title: Preparation of a fast dissolving oral thin film containing dexamethasone: a possible application to antiemesis during cancer chemotherapy.
abstract: We prepared fast dissolving oral thin film that contains dexamethasone and base materials, including microcrystalline cellulose, polyethylene glycol, hydroxypropylmethyl cellulose, polysorbate 80 and low-substituted hydroxypropyl cellulose. This preparation showed excellent uniformity and stability, when stored at 40 degrees C and 75% in humidity for up to 24 weeks. The film was disintegrated within 15s after immersion into distilled water. The dissolution test showed that approximately 90% of dexamethasone was dissolved within 5 min. Subsequently, pharmacokinetic properties of dexamethasone were compared in rats with oral administration of 4 mg dexamethasone suspension or topical application of the film preparation containing 4 mg dexamethasone to the oral cavity. Pharmacokinetic parameters were similar between the two groups in which C(max) (h), T(max) (microg/mL), AUC (microg/mL/h) and half-life (h) were 12.7+/-6.6 (mean+/-SD, N=10), 3.4+/-1.4, 93.6+/-37.8 and 1.66+/-0.07, respectively, for oral suspension and 13.3+/-4.0, 3.2+/-1.0, 98.0+/-22.3 and 1.65+/-0.06, respectively, for film preparation. These findings suggest that the fast dissolving oral thin film containing dexamethasone is likely to become one of choices of dexamethasone preparations for antiemesis during cancer chemotherapy.
authors.affiliation: Department of Pharmacy, Gifu University Hospital, Gifu, Japan.
authors.forename: Hiroyoshi
authors.initials: H
authors.lastname: Shimoda
authors.forename: Kazumi
authors.initials: K
authors.lastname: Taniguchi
authors.forename: Misao
authors.initials: M
authors.lastname: Nishimura
authors.forename: Katsuhiko
authors.initials: K
authors.lastname: Matsuura
authors.forename: Tadao
authors.initials: T
authors.lastname: Tsukioka
authors.forename: Hirotaka
authors.initials: H
authors.lastname: Yamashita
authors.forename: Naoki
authors.initials: N
authors.lastname: Inagaki
authors.forename: Kazuyuki
authors.initials: K
authors.lastname: Hirano
authors.forename: Mayumi
authors.initials: M
authors.lastname: Yamamoto
authors.forename: Yasutomi
authors.initials: Y
authors.lastname: Kinosada
authors.forename: Yoshinori
authors.initials: Y
authors.lastname: Itoh
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000932:Antiemetics / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D000970:Antineoplastic Agents / Q000009:adverse effects; D019540:Area Under Curve; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003907:Dexamethasone / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D004337:Drug Carriers / Q000737:chemistry*; D004355:Drug Stability; D004356:Drug Storage; D005079:Excipients / Q000737:chemistry*; D006207:Half-Life; D008297:Male; D009325:Nausea / Q000139:chemically induced / Q000517:prevention & control; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D014839:Vomiting / Q000139:chemically induced / Q000517:prevention & control
chemical_list: D000932:Antiemetics; D000970:Antineoplastic Agents; D004337:Drug Carriers; D005079:Excipients; D003907:Dexamethasone