Jornal de Bioequivalência e Biodisponibilidade

Abstrato

Formulation and Pharmacokinetics of Ketorolac Tromethamine Floating Compression Coated Mini-Tablets

Vemula SK, Venisetty RK and Veerareddy PR

Present research is intended to develop the Ketorolac Tromethamine (KTM) effervescent floating mini-tablets using compression coating method. Mini-tablets have the advantages of both tablets and multiparticulate formulations such as pellets. The main principle of floating mini-tablets can be applied to decrease the irritant effect of KTM on the stomach by avoiding the direct contact with the gastric mucosa and obtaining a low dosage for prolonged periods. KTM mini-tablets were prepared using 4 mm round flat punches and compression coated with hydroxypropyl methylcellulose and effervescent mixture. The prepared tablets were evaluated for weight variation, thickness, friability, hardness, drug content, in vitro buoyancy and in vitro release and the best formulation was subjected to further in vivo examination. The prepared mini-tablets exhibited satisfactory physicochemical characteristics. Formulation F3 offered the best controlled drug release (99.46 ± 0.93% in 12 h and T80%=9.4 h) along with floating lag time <30 s and total floating time >12 h. Pharmacokinetic studies of F3 formulation in male albino rabbits showed 2.25-fold higher bioavailability and 1.35-fold higher Cmax compared to immediate release core mini-tablets. Hence development of KTM effervescent compression-coated floating mini-tablets is the best way to give through oral route to maximize the therapy.