恩諾沙星納米混懸注射劑的制備及在豬體內(nèi)藥動學(xué)研究
發(fā)布時間:2018-03-15 18:26
本文選題:高壓均質(zhì)法 切入點:恩諾沙星 出處:《中國獸醫(yī)學(xué)報》2017年08期 論文類型:期刊論文
【摘要】:采用高壓均質(zhì)法制備恩諾沙星納米混懸注射劑并對其制備工藝和質(zhì)量進行考察、評價;采用高效液相色譜法測定豬血漿中恩諾沙星的濃度,以拜有利注射劑為參照考察恩諾沙星納米混懸注射劑在豬體內(nèi)的藥動學(xué)。結(jié)果顯示:制備的恩諾沙星納米混懸注射劑,恩諾沙星的含量為97.9%,平均粒徑為(613.21±5.78)nm、PDI(0.22±0.02)、Zeta電位為-2.02mV。恩諾沙星納米混懸注射劑和拜有利注射劑在豬體內(nèi)的達峰濃度(Cmax)分別為(0.32±0.12)、(0.67±0.09)mg/L,達峰時間(Tmax)分別為(2.88±0.96)、(0.79±0.26)h,消除半衰期(t1/2ke)分別為(5.99±1.37)、(4.49±1.25)h,AUClast分別為每小時(4.63±1.30)、(4.40±0.45)mg/L,MRTlast分別為(9.59±2.34)、(5.41±1.10)h;與拜有利注射劑相比,恩諾沙星納米混懸注射劑相對生物利用度為105.2%。結(jié)論:高壓均質(zhì)法制備的恩諾沙星納米混懸注射劑操作簡單、不易沉降、再分散性好,理化性質(zhì)較穩(wěn)定;與拜有利注射劑相比其Tmax、t1/2k明顯增加(P0.01),MRT顯著延長(P0.01)表明恩諾沙星納米混懸注射劑具有明顯緩釋作用且消除緩慢。
[Abstract]:High pressure homogenization method was used to prepare enrofloxacin nano-suspension injection and its preparation technology and quality were investigated and evaluated, and the concentration of enrofloxacin in pig plasma was determined by HPLC. The pharmacokinetics of enrofloxacin nano-suspension injection in pigs was investigated by using Baiyi injection as a reference. The results showed that the prepared enrofloxacin nano-suspension injection was prepared. The content of enrofloxacin is 97.9, the average particle size is 613.21 鹵5.78nmmg / L, the Zeta potential is -2.02mV. the peak concentration of enrofloxacin nano-suspension injection and benazepam injection in pigs is 0.32 鹵0.1212ng / L, and the peak time is 2.88 鹵0.96nmg / L and 0.79 鹵0.26hrespectively, and the elimination of half-life is 5.99 鹵1.37hAUClast, respectively. The MRTlast was 4.63 鹵1.30 mg / h, 4.40 鹵0.45 mg / L MRTlast was 9.59 鹵2.34 mg-1 / h and 5.41 鹵1.10 / h, respectively. The relative bioavailability of enrofloxacin nano-suspension injection was 105.2. Conclusion: the preparation of enrofloxacin nano-suspension injection by high pressure homogenization method is easy to operate, easy to settle, good dispersion and stable physical and chemical properties. Compared with the injection, its Tmax1 / 2k increased significantly (P 0.01) and MRT significantly prolonged (P 0.01). The results showed that enrofloxacin nano-suspension injection had obvious slow-release and slow elimination.
【作者單位】: 華南農(nóng)業(yè)大學(xué)國家殘留基準實驗室;廣東溫氏大華農(nóng)生物科技有限公司;
【基金】:國家自然科學(xué)基金資助項目(31372479)
【分類號】:S859.5;S859.7
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