Bioequivalence Assesment of Tiropramide in Korean Male Volunteers

Two formulations of tiropramide {(${\pm}$)${\alpha}$-(benzoylamino)-4-[2-(diethylamino)-ethoxy]-N,N-dipropyl-benzenepropanamide hydrochloride}, an antispasmodic agent, were orally administered to 16 healthy Korean male volunteers by Latin crossover design with the purpose of evaluating bioeqivalence and phamacokinetics of tiropramide. Tiropramide in human plasma was determined by a gas chromatography/nitrogen phosphorus detector. Detection limit of tiropramide was 5 ng/ml. C$\_$max/ values in test and reference formulations were 93.9 ${\pm}$ 54.3 and 96.4 ${\pm}$ 51.6 ng/ml, respectively. AUC$\_$0\longrightarrowlast/ and AUC$\_$0\longrightarrowinf/ were, respectively, 330.7 ${\pm}$ 193.9 and 349.5 ${\pm}$ 205.3 ng.hr/ml for test formulation, 348.9 ${\pm}$ 207.7 and 380.8 ${\pm}$ 239.0 ng.hr/ml for reference formulation. Terminal half-life was 2.3-2.6 hr. Bioavailability differences for C/aub max/ and AUC$\_$0\longrightarrowlast/ were 2.48% and 5.22%, respectively. Minimum detection differences were less than 20% in both C$\_$max/ AUC. Based on this results, two formulations of tiropramide were considered to be bioequivalent