The bioavailability of sulpiride taken as a film-coated tablet with sodium bicarbonate, cimetidine, natural orange juice or hydrochloric acid.
The bioavailability of sulpiride taken in film-coated tablet form with sodium bicarbonate or cimetidine or with natural orange juice or diluted hydrochloric acid was studied. A commercial sulpiride film-coated tablet (100 mg/T) treated with polyvinylacetal diethylaminoacetate (AEA), which remain undissolved at pH above 4-5, was given to four healthy volunteers who had fasted overnight. The subjects were divided into two groups, those showing high and low bioavailability of sulpiride from an AEA film-coated tablet. The two high bioavailability subjects took one tablet (100 mg) with 100 ml of water (1) alone, (2) together with 1 g of sodium bicarbonate or (3) during concurrent dosing with cimetidine, 200 mg three times a day. The two low bioavailability subjects swallowed one tablet with 100 ml of (1) water, (2) natural orange juice, or (3) diluted hydrochloric acid. Urine samples were collected over a 48-h period following sulpiride administration to determine sulpiride concentrations by HPLC. The bioavailability was estimated from the cumulative amount excreted unchanged in urine over 48 h (Du48). In the high bioavailability subjects, the bioavailability of sulpiride markedly decreased with the coadministration of sodium bicarbonate or cimetidine compared to when the tablet was taken alone. In the low bioavailability subjects, the bioavailability remarkably increased with the concomitant intake of orange juice or diluted hydrochloric acid over that with only water. These results suggest that the bioavailability of sulpiride from AEA film-coated tablet is influenced by the individual's gastric acidity and by coadministered drug and drink which affect gastric acidity.
Shinkuma
D
D
Department of Pharmacy, Hyogo College of Medicine, Japan.
Hamaguchi
T
T
Kobayashi
M
M
Yamanaka
Y
Y
Mizuno
N
N
D000328:Adult; D001628:Beverages; D001639:Bicarbonates; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D002927:Cimetidine; D002957:Citrus; D004347:Drug Interactions; D006801:Humans; D006851:Hydrochloric Acid; D006863:Hydrogen-Ion Concentration; D008297:Male; D008875:Middle Aged; D012964:Sodium; D017693:Sodium Bicarbonate; D013469:Sulpiride / Q000008:administration & dosage / Q000493:pharmacokinetics*; D013607:Tablets
D001639:Bicarbonates; D013607:Tablets; D013469:Sulpiride; D002927:Cimetidine; D017693:Sodium Bicarbonate; D012964:Sodium; D006851:Hydrochloric Acid