目的 研究酒石酸溴莫尼定浓度、流速对体内外自制微透析探针回收率的影响,为进一步的眼部微透析药动学试验提供依据。方法 以酒石酸溴莫尼定为模型药物,分别测定微透析探针在不同药物浓度、不同灌流速度时,体外正向、反向回收率及体内反向回收率。结果 微透析探针体内外回收率与药物浓度无关,与流速成反比。探针体外正向、反向回收率在1.0 μL·min-1时有差异,在2.0、3.0 μL·min-1时无明显差异;且均大于体内反向回收率。结论 自制微透析探针回收率稳定,可用于酒石酸溴莫尼定的眼部药动学研究。
Abstract
OBJECTIVE To evaluate the effects of drug concentration and perfusion rate on the recoveries of self-made linear microdialysis probes for further ocular pharmacokinetic study. METHODS Brimonidine tartrate was selected as the model drug. The in vitro recovery was determined using positive dialysis and retrodialysis at different perfusion rates and drug concentrations. And the in vivo recovery was determined using retrodialysis method. RESULTS The microdialysis recoveries of brimonidine tartrate were inversely proportional to perfusion rate,while independent of drug concentration. The positive dialysis and retrodialysis recoveries in vitro were different at 1.0 μL·min-1, but no significant difference at 2.0 and 3.0 μL·min-1. The in vitro recoveries were greater than those in vivo. CONCLUSION The self-made microdialysis probe has stable recovery and can be used in ocular pharmacokinetic study of brimonidine tartrate.
关键词
酒石酸溴莫尼定 /
微透析 /
探针回收率 /
体外 /
体内 /
眼
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Key words
brimonidine tartrate /
microdialysis /
probe recovery /
in vivo /
in vitro /
ocular
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中图分类号:
R969.1
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参考文献
[1] TORIS C B, CAMRAS C B, YABLONSKI M E. Acute versus chronic effects of brimonidine on aqueous humor dynamics in ocular hypertensive patients. Am J Ophthalmol, 1999, 128(1):8-14.
[2] ACHEAMPONG A A, SMALL D, BAUMGARTEN V, et al. Formulation effects on ocular absorption of brimonidine in rabbit eyes. J Ocul Pharmacol Ther, 2002, 18(4):325-337.
[3] SHEN J, DURAIRAJ C, LIN T, et al. Ocular pharmacokinetics of intravitreally administered brimonidine and dexamethasone in animal models with and without blood-retinal barrier breakdown. Invest Ophthalmol Vis Sci, 2014, 55(2):1056-1066.
[4] DARVESH A S, CARROLL R T, GELDENHUYS W J, et al. In vivo brain microdialysis:advances in neuropsychopharmacology and drug discovery. Expert Opin Drug Discov, 2011, 6(2):109-127.
[5] TANG Z, WANG Q. Application of microdialysis in ocular pharmacokinetics. Chin J New Drugs(中国新药杂志), 2013, 22(7):802-808.
[6] LIU Z, ZHANG X, WU H, et al. Preparation and evaluation of solid lipid nanoparticles of baicalin for ocular drug delivery system in vitro and in vivo. Drug Dev Ind Pharm, 2011, 37(4):475-481.
[7] DE LANGE E C, DE BOER A G, BREIMER D D. Methodological issues in microdialysis sampling for pharmacokinetic studies. Adv Drug Deliv Rev, 2000, 45(2-3):125-148.
[8] SØRENSEN O, ANDERSEN A, OLSEN H, et al. Validation and use of microdialysis for determination of pharmacokinetic properties of the chemotherapeutic agent mitomycin C-an experimental study. BMC Cancer, 2010, 10(9):469-478.
[9] DEY S, GUNDA S, MITRA A K. Pharmacokinetics of erythromycin in rabbit corneas after single-dose infusion:role of P-glycoprotein as a barrier to in vivo ocular drug absorption. J Pharmacol Exp Ther, 2004, 311(1):246-255.
[10] LI X M, CAO G, SHAN Q Y, et al. Application progress of microdialysis in eye drug research.Chin Pharm J(中国药学杂志), 2012, 47(9):657-659.
[11] CHEN T F, LIU J X, ZHANG Y, et al. Analysis on microdialysis probe recovery of baicalin in vitro and in vivo based on LC-MS/MS. Chin Pharm J(中国药学杂志), 2017, 42(11):2168-2174.
[12] ZHANG Y, HE Z F, TANG Z, et al. Microdialysis recovery of oxymatrine in vitro and in vivo. Chin J Trad Chin Med Pharm(中华中医药杂志), 2015, 30(9):3108-3111.
[13] ZHANG Y, HE Z F, TANG Z, et al. In vitro and in vivo microdialysis recovery of matrine. Chin Pharm J(中国药学杂志), 2014, 49(22):2031-2035.
[14] XU H Y, TANG Z, WANG Q, et al. In vitro and in vivo microdialysis recovery of tetramethylpyrazine. Chin Pharm J(中国药学杂志), 2012, 47(21):1750-1753.
[15] YANG CH, BAI J, DU S Y, et al. In vitro and in vivo recoveries of cutaneous microdialysis probe of paeonol, eugenol and piperine. Chin Pharm J(中国药学杂志), 2016, 41(22):4247-4253.
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基金
浙江省科技计划项目资助(2017F30005);浙江省公益基金项目资助(2016C37074)
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