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

BACKGROUND: 101BHG-D01 is a novel selective anti-muscarinic (M) 3 receptor-blocking drug. 101BHG-D01 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 m...

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Detalles Bibliográficos
Autores principales: Wei, Hao, Wu, Lei, Jia, Yongliang, Shen, Jian, Li, Yanyou, Sun, Peng, Xie, Qiangmin, Chen, Xiaoping, Xie, Yicheng, Wang, Yingshuo, Zhao, Ziming
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Bentham Science Publishers 2022
Materias:
Drug Design and Discovery, Drug Metabolism
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10186379/
https://www.ncbi.nlm.nih.gov/pubmed/36464876
http://dx.doi.org/10.2174/1389200224666221201123254
Descripción
Sumario:BACKGROUND: 101BHG-D01 is a novel selective anti-muscarinic (M) 3 receptor-blocking drug. 101BHG-D01 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 HPLC-MS/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 101BHG-D01 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.

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