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The Influence of Gastric Emptying on Droxicam Pharmacokinetics
Author(s) -
Sánchez J.,
Martínez L.,
GarcíaBarbal J.,
Roser R.,
Bartlett A.,
Sagarra R.
Publication year - 1989
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1989.tb03409.x
Subject(s) - gastric emptying , metoclopramide , pharmacokinetics , piroxicam , bioavailability , pharmacology , absorption (acoustics) , chemistry , cisapride , medicine , stomach , physics , alternative medicine , pathology , acoustics , vomiting
Droxicam is a new nonsteroidal anti‐inflammatory drug that is a pro‐drug of piroxicam. The influence of gastric emptying rate on droxicam pharmacokinetics has been investigated in eight healthy male volunteers. A single, 20 mg dose was administered p.o. together with 1500 mg of paracetamol. Gastric transit was experimentally modified by administration of propantheline (45 mg, p.o.) or metoclopramide (10 mg, i.v.) simultaneously with the droxicam and the paracetamol. Plasma levels of paracetamol were used as markers of gastric transit. The plasma concentrations of piroxicam, the active substance from droxicam, were determined by a high‐performance liquid chromatographic method. The pharmacokinetic parameters of droxicam were: C max = 1.03 ± 0.16 μg/mL (mean ± SD), T max = 11.1 ± 5.7 hr, AUC = 115.7 ± 29.6 μg hr/mL, T 1/2 a = 2.64 ± 0.72 hr, T 1/2 el = 73.6 ± 16.7 hr, CL/F = 3.06 ± 0.80 mL/min and MRT = 111.1 ± 23.5 hr. Following modification of gastric emptying, only T max (droxicam + metoclopramide = 25.0 ± 10.8 hr and droxicam + propantheline = 20.8 ± 8.8 hr) underwent significant change ( P < 0.05). These results indicate that absorption rate of droxicam has been modified but bioavailability does not suffer modification in conditions of altered gastric emptying .