{"title":"液相色谱-质谱联用法测定血浆中fostemsavir含量的验证","authors":"Siddhartha Lolla , Kumar Shiva Gubbiyappa , Shankar Cheruku , D.V.R.N. Bhikshapathi","doi":"10.1016/j.vascn.2023.107254","DOIUrl":null,"url":null,"abstract":"<div><h3>Background</h3><p>A novel, sensitive and specific LC-MS/MS technique was developed and validated for the quantification of fostemsavir in human plasma and its pharmacokinetic application in rabbits.</p></div><div><h3>Methods</h3><p>Chromatographic separation of the fostemsavir and fosamprenavir (internal standard) were achieved on Zorbax C18 (50 mm × 2 mm × 5 μm) column with 0.80 mL/min flow rate and coupled with API6000 triple quadrupole MS in multi reaction monitoring mode by applying mass transitions <em>m</em>/<em>z</em> 584.16/105.03 for fostemsavir and m/z 586.19/57.07 for the internal standard.</p></div><div><h3>Results</h3><p>The calibration curve exhibited linearity in concentration range of 58.5–2340.0 ng/mL for fostemsavir. The LLOQ was 58.5 ng/mL. The validated LC–MS/MS process was effectively applied for the analysis of plasma in healthy rabbits for determinations of Fostemsavir. From the pharmacokinetic data, the mean of C<sub>max</sub> and T<sub>max</sub> were 198.19 ± 5.85 ng/mL and 2.42 ± 0.13, respectively. Plasma concentration reduced with t<sub>1/2</sub> of 7.02 ± 0.14. AUC<sub>0→Last</sub> value obtained was 2374.87 ± 29.75 ng. h/ml, respectively.</p></div><div><h3>Conclusion</h3><p>In summary, the developed method has been successfully validated and pharmacokinetic parameters were demonstrated after oral administration of Fostemsavir to healthy rabbits.</p></div>","PeriodicalId":16767,"journal":{"name":"Journal of pharmacological and toxicological methods","volume":null,"pages":null},"PeriodicalIF":1.3000,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"1","resultStr":"{\"title\":\"Validation of an LC–MS/MS method for quantitation of fostemsavir in plasma\",\"authors\":\"Siddhartha Lolla , Kumar Shiva Gubbiyappa , Shankar Cheruku , D.V.R.N. Bhikshapathi\",\"doi\":\"10.1016/j.vascn.2023.107254\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Background</h3><p>A novel, sensitive and specific LC-MS/MS technique was developed and validated for the quantification of fostemsavir in human plasma and its pharmacokinetic application in rabbits.</p></div><div><h3>Methods</h3><p>Chromatographic separation of the fostemsavir and fosamprenavir (internal standard) were achieved on Zorbax C18 (50 mm × 2 mm × 5 μm) column with 0.80 mL/min flow rate and coupled with API6000 triple quadrupole MS in multi reaction monitoring mode by applying mass transitions <em>m</em>/<em>z</em> 584.16/105.03 for fostemsavir and m/z 586.19/57.07 for the internal standard.</p></div><div><h3>Results</h3><p>The calibration curve exhibited linearity in concentration range of 58.5–2340.0 ng/mL for fostemsavir. The LLOQ was 58.5 ng/mL. The validated LC–MS/MS process was effectively applied for the analysis of plasma in healthy rabbits for determinations of Fostemsavir. From the pharmacokinetic data, the mean of C<sub>max</sub> and T<sub>max</sub> were 198.19 ± 5.85 ng/mL and 2.42 ± 0.13, respectively. Plasma concentration reduced with t<sub>1/2</sub> of 7.02 ± 0.14. AUC<sub>0→Last</sub> value obtained was 2374.87 ± 29.75 ng. h/ml, respectively.</p></div><div><h3>Conclusion</h3><p>In summary, the developed method has been successfully validated and pharmacokinetic parameters were demonstrated after oral administration of Fostemsavir to healthy rabbits.</p></div>\",\"PeriodicalId\":16767,\"journal\":{\"name\":\"Journal of pharmacological and toxicological methods\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":1.3000,\"publicationDate\":\"2023-03-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"1\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of pharmacological and toxicological methods\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S1056871923000059\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of pharmacological and toxicological methods","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1056871923000059","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Validation of an LC–MS/MS method for quantitation of fostemsavir in plasma
Background
A novel, sensitive and specific LC-MS/MS technique was developed and validated for the quantification of fostemsavir in human plasma and its pharmacokinetic application in rabbits.
Methods
Chromatographic separation of the fostemsavir and fosamprenavir (internal standard) were achieved on Zorbax C18 (50 mm × 2 mm × 5 μm) column with 0.80 mL/min flow rate and coupled with API6000 triple quadrupole MS in multi reaction monitoring mode by applying mass transitions m/z 584.16/105.03 for fostemsavir and m/z 586.19/57.07 for the internal standard.
Results
The calibration curve exhibited linearity in concentration range of 58.5–2340.0 ng/mL for fostemsavir. The LLOQ was 58.5 ng/mL. The validated LC–MS/MS process was effectively applied for the analysis of plasma in healthy rabbits for determinations of Fostemsavir. From the pharmacokinetic data, the mean of Cmax and Tmax were 198.19 ± 5.85 ng/mL and 2.42 ± 0.13, respectively. Plasma concentration reduced with t1/2 of 7.02 ± 0.14. AUC0→Last value obtained was 2374.87 ± 29.75 ng. h/ml, respectively.
Conclusion
In summary, the developed method has been successfully validated and pharmacokinetic parameters were demonstrated after oral administration of Fostemsavir to healthy rabbits.
期刊介绍：
Journal of Pharmacological and Toxicological Methods publishes original articles on current methods of investigation used in pharmacology and toxicology. Pharmacology and toxicology are defined in the broadest sense, referring to actions of drugs and chemicals on all living systems. With its international editorial board and noted contributors, Journal of Pharmacological and Toxicological Methods is the leading journal devoted exclusively to experimental procedures used by pharmacologists and toxicologists.
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