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- W2362350195 abstract "Aim:To investigate the pharmacokinetic profile and tissue distribution of a novel phosphodiesterase type 5 inhibitor,5-ethyl-2-{5-[4-(2-hydroxy-ethyl)-piperazine- 1-sulfonyl]-2-propoxy-phenyl}-7-propyl-3,5-dihydro-pyrrolo(3,2-d)pyrimidin-4- one(SK-3530),in rats after administration of the ~(14)C-labeled compound.Methods: The pharmacokinetic parameters of SK-3530 were measured based on the total radioactivity and parent SK-3530 concentration in rat plasma after intravenous and oral administration.The tissue distribution of total radioactivity after a single oral administration of[~(14)C]SK-3530 at a dose of 40 mg/kg was assayed.The plasma protein binding rates of SK-3530 were assessed by in vitro and ex vivo assay.Results:The total radioactivity profiles showed linear pharmacokinetics. The maximum plasma concentration and area under the curve of the parent SK3530 were 10%-20% compared to those of the total radioactivity.After the oral admin- istration of[~(14)C]SK-3530,the radioactivity was widely distributed in all tissues, and the tissue/plasma ratio of the radioactivity 1 h after administration was calcu- lated as 0.5-2.6 with the exception of excretory organs.A relatively high penetra- tion was shown in the adrenal glands,liver,and lung.In vitro and ex vivo plasma protein binding assay by ultrafiltration showed a considerably high binding rate of more than 97%.Conclusion:SK-3530 was relatively well absorbed in the gas- trointestinal tract and showed linear pharmacokinetics over the investigated dose range.SK-3530 had low oral bioavailability due to a high,first-pass metabolism." @default.
- W2362350195 created "2016-06-24" @default.
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- W2362350195 date "2007-01-01" @default.
- W2362350195 modified "2023-09-23" @default.
- W2362350195 title "Pharmacokinetics and tissue distribution of a novel PDE5 inhibitor,SK-3530,in rats" @default.
- W2362350195 hasPublicationYear "2007" @default.
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