Bioequivalence evaluation and food effect assessment of Lisinopril/amlodipine tablets in healthy Chinese subjects under fasting and fed conditions
Abstract Purpose The combination of lisinopril and amlodipine has a marked additional effect on blood pressure and fewer side effects than individual monotherapy. This study was conducted to compare the pharmacokinetic parameters and evaluate the bioequivalence between two Lisinopril/amlodipine tabl...
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| Format: | Article |
| Language: | English |
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BMC
2022-07-01
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| Series: | BMC Pharmacology and Toxicology |
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| Online Access: | https://doi.org/10.1186/s40360-022-00590-6 |
| _version_ | 1828760934698450944 |
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| author | Ting Li Yan-ping Liu Shu-qin Liu Ping Shi Xin Jiang Ye Tao Xiao-meng Gao Ya-ping Ma Yu Cao |
| author_facet | Ting Li Yan-ping Liu Shu-qin Liu Ping Shi Xin Jiang Ye Tao Xiao-meng Gao Ya-ping Ma Yu Cao |
| author_sort | Ting Li |
| collection | DOAJ |
| description | Abstract Purpose The combination of lisinopril and amlodipine has a marked additional effect on blood pressure and fewer side effects than individual monotherapy. This study was conducted to compare the pharmacokinetic parameters and evaluate the bioequivalence between two Lisinopril/amlodipine tablets in healthy Chinese subjects. Methods A single center, randomized, open-label, single-dose, two-period crossover bioequivalence study was designed in healthy Chinese subjects under both fasting and fed conditions. Blood samples were collected before drug administration and at 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 24, 36, 48, 72, 96, 144, 168 h after administration. Liquid chromatography-tandem mass spectrometry (LC–MS/MS) was applied to determine the plasma concentration of lisinopril and amlodipine. Maximum concentration (Cmax) and area under the concentration–time curve (AUC) were used to evaluate bioequivalence. Adverse events were recorded. Results Ninety-two healthy subjects were enrolled, and 75 completed the study. The 90% confidence intervals (CIs) of the ratio of geometric means (GMRs) of Cmax, AUC0-t, and AUC0-∞ of lisinopril and amlodipine under both fasting and fed conditions fell within the conventional bioequivalence criteria of 0.80–1.25. A high-fat meal appeared to decrease the Cmax and AUC of lisinopril. No severe adverse events were observed. Conclusion The trial demonstrated that the test and the reference lisinopril/amlodipine tablets were bioequivalent and well tolerated in Chinese people under fasting and fed conditions. Trial registration Clinical Trails.gov identifier, NCT04885660 (retrospectively registered in 13/05/ 2021). |
| first_indexed | 2024-12-11T01:22:20Z |
| format | Article |
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| institution | Directory Open Access Journal |
| issn | 2050-6511 |
| language | English |
| last_indexed | 2024-12-11T01:22:20Z |
| publishDate | 2022-07-01 |
| publisher | BMC |
| record_format | Article |
| series | BMC Pharmacology and Toxicology |
| spelling | doaj.art-b400df77e977430e8e99dd48f1e4c3502022-12-22T01:25:40ZengBMCBMC Pharmacology and Toxicology2050-65112022-07-0123111110.1186/s40360-022-00590-6Bioequivalence evaluation and food effect assessment of Lisinopril/amlodipine tablets in healthy Chinese subjects under fasting and fed conditionsTing Li0Yan-ping Liu1Shu-qin Liu2Ping Shi3Xin Jiang4Ye Tao5Xiao-meng Gao6Ya-ping Ma7Yu Cao8Phase I Clinical Research Center, The Affiliated Hospital of Qingdao UniversityPhase I Clinical Research Center, The Affiliated Hospital of Qingdao UniversityPhase I Clinical Research Center, The Affiliated Hospital of Qingdao UniversityPhase I Clinical Research Center, The Affiliated Hospital of Qingdao UniversityPhase I Clinical Research Center, The Affiliated Hospital of Qingdao UniversityPhase I Clinical Research Center, The Affiliated Hospital of Qingdao UniversityPhase I Clinical Research Center, The Affiliated Hospital of Qingdao UniversityPhase I Clinical Research Center, The Affiliated Hospital of Qingdao UniversityPhase I Clinical Research Center, The Affiliated Hospital of Qingdao UniversityAbstract Purpose The combination of lisinopril and amlodipine has a marked additional effect on blood pressure and fewer side effects than individual monotherapy. This study was conducted to compare the pharmacokinetic parameters and evaluate the bioequivalence between two Lisinopril/amlodipine tablets in healthy Chinese subjects. Methods A single center, randomized, open-label, single-dose, two-period crossover bioequivalence study was designed in healthy Chinese subjects under both fasting and fed conditions. Blood samples were collected before drug administration and at 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 24, 36, 48, 72, 96, 144, 168 h after administration. Liquid chromatography-tandem mass spectrometry (LC–MS/MS) was applied to determine the plasma concentration of lisinopril and amlodipine. Maximum concentration (Cmax) and area under the concentration–time curve (AUC) were used to evaluate bioequivalence. Adverse events were recorded. Results Ninety-two healthy subjects were enrolled, and 75 completed the study. The 90% confidence intervals (CIs) of the ratio of geometric means (GMRs) of Cmax, AUC0-t, and AUC0-∞ of lisinopril and amlodipine under both fasting and fed conditions fell within the conventional bioequivalence criteria of 0.80–1.25. A high-fat meal appeared to decrease the Cmax and AUC of lisinopril. No severe adverse events were observed. Conclusion The trial demonstrated that the test and the reference lisinopril/amlodipine tablets were bioequivalent and well tolerated in Chinese people under fasting and fed conditions. Trial registration Clinical Trails.gov identifier, NCT04885660 (retrospectively registered in 13/05/ 2021).https://doi.org/10.1186/s40360-022-00590-6LisinoprilAmlodipineBioequivalencePharmacokineticFood effect |
| spellingShingle | Ting Li Yan-ping Liu Shu-qin Liu Ping Shi Xin Jiang Ye Tao Xiao-meng Gao Ya-ping Ma Yu Cao Bioequivalence evaluation and food effect assessment of Lisinopril/amlodipine tablets in healthy Chinese subjects under fasting and fed conditions BMC Pharmacology and Toxicology Lisinopril Amlodipine Bioequivalence Pharmacokinetic Food effect |
| title | Bioequivalence evaluation and food effect assessment of Lisinopril/amlodipine tablets in healthy Chinese subjects under fasting and fed conditions |
| title_full | Bioequivalence evaluation and food effect assessment of Lisinopril/amlodipine tablets in healthy Chinese subjects under fasting and fed conditions |
| title_fullStr | Bioequivalence evaluation and food effect assessment of Lisinopril/amlodipine tablets in healthy Chinese subjects under fasting and fed conditions |
| title_full_unstemmed | Bioequivalence evaluation and food effect assessment of Lisinopril/amlodipine tablets in healthy Chinese subjects under fasting and fed conditions |
| title_short | Bioequivalence evaluation and food effect assessment of Lisinopril/amlodipine tablets in healthy Chinese subjects under fasting and fed conditions |
| title_sort | bioequivalence evaluation and food effect assessment of lisinopril amlodipine tablets in healthy chinese subjects under fasting and fed conditions |
| topic | Lisinopril Amlodipine Bioequivalence Pharmacokinetic Food effect |
| url | https://doi.org/10.1186/s40360-022-00590-6 |
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