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Lack of Effect of Sucralfate on the Absorption and Pharmacokinetics of Rosiglitazone
Author(s) -
Rao Mamidi N.V.S.,
Mullangi Ramesh,
Katneni Kasiram,
Ravikanth Bhamidipati,
Babu Aravind P.,
Rani Usha P.,
Naidu M.U.R.,
Srinivas Nuggehally R.,
Rajagopalan Ramanujam
Publication year - 2002
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/00970002042006010
Subject(s) - rosiglitazone , sucralfate , pharmacokinetics , medicine , crossover study , cmax , bioequivalence , pharmacology , placebo , insulin , alternative medicine , pathology
The aim of the present study was to investigate the effect of sucralfate pretreatment on the pharmacokinetics of rosiglitazone following a single oral dose in healthy male volunteers. After an overnight fast, and according to a randomized schedule, each volunteer (n = 9) received a single oral dose of rosiglitazone 8 mg (Avandia® tablets, 4 mg × 2) with or without pretreatment of sucralfate 2 g (Recolfate® tablets, 1 g × 2) in an open‐label crossover study with a 2‐week washout period. Plasma samples were collected over a period of 24 hours at regular intervals. Safety assessment included monitoring of the vital signs, blood parameters, and ECG. No statistically significant differences (p > 0.05) were observed for any of the calculated rosiglitazone pharmacokinetic parameters in the two treatment groups. The mean parameters, AUC 0‐∞ and C max , following rosiglitazone administration alone were 3825.02 ng·h/ml and 664.47 ng/ml, respectively, and for rosiglitazone administered after pretreatment with sucralfate were 4848.19 ng·h/ml and 624.88 ng/ml, respectively. The t max for rosiglitazone alone and for rosiglitazone after sucralfate treatments was 1.11 and 1.67 hours, respectively The mean elimination half‐life for rosiglitazone and rosiglitazone after sucralfate treatment was 4.35 and 4.51 hours, respectively. Fraction of rosiglitazone absorbed was calculated by the Wagner‐Nelson method, and no statistically significant difference (p > 0.05) was observed for the two treatments. Since sucralfate pretreatment did not show any significant difference in the pharmacokinetics of rosiglitazone, no dose adjustment is warranted for rosiglitazone when it is administered with sucralfate.