Study on the pharmacokinetics, tissue distribution and excretion of laurolitsine from Litsea glutinosa in Sprague-Dawley rats
Context Laurolitsine is an aporphine alkaloid and exhibits potent antihyperglycemic and antihyperlipidemic effects in ob/ob mice. Objective To investigate the pharmacokinetics, tissue distribution and excretion of laurolitsine. Materials and methods A LC-MS/MS method was established and validated to...
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2021-01-01
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| Series: | Pharmaceutical Biology |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/13880209.2021.1944221 |
| _version_ | 1818654920161624064 |
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| author | Yin-Feng Tan Rui-Qi Wang Wen-Ting Wang Ying Wu Ning Ma Wei-Ying Lu Yong Zhang Xiao-Po Zhang |
| author_facet | Yin-Feng Tan Rui-Qi Wang Wen-Ting Wang Ying Wu Ning Ma Wei-Ying Lu Yong Zhang Xiao-Po Zhang |
| author_sort | Yin-Feng Tan |
| collection | DOAJ |
| description | Context Laurolitsine is an aporphine alkaloid and exhibits potent antihyperglycemic and antihyperlipidemic effects in ob/ob mice. Objective To investigate the pharmacokinetics, tissue distribution and excretion of laurolitsine. Materials and methods A LC-MS/MS method was established and validated to determine laurolitsine concentrations in the biological matrix of rats (plasma, tissue homogenate, urine and faeces). 10 Sprague-Dawley (SD) rats were used for plasma exposure study: 5 rats were injected with 2.0 mg/kg of laurolitsine via the tail vein, and the other 5 rats were administered laurolitsine (10.0 mg/kg) by gavage. 25 SD rats used for tissue distribution study and 5 SD rats for urine and faeces excretion study: rats administered laurolitsine (10.0 mg/kg) by gavage. After administered, serial blood, tissue, urine and faeces were collected. Analytical quantification was performed by a previous LC-MS/MS method. The pharmacokinetics, bioavailability, tissue distribution and excretion of laurolitsine were described. Results The pharmacokinetic parameters of oral and intravenous administration with Tmax were 0.47 and 0.083 h, t1/2 were 3.73 and 1.67 h, respectively. Oral bioavailability was as low as 18.17%. Laurolitsine was found at a high concentration in the gastrointestinal tract, liver, lungs and kidneys (26 015.33, 905.12, 442.32 and 214.99 ng/g at 0.5 h, respectively) and low excretion to parent laurolitsine in urine and faeces (0.03 and 1.20% in 36 h, respectively). Conclusions This study established a simple, rapid and accurate LC-MS/MS method to determine laurolitsine in different rat samples and successful application in a pharmacokinetic study. |
| first_indexed | 2024-12-17T03:01:27Z |
| format | Article |
| id | doaj.art-b8e4a5bb56d64d64991e19619c2a9e4d |
| institution | Directory Open Access Journal |
| issn | 1388-0209 1744-5116 |
| language | English |
| last_indexed | 2024-12-17T03:01:27Z |
| publishDate | 2021-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Pharmaceutical Biology |
| spelling | doaj.art-b8e4a5bb56d64d64991e19619c2a9e4d2022-12-21T22:06:04ZengTaylor & Francis GroupPharmaceutical Biology1388-02091744-51162021-01-0159188489210.1080/13880209.2021.19442211944221Study on the pharmacokinetics, tissue distribution and excretion of laurolitsine from Litsea glutinosa in Sprague-Dawley ratsYin-Feng Tan0Rui-Qi Wang1Wen-Ting Wang2Ying Wu3Ning Ma4Wei-Ying Lu5Yong Zhang6Xiao-Po Zhang7Key Laboratory of Tropical Translational Medicine of Ministry of Education, Hainan Key Laboratory for Research and Development of Tropical Herbs, School of Pharmacy, Hainan Medical UniversityKey Laboratory of Tropical Translational Medicine of