|
|
|
|
|
| Pharmacokinetics of Quinocetone and Its Major Metabolites in Swine After Intravenous and Oral Administration |
Laboratory of Veterinary Pharmacology, College of Veterinary Medicine, South China Agricultural University |
|
|
|
摘要 The pharmacokinetics of quinocetone and its major metabolites in healthy swine was investigated in this paper.Quinocetone was administered to 8 healthy cross-bread swine intravenously and orally at a dosage of 4 and 40 mg kg-1body weight respectively in a randomized crossover design test with two-week washout period. A sensitive highperformanceliquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed for thedetermination of quinocetone and its metabolite 1-desoxyquinocetone in plasma. Plasma concentration versus timeprofiles of quinocetone and its metabolite 1-desoxyquinocetone were analyzed by non-compartmental analysis usingWinnonlin 5.2 software. Mean maximum concentrations (Cmax) for quinocetone was found to be (0.56±0.13) μg mL-1 at 2.92 h,after oral administration of quinocetone. Mean maximum concentrations (Cmax) for 1-desoxyquinocetone after intravenousor oral administration of quinocetone were (0.0095±0.0012) μg mL-1 at 0.083 h and (0.0067±0.0053) μg mL-1 at 3.08 h. Theapparent elimination half-lives (T1/2) for quinocetone and its metabolite 1-desoxyquinocetone were (2.24±0.24) and(5.23±0.56) h after intravenous administration of quinocetone and (2.91±0.29) and (11.85±2.89) h after oral administrationof quinocetone, respectively. Mean areas under the plasma concentration-time curve (AUC0- ) for quinocetone and 1-desoxyquinocetone were (2.02±0.15) and (0.2±0.002) μg h mL-1 respectively after intravenous administration of quinocetone,and (3.5±0.79) and (0.053±0.03) μg h mL-1 after oral administration of quinocetone, respectively. Quinocetone was rapidlyabsorbed and metabolized in swine after oral and intravenous administration. The plasma concentration-time curve(AUC0- ) of 1-desoxyquinocetone were much smaller than those of quinocetone, while the elimination half-lives (T1/2) weremuch longer than those of quinocetone after intravenously (i.v.) or oral administration.
Abstract The pharmacokinetics of quinocetone and its major metabolites in healthy swine was investigated in this paper.Quinocetone was administered to 8 healthy cross-bread swine intravenously and orally at a dosage of 4 and 40 mg kg-1body weight respectively in a randomized crossover design test with two-week washout period. A sensitive highperformanceliquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed for thedetermination of quinocetone and its metabolite 1-desoxyquinocetone in plasma. Plasma concentration versus timeprofiles of quinocetone and its metabolite 1-desoxyquinocetone were analyzed by non-compartmental analysis usingWinnonlin 5.2 software. Mean maximum concentrations (Cmax) for quinocetone was found to be (0.56±0.13) μg mL-1 at 2.92 h,after oral administration of quinocetone. Mean maximum concentrations (Cmax) for 1-desoxyquinocetone after intravenousor oral administration of quinocetone were (0.0095±0.0012) μg mL-1 at 0.083 h and (0.0067±0.0053) μg mL-1 at 3.08 h. Theapparent elimination half-lives (T1/2) for quinocetone and its metabolite 1-desoxyquinocetone were (2.24±0.24) and(5.23±0.56) h after intravenous administration of quinocetone and (2.91±0.29) and (11.85±2.89) h after oral administrationof quinocetone, respectively. Mean areas under the plasma concentration-time curve (AUC0- ) for quinocetone and 1-desoxyquinocetone were (2.02±0.15) and (0.2±0.002) μg h mL-1 respectively after intravenous administration of quinocetone,and (3.5±0.79) and (0.053±0.03) μg h mL-1 after oral administration of quinocetone, respectively. Quinocetone was rapidlyabsorbed and metabolized in swine after oral and intravenous administration. The plasma concentration-time curve(AUC0- ) of 1-desoxyquinocetone were much smaller than those of quinocetone, while the elimination half-lives (T1/2) weremuch longer than those of quinocetone after intravenously (i.v.) or oral administration.
|
|
Received: 30 January 2011
Accepted:
|
|
Corresponding Authors:
Correspondence DING Huan-zhong, Associate Professor, Ph D, Tel: +86-20-85284896,Mobile: 13751886811, E-mail: hzding@scau.edu.cn
E-mail: 365307563@qq.com
|
| About author: ZHONG Jia-lin, MSc, Tel: +86-20-85284896, E-mail: 365307563@qq.com |
Cite this article:
ZHONG Jia-lin, ZHANG Gui-jun, SHEN Xiang-guang, WANG Lin, FANG Bing-hu, DING Huan-zhong.
