ED), difference factor (f1), similarity factor (f2) and Rescigno index (xi1 and xi2) can be used to characterize drug dissolution/release profiles.
近年来，固体药物剂型的药物释放/溶出一直是大量科学研究且成果丰硕的主题。每当开发或生产一种新的固体剂型时，都必须确保药物以适当的方式溶解。如今，制药行业和注册机构确实专注于药物溶出度研究。当使用将溶出结果表示为某些剂型特征函数的数学公式时，对溶出/释放试验中获得的值进行定量分析会更容易。在某些情况下，这些数学模型源自对发生过程的理论分析。在大多数情况下，不存在理论概念，一些经验方程已被证明更合适。固体剂型的药物溶出已通过动力学模型进行描述，其中药物的溶解量（Q）是试验时间t的函数，即Q = f(t)。Q(t)函数的一些分析定义常用，如零级、一级、希克森-克劳威尔、威布尔、 Higuchi、贝克-朗斯代尔、科尔斯梅尔-佩帕斯和霍普芬伯格模型。其他释放参数，如溶出时间（tx%）、测定时间（tx分钟）、溶出效率（ED）、差异因子（f1）、相似因子（f2）和雷西格诺指数（xi1和xi2）可用于表征药物溶出/释放曲线。
