[Development of nasal dosage form of oxatomide for rhinitis].
The possibility of oxatomide as the nasal dosage drug for the therapy of nasal allergy was studied. Oxatomide was well absorbed from the nasal cavity, indicating a high permeability to nasal epithelial layer after nasal administration. Acidic pH condition further enhanced the permeation of oxatomide across Caco-2 monolayers, due to the high solubility at the low pH range. Nasal dosage forms for oxatomide (dextrin form, hydroxypropyl-gamma-cyclodextrin form and the suspension of polyethylene glycol) was, therefore, adjusted to pH 5.0. This pH allowed a high solubility of oxatomide without the irritation to nasal epithelium. The effect of nasal administration of oxatomide was studied on experimental allergic rhinitis in sensitized guinea pig. All dosage forms of oxatomide significantly inhibited the dye leakage into the nasal cavity, and among three forms, dextrin form showed the highest effect. High viscosity of dextrin solution was considered to stabilize the dispersion of oxatomide and enhance the retention in the nasal cavity. These results suggest that oxatomide should be useful as nasal dosage drug for allergic rhinitis.
Furubayashi
Tomoyuki
T
Research and development division, Toko Pharmaceutical Industries, LTD.
Kobayashi
Yoichi
Y
Yamashita
Shinji
S
Sakane
Toshiyasu
T
Kawauchi
Hideyuki
H
D000281:Administration, Intranasal; D000818:Animals; D018926:Anti-Allergic Agents / Q000008:administration & dosage*; D006168:Guinea Pigs; D008297:Male; D010879:Piperazines / Q000008:administration & dosage*; D051381:Rats; D017208:Rats, Wistar; D012130:Respiratory Hypersensitivity / Q000188:drug therapy*; D012220:Rhinitis / Q000188:drug therapy*
D018926:Anti-Allergic Agents; D010879:Piperazines; C015408:oxatomide