Authors: Ann K Miller Anne Inglis Kathleen Thompson Culkin Diane K Jorkasky Martin I Freed
Publish Date: 2014/02/07
Volume: 57, Issue: 2, Pages: 105-109
Abstract
Objectives To investigate whether treatment with acarbose alters the pharmacokinetics PK of coadministered rosiglitazone Methods Sixteen healthy volunteers 24–59years old received a single 8mg dose of rosiglitazone on day 1 followed by 7 days of repeat dosing with acarbose 100 mg three times daily tid with meals On the last day of acarbose tid dosing day 8 a single dose of rosiglitazone was given with the morning dose of acarbose PK profiles following rosiglitazone dosing on days 1 and 8 were compared and point estimates PE and associated 95 confidence intervals CI were calculated Results Rosiglitazone absorption as measured with peak plasma concentration Cmax and time to peak concentration Tmax was unaffected by acarbose The area under the concentration–time curve from time zero to infinity AUC0– ∞ was on average 12 lower 95 CI –21 –2 during rosiglitazone + acarbose coadministration and was accompanied by an approximate 1h 23 reduction in terminal elimination halflife t 1/2 49 h versus 38 h This small decrease in AUC0– ∞ appears to be due to an alteration in systemic clearance of rosiglitazone and not changes in absorption These observed changes in AUC0– ∞ and t 1/2 are not likely to be clinically relevant Coadministration of rosiglitazone and acarbose was well tolerated Conclusion Acarbose administered at therapeutic doses has a small but clinically insignificant effect on rosiglitazone pharmacokinetics
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