Preclinical Pharmacokinetics and Bioavailability of Oxypeucedanin in Rats after Single Intravenous and Oral Administration
Oxypeucedanin, a furanocoumarin extracted from many traditional Chinese herbal medicines, has a variety of pharmacological effects. However, the independent pharmacokinetic characteristics and bioavailability of this compound remains elusive. In this study, a rapid, sensitive, and selective method u...
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MDPI AG
2022-06-01
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| Online Access: | https://www.mdpi.com/1420-3049/27/11/3570 |
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| author | Ming-Cong Zheng Wen-Ting Tang Lu-Lu Yu Xun-Jia Qian Jie Ren Jie-Jia Li Wei-Wei Rong Jun-Xu Li Qing Zhu |
| author_facet | Ming-Cong Zheng Wen-Ting Tang Lu-Lu Yu Xun-Jia Qian Jie Ren Jie-Jia Li Wei-Wei Rong Jun-Xu Li Qing Zhu |
| author_sort | Ming-Cong Zheng |
| collection | DOAJ |
| description | Oxypeucedanin, a furanocoumarin extracted from many traditional Chinese herbal medicines, has a variety of pharmacological effects. However, the independent pharmacokinetic characteristics and bioavailability of this compound remains elusive. In this study, a rapid, sensitive, and selective method using ultra-high performance liquid chromatography–tandem mass spectrometry (UPLC/MS/MS) was developed for evaluating the intravenous and oral pharmacokinetics of oxypeucedanin. After intravenous administration of oxypeucedanin (2.5, 5, and 10 mg/kg), and intragastric administration of oxypeucedanin (20 mg/kg), blood samples were collected periodically from the tail vein. The plasma concentration-time curves were plotted, and the pharmacokinetic parameters were calculated using a non-compartmental model analysis. After intravenous administration of oxypeucedanin (single dosing at 2.5, 5, and 10 mg/kg) to rats, the pharmacokinetics fit the linear kinetics characteristics, which showed that some parameters including average elimination half-life (T<sub>1/2Z</sub> of 0.61~0.66 h), mean residence time (MRT of 0.62~0.80 h), apparent volume of distribution (V<sub>Z</sub> of 4.98~7.50 L/kg), and systemic clearance (CL<sub>Z</sub> of 5.64~8.55 L/kg/h) are dose-independent and the area under concentration-time curve (AUC) increased in a dose-proportional manner. Single oral administration of oxypeucedanin (20 mg/kg) showed poor and slow absorption with the mean time to reach the peak concentration (T<sub>max</sub>) of 3.38 h, MRT of 5.86 h, T<sub>1/2Z</sub> of 2.94 h, and a mean absolute bioavailability of 10.26% in rats. These results provide critical information for a better understanding of the pharmacological effect of oxypeucedanin, which will facilitate its research and development. |
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| language | English |
| last_indexed | 2024-03-10T01:03:22Z |
| publishDate | 2022-06-01 |
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| spelling | doaj.art-28cdf669548641a2a32547c4af2965ff2023-11-23T14:30:55ZengMDPI AGMolecules1420-30492022-06-012711357010.3390/molecules27113570Preclinical Pharmacokinetics and Bioavailability of Oxypeucedanin in Rats after Single Intravenous and Oral AdministrationMing-Cong Zheng0Wen-Ting Tang1Lu-Lu Yu2Xun-Jia Qian3Jie Ren4Jie-Jia Li5Wei-Wei Rong6Jun-Xu Li7Qing Zhu8School of Pharmacy, Nantong University, Nantong 226001, ChinaSchool of Pharmacy, Nantong University, Nantong 226001, ChinaSchool of Pharmacy, Nantong University, Nantong 226001, ChinaSchool of Pharmacy, Nantong University, Nantong 226001, ChinaSchool of Pharmacy, Nantong University, Nantong 226001, ChinaState Key Laboratory for the Quality Research of Chinese Medicine, School of Pharmacy, Macau University of Science and Technology, Macau 999078, ChinaSchool of Pharmacy, Nantong University, Nantong 226001, ChinaSchool of Pharmacy, Nantong University, Nantong 226001, ChinaSchool of Pharmacy, Nantong University, Nantong 226001, ChinaOxypeucedanin, a furanocoumarin extracted from many traditional Chinese herbal medicines, has a variety of pharmacological effects. However, the independent pharmacokinetic characteristics and bioavailability of this compound remains elusive. In this study, a rapid, sensitive, and selective method using ultra-high performance liquid chromatography–tandem mass spectrometry (UPLC/MS/MS) was developed for evaluating the intravenous and oral pharmacokinetics of oxypeucedanin. After intravenous administration of oxypeucedanin (2.5, 5, and 10 mg/kg), and intragastric administration of oxypeucedanin (20 mg/kg), blood samples were collected periodically from the tail vein. The plasma concentration-time curves were plotted, and the pharmacokinetic parameters were calculated using a non-compartmental model analysis. After intravenous administration of oxypeucedanin (single dosing at 2.5, 5, and 10 mg/kg) to rats, the pharmacokinetics fit the linear kinetics characteristics, which showed that some parameters including average elimination half-life (T<sub>1/2Z</sub> of 0.61~0.66 h), mean residence time (MRT of 0.62~0.80 h), apparent volume of distribution (V<sub>Z</sub> of 4.98~7.50 L/kg), and systemic clearance (CL<sub>Z</sub> of 5.64~8.55 L/kg/h) are dose-independent and the area under concentration-time curve (AUC) increased in a dose-proportional manner. Single oral administration of oxypeucedanin (20 mg/kg) showed poor and slow absorption with the mean time to reach the peak concentration (T<sub>max</sub>) of 3.38 h, MRT of 5.86 h, T<sub>1/2Z</sub> of 2.94 h, and a mean absolute bioavailability of 10.26% in rats. These results provide critical information for a better understanding of the pharmacological effect of oxypeucedanin, which will facilitate its research and development.https://www.mdpi.com/1420-3049/27/11/3570oxypeucedaninpharmacokineticsbioavailabilityUPLC/MS/MSrats |
| spellingShingle | Ming-Cong Zheng Wen-Ting Tang Lu-Lu Yu Xun-Jia Qian Jie Ren Jie-Jia Li Wei-Wei Rong Jun-Xu Li Qing Zhu Preclinical Pharmacokinetics and Bioavailability of Oxypeucedanin in Rats after Single Intravenous and Oral Administration Molecules oxypeucedanin pharmacokinetics bioavailability UPLC/MS/MS rats |
| title | Preclinical Pharmacokinetics and Bioavailability of Oxypeucedanin in Rats after Single Intravenous and Oral Administration |
| title_full | Preclinical Pharmacokinetics and Bioavailability of Oxypeucedanin in Rats after Single Intravenous and Oral Administration |
| title_fullStr | Preclinical Pharmacokinetics and Bioavailability of Oxypeucedanin in Rats after Single Intravenous and Oral Administration |
| title_full_unstemmed | Preclinical Pharmacokinetics and Bioavailability of Oxypeucedanin in Rats after Single Intravenous and Oral Administration |
| title_short | Preclinical Pharmacokinetics and Bioavailability of Oxypeucedanin in Rats after Single Intravenous and Oral Administration |
| title_sort | preclinical pharmacokinetics and bioavailability of oxypeucedanin in rats after single intravenous and oral administration |
| topic | oxypeucedanin pharmacokinetics bioavailability UPLC/MS/MS rats |
| url | https://www.mdpi.com/1420-3049/27/11/3570 |
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