Open AccessGastrointestinal Absorption of a New Reversible Proton Pump Inhibitor, YJA‐20379‐8, and its Pharmacokinetics after Oral Administration in Acetic Acid‐induced Gastric Ulcer in Rats
Author(s) -
CHUNG SU Y.,
HAN KYE S.,
KIM HO J.,
KIM JONGHAN,
CHANG MAN S.,
LEE MYUNG G.
Publication year - 1999
Publication title -
journal of pharmacy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.745
H-Index - 118
eISSN - 2042-7158
pISSN - 0022-3573
DOI - 10.1211/0022357991773500
Subject(s) - pharmacokinetics , jejunum , oral administration , ileum , stomach , duodenum , absorption (acoustics) , pharmacology , proton pump inhibitor , chemistry , medicine , acetic acid , gastroenterology , biochemistry , physics , acoustics
The absorption of YJA‐20379‐8 (3‐butyryl‐4‐[5‐(R)‐(+)‐methylbenzylamino]‐8‐ethoxy‐1,7‐naphthyridine) from various rat gastrointestinal segments was evaluated using in‐situclosed‐loops. The pharmacokinetics of the drug were also evaluated after oral administration to rats with acetic acid‐induced gastric ulcer (AIURs). The concentrations of YJA‐20379‐8 in the biological samples were analyzed by HPLC. The absorption of YJA‐20379‐8 from stomach and jejunum was fast, but approximately 50% of the drug was recovered from each segment at 24 h. The total areas under the plasma concentration‐time curves from time zero to 24 h (AUC 0‐24h ) were 161, 392, 233, 365, and 226 μg min mL −1 for stomach, duodenum, jejunum, ileum, and colon, respectively. After oral administration of the drug, the plasma concentrations and the resultant AUC 0‐12h were not significantly different between control and AIURs. The detection limits of YJA‐20379‐8 in human plasma and urine were 50 and 100ng mL −1 , respectively. The results suggest that modification of the oral dose of YJA‐20379‐8 may not be required in gastric ulcer patients if the present rat pharmacokinetic data could be extrapolated to man.