Xiangya School of Pharmaceutical Science, Central South University, 172 Tongzipo Road, Changsha, Hunan 410013, China.
School of Electrical & Information Engineering, Changsha University of Science & Technology, 2nd Section, 960 South Wanjiali Road, Changsha, Hunan 410114, China.
J Pharm Sci. 2020 May;109(5):1802-1810. doi: 10.1016/j.xphs.2020.01.025. Epub 2020 Feb 4.
This article describes a new method of estimating the absorption rate constant (k) of a 2-compartment model with extravascular administration, which is called an alternative method. The method was based on approximating the distribution and elimination phases of a 2-compartment model to the elimination phase of a one-compartment model. By using the model equation t=lnk-ln(k+k)k-(k+k), first, we obtained the peak time (t) and the sum value of the first-order elimination rate constant (k) and the distribution rate constant (k), then the iterative method was used to obtain estimated value. And the estimation results were compared with the results obtained by the Loo-Riegelman and statistical moment methods and the factors affecting the estimation results of alternative method were explored. Finally, verification experiments were carried out with actual data in the literature. In general, a good estimation effect on the value of k in the extravascular administration of the 2-compartment model was obtained by this method, with less errors compared with the commonly used 2 other methods (p < 0.05). Changes in k, k, k, and another distribution rate constant (k) all influenced the estimation results. The alternative method also showed good results in estimating k of compounds in the literature.
本文描述了一种新的估计血管外给药的二房室模型吸收速率常数(k)的方法,称为替代方法。该方法基于将二房室模型的分布相和消除相近似为单房室模型的消除相。通过使用模型方程 t=lnk-ln(k+k)k-(k+k),首先得到了峰时间(t)和一级消除速率常数(k)和分布速率常数(k)的和值,然后使用迭代法得到估计值。并将估计结果与 Loo-Riegelman 和统计矩方法的结果进行比较,探讨了替代方法的估计结果的影响因素。最后,通过文献中的实际数据进行了验证实验。一般来说,该方法对二房室模型血管外给药 k 值的估计效果较好,与常用的另外两种方法相比误差较小(p<0.05)。k、k、k 和另一个分布速率常数(k)的变化都会影响估计结果。替代方法在估计文献中化合物的 k 值时也表现出良好的效果。