非洛地平纳米混悬液固化方法的考察

杜郁茜,李艳,魏巍,付强,何仲贵,孙进,*

中国药学杂志 ›› 2014, Vol. 49 ›› Issue (13) : 1152-1155.

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中国药学杂志 ›› 2014, Vol. 49 ›› Issue (13) : 1152-1155. DOI: 10.11669/cpj.2014.13.013
论著

非洛地平纳米混悬液固化方法的考察

  • 杜郁茜1,李艳1,魏巍1,付强1,何仲贵1,孙进12*
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Investigation of Two Kinds of Solidification Methods for Felodipine Nanosuspension: Flocculation Versus Lyophilization

  • DU Yu-qian1, LI Yan1, WEI Wei1, FU Qiang1, HE Zhong-gui1, SUN Jin1,2*
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摘要

目的 非洛地平纳米混悬液存在物理不稳定性,本实验旨在采用固化方法提高其物理稳定性。 方法 分别采用絮凝法和冷冻干燥法对非洛地平纳米混悬液进行固化。结果 非洛地平纳米混悬液的平均粒径为151 nm,呈单峰分布。絮凝后仅有76.7% 小于1 μm,且呈三峰分布;以20%甘露醇-甘氨酸 (1∶1,W/W)组对混悬剂的保护作用冻干效果最好,平均粒径在375 nm左右的粒子占80%左右,其余粒径更小。结论 选择冷冻干燥法固化非洛地平纳米混悬液,并且采用20%的甘露醇-甘氨酸 (1∶1,W/W)溶液为保护剂时,冻干效果最好。

Abstract

OBJECTIVE To solve the stability problem of felodipine nanosuspension which is a physically unstable colloidal dispersion by solidification method. METHODS Two different methods, flocculation and lyophilization, were applied to solidify the felodipine nanosuspension. RESULTS The mean particle size of the felodipine nanosuspension was 151 nm and was unimodally distributed, but only 76.7% particulates were smaller than 1 μm following flocculation. For lyophilization, it was shown that 20%(W/V) of mannitol-glycine (1∶1,W/W) could stabilize the colloidal system best. CONCLUSION Lyophilization is considered to be superior to flocculation in the aspects of redispersed particle size, and 20%(W/V) of mannitol-glycine (1∶1,W/W) is selected as the optimal cryoprotectant.

关键词

非洛地平 / 纳米混悬液 / 物理稳定性 / 絮凝法 / 冷冻干燥法

Key words

felodipine / nanosuspension / physical stability / flocculation / lyophilization

引用本文

导出引用
杜郁茜,李艳,魏巍,付强,何仲贵,孙进,*. 非洛地平纳米混悬液固化方法的考察[J]. 中国药学杂志, 2014, 49(13): 1152-1155 https://doi.org/10.11669/cpj.2014.13.013
DU Yu-qian, LI Yan, WEI Wei, FU Qiang, HE Zhong-gui, SUN Jin,*. Investigation of Two Kinds of Solidification Methods for Felodipine Nanosuspension: Flocculation Versus Lyophilization[J]. Chinese Pharmaceutical Journal, 2014, 49(13): 1152-1155 https://doi.org/10.11669/cpj.2014.13.013
中图分类号: R944   

参考文献

[1] FU Q, SUN J, HE Z G. Progress for nanocrystals . J Shenyang Pharm Univ (沈阳药科大学学报), 2010, 27(12): 952-960.[2] MOU D, CHEN H, WAN J, et al. Potent dried drug nanosuspensions for oral bioavailability enhancement of poorly soluble drugs with pH-dependent solubility . Int J Pharm, 2011, 413(1): 237-244.[3] VAN E B, FROYEN L, VAN H J, et al. Drying of crystalline drug nanosuspensions-the importance of surface hydrophobicity on dissolution behavior upon redispersion . Eur J Pharm Sci, 2008, 35(1): 127-135.[4] SHEGOKAR R, MULLER R H. Nanocrystals: Industrially feasible multifunctional formulation technology for poorly soluble actives . Int J Pharm, 2010, 399(1): 129-139.[5] MATTEUCCI M E, PAGUIO J C, MILLER M A, et al. Flocculated amorphous nanoparticles for highly supersaturated solutions . Pharm Res, 2008, 25(11): 2477-2487. [6] LIMAYEM I, CHARCOSSET C, FESSI H. Purification of nanoparticle suspensions by a concentration/diafiltration process . Sep Purif Technol, 2004, 38(1): 1-9.[7] HE Z G, SUN J, WANG Y J, et al. Preparation and characterization of felodipine nanosuspension. 2010 China Pharmacy Conference and the 10th China Pharmacist Week (2010年中国药学大会暨第十届中国药师周), Tianjin, November 5-7, 2010 . Beijing: Chinese Pharmaceutical Association, 2311-2320.[8] HEIATI H, TAWASHI R, PHILLIPS N C. Drug retention and stability of solid lipid nanoparticles containing azidothymidine palmitate after autoclaving, storage and lyophilization . J Microencapsulation, 1998, 15(2): 173-184.[9] ABDELWAHED W, DEGOBERT G, STAINMESSE S, et al. Freeze-drying of nanoparticles: Formulation, process and storage considerations . Adv Drug Deliv Rev, 2006, 58(15): 1688-1713. ABDELWAHED W, DEGOBERT G, FESSI H. Investigation of nanocapsules stabilization by amorphous excipients during freeze-drying and storage . Eur J Pharm Biopharm, 2006, 63(2): 87-94. KONAN Y N, GUMY R, ALLEMANN E. Preparation and characterization of sterile and freeze-dried sub-200 nm nanoparticles . Int J Pharm, 2002, 233(1): 239-252.

基金

国家基础科学人才培养基金项目(J1103606);国家自然科学基金资助项目(81173008); 国家重大基础研究计划(973计划)“纳米技术增加难溶药物的水溶性及作用机理研究”(2009CB930300)
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