Oral delivery of diclofenac sodium using a novel solid-in-oil suspension.
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 LD(50) 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.
Piao
Hongyu
H
Department of Applied Chemistry, Graduate School of Engineering, Kyushu University, 744 Motooka, Fukuoka 819-0395, Japan.
Kamiya
Noriho
N
Watanabe
Junji
J
Yokoyama
Hideakira
H
Hirata
Akihiko
A
Fujii
Takeru
T
Shimizu
Ichiro
I
Ito
Susumu
S
Goto
Masahiro
M
D000284:Administration, Oral; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000633:toxicity*; D002626:Chemistry, Pharmaceutical; D004008:Diclofenac / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000633:toxicity*; D004655:Emulsions; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D012995:Solubility; D013024:Soybean Oil / Q000737:chemistry*; D013276:Stomach Ulcer / Q000209:etiology / Q000473:pathology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004655:Emulsions; D004008:Diclofenac; D013024:Soybean Oil