SHORT-TERM SUCRALFATE ADMINISTRATION ALTERS POTASSIUM DICLOFENAC ABSORPTION IN HEALTHY MALE-VOLUNTEERS

Citation
Jp. Pedrazzoli et al., SHORT-TERM SUCRALFATE ADMINISTRATION ALTERS POTASSIUM DICLOFENAC ABSORPTION IN HEALTHY MALE-VOLUNTEERS, British journal of clinical pharmacology, 43(1), 1997, pp. 104-108
Citations number
37
Categorie Soggetti
Pharmacology & Pharmacy
ISSN journal
03065251
Volume
43
Issue
1
Year of publication
1997
Pages
104 - 108
Database
ISI
SICI code
0306-5251(1997)43:1<104:SSAAPD>2.0.ZU;2-6
Abstract
Aims Since patients who regularly take NSAIDS may use sucralfate becau se of its cytoprotective properties, we examined the influence of this compound on the pharmacokinetics of diclofenac. Methods Potassium dic lofenac (105 mg) was administered orally to eighteen healthy male volu nteers with or without a 5-day pre-treatment with sucralfate (2000 mg twice daily). Blood samples were collected at intervals post-dose and serum concentrations of diclofenac were determined by reverse-phase h. p.l.c. Results Pre-treatment with sucralfate significantly decreased b oth the AUC(0,8 h) [2265ng h ml(-1) (geometric mean) (range 1815-2827) vs 1821ng h ml(-1) (1295-2562)] and the C-max [1135 ng ml(-1) (geomet ric mean) (range 898-1436) vs 701 ng ml(-1) (501-981)] with no signifi cant delay in absorption [t(max) 1.0 h (median) (range 0.5-2.0) vs 1.0 h (0.5-4.0)]. Conclusions The short-term treatment of healthy male vo lunteers with sucralfate decreases potassium diclofenac bioavailabilit y,; These findings suggest that either an appropriate increase in the diclofenac intake or the use of another gastric mucosa protector must be adopted.