HPLC法测定枸橼酸他莫昔芬磁性微球的载药量和包封率

目的: 建立高效液相色谱法测定枸橼酸他莫昔芬磁性微球的载药量和包封率。 方法: 采用Dikma Diamonsil C₁₈(4.6 mm×250 mm,5 μm)色谱柱,以甲醇-水-三乙胺(86:14:0.36)为流动相,流速1.0 mL·min^-1,检测波长278 nm,柱温为35 ℃。 结果: 线性范围为4～200 μg·mL^-1,r=0.9999。低、中、高3个浓度平均回收率(n=3)分别为101.6%,101.1%,100.0%;RSD分别为0.2%,0.2%,0.4%。 结论: 该法准确可靠,快速简便,适用于测定枸橼酸他莫昔芬磁性微球的载药量和包封率。

Objective: To establish an HPLC method for determination of drug loading and encapsulated efficiency of tamoxifen citrate-magnetic microspheres. Methods: A Dikma Diamonsil C₁₈(4.6 mm×250 mm,5 μm)column was adopted with a mobile phase of methanol-water-triethylamine(86∶ 14∶ 0.36)at the flow rate of 1.0 mL·min^-1;The detection wavelength was set at 278 nm and the column temperature was 35 ℃. Results: The calibration curve was linear in the range of 4-200 μg·mL^-1,r=0.9999.The average recoveries(n=3)of low,middle,high concentrations were 101.6%,101.1%,100.0% and RSD were 0.2%,0.2%,0.4%,respectively. Conclusion: The method is accurate,reliable,rapid and simple for determination of drug loading and encapsulated efficiency of tamoxifen citrate-magnetic microspheres.

[1] Crofskey S.Persistent effects with tamoxifen in breast cancer prevention.Inpharm Weekly,2007(1573):11
[2] Freedman AN,Graubard BI,Rao SR,et al.Estimates of the number of U.S.women who could benefit from tamoxifen for breast cancer chemoprevention.J Natl Cancer Inst,2003,95(7):526
[3] SUN Jing-zhong(孙靖中),YANG Qi-feng(杨其峰),SONG Ke-ying(宋科瑛).The side effects of tamoxifen in treatment of breast cancer(他莫昔芬治疗乳腺癌的副作用).China Oncol(中国癌症杂志),1999,9(5-6):489
[4] PING Qi-neng(平其能).Modern Pharmaceutics(现代药剂学).Beijing(北京):China Medical Science Press(中国医药科技出版社),2001.664
[5] TAO Kai-xiong(陶凯雄),CHEN Dao-da(陈道达),TIAN Yuan(田源).Pharmacokinetics of magnetic anticancer drugs target-administered via digestive canal or vein(抗癌药物磁性微球靶向给药的药代动力学研究).Pract J Cancer(实用癌症杂志),2000,15(4):347
[6] Asmatulu R,Zalich MA,Claus RO,et al.Synthesis,characterization and targeting of biodegradable magnetic nanocomposite particles by external magnetic fields.J Magn Magn Mater,2005,292(3):108
[7] LI Ke-xin(李可欣),CHEN Da-wei(陈大为),ZHAO Xiu-li(赵秀丽),et al.RP-HPLC determination of encapsulated efficiency of 5-luorouracil in chitosan microspheres(RP-HPLC法测定壳聚糖微球中5-氟尿嘧啶的包封率).J Shenyang Pharm Univ(沈阳药科大学学报),2006,22(6):434
[8] CAO Feng-liang(曹丰亮),XI Yan-wei(席延伟),TANG Lin(唐琳),et al.Preparation and characterization of curcum in loaded gelatin microspheres for lung targeting(姜黄素肺靶向明胶微球的制备及性质研究).J Chin Med Mater(中药材),2009,32(3):423
[9] DENG Rong(邓嵘),CHEN Ji-min(陈济民),GAO Sheng-chuan(高声传),et al.Determination of zedoary turmeric oil gelatin microspheres(莪术油明胶微球剂的含量测定).Chin Hosp Pharm J(中国医院药学杂志),2001,21(2):79