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Preparation of bisoprolol fumarate nasal spray and its nasal delivery in rats.

Authors: Gu, Fugen; Hao, Duo; Meng, Gendalai; Wu, Chunzhi; Wang, Yi;

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.

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Keywords

Aerosols, Chemistry, Pharmaceutical, Biological Availability, Adrenergic beta-1 Receptor Antagonists, Risk Assessment, Bufonidae, Nasal Mucosa, Mucociliary Clearance, Toxicity Tests, Animals, Bisoprolol, Technology, Pharmaceutical, Rats, Wistar, Administration, Intranasal

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Powered by OpenAIRE graph
Found an issue? Give us feedback
selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
2
Average
Average
Average
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