Pharmacokinetic study of olprinone hydrochloride injection in healthy volunteers
Author(s): QIN Yong-ping, MIAO Jia, MEI Ya-jun, WANG Ying, NAN Feng, ZHU Xiao-hong, XIANG Jin, SHU Shi-qing, YU Qin, LI Mei, LIANG Mao-zhi, Department of Clinical Pharmacology, West China Hospital, Sichuan University, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Key Laboratory of Standardization of Chinese Herbal Medicines of Ministry of Education
Pages: 1397-1400+1403
Year: 2015 Issue: 12
Journal: Chinese Journal of New Drugs
Keyword: olprinone hydrochloride; pharmacokinetics; HPLC-MS /MS;
Abstract: Objective:To investigate the pharmacokinetics of olprinone hydrochloride injection in Chinese healthy volunteers. Methods: Twelve volunteers( six men and six women) were divided into six groups by 3 × 3 design and given different doses(5,10 and 20 μg·kg- 1) of olprinone hydrochloride injection by intravenous bolus in three periods,respectively. The method of HPLC-MS / MS was used for the determination of plasma concentration of olprinone. The Phoenix TM Win Nonlin 6. 1 program was used to calculate the pharmacokinetic parameters. The urine concentration at middle dose was determined,and the excretion rate of olprinone through urinary system was calculated. Results: After single dose intravenous injection at 5,10 and 20 μg·kg- 1,the main pharmacokinetic parameters of olprinone hydrochloride injection were as follows: Cmaxwere(17. 74 ± 9. 82),(40. 31 ± 11. 80) and(75. 00 ± 31. 52) μg·L- 1,Tmaxwere( 7. 92 ± 3. 96),( 5. 42 ± 1. 44) and( 5. 00 ± 0. 00) min,t1 /2were(61. 20 ± 14. 42),(72. 01 ± 14. 40) and(69. 87 ± 14. 48) min,AUC0- t were(463. 01 ± 105. 89),(849. 54 ±149. 23) and(1 758. 35 ± 378. 46) μg·L- 1·min- 1,and AUC0- ∞were(470. 64 ± 106. 65),(863. 46 ± 153. 24)and(1 783. 07 ± 388. 52) μg·L- 1·min- 1,respectively. The accumulation excretion rate of olprinone at the medium dose in the healthy volunteers was(61. 79 ± 5. 465) %. Conclusion: Olprinone hydrochloride injection may have linear pharmacokinetic feature in the dose range of 5 ~ 20 μg·kg- 1in human body,and it is mainly eliminated through kidney.
Pages: 1397-1400+1403
Year: 2015 Issue: 12
Journal: Chinese Journal of New Drugs
Keyword: olprinone hydrochloride; pharmacokinetics; HPLC-MS /MS;
Abstract: Objective:To investigate the pharmacokinetics of olprinone hydrochloride injection in Chinese healthy volunteers. Methods: Twelve volunteers( six men and six women) were divided into six groups by 3 × 3 design and given different doses(5,10 and 20 μg·kg- 1) of olprinone hydrochloride injection by intravenous bolus in three periods,respectively. The method of HPLC-MS / MS was used for the determination of plasma concentration of olprinone. The Phoenix TM Win Nonlin 6. 1 program was used to calculate the pharmacokinetic parameters. The urine concentration at middle dose was determined,and the excretion rate of olprinone through urinary system was calculated. Results: After single dose intravenous injection at 5,10 and 20 μg·kg- 1,the main pharmacokinetic parameters of olprinone hydrochloride injection were as follows: Cmaxwere(17. 74 ± 9. 82),(40. 31 ± 11. 80) and(75. 00 ± 31. 52) μg·L- 1,Tmaxwere( 7. 92 ± 3. 96),( 5. 42 ± 1. 44) and( 5. 00 ± 0. 00) min,t1 /2were(61. 20 ± 14. 42),(72. 01 ± 14. 40) and(69. 87 ± 14. 48) min,AUC0- t were(463. 01 ± 105. 89),(849. 54 ±149. 23) and(1 758. 35 ± 378. 46) μg·L- 1·min- 1,and AUC0- ∞were(470. 64 ± 106. 65),(863. 46 ± 153. 24)and(1 783. 07 ± 388. 52) μg·L- 1·min- 1,respectively. The accumulation excretion rate of olprinone at the medium dose in the healthy volunteers was(61. 79 ± 5. 465) %. Conclusion: Olprinone hydrochloride injection may have linear pharmacokinetic feature in the dose range of 5 ~ 20 μg·kg- 1in human body,and it is mainly eliminated through kidney.
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