The in-vitro adsorption of some antirheumatics on antacids.
The adsorption of sodium salicylate, salicylamide, acetylsalicylic acid, paracetamol, mefenamic acid, flufenamic acid, phenylbutazone, oxyphenbutazone, phenazone, aminophenazone, indometacin and methiazinic acid on some antacids was studied. The antacids used were magnesium trisilicate, magnesium oxide, aluminium hydroxide, bismuth oxycarbonate, calcium carbonate and kaolin. Magnesium oxide, followed by aluminium hydroxide and bismuth oxycarbonate showed a fairly high adsorptive capacity for salicylates, mefenamic acid, flufenamic acid, methiazinic acid, indometacin and to a lesser extent for phenylbutazone and oxyphenbutazone. On the other hand, magnesium trisilicate exhibited a tendency to adsorb phenazone, aminophenazone, indometacin and methiazinic acid. Kaolin was found to be a good adsorbent for anthranilic acid derivatives, indometacin and methiazinic acid. Calcium carbonate showed a weak adsorptive capacity for all drugs tested. The adsorption of phenylbutazone and salicylates on magnesium oxide, aluminium hydroxide and/or bismuth oxycarbonate obeyed the Freundlich adsorption isotherm. Elution study showed that salicylates and anthranilic acid derivatives were tenaciously held by magnesium oxide while magnesium trisilicate showed an intermediate retention power for phenazone and aminophenazone. Sodium hydrogen carbonate solution gave, in general, a higher eluting power than hydrochloric acid solution. A marked reduction in the apparent partition coefficients of all drugs tested was observed in the presence of magnesium trisilicate or aluminium hydroxide. Careful in vitro and in vivo testing of drug availability is advisable prior to the concomitant administration of antirheumatics with antacids or other adsorbents.
D000327:Adsorption; D000863:Antacids / Q000378:metabolism*; D000893:Anti-Inflammatory Agents / Q000378:metabolism*; D001682:Biological Availability; D001702:Biopharmaceutics; D002021:Buffers; D002463:Cell Membrane Permeability; D004357:Drug Synergism; D066298:In Vitro Techniques
D000863:Antacids; D000893:Anti-Inflammatory Agents; D002021:Buffers