Formulation design for orally disintegrating tablets containing enteric-coated particles.
The purpose of this study was to investigate the applicability of our newly developed technology (RACTAB® technology) for preparing orally disintegrating tablets (ODTs) containing enteric-coated particles. Tamsulosin hydrochloride (TAM) was used as a model drug contained in the enteric-coated particles. Enteric-coated particles containing TAM (ECP-T) were prepared by spray coating a mixture of TAM with controlled-release materials. ECP-T was then mixed with rapidly disintegrating granules (RDGs), which were prepared using the suspension spray-coating method, and was tableted to form ODTs (ODTRAC). ODTRAC was evaluated for its hardness, thickness, internal structure (X-ray-CT scanning), functional properties (controlled-release profile), and in vivo disintegration time. Since RDGs with micronized ethylcellulose (MEC) increased tablet hardness by increasing the contact frequency between granules, ODTRAC containing ECP-T exhibited high hardness (>50 N) and low friability (<0.5%) with a relatively low compression force. After tableting, the structure of ECP-T in ODTRAC remained intact and no damage was observed on the surface. ECP-T recovered from ODTRAC showed the same dissolution profile of TAM in Japanese Pharmacopoeia (JP) 1st and JP 2nd media as that of intact ECP-T, which indicated that the tableting process did not affect the acid-resistibility of the particle. In addition, ODTRAC rapidly disintegrated in vivo (< 30 s), even at a high compression force (at 9 kN). These findings clearly suggest that RACTAB® technology is a useful approach to prepare ODTs containing enteric-coated particles.
Towa Pharmaceutical Co., Ltd.
Yutaka
Y
Okuda
Yasunobu
Y
Okamoto
Yosuke
Y
Irisawa
Kazuto
K
Okimoto
Takashi
T
Osawa
Shinji
S
Yamashita
D000284:Administration, Oral; D015195:Drug Design; D010316:Particle Size; D013449:Sulfonamides / Q000008:administration & dosage / Q000737:chemistry*; D013499:Surface Properties; D013608:Tablets, Enteric-Coated / Q000008:administration & dosage / Q000737:chemistry*; D000077409:Tamsulosin
D013449:Sulfonamides; D013608:Tablets, Enteric-Coated; D000077409:Tamsulosin