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血管外给药估算双室模型吸收速度常数的新方法。

A New Method for the Estimation of Absorption Rate Constant in Two-Compartment Model by Extravascular Administration.

机构信息

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.

出版信息

J Pharm Sci. 2020 May;109(5):1802-1810. doi: 10.1016/j.xphs.2020.01.025. Epub 2020 Feb 4.

DOI:10.1016/j.xphs.2020.01.025
PMID:32032589
Abstract

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.

摘要

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。

相似文献

1
A New Method for the Estimation of Absorption Rate Constant in Two-Compartment Model by Extravascular Administration.血管外给药估算双室模型吸收速度常数的新方法。
J Pharm Sci. 2020 May;109(5):1802-1810. doi: 10.1016/j.xphs.2020.01.025. Epub 2020 Feb 4.
2
A novel method to estimate the absorption rate constant for two-compartment model fitted drugs without intravenous pharmacokinetic data.一种在无静脉药代动力学数据情况下估算二室模型拟合药物吸收速率常数的新方法。
Front Pharmacol. 2023 May 4;14:1087913. doi: 10.3389/fphar.2023.1087913. eCollection 2023.
3
Estimation of absorption rate constant (ka) following oral administration by Wagner-Nelson, Loo-Riegelman, and statistical moments in the presence of a secondary peak.在存在二次峰的情况下,采用瓦格纳-尼尔森法、卢-里格尔曼法和统计矩法估算口服给药后的吸收速率常数(ka)。
Drug Metabol Drug Interact. 2004;20(1-2):85-100. doi: 10.1515/dmdi.2004.20.1-2.85.
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Application of the Loo-Riegelman absorption method.鲁-里格尔曼吸收法的应用。
J Pharmacokinet Biopharm. 1975 Feb;3(1):51-67. doi: 10.1007/BF01066595.
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Simple method for the estimation of absorption rate constant(ka) after oral administration.口服给药后吸收速率常数(ka)估算的简单方法。
Am J Ther. 1998 Nov;5(6):377-81. doi: 10.1097/00045391-199811000-00004.
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Critical analysis of "flip-flop" phenomenon in two-compartment pharmacokinetic model.两室药代动力学模型中“翻转”现象的批判性分析
J Pharm Sci. 1976 Aug;65(8):1140-4. doi: 10.1002/jps.2600650804.
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Effects of variation in drug elimination on five methods for assessing zero-order drug absorption rates.药物消除变化对五种评估零级药物吸收率方法的影响。
Pharm Res. 1990 Jan;7(1):76-9. doi: 10.1023/a:1015843811150.
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Factors affecting the error in the Loo-Riegelman method for estimating the rate of drug absorption. Some suggestions for a practical sampling schedule.影响用于估算药物吸收速率的卢-里格尔曼方法误差的因素。关于实际采样方案的一些建议。
Arzneimittelforschung. 1983;33(5):757-60.
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Stepwise determination of multicompartment disposition and absorption parameters from extravascular concentration-time data. Application to mesoridazine, flurbiprofen, flunarizine, labetalol, and diazepam.从血管外浓度-时间数据逐步确定多室处置和吸收参数。应用于甲砜哒嗪、氟比洛芬、氟桂利嗪、拉贝洛尔和地西泮。
J Pharmacokinet Biopharm. 1991 Aug;19(4):413-55. doi: 10.1007/BF01061665.
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The Bateman function revisited: a critical reevaluation of the quantitative expressions to characterize concentrations in the one compartment body model as a function of time with first-order invasion and first-order elimination.重新审视贝特曼函数:对单室体内模型中作为时间函数的浓度进行定量表达的批判性重新评估,该模型具有一级侵入和一级消除过程。
J Pharmacokinet Biopharm. 1994 Apr;22(2):103-28. doi: 10.1007/BF02353538.

引用本文的文献

1
A novel method to estimate the absorption rate constant for two-compartment model fitted drugs without intravenous pharmacokinetic data.一种在无静脉药代动力学数据情况下估算二室模型拟合药物吸收速率常数的新方法。
Front Pharmacol. 2023 May 4;14:1087913. doi: 10.3389/fphar.2023.1087913. eCollection 2023.