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

• Published in: Current drug metabolism Vol. 23; no. 13; p. 1080
• Main Authors: Wei, Hao, Wu, Lei, Jia, Yongliang, Shen, Jian, Li, Yanyou, Sun, Peng, Xie, Qiangmin, Chen, Xiaoping, Xie, Yicheng, Wang, Yingshuo, Zhao, Ziming
• Format: Journal Article
• Language: English
• Published: Netherlands 01.11.2022
• Subjects: M3 receptor blocker; pharmacokinetics; cholinergic receptors; Parkinson's disease; nasal spray; tissue distribution
• ISSN: 1875-5453
• DOI: 10.2174/1389200224666221201123254

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