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Pharmacokinetics of a non‐narcotic analgesic, DA‐5018, in rats
Author(s) -
Lee Jong J.,
Shim Hyun J.,
Kim So H.,
Lee Sang D.,
Kim Won B.,
Yang Junnick,
Lee Myung G.
Publication year - 1998
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/(sici)1099-081x(199803)19:2<101::aid-bdd81>3.0.co;2-b
Subject(s) - analgesic , pharmacokinetics , narcotic , pharmacology , medicine , morphine , narcotic analgesics , anesthesia
The pharmacokinetics of a non‐narcotic analgesic, DA‐5018, were compared after single intravenous (IV), subcutaneous (SC), and oral administrations, and after multiple (seven consecutive days) SC administration to rats. After IV administration of DA‐5018, 1, 2, and 5 mg kg −1 , the pharmacokinetic parameters of DA‐5018 were independent of the dose ranges studied. After oral administration of DA‐5018, absorption of the drug from gastrointestinal (GI) tract was fast, but the extent of absolute bioavailability ( F ) was low; the values were 23.2, 23.0, and 27.3% for 2, 5, and 10 mg kg −1 , respectively. After single SC administration of DA‐5018, absorption of the drug from the injected site was fast and the extent of absorption was fairly good; the F values were 74.5 and 71.8% for 2 and 5 mg kg −1 , respectively. The lower F values after oral administration of DA‐5018 to rats could be due to degradation of the drug in rat GI tract and/or considerable first‐pass effect. After IV, oral, and SC administration of DA‐5018, the drug had a strong affinity to the rat tissues studied as reflected in the greater‐than‐unity tissue to plasma ratio. After IV, oral, and SC administration of the drug, the biliary and urinary excretion of unchanged DA‐5018 were negligible. There was no significant difference in the pharmacokinetics or tissue distribution of DA‐5018 between single and multiple SC administration of the drug, 5 mg kg −1 , to rats, indicating that there could be no tissue accumulation of the drug after multiple SC administration of the drug to rats. © 1998 John Wiley & Sons, Ltd.