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Current Drug Metabolism


ISSN (Print): 1389-2002
ISSN (Online): 1875-5453

Research Article

Pharmacokinetics and Tissue Distribution of Nasal Spray of a Novel Muscarinic Receptor Blocker, 101BHG-D01, in Dogs and Rats

Author(s): Hao Wei, Lei Wu, Yongliang Jia, Jian Shen, Yanyou Li, Peng Sun, Qiangmin Xie, Xiaoping Chen, Yicheng Xie*, Yingshuo Wang* and Ziming Zhao*

Volume 23, Issue 13, 2022

Published on: 21 December, 2022

Page: [1080 - 1088] Pages: 9

DOI: 10.2174/1389200224666221201123254

open access plus


Background: 101BHG-D01 is a novel selective anti-muscarinic (M) 3 receptor-blocking drug. 101BHGD01 nasal spray is intended to be used to relieve sneezing and runny nose symptoms caused by allergic rhinitis.

Methods: In this study, we examined the plasma pharmacokinetics, tissue distribution, and major excretion mode of 101BHG-D01 in Beagle dogs and rats following nasal spray and intranasal administration, respectively, using HPLCMS/ MS.

Results/Discussion: We found that the pharmacokinetics of 101BHG-D01 was linear in dogs. 101BHG-D01 entered the bloodstream rapidly following nasal spray. Its plasma half-life was approximately 6 h and resided at least 24 h in the body. Moreover, 101BHG-D01 retained a significant amount in the nasal cavity. Finally, we found that 101BHGD01 was eliminated mainly in the form of stools in rats.

Conclusion: In conclusion, we provided pertinent reference information regarding the design and optimization of drug delivery regimens for clinical trials.

Keywords: M3 receptor blocker, nasal spray, pharmacokinetics, tissue distribution, cholinergic receptors, Parkinson's disease.

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