2011.
Pharmacokinetics of Quinocetone and Its Major Metabolites in Swine After Intravenous and Oral Administration. Journal of Integrative Agriculture, 10(8): 1292-1300.
|
| [1] Ban M M, Zhang K Y, Jiang S X, Xue F Q. 2010. Cytotoxicityof quinocetone and olaquindox on human liver cells. ChineseJournal of Veterinary Science, 30, 1517-1521.[2] (in Chinese)Benet L Z, Galeazzi R L. 1979. Noncompartmental determinationof the steady-state volume of distribution. Journal ofPharmaceutical Sciences, 68, 1071-1074.[3] Cutler D J. 1978. Theory of the absorption time, an adjunct toconventional bioavailability studies. Journal of Pharmacyand Pharmacology, 30, 476-478.[4] Gibaldi M, Perrier D. 1982. Pharmacokinetics. 2nd ed. MarrcelDekker, New York. pp. 409-417.[5] Li J Y, Zhou X Z, Li J S, Zhao R C, Miao X L, Zhang J Y. 2005.The pharmacokinetics of quinocetone in pigs. Chinese Journalof Veterinary Drug, 39, 1-3. (in Chinese)[6] Li J W, Huang F, Zhou Y P, Liu J. 2010. Effect of quinocetone ongrowth of allogynogentic crucian and its metabolism in vivo.Cereal & Feed Industry, 5, 45-48. (in Chinese)[7] Li J Y, Li J S, Xu Z Z, Du X L, Miao X L, Zhao R C, Liu J X, XueF Q. 2002. Studies on the pharmacokinetics of quinocetonein pigs and chickens. Acta Veterinaria et Zootechnica Sinica,34, 94-97. (in Chinese)[8] Liu Y T, Guo D F, Yang L, Yang H, Yuan K P, Ai X H. 2009.Study on residues of quinocetone in Jian carp (Cyprinuscarpio var. jian) and channel catfish (Ictalurus punctatus).Journal of Hydroecology, 2, 95-97. (in Chinese)[9] Shen J Z, Yang C Y, Wu C M, Feng P S, Wang Z H, Li Y, Li Y S,Zhang S X. 2010. Identification of the major metabolites ofquinocetone in swine urine using ultra-performance liquidchromatography/electrospray ionization quadrupole time-offlighttandem mass spectrometry. Rapid Communications inMass Spectrometry, 24, 375-383.[10] Wang Y C, Zhao R C, Yan X L, Li J S, Du X L, Zhang S Z, XueF Q, Xu Z Z, Liang J P, Zhang J Y. 1995. Carcinogenicitystudy of quinocetone on mice. Chinese Journal of Veterinary Science and Technology, 25, 24-25. (in Chinese)[11] Wang Y C, Zhao R C, Yan X L, Li J S, Xu Z Z, Xue F Q, Liang JP, Yao S L, Wang F L. 1995. Effect of quinocetone on growthof chickens. Chinese Journal of Veterinary Science andTechnology, 25, 36-38. (in Chinese)[12] Xu J N, Wang Q K, Cui T, Huang Q Y, Wang J G. 2005. Studieson the subchronic oral toxicity of quinocetone. ChineseJournal of Veterinary Drug, 39, 10-15. (in Chinese)[13] Xu Z Z, Li J S, Zhao R C, Wang Y C, Xue F Q, Liang J P, Yan XL, Du X L, Zang J Y, He Z L. 1995. Effect of quinocetone ongrowth of piglets. Chinese Journal of Veterinary Science andTechnology, 25, 37-39. (in Chinese)[14] Yamaoka K, Nakagawa T, Uno T. 1978. Statistical moments inpharmacokinetics. I. Pharmacokinet. Biopharm, 6, 547-558.[15] Yang L,Wang K Y, Ai X H,Yuan K P, Liu Y T. 2010.Pharmacokinetics and tissue distribution of quinocetone incarp and channel catfish. Chinese Veterinary Science, 40,537-542. (in Chinese)[16] Zhang W, Peng D P, Huang L L, Wang Y L, Yuan Z H. 2007.Study on genotoxicity of quinocetone. Journal of Toxicology,21, 335. |
| No Suggested Reading articles found! |
|
|
Viewed |
|
|
|
Full text
|
|
|
|
|
Abstract
|
|
|
|
|
Cited |
|
|
|
|
| |
Shared |
|
|
|
|
| |
Discussed |
|
|
|
|
