Pharmacokinetic study of ranolazine in Chinese healthy volunteers
Objective To evaluate pharmacokinetics after administration of ranolazine sustained release tablets at a single and multiple dose to healthy Chinese volunteers. Methods A self-controlled trial design was used. In the single-time group, 10 healthy volunteers, half male and half female, were included,...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | zho |
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Editorial Office of Journal of Third Military Medical University
2019-01-01
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| Series: | Di-san junyi daxue xuebao |
| Subjects: | |
| Online Access: | http://aammt.tmmu.edu.cn/Upload/rhtml/201808200.htm |
| _version_ | 1818902594475524096 |
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| author | YU Mingjie XIANG Rongfeng XIONG Lirong LI Xiaoyu DAI Qing CHEN Yongchuan |
| author_facet | YU Mingjie XIANG Rongfeng XIONG Lirong LI Xiaoyu DAI Qing CHEN Yongchuan |
| author_sort | YU Mingjie |
| collection | DOAJ |
| description | Objective To evaluate pharmacokinetics after administration of ranolazine sustained release tablets at a single and multiple dose to healthy Chinese volunteers. Methods A self-controlled trial design was used. In the single-time group, 10 healthy volunteers, half male and half female, were included, and 500, 1 000 and 1 500 mg ranolazine sustained-release tablets were taken sequentially in 3 cycles. For the multiple-dose group, 10 individuals of both sexes were enrolled, and 500 and 1 000 mg ranolazine sustained-release tablets were sequentially administered in 2 cycles. The concentration of ranolazine in plasma samples was determined by LC-MS-MS, and the main pharmacokinetic parameters were calculated. Results The linear concentration of ranolazine in plasma ranged from 40 to 4 000 μg/L, and the LLOQ was 40 μg/L. The intra-assay and inter-assay precision were less than 15%. After single dose, the main parameters in doses 500, 1 000, 1 500 mg were Cmax: 774±157, 1 818±554 and 2 762±1 099 μg/L, respectively; tmax: 4.9±1.8, 4.9±2.6 and 4.9±1.5 h, respectively; t1/2z: 8.2±6.8, 10.3±8.7 and 9.7±12.0 h, respectively; AUC0-t: 8 470±2 765, 20 936±6 957 and 32 554±17 780 μg·h/L, respectively. After multiple dose, the main parameters in doses 500, 1 000 mg were Cmaxss: 1 826±904 and 3 635±620 μg/L; Cminss: 1 022±3 and 2 282±163 μg/L; Cav: 1 253±634 and 2 615±536 μg/L; AUC0-t: 22 452±12 359 and 53 232±15 909 μg·h/L; MRT0-t: 8.7±2.3 and 10.6±2.6; RAUC: 3.11±2.60 and 2.86±1.54. Conclusion In a single administration trial, Cmax and AUC are increased proportionally to the dose, and there is a good linear relationship between the three doses. Multiple dose tests have found that ranolazine has a certain accumulation in the body. |
| first_indexed | 2024-12-19T20:38:08Z |
| format | Article |
| id | doaj.art-cb68139a02fd4c26aacb7315353ce4bc |
| institution | Directory Open Access Journal |
| issn | 1000-5404 |
| language | zho |
| last_indexed | 2024-12-19T20:38:08Z |
| publishDate | 2019-01-01 |
| publisher | Editorial Office of Journal of Third Military Medical University |
| record_format | Article |
| series | Di-san junyi daxue xuebao |
