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Article

Study of Bitespiramycin Distribution in Rats and Cerebrospinal Fluid of Patients by a Sensitive LC-MS/MS Method with Rapid Sample Preparation

1
School of Pharmacy, Southwest Medical University, Luzhou 646000, China
2
Shanghai Tonglian Pharmaceutical Co., Ltd., Shanghai 201611, China
3
Luzhou New Drug Safety Evaluation Research Center, Luzhou 646000, China
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2024, 29(5), 1037; https://doi.org/10.3390/molecules29051037
Submission received: 4 February 2024 / Revised: 23 February 2024 / Accepted: 25 February 2024 / Published: 28 February 2024
(This article belongs to the Special Issue Advances in Pharmaceutical Analytical Technologies)

Abstract

Bitespiramycin, has been shown to have a therapeutic effect against respiratory tract inflammation, including a potential effect against COVID-19. A current clinical trial in China showed that bitespiramycin was an effective treatment for severe pneumonia and intracranial infection. However, there is lack of an analytical method to elucidate the distribution of bitespiramycin. In this study, a highly sensitive, rapid and reliable UPLC–MS/MS method was developed to comprehensively characterize the bitespiramycin distribution in various bio-samples, which is significantly improved upon the published work. A rapid sample preparation method was developed by using n-butanol as the solvent to extract bitespiramycin from different bio-samples. The extract was then directly analyzed by UPLC–MS/MS coupled with an alkaline-resistant column after centrifugation which avoids the time-consuming concentration process under nitrogen and redissolution. The method was employed to accurately quantify bitespiramycin and its metabolites in rat plasma, tissues, and human cerebrospinal fluid. Notably, the presence of bitespiramycin and its metabolites was identified for the first time in various rat organs including brain, testis, bladder and prostate as well as in human cerebrospinal fluid. This newly developed approach shows great promise for drug distribution assays including other antibiotics and can help elucidate the ADME of bitespiramycin.
Keywords: bitespiramycin; distribution; LC–MS/MS; rat; human cerebrospinal fluid bitespiramycin; distribution; LC–MS/MS; rat; human cerebrospinal fluid
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MDPI and ACS Style

Zhang, Y.; Cao, J.; Su, J.; He, T.; Wang, Q.; Wei, F.; Guo, X.; Mei, Q.; Zeng, J. Study of Bitespiramycin Distribution in Rats and Cerebrospinal Fluid of Patients by a Sensitive LC-MS/MS Method with Rapid Sample Preparation. Molecules 2024, 29, 1037. https://doi.org/10.3390/molecules29051037

AMA Style

Zhang Y, Cao J, Su J, He T, Wang Q, Wei F, Guo X, Mei Q, Zeng J. Study of Bitespiramycin Distribution in Rats and Cerebrospinal Fluid of Patients by a Sensitive LC-MS/MS Method with Rapid Sample Preparation. Molecules. 2024; 29(5):1037. https://doi.org/10.3390/molecules29051037

Chicago/Turabian Style

Zhang, Yujie, Jingjie Cao, Jiahan Su, Tingting He, Qianru Wang, Feng Wei, Xin Guo, Qibing Mei, and Jing Zeng. 2024. "Study of Bitespiramycin Distribution in Rats and Cerebrospinal Fluid of Patients by a Sensitive LC-MS/MS Method with Rapid Sample Preparation" Molecules 29, no. 5: 1037. https://doi.org/10.3390/molecules29051037

APA Style

Zhang, Y., Cao, J., Su, J., He, T., Wang, Q., Wei, F., Guo, X., Mei, Q., & Zeng, J. (2024). Study of Bitespiramycin Distribution in Rats and Cerebrospinal Fluid of Patients by a Sensitive LC-MS/MS Method with Rapid Sample Preparation. Molecules, 29(5), 1037. https://doi.org/10.3390/molecules29051037

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