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首页> 外文期刊>Journal of pharmacokinetics and biopharmaceutics >The pharmacokinetics of saquinavir: a Markov chain Monte Carlo population analysis.
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The pharmacokinetics of saquinavir: a Markov chain Monte Carlo population analysis.

机译：沙奎那韦的药代动力学：马尔可夫链蒙特卡洛人口分析。

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摘要

Saquinavir is an HIV proteinase inhibitor marketed as a treatment for HIV infection. The drug has potent (Ki approximately 0.1 nM) antiviral activity and acts by inhibiting the processing of gag and gag-pol polyproteins, thus blocking the maturation of replicated viral particles. By assuming standard two-compartment disposition kinetics in combination with a variety of absorption processes we have identified two structural models that perform well with respect to describing the pharmacokinetic behavior of saquinavir when administered to healthy human volunteers from various Phase I studies. These structural models have been implemented for population analysis of these Phase I data via the Bayesian Markov chain Monte Carlo approach. We conclude that saquinavir exhibits complex and highly variable behavior, but can be modeled adequately using a two-compartment zero-order absorption model. There is also an indication that saquinavir kinetics may be time-dependent.
机译：Saquinavir是市售的HIV蛋白酶抑制剂，可用于治疗HIV感染。该药物具有有效的（Ki约为0.1 nM）抗病毒活性，并通过抑制gag和gag-pol多蛋白的加工而发挥作用，从而阻止了复制的病毒颗粒的成熟。通过假设标准的两室处置动力学与各种吸收过程相结合，我们确定了两种结构模型，这些模型在描述沙奎那韦从一期研究的健康人类志愿者中给药时的药代动力学行为方面表现良好。这些结构模型已经通过贝叶斯马尔可夫链蒙特卡洛方法实现了对这些I期数据的总体分析。我们得出结论，沙奎那韦表现出复杂且高度可变的行为，但可以使用两室零阶吸收模型进行充分建模。也有迹象表明沙奎那韦动力学可能是时间依赖性的。

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