| spelling | doaj.art-cb68139a02fd4c26aacb7315353ce4bc2022-12-21T20:06:28ZzhoEditorial Office of Journal of Third Military Medical UniversityDi-san junyi daxue xuebao1000-54042019-01-0141217718210.16016/j.1000-5404.201808200Pharmacokinetic study of ranolazine in Chinese healthy volunteersYU Mingjie0XIANG Rongfeng1XIONG Lirong2LI Xiaoyu3DAI Qing4CHEN Yongchuan5Department of Pharmacy, First Affiliated Hospital, Army Medical University(Third Military Medical University), Chongqing, 400038Department of Pharmacy, First Affiliated Hospital, Army Medical University(Third Military Medical University), Chongqing, 400038Department of Pharmacy, First Affiliated Hospital, Army Medical University(Third Military Medical University), Chongqing, 400038Department of Pharmacy, Handan Branch of No. 980 Hospital of PLA, Handan, Hebei Province, 056001, China Department of Pharmacy, First Affiliated Hospital, Army Medical University(Third Military Medical University), Chongqing, 400038Department of Pharmacy, First Affiliated Hospital, Army Medical University(Third Military Medical University), Chongqing, 400038Objective To evaluate pharmacokinetics after administration of ranolazine sustained release tablets at a single and multiple dose to healthy Chinese volunteers. Methods A self-controlled trial design was used. In the single-time group, 10 healthy volunteers, half male and half female, were included, and 500, 1 000 and 1 500 mg ranolazine sustained-release tablets were taken sequentially in 3 cycles. For the multiple-dose group, 10 individuals of both sexes were enrolled, and 500 and 1 000 mg ranolazine sustained-release tablets were sequentially administered in 2 cycles. The concentration of ranolazine in plasma samples was determined by LC-MS-MS, and the main pharmacokinetic parameters were calculated. Results The linear concentration of ranolazine in plasma ranged from 40 to 4 000 μg/L, and the LLOQ was 40 μg/L. The intra-assay and inter-assay precision were less than 15%. After single dose, the main parameters in doses 500, 1 000, 1 500 mg were Cmax: 774±157, 1 818±554 and 2 762±1 099 μg/L, respectively; tmax: 4.9±1.8, 4.9±2.6 and 4.9±1.5 h, respectively; t1/2z: 8.2±6.8, 10.3±8.7 and 9.7±12.0 h, respectively; AUC0-t: 8 470±2 765, 20 936±6 957 and 32 554±17 780 μg·h/L, respectively. After multiple dose, the main parameters in doses 500, 1 000 mg were Cmaxss: 1 826±904 and 3 635±620 μg/L; Cminss: 1 022±3 and 2 282±163 μg/L; Cav: 1 253±634 and 2 615±536 μg/L; AUC0-t: 22 452±12 359 and 53 232±15 909 μg·h/L; MRT0-t: 8.7±2.3 and 10.6±2.6; RAUC: 3.11±2.60 and 2.86±1.54. Conclusion In a single administration trial, Cmax and AUC are increased proportionally to the dose, and there is a good linear relationship between the three doses. Multiple dose tests have found that ranolazine has a certain accumulation in the body.http://aammt.tmmu.edu.cn/Upload/rhtml/201808200.htmranolazinesustained release tabletshplc-ms-mspharmacokinetics |
| spellingShingle | YU Mingjie XIANG Rongfeng XIONG Lirong LI Xiaoyu DAI Qing CHEN Yongchuan Pharmacokinetic study of ranolazine in Chinese healthy volunteers Di-san junyi daxue xuebao ranolazine sustained release tablets hplc-ms-ms pharmacokinetics |
| title | Pharmacokinetic study of ranolazine in Chinese healthy volunteers |
| title_full | Pharmacokinetic study of ranolazine in Chinese healthy volunteers |
| title_fullStr | Pharmacokinetic study of ranolazine in Chinese healthy volunteers |
| title_full_unstemmed | Pharmacokinetic study of ranolazine in Chinese healthy volunteers |
| title_short | Pharmacokinetic study of ranolazine in Chinese healthy volunteers |
| title_sort | pharmacokinetic study of ranolazine in chinese healthy volunteers |
| topic | ranolazine sustained release tablets hplc-ms-ms pharmacokinetics |
| url | http://aammt.tmmu.edu.cn/Upload/rhtml/201808200.htm |
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