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ABSTRACT
Objective: Rosuvastatin, a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor used for the treatment of dyslipidaemia, may be co-administered with antacids in clinical practice. This trial assessed the effect of simultaneous and separated administration of an antacid preparation containing aluminium hydroxide 220 mg/5 mL and magnesium hydroxide 195 mg/5 mL (co-magaldrox 195/220) on the pharmacokinetics of rosuvastatin.
Research design and methods: A randomised, open-label, three-way crossover trial was performed. Healthy male volunteers (n = 14) received a single dose of rosuvastatin 40 mg alone, rosuvastatin 40 mg plus 20 mL antacid suspension taken simultaneously, and rosuvastatin 40 mg plus 20 mL antacid suspension taken 2 h after rosuvastatin on three separate occasions with a washout of ≥ 7 days between each.
Main outcome measures: The primary parameters were area under the rosuvastatin plasma concentration–time curve from time zero to the last quantifiable concentration (AUC(0–t)) and maximum observed rosuvastatin plasma concentration (Cmax) in the absence and presence of antacid.
Results: When rosuvastatin and antacid were given simultaneously, the antacid reduced the rosuvastatin AUC(0–t) by 54% (90% confidence interval [CI] for the treatment 0.40–0.53) and Cmax by 50% (90% CI 0.41–0.60). When the antacid was given 2 h after rosuvastatin, the antacid reduced the rosuvastatin AUC(0–t) by 22% (90% CI 0.68–0.90) and the Cmax by 16% (90% CI 0.70–1.01). The effect of repeated antacid administration was not studied and it cannot be discounted that this may have resulted in a stronger interaction than that observed here.
Conclusions: Simultaneous dosing with rosuvastatin and antacid resulted in a decrease in rosuvastatin systemic exposure of approximately 50%. This effect was mitigated when antacid was administered 2 h after rosuvastatin.