title: Preparation of bisoprolol fumarate nasal spray and its nasal delivery in rats.
abstract: The aim of the present work was to prepare a nasal spray of bisoprolol fumarate (BF). The Pharmacokinetics and relative bioavailability of the BF nasal formulation were evaluated in Wistar rats. The BF nasal spray after administration exhibited very fast absorption and higher plasma drug concentration. The maximum plasma concentration (C(max)) and the time to reach it (T(max)) were 409.5 ng/ml and 3.6 min for the BF nasal spray, 39.4 ng/ml and 26.7 min for the drug solution, respectively. The bioavailability of the BF nasal spray was greater than 1500.0%. Meantime, the effect of the BF nasal spray on nasal mucociliary movement was also studied with a toad palate model. The BF nasal preparation showed minor ciliotoxicity, but the adverse effect was temporary and reversible.
authors.affiliation: Department of Pharmaceutics, Affiliated Hospital, Inner Mongolia Medical University, Hohhot, PR China.
authors.forename: Gu
authors.initials: G
authors.lastname: Fugen
authors.affiliation: School of Pharmacy, Inner Mongolia Medical University, Hohhot, PR China.
authors.forename: Hao
authors.initials: H
authors.lastname: Duo
authors.affiliation: Department of Pharmaceutics, Affiliated Hospital, Inner Mongolia Medical University, Hohhot, PR China.
authors.forename: Meng
authors.initials: M
authors.lastname: Gendalai
authors.affiliation: Department of Pharmaceutics, Affiliated Hospital, Inner Mongolia Medical University, Hohhot, PR China.
authors.forename: Wu
authors.initials: W
authors.lastname: Chunzhi
authors.affiliation: Department of Pharmaceutics, Affiliated Hospital, Inner Mongolia Medical University, Hohhot, PR China.
authors.forename: Wang
authors.initials: W
authors.lastname: Yi
mesh_terms: D000281:Administration, Intranasal; D058671:Adrenergic beta-1 Receptor Antagonists / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D000336:Aerosols; D000818:Animals; D001682:Biological Availability; D017298:Bisoprolol / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D002025:Bufonidae; D002626:Chemistry, Pharmaceutical; D009079:Mucociliary Clearance / Q000187:drug effects; D009297:Nasal Mucosa / Q000187:drug effects / Q000378:metabolism; D017208:Rats, Wistar; D018570:Risk Assessment; D013678:Technology, Pharmaceutical / Q000379:methods; D018675:Toxicity Tests
chemical_list: D058671:Adrenergic beta-1 Receptor Antagonists; D000336:Aerosols; D017298:Bisoprolol