The effect of histamine H2-receptor blockade on bismuth absorption from three ulcer-healing compounds.
Twelve healthy male subjects were dosed with six regimens: ranitidine and De-Noltab (tripotassium dicitrato bismuthate; Gist-Brocades Ltd., Weybridge, England), placebo and De-Noltab, ranitidine and Pepto-Bismol liquid [bismuth salicylate; Procter & Gamble (Health and Beauty Care) Ltd., Egham, England], placebo and Pepto-Bismol, ranitidine and Roter tablets (bismuth subnitrate; Roter Pharma Ltd., Ashford, England), and placebo and Roter. Ranitidine, 300 mg, or placebo was administered at 10 PM (night before) and at 7 AM; at 9 AM, the oral dose of bismuth was either 2 De-Noltabs, 3 30-mL doses of Pepto-Bismol liquid, or 2 Roter tablets. When predosed with placebo, the median integrated 8-hour plasma bismuth concentration was significantly greater after dosing with De-Noltabs than after dosing with either Pepto-Bismol or Roter (61, 8, and 8 ng.h/mL, respectively), with a similar trend for 8-hour median urinary bismuth excretion (213, 40, and 6 micrograms, respectively). When predosed with ranitidine, only after De-Noltab administration were there significant increases in the 8-hour plasma bismuth concentration (147 ng.h/mL), and 8-hour urinary bismuth excretion (686 micrograms). Eliminating intragastric acidity may enhance bismuth absorption after oral dosing with De-Noltabs by maintaining intragastric tripotassium dicitrato bismuthate as a colloidal suspension.
Nwokolo
C U
CU
University Department of Medicine, Royal Free Hospital School of Medicine, London, England.
Prewett
E J
EJ
Sawyerr
A M
AM
Hudson
M
M
Pounder
R E
RE
D000328:Adult; D000897:Anti-Ulcer Agents / Q000493:pharmacokinetics*; D001729:Bismuth / Q000493:pharmacokinetics*; D004311:Double-Blind Method; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects; D008297:Male; D009942:Organometallic Compounds / Q000493:pharmacokinetics; D010919:Placebos; D011899:Ranitidine / Q000494:pharmacology*; D011970:Receptors, Histamine H2 / Q000187:drug effects*; D012459:Salicylates / Q000493:pharmacokinetics
D000897:Anti-Ulcer Agents; D009942:Organometallic Compounds; D010919:Placebos; D011970:Receptors, Histamine H2; D012459:Salicylates; C015715:bismuth subsalicylate; D011899:Ranitidine; C010804:bismuth subnitrate; C002791:bismuth tripotassium dicitrate; D001729:Bismuth