Lack of Effect of Sucralfate on the Absorption and Pharmacokinetics of Rosiglitazone

• Published in: Journal of clinical pharmacology 2002-06, Vol.42 (6), p.670-675
• Main Authors: 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
• Format: Article
• Language: English
• Subjects: Administration, Oral; Adult; Biological and medical sciences; Cross-Over Studies; Drug Interactions; General and cellular metabolism. Vitamins; Humans; Hypoglycemic Agents - pharmacokinetics; Intestinal Absorption; Male; Medical sciences; Pharmacology. Drug treatments; Rosiglitazone; Sucralfate - pharmacology; Thiazoles - adverse effects; Thiazoles - pharmacokinetics; Thiazolidinediones
• ISSN: 0091-2700; 1552-4604
• DOI: 10.1177/00970002042006010

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, AUC0‐∞ and Cmax, 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 tmax 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.