Development of a Tamsulosin Hydrochloride Controlled-Release Capsule Consisting of Two Different Coated Pellets

Abstract

Tamsulosin hydrochloride (TSH) controlled-release capsule (pellets) was successfully prepared using a novel, simple, and flexible multiunit drug delivery system, which consisted of two different coated pellets. The TSH-loaded core pellets consisting of microcrystalline cellulose (MCC), lactose, Carbopol^® 974P, and the active agent, were prepared by extrusion/spheronization method. Eudragit^® NE30D and Eudragit^® L30D-55 were used as the coating materials to prepare sustained-release (SR) pellets and enteric-release (ER) pellets. The coated pellets were prepared using two different equipments: centrifugal coater and fluidized-bed coater. By adjusting the ratio of SR and ER pellets, more than one blend ratios, which meet the in vitro release criterion were obtained. A similarity factor (f₂) was employed to choose the optimum proportion compared with the commercial product (Harnal^® capsule). The morphology of the pellet surfaces was examined by scanning electron microscopy (SEM) before and after dissolution. The release profiles were significantly affected by changing the proportions of SR and ER. The optimum ratio is SR:ER = 2:1 using a centrifugal coater (f₂ = 61.93) and SR:ER = 3:1 using a fluidized coater (f₂ = 66.42). This result suggests that blending these two-part pellets (SR and ER) can provide an alternative to preparing a controlled-release dosage form, instead of blending of the coating polymer.

Keywords:

• controlled-release pellets
• extrusion/spheronization
• tamsulosin hydrochloride
• Eudragit^® NE30D
• similarity factor

ACKNOWLEDGMENT

The authors would like to thank Evonik-Degussa Company for technical support and supplying samples.