TY - JOUR
T1 - Oral delivery of diclofenac sodium using a novel solid-in-oil suspension
AU - Piao, Hongyu
AU - Kamiya, Noriho
AU - Watanabe, Junji
AU - Yokoyama, Hideakira
AU - Hirata, Akihiko
AU - Fujii, Takeru
AU - Shimizu, Ichiro
AU - Ito, Susumu
AU - Goto, Masahiro
N1 - Funding Information:
The present work was supported partly by the 21st Century COE Program, “Functional Innovation of Molecular Informatics” from the Ministry of Education, Culture, Science, Sports and Technology of Japan (to M.G.).
PY - 2006/4/26
Y1 - 2006/4/26
N2 - The present work reports on a new pharmaceutical formulation for oral delivery of diclofenac sodium (DFNa), a non-steroidal anti-inflammatory drug (NSAID). Although DFNa itself is water-soluble at neutral pH, it was readily suspended in soybean oil via complex formation with an edible lipophilic surfactant and a matrix protein. The resulting solid-in-oil (S/O) suspension containing stably encapsulated DFNa in an oil phase markedly reduced the risks for gastrointestinal ulcers upon oral administration even at the LD50 level in rats (ca. 50 mg/kg DFNa). In addition, plasma concentration of DFNa upon administration of an S/O suspension was comparable with that of the aqueous counterpart at the same DFNa dose. These results indicate the potential use of S/O suspensions as novel oil-based pharmaceutical formulations for oral delivery of water-soluble drugs without causing severe mucitis.
AB - The present work reports on a new pharmaceutical formulation for oral delivery of diclofenac sodium (DFNa), a non-steroidal anti-inflammatory drug (NSAID). Although DFNa itself is water-soluble at neutral pH, it was readily suspended in soybean oil via complex formation with an edible lipophilic surfactant and a matrix protein. The resulting solid-in-oil (S/O) suspension containing stably encapsulated DFNa in an oil phase markedly reduced the risks for gastrointestinal ulcers upon oral administration even at the LD50 level in rats (ca. 50 mg/kg DFNa). In addition, plasma concentration of DFNa upon administration of an S/O suspension was comparable with that of the aqueous counterpart at the same DFNa dose. These results indicate the potential use of S/O suspensions as novel oil-based pharmaceutical formulations for oral delivery of water-soluble drugs without causing severe mucitis.
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U2 - 10.1016/j.ijpharm.2006.02.003
DO - 10.1016/j.ijpharm.2006.02.003
M3 - Article
C2 - 16530362
AN - SCOPUS:33645313195
VL - 313
SP - 159
EP - 162
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
SN - 0378-5173
IS - 1-2
ER -