Carvedilol (BCS Class II drug) is a nonselective β-adrenergic blocking agent with α1-blocking activity having poor oral bioavailability. The objective of this study is to enhance the oral bioavailability of carvedilol. To improve oral bioavailability of carvedilol, carvedilol β-Cyclodextrin complex were formulated by employing the kneading method with the drug: complexing agent1:2. The complexes and pure drug were subjected to pharmacokinetic studies in rabbits. The plasma samples were analyzed by LC-MS/MS method. Various pharmacokinetic parameters were calculated. Carvedilol β-Cyclodextrin complex showed higher Ka, AUC values compared with pure drug. Carvedilol β-Cyclodextrin complex showed 1.78 fold increases in extent of absorption.