| 猫经口内服2种米尔贝肟吡喹酮片的药代动力学比较研究 |
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| 引用本文： | 金之源,周泽伟,王雅琴,卜仕金.猫经口内服2种米尔贝肟吡喹酮片的药代动力学比较研究[J].中国畜牧兽医,2014,41(12):157-160. |
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| 作者姓名： | 金之源 周泽伟 王雅琴 卜仕金 |
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| 作者单位： | 1. 扬州大学兽医学院, 江苏扬州 225009;2. 江苏省动物重要疫病与人兽共患病防控协同创新中心, 江苏扬州 225009 |
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| 基金项目： | 江苏高校优势学科建设工程资助项目(PAPD). |
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| 摘 要： | 本试验将16只成年健康猫随机分成2组,每组8只(公母各半),采用单剂量随机平行对照试验设计,分别单剂量(4 mg/kg体重,以米尔贝肟计)经口内服国产(受试品)和进口(对照品)米尔贝肟吡喹酮片,进行其在猫体内的药代动力学比较研究.给药后按预定时间采集血样,采用HPLC法进行血浆中米尔贝肟和吡喹酮含量的测定,实测血药浓度—时间数据采用Winnonlin 5.2药代动力学分析软件计算药代动力学参数.结果显示,米尔贝肟吡喹酮片对照品单剂量内服后,米尔贝肟的消除半衰期(T1/2β)为(20.08±7.57)h,达峰时间(Tmax)和峰值浓度(Cmax)分别为6.00 h和(764.43±251.40)ng/mL,平均曲线下面积(AUC)为(15.00±5.05)ng/(L·h),平均滞留时间(MRT)(18.60±1.52)h;吡喹酮的消除半衰期(T1/2β)为(6.27±5.26)h,达峰时间(Tmax)和峰值浓度(Cmax)分别为(3.88±0.35)h和(1018.25±200.19)ng/mL,平均曲线下面积(AUC)为(8.69±2.07)ng/(L·h),平均滞留时间(MRT)(6.56±1.07)h.米尔贝肟吡喹酮片受试品单剂量内服后,米尔贝肟的消除半衰期(T1/2β)为(15.07±4.05)h,达峰时间(Tmax)和峰值浓度(Cmax)分别为(5.25±1.04)h和(806.65±299.01)ng/mL,平均曲线下面积(AUC)为(15.18±5.97)ng/(L·h),平均滞留时间(MRT)(17.47±1.97)h,相对生物利用度为101.20%;吡喹酮的消除半衰期(T1/2β)为(11.11±4.62)h,达峰时间(Tmax)和峰值浓度(Cmax)分别为(5.25±1.04)h和(880.47±241.27)ng/mL,平均曲线下面积(AUC)为(9.64±2.76)ng/(L·h),平均滞留时间(MRT)(10.52±1.52)h,相对生物利用度为119.16%.与对照品相比,受试品的药代动力学参数中除米尔贝肟的消除半衰期显著缩短、吡喹酮的达峰时间显著延迟外(P<0.05),其他药代动力学参数差异均不显著(P>0.05).结果表明,猫经口内服米尔贝肟吡喹酮片受试品与对照品后具有相似的药代动力学特征.
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| 关 键 词： | 米尔贝肟吡喹酮片 猫 经口内服 药代动力学 |
| 收稿时间： | 2014-06-20 |
Comparative Study on Pharmacokinetics of Two Milbemycin Oxime-praziquantel Tablets by Oral Administration in Cats |
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| JIN Zhi-yuan,ZHOU Ze-wei,WANG Ya-qin,BU Shi-jin.Comparative Study on Pharmacokinetics of Two Milbemycin Oxime-praziquantel Tablets by Oral Administration in Cats[J].China Animal Husbandry & Veterinary Medicine,2014,41(12):157-160. |
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| Authors: | JIN Zhi-yuan ZHOU Ze-wei WANG Ya-qin BU Shi-jin |
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| Institution: | 1. College of Veterinary Medicine, Yangzhou University, Yangzhou 225009, China;2. Jiangsu Co-innovation Center for Prevention and Control of Important Animal Infectious Diseases and Zoonoses, Yangzhou 225009, China |
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| Abstract: | 16 healthy cats were randomly divided into two equal groups, a single dose of parallel test design was used. The pharmacokinetics of test substance and reference substance milbemycin oxime-praziquantel tablets were studied in cats by oral route (4 mg/kg·bw). The plasma concentrations of milbemycin oxime and praziquantel were determined by high-performance liquid chromatographic method, and pharmacokinetic parameters were calculated by kinetica program. The main parameters of reference substance were as follows, T1/2β, Tmax, Cmax, AUC and MRT of milbemycin oxime were (20.08±7.57)h, 6.00 h, (764.43±251.40)ng/mL, (15.00±5.05)ng/(L·h) and (18.60±1.52)h, respectively; and T1/2β, Tmax, Cmax, AUC and MRT of praziquantel were (6.27±5.26)h, (3.88±0.35)h, (1018.25±200.19)ng/mL, (8.69±2.07)ng/(L·h) and MRT (6.56±1.07)h, respectively. The main parameters of test substance were as follows, T1/2β, Tmax, Cmax, AUC and MRT of milbemycin oxime were (15.07±4.05)h, (5.25±1.04)h, (806.65±299.01)ng/mL, (15.18±5.97)ng/(L·h) and (17.47±1.97)h, respectively, and the relative bioavailability was 101.20%; T1/2β, Tmax, Cmax, AUC and MRT of praziquantel were (11.11±4.62)h, (5.25±1.04)h, (880.47±241.27)ng/mL, (9.64±2.76)ng/(L·h) and (10.52±1.52)h, respectively, and the relative bioavailability was 119.16%. Compared with reference substance, significant difference in T1/2β was observed in milbemycin oxime (P<0.05), and significant difference in Tmax was also observed in praziquantel (P<0.05), other parameters were no significant differences (P>0.05).The results showed that the test substance of milbemycin oxime-praziquantel tablets compared with the reference substance had similar pharmacokinetic characteristics in cats by oral route. |
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| Keywords: | milbemycin oxime-praziquantel tablets cats oral administration pharmacokinetic |
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