Effect of antacids on aspirin dissolution and bioavailability |
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Authors: | Ramchandra K Nayak Robert D Smyth Andrew Poik Tihamer Herczeg Victoria Carter Anthony J Visalli Nelson H Reavey-Cantwell |
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Institution: | (1) Research Laboratories Division, William H. Rorer, Inc., 19034 Fort Washington, Pennsylvania;(2) Present address: McNeil Laboratories, Inc., Camp Hill Road, 19034 Fort Washington, Pennsylvania;(3) Bristol Laboratories, Syracuse, New York |
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Abstract: | The in vitrodissolution profile, in vitroand in vivobuffering characteristics, and single-dose bioavailability of various buffered aspirin tablet formulations were studied. Buffering agents,such as magnesium and aluminum hydroxides (formulations B and C) or magnesium carbonate and aluminum glycinate (formulation D), significantly increased the rate of aspirin dissolution from solid dosage forms as compared to an unbuffered tablet (formulation A). The extent of aspirin absorption was equivalent with all formulations;however, the faster rate of dissolution (t50
and t90)with buffered formulations resulted in earlier and higher peak concentration of salicylate compared to that with unbuffered formulation, following a two-tablet dose in the fasting state. A comparison of the in vivobuffer capacity of a four-tablet dose of formulations B and D was performed in the postcibal state at the time of maximal meal-induced acid secretion, using a radiotelemetry procedure for determination of pH. Formulation B prolonged the interval of elevation of intragastric pH > 3 for 32 min as compared to 12 min for D. |
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Keywords: | aspirin dissolution bioavailability effect of antacids acid capacity consuming in vivo buffering effect |
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