Physicochemical Characterization of Bi-Layered Terbutaline Sulfate Tablets for Chronotherapeutic Pulsatile Drug Delivery Design Based on Natural and Synthetic Polymer using Direct Compression Technique

Abstract

The aim of the strategy to formulate the pulsatile drug delivery system using terbutaline sulfate by direct compression technique and evaluate the effects of formulation and dissolution medium on the behavior of drug release, and to clarify the drug release mechanism based on acquiring results. Pulsatile release tablets include a drug and disintegrating agent-containing core and swellable external layers for slow down drug release, then rupturing the nearby surrounding outer layer for fast release. Core tablets prepared using disintegrating agent by direct compression method and coated with polymers like HPMC K100M, ethyl cellulose, karaya gum in different quantities. Several physical parameters of the tablets evaluated such as stiffness, thickness, friability, weight variation, disintegration, drug content and dissolution test. Terbutaline sulfate released from bi-layered tablets with pulsatile behaviors. In-vitro drug release rate readings showed that F3 and F6 are best based on the less quantity of drug release during the lag time (11% and 14% in 5 h). So, from the result, the F6 has nominated the best formulation. Thus, by the direct compression method prepared, coated tablets before drug release with an obvious lag time is possibly useful preparation for the medication of osteoarthritis, rheumatoid arthritis, dysmenorrhea, asthma which follows a circadian rhythm. It confirmed that eroding, diffusion, and swelling mechanisms were responsible for drug release. Ultimate pulsatile release activities may be done by modifying polymeric membrane quantities and proportions to meet the condition of pulsatile activities.