Role of the Lipid Emulsion on an Injectable Formulation of Lipophilic KW-3902, a Newly Synthesized Adenosine A_1-Receptor Antagonist
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概要
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KW-3902 (a newly synthesized adenosine A_1-receptor antagonist) has potent diuretic and renal protective activities. We investigated the influence of the emulsion formulation on the pharmacokinetics of KW-3902 and its metabolite (M1) in rats using three different formulations, i.e., a lipid emulsion about 130 nm in diameter composed of egg yolk lecithin: soybean oil: oleic acid=1:1:0.048, a liposome about 100 nm in diameter composed of egg yolk lecithin, and a saline solution containing 1% (v/v) each of dimethyl sulfoxide and 1_N NaOH. There was no significant difference in the pharmacokinetic parameters of KW-3902 (elimination half-life (T_<1/2>), area under the plasma concentration-time curves (AUC_<0-∞>), total body clearance (CL), mean residence time (MRT) and volume of distribution at steady-state (V_<dSS>)) and M1 (C_<max>, T_<1/2>, AUC_<0-∞> and MRT) after injection of these three dosage forms. Moreover, we investigated in vitro the binding of KW-3902 to blood components using these three formulations. KW-3902 was completely partitioned into the blood components regardless of its dosage form. These findings suggested that KW-3902 dissociated rapidly from the lipid emulsion or liposome in blood after injection and showed intrinsic pharmacokinetics of KW-3902 at doses of 0.1 and 1 mg/kg. Thus, the lipid emulsion formulation of KW-3902 was defined as a solvent, which was a vehicle for dissolving the drugs to prepare the injection, at its expected effective doses.
- 公益社団法人日本薬学会の論文
- 2002-04-01
著者
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Kato Y
Institute Of Cosmetic Sciences Club Cosmetics Co. Ltd.
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Yamauchi M
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Yamauchi M
School Of Engineering Kinki University
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Iwata Kenji
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Yamauchi Masahiro
Pharmaceutical Research Center, KYOWA HAKKO KOGYO CO., LTD.
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KATO Yasuki
Drug Formulation Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.
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HOSOKAWA Toshihito
Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.
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YAMAMOTO Yoshihiko
Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.
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KATO Yasuki
Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.
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MOCHIZUKI Harumi
Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.
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岩田 建
Department Of Pharmaceutics Faculty Of Pharmaceutical Sciences Okayama University
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Kato Yasuki
協和醗酵工業
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Yamamoto Yoshihiko
Graduate School Of Pharmaceutical Sciences Kumamoto University
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Kato Yasuki
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Yamamoto Yoshihiko
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Mochizuki Harumi
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Yamauchi Masahiro
Pharmaceutical Research Center Kyowa Hakko Kogyo Co. Ltd.
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Hosokawa T
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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