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1 38 4 Vol. 38, No ACTA HYDROBIOLOGICA SINICA Jul., doi: / 赵 依 妮 李 怡 胡 鲲 阮 记 明 叶 鑫 杨 先 乐 (,, ) : -, -, T 1/2 ka 8, 2, T 1/2α T 1/2β, (CLs) 1/2; 5 10,,, (AUC) -,,, : ; ; ; ; 中 图 分 类 号 : S948 文 献 标 识 码 : A 文 章 编 号 : (2014) ,,,, [1],,, [2],,, [2], [3],,,,,, [4],,, [5],, [6], [7],,,, (Norfloxacin, NFLX) [8, 9], [9], 收 稿 日 期 : ; 修 订 日 期 : 基 金 项 目 : ( ) 863 (2011AA10A216) 作 者 简 介 :, (1992 ),, ; ; zhaoyini21@126.com 通 信 作 者 :, xlyang@shou.edu.cn

2 676 38,,, (Ctenopharyngodon idellus),, (100 ± 10) g,, 2%NaCl 10min, (100 cm 80 cm 80 cm) 1,, (23 ± 2),, 24h ; ; 1, 1/3; NFLX NFLX ( 99.50%), ; NFLX ( 97.8%), ; HPLC ; -, (w/w) , NFLX, 2%, 40%, 15min,, 50,,, 1/5 1/10 NFLX, 1/5 NFLX 1/10 NFLX 1.2 Aglient-1100 (METTLER AB104-N) : ZORBAX SB2C-18 (150 mm 4.6 mm, 5 μm) : : (0.030 mol/l ph 3.1)=5..95(v/v); 276 nm; 1.5 ml/min; 40 ; 10 μl , 3, 54, 6, 40 mg/kg,, ; 1..5 ; h, 5h, h, ; HPLC, 1 ml 5 ml ( ), 10min, r/min 10min,, 45, 1 ml, 0.45 μm 300 μl HPLC [10] 1.5 ; μg/ml, HPLC,, 1.6 DAS3.0 Microsoft Excel ,,,, ( ) μg/ml Ai=1444.3Ci ( ) μg/ml (r=0.999),, 0.01 μg/ml

3 4 : 677 (94.32 ± 6.23)%, (6.28 ± 0.83)% μg/ml, 1, (Two-compartment open model), 1,,,,, (T max ) 0.494h, (K a ) /h,, (t 1/2α ) 0.264h, NFLX 表 1 草 鱼 单 剂 量 口 灌 诺 氟 沙 星 动 力 学 参 数 Tab.1 Pharm-acokinetics parameters following single oral administration of 40 μg/ml of NFLX to Ctenopharyngodon idellus Parameter Value Unit NFLX 1/5 NFLX 1/10 NFLX Dose mg/kg Cor Co µg/ml K a /h K 12 /h K 21 /h K 10 /h t 1/2α h t 1/2β h t 1/2Ka h AUC μg/(l h) C max μg/ml T max h CLs ml/(kg h) NFLX ( %), 40 mg, 1 MCPKP,, NFLX, 1 1,, NFLX ; 5, NFLX 1.107h μg/ml,, NFLX, h μg/ml, 48h μg/ml, 1h 1/6, 96h μg/ml, 196h, μg/ml; 10, NFLX 1.562h μg/ml,, 5, h μg/ml, 196h μg/ml, 5 96h 1,, (T 1/2 ka ) (T 1/2α ) (T 1/2β ), (T p ), (C max ) (CLs) ; (AUC), 5 NFLX , 10 NFLX (T 1/2 ka ) (T 1/2α ) (T 1/2β ) ; (T max ), (C max ) ; (CLs) (AUC) 3 1 Fig. 1 The concentration-time curves of NFLX and NFLX-embeded in plasma,, [11],,

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6 THE ANALYSIS OF THE CONTROLLED-RELEASE PROPERTIES OF NORFLOXACIN MICROENCAPSULATION ZHAO Yi-Ni, LI Yi, HU Kun, RUAN Ji-Ming, YE Xin and YANG Xian-Le (State Collection Center of Aquatic Pathogen, Shanghai Ocean University, Shanghai , China) Abstract: In this study, we determined the controlled-release properties of Norfloxacin (NFLX) microencapsulation which was embedded with chitosan. We approached this goal by examining the pharmacokinetic activity of NFLX in the plasma of Ctenopharyngodon idellus. The results showed that the base line was smooth and the object peak of NFLX was clearly separated from the others. The mean recovery rate of NFLX in plasma was (94.328±6.231)%. The results of the precision test were satisfying. The intra-days and extra-days precision values were 1.988% and 2.648% respectively. We compared the pharmacokinetic properties of embedded and un-embedded NFLX in the plasma of Ctenopharyngodon idellus. Chitosan was a key factor that accounted for the differences between these two groups. The embedded NFLX exhibited the delayed absorption speed, distribution, and elimination in the Plasma. The T 1/2 ka of embedded group was about eight times higher than that of the un-embedded group. The T 1/2α and T 1/2β of the embedded group were much longer too. The T p of embedded group was more than two times higher than that of the un-embedded group. The CLs of the embedded group was about half of that of the un-embedded group. The absorption speed of the 5-time embedded group was higher than that of the 10-time embedded group. The T 1/2α and AUC of the 5-time embedded group were close to that of the 10-time embedded group. However, the absorption and elimination speeds of the former group were faster than those of the latter. The pharmacokinetic differences between norfloxacin-chitosan microcapsules and norfloxacin alone in grass carp suggested that the chitosan embedding should affect the release efficacy, the absorption, and metabolism of NFLX in fish. In real production we can use chitosan as a release agent to preserve the effects of NFLX and to delay absorption and metabolism of the drug in the organism, hereby to improve its effects. Key words: Norfloxacin; Chitosan; Microcapsule; Ctenopharyngodon idellus; Pharmacokinetic