Preparation of carteolol hydrochloride matrix sustained-release pellets and evaluation in vitro/in vivo

Abstract

The aim of this study was to prepare carteolol hydrochloride matrix sustained-release pellets, and to compare its performance in vivo with carteolol common tablets. The formula was optimized according to the roundness and the release of pellets with single-factor, and orthogonal test. The carteolol hydrochloride matrix sustained-release pellets were got by extrusion-spheronisaion, while the release rate in vitro was determined by rotate basket method with UV detection. The carteolol hydrochloride sustained release property was studied in New Zealand white rabbits after oral administration. The optimized prescription is composed of carteolol hydrochloride 5.5 g, MCC 6.0 g, SA 26.3 g, EC 21.0 g, CMC-Na 1.2 g. Drug release property in vitro were as follows: the release time is over 12 h, the drug release behaviors follow the first order equation and the process of drug releasing is drug diffusion with frame erosion. The Cmax, Tmax and AUC(0→24) of the pellets were 2.58 ± 0.43 (mg/ml), 4.20 ± 0.87 (h) and 22.19 ± 4.23 (mg/ml h), respectively. The Cmax, Tmax and AUC(0→24) of the tablets were 3.75 ± 0.59 (mg/ml), 1.00 ± 0.72 (h) and 18.70 ± 3.75 (mg/ml h). The carteolol hydrochloride sustained-release pellets have reasonable formulation and simple preparation technology; the pellets acquired perfect sustained-release properties in vitro/in vivo. Key words: Carteolol hydrochloride, sustained-release, pellets, in vitro, in vivo, evaluation