Development of Terbutaline Sulfate Sustained-Release Coated Pellets

Abstract

Sustained-release coated pellets containing terbutaline sulfate (TS) 1.8% w/w were prepared. The suitable core formulation that gave round-shape TS pellets was preformulated and was composed of microcrystalline cellulose:lactose 38.61%:57.92%, hydroxypropyl cellulose (HPC-M) 1.67%, and water 40%, respectively. The core pellets containing active drug were coated with various amounts of ethylcellulose (EC) and a combination of EC/HPC-M polymers. The effects of fluidized bed polymeric film coats on drug release were studied in vitro. The dissolution characteristics were also investigated. The release of the active drug decreased as the amount of EC increased. This may be due to water-insoluble EC film, leading to decreased permeability in water. In the case of the combination of EC/HPC-M, the release of the active drug increased as the amount of HPC-M in the coating solution increased. Since HPC-M is a water-soluble polymer, it may be suggested that formation of pores were increased in the coating layer. Among five coating formulas in this study, formulation 1 (F1) (at 1.1% EC concentration) shows a similar dissolution profile to Bricanyl Durules; however, lag time for the release occurred. In conclusion, the formulation that gave an insignificant release profile (p < .01) when compared with commercial product was the capsule containing F1 (at 1.1% EC concentration) mixed with uncoated pellets at a ratio of 7:1, and the release was found to be reproducible.

Novel Film Modifiers to Alter the Physical Properties of Composite Ethylcellulose Films

“…A number of studies were directed at employing additives to modify the permeability of EC films: hydroxypropyl methylcellulose (11,12), hydroxypropyl cellulose (13), carboxy methylcellulose (14), acrylates (15)(16)(17), pectin (18), maltodextrins (19), xylitol (19), and polyethylene glycol (19,20). Among these studies, the influence of hydroxypropyl methylcellulose on the properties of ethylcellulose films has been most extensively investigated.…”

Formulation and In Vitro and In Vivo Evaluation of Lipid-Based Terbutaline Sulphate Bi-layer Tablets for Once-Daily Administration

“…Several sustained-release formulation approaches have been developed for oral TBS administration such as microcapsules [6,7], microspheres [8,9], sustained-release coated pellets [10,11], gastroretentive floating tablets [3], asymmetric membrane osmotic capsules [12], and polymeric matrix tablets [13][14][15].…”

Recent progress in preparation and agricultural application of microcapsules

“…The composition of PLA and PLA/PLGA is widely used to prepare microcapsules with the sustained release property (Schachter & Kohn, 2002). ( Benita & Donbrow, 1982;El-Habashy et al, 2016;Gupta et al, 2013;Kim et al, 2014;Mirabedini et al, 2012;Morgen et al, 2012;Murtaza, 2012;Oh & Lee, 1982;Prasertmanakit et al, 2009;Shi & Tan, 2002;Umprayn et al, 1999;Wei et al, 2008;Yang et al, 2001) Inorganic materials The centrifugal coating granulation assay, LBL assembly, electrospray, etc.…”