摘要
目的建立体外磷酸盐缓冲溶液（PBS）聚乳酸／羟基乙酸（PLGA）缓释卡氮芥（BCNU）微球药物浓度的高效液相色谱分析方法，并用此法研究缓释微球的体外释放动力学特征。方法采用依利特Hypersil ODS2 C18色谱柱（5μm，4．6mm×150mm），以甲醇：水（50：50）为流动相，流速1．0ml／min，紫外光检测波长237nm。结果BCNU在0．005—0．35μmol／ml范围内呈线性（r=0．9992），最低检测下限为0．005μmol／ml。采用低、中、高浓度（0．03、0．1、0．3μmol／m1）的方法回收率分别为103．33％、101．43％和102．04％，日间及日内相对标准偏差（RSD）分别〈4％和〈1％。体外药物释放动力学研究表明，PLGA缓释BCNU时间可达3w以上。结论本法准确可靠，操作简便，适用于缓释BCNU微球的体外药物释放动力学研究。
Objective To establish a method for the detection of carmustine （1,3-bis（ 2-chloroethyl ）-1- nitrosourea, BCNU） dose in phosphate-buffered solution （PBS） from BCNU-loaded （polylactic-co-glycolic acid, PIGA） microspheres and to study the releasing kinetics of BCNU-PIGA microspheres in vitro. Methods BCNU concentration was detected by an ultraviolet （UV） detector at 237 nm with a Hypersil ODS2 C18 column （5 μm, 4.6mm × 150 mm）. The mixture of methanol and water （50 ： 50） was used as the mobile phase. The flow rate was 1.0 ml/min. Results The calibration curve was linear within the range of 0. 005 ～ 0.35 μmol/ml and the measurable lowest limit was 0.005 μmol/ml. The average recovery rate of BCNU at the concentrations of 0.03, 0. 1 and 0. 3 μmol/ml was 103.33%, 101.43% and 102. 04% respectively. The relative standard deviation （RSD） of the within-day and between-days variation was less than 4% and 1% respectively. The results showed that the microspheres could release BCNU for over 3 weeks. Conclusion This high performance liquid chromatography method is simple, sensitive and accurate. It is suitable for released kinetics study of controlledrelease microspheres of BCNU loading in vitro.
出处
《中华神经外科疾病研究杂志》
CAS
2006年第6期522-525,共4页
Chinese Journal of Neurosurgical Disease Research
关键词
聚乳酸/羟基乙酸
卡氮芥
高效液相色谱法
药物释放动力学
Polylactic-co-glycolic acid
1,3-bis（2-chloroethyl）-1-nitrosourea
High performance liquid chromatography
Released kinetics
