Estimating unbound volume of distribution and tissue binding by in vitro HPLC-based human serum albumin and immobilised artificial membrane-binding measurements.

Valko KL; Nunhuck SB; Hill AP

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Estimating unbound volume of distribution and tissue binding by in vitro HPLC-based human serum albumin and immobilised artificial membrane-binding measurements.

机译：通过体外基于HPLC的人血清白蛋白和固定化人工膜结合测量法估算未结合的分布体积和组织结合。

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The in vivo unbound volume of distribution (V(du)) can be used to estimate the free steady-state plasma concentration with a given dose of a drug administered intravenously. We have demonstrated that the calibrated HPLC retention times obtained on biomimetic stationary phases, such as immobilised human serum albumin and phosphatidyl-choline, can be used to estimate compounds' in vivo behaviour. The mechanistic models are based on the assumption that the sum of the albumin and phospholipid binding has the most significant impact on reducing compounds' free concentration both in plasma and in tissues. The model equations were obtained using the literature human volume of distribution and fraction unbound in plasma values of 135 known drug molecules and have been tested on a further 300 in-house compounds. The model can be used to design compounds with low V(du) values and high fraction unbound in tissues which will minimise the required dose to achieve the efficacious free concentration at the target organ (excluding possible active transport processes).

机译：体内未结合的分布体积（V（du））可用于估算给定剂量的静脉内给药药物的游离稳态血浆浓度。我们已经证明，在仿生固定相（例如固定的人血清白蛋白和磷脂酰胆碱）上获得的校准的HPLC保留时间可用于评估化合物的体内行为。机理模型基于以下假设：白蛋白和磷脂结合的总和对降低化合物在血浆和组织中的自由浓度具有最大的影响。使用包括135种已知药物分子的血浆中人体的分布体积和未绑定分数的文献获得模型方程，并已在另外300种内部化合物上进行了测试。该模型可用于设计具有低V（du）值和组织中未结合的高比例化合物，这将使所需剂量最小化，以在目标器官上实现有效的自由浓度（不包括可能的主动转运过程）。

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《Journal of pharmaceutical sciences.》 |2011年第3期|共14页
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Valko KL; Nunhuck SB; Hill AP;
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中图分类药学;
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1. Estimating unbound volume of distribution and tissue binding by in vitro HPLC-based human serum albumin and immobilised artificial membrane-binding measurements. [J] . Valko KL, Nunhuck SB, Hill AP Journal of pharmaceutical sciences. . 2011,第3期

机译：通过体外基于HPLC的人血清白蛋白和固定化人工膜结合测量法估算未结合的分布体积和组织结合。
2. Prediction of in vivo tissue distribution from in vitro data. 2. Influence of albumin diffusion from tissue pieces during an in vitro incubation on estimated tissue-to-unbound plasma partition coefficients (Kpu). [J] . Ballard P, Arundel PA, Leahy DE, Pharmaceutical research . 2003,第6期

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Estimating unbound volume of distribution and tissue binding by in vitro HPLC-based human serum albumin and immobilised artificial membrane-binding measurements.

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