Bioavailability Assessment of Arginine-Vasopressin (AVP) Using Pharmacokinetic-Pharmacodynamic (PK-PD) Modeling in the Rat
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概要
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A novel method of assessing the extent of oral bioavailability of arginine-vasopressin (AVP) from pharmacological data was presented. After intravascular administration (i.v. bolus or short-term infusion) of AVP to rats, the relationship between blood concentrations and its effect on both mean arterial pressure (hemodynamic effect) and urinary sodium concentration (anti-diuretic effect) was described on the basis of an integrated pharmacokinetic-pharmacodynamic (PK-PD) model. A direct model was used for the hemodynamic response, while an indirect response model, rather than a hypothetical link model was used for the anti-diuretic response. A sigmoid E_<max> model was applied to describe the drug-receptor interaction. Pharmacological responses after intravascular administration of AVP were reasonably described by the PK-PD model. However, PD parameters estimated by the PK-PD analysis suggested that apparent receptor affinity rather than efficacy in i.v. bolus study was significantly higher than that in the short-term infusion study. This fact indicated that PK-PD relationship was influenced by the intravascular input rate of AVP. We than investigated the relationship between plasma concentration and amount of AVP bound to the V_2 receptors in the kidney. The result indicated that the amount of AVP bound to the receptors after i.v. bolus injection was always greater than that after short-infusion. Since the PK-PD relationship after oral administration was almost identical with that after short-term infusion, the PK-PD model obtained in the short-term infusion study was used to assess the extent of oral bioavailability (EBA_<p.o.>). The EBA_<p.o.> values, estimated from pharmacological effects (hemodynamic effect and anti-diuretic effect) after oral administration of 5μg/kg of AVP were 0.68% to 0.93% and were almost identical with the actual EBA_<p.o.> value (0.81%). From these results, we concluded that oral bioavailability of AVP was reasonably predicted by the PK-PD model, provided that appropriate pharmacological effects and appropriate intravascular dosing rate as a reference formulation are available. The method may be an alternative to methods based on plasma concentrations, when drug concentration cannot be measured and when appropriate pharmacological data are available.
- 公益社団法人日本薬学会の論文
- 2000-01-01
著者
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Kakemi M
Department Of Pharmaceutics Osaka University Of Pharmaceutical Sciences
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Kakemi Masao
大阪薬科大学 薬剤学
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MORIMOTO Kazuhiro
Department of Pharmaceutics, Graduate School of Pharmaceutical Sciences, Hokkaido Pharmaceutical Uni
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MIYAZAKI Makoto
Department of Pharmaceutics, Osaka University of Pharmaceutical Sciences
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IWANAGA Kazunori
Department of Pharmaceutics, Osaka University of Pharmaceutical Sciences
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SAWADA Shin-ichi
Department of Research Planning, National Institute of Industrial Health
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Miyazaki Michiko
School of Pharmaceutical Sciences, Showa University
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Kakemi M
Osaka Univ. Pharmaceutical Sci. Takatsuki Jpn
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KAKEMI Masawo
Department of Pharmaceutics, Osaka University of Pharmaceutical Sciences
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Miyazaki Makoto
Department Of Pharmaceutics Osaka University Of Pharmaceutical Sciences
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Morimoto Kazuhiro
Department Of Applied Chemistry Faculty Of Engineering Doshisha University
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Morimoto K
Hokkaido Pharmaceutical University School Of Pharmacy
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NISHIDE Takayoshi
Department of Pharmaceutics, Osaka University of Pharmaceutical Sciences
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Sawada S
Department Of Pharmaceutics Osaka University Of Pharmaceutical Sciences
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Iwanaga Kazunori
Department Of Pharmaceutics Osaka University Of Pharmaceutical Sciences
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Nishide Takayoshi
Department Of Pharmaceutics Osaka University Of Pharmaceutical Sciences
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Sawada Shin-ichi
Department Of Engineering Science Kyoto University
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Miyazaki Makoto
Department Of Mechanical Engineering And Intelligent Systems The University Of Electro-communication
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Sawada Shin-ichi
Department Of Botany Faculty Of Science University Of Tokyo
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Miyazaki Makoto
Department of Applied Chemistry, Faculty of Engineering, Kansai University
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