Ministry of Education, Hainan Key Laboratory for Research and Development of Tropical Herbs, School of Pharmacy, Hainan Medical UniversityReproductive Medical Center, Hainan Women and Children’s Medical CenterReproductive Medical Center, Hainan Women and Children’s Medical CenterReproductive Medical Center, Hainan Women and Children’s Medical CenterReproductive Medical Center, Hainan Women and Children’s Medical CenterDepartment of Pharmacology, Hainan Medical UniversityKey Laboratory of Tropical Translational Medicine of Ministry of Education, Hainan Key Laboratory for Research and Development of Tropical Herbs, School of Pharmacy, Hainan Medical UniversityContext Laurolitsine is an aporphine alkaloid and exhibits potent antihyperglycemic and antihyperlipidemic effects in ob/ob mice. Objective To investigate the pharmacokinetics, tissue distribution and excretion of laurolitsine. Materials and methods A LC-MS/MS method was established and validated to determine laurolitsine concentrations in the biological matrix of rats (plasma, tissue homogenate, urine and faeces). 10 Sprague-Dawley (SD) rats were used for plasma exposure study: 5 rats were injected with 2.0 mg/kg of laurolitsine via the tail vein, and the other 5 rats were administered laurolitsine (10.0 mg/kg) by gavage. 25 SD rats used for tissue distribution study and 5 SD rats for urine and faeces excretion study: rats administered laurolitsine (10.0 mg/kg) by gavage. After administered, serial blood, tissue, urine and faeces were collected. Analytical quantification was performed by a previous LC-MS/MS method. The pharmacokinetics, bioavailability, tissue distribution and excretion of laurolitsine were described. Results The pharmacokinetic parameters of oral and intravenous administration with Tmax were 0.47 and 0.083 h, t1/2 were 3.73 and 1.67 h, respectively. Oral bioavailability was as low as 18.17%. Laurolitsine was found at a high concentration in the gastrointestinal tract, liver, lungs and kidneys (26 015.33, 905.12, 442.32 and 214.99 ng/g at 0.5 h, respectively) and low excretion to parent laurolitsine in urine and faeces (0.03 and 1.20% in 36 h, respectively). Conclusions This study established a simple, rapid and accurate LC-MS/MS method to determine laurolitsine in different rat samples and successful application in a pharmacokinetic study.http://dx.doi.org/10.1080/13880209.2021.1944221aporphine alkaloidlc-ms/ms |
| spellingShingle | Yin-Feng Tan Rui-Qi Wang Wen-Ting Wang Ying Wu Ning Ma Wei-Ying Lu Yong Zhang Xiao-Po Zhang Study on the pharmacokinetics, tissue distribution and excretion of laurolitsine from Litsea glutinosa in Sprague-Dawley rats Pharmaceutical Biology aporphine alkaloid lc-ms/ms |
| title | Study on the pharmacokinetics, tissue distribution and excretion of laurolitsine from Litsea glutinosa in Sprague-Dawley rats |
| title_full | Study on the pharmacokinetics, tissue distribution and excretion of laurolitsine from Litsea glutinosa in Sprague-Dawley rats |
| title_fullStr | Study on the pharmacokinetics, tissue distribution and excretion of laurolitsine from Litsea glutinosa in Sprague-Dawley rats |
| title_full_unstemmed | Study on the pharmacokinetics, tissue distribution and excretion of laurolitsine from Litsea glutinosa in Sprague-Dawley rats |
| title_short | Study on the pharmacokinetics, tissue distribution and excretion of laurolitsine from Litsea glutinosa in Sprague-Dawley rats |
| title_sort | study on the pharmacokinetics tissue distribution and excretion of laurolitsine from litsea glutinosa in sprague dawley rats |
| topic | aporphine alkaloid lc-ms/ms |
| url | http://dx.doi.org/10.1080/13880209.2021.1944221 |
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