Pharmacokinetics and Tissue Distribution of Nasal Spray of a Novel Muscarinic Receptor Blocker, 101BHG-D01, in Dogs and Rats-Reference-Cited by-同舟云学术

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

Published:2022-11 Issue:13 Volume:23 Page:1080-1088
ISSN:1389-2002
Container-title:Current Drug Metabolism
language:en
Short-container-title:CDM

Author:

Xie Yicheng¹²,Wang Yingshuo¹,Zhao Ziming³,Wei Hao³¹,Wu Lei¹,Jia Yongliang²,Shen Jian²,Li Yanyou⁴,Sun Peng⁵,Xie Qiangmin⁶,Chen Xiaoping⁴

Affiliation:

1. Department of Pulmonology, The Children’s Hospital, National Clinical Research Center For Child Health, Zhejiang University School of Medicine, Hangzhou, 310052, China

2. Key Laboratory of Respiratory Drugs Research, Zhejiang University School of Medicine, Hangzhou, 310058, China

3. Department of Pharmacy, Xuzhou Medical University, Xuzhou, 221004, China

4. Beijing Showby Pharmaceutical Co., LTD, Beijing, China

5. Innovation Research Institute of Chinese Medicine, Shandong University of Traditional Chinese Medicine, Jinan, 250355, China

6. Key Laboratory of Respiratory Drugs Research, Zhejiang University School of Medicine, Hangzhou, 310058, China

Abstract

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.

Funder

National Natural Science Foundation of China

National Key R&D Program of China

Zhejiang Province Public Welfare Technology Application Research Project

Publisher

Bentham Science Publishers Ltd.

Subject

Clinical Biochemistry,Pharmacology

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1. Pharmacokinetics, Mass Balance, Tissue Distribution and Metabolism of [14C]101BHG-D01, a Novel Muscarinic Receptor Antagonist, in Rats;Current Drug Metabolism;2023-11

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