橙皮素纳米晶体制备中药物结晶度、微结构对粒径减小效率的影响

刘涛 ,尹海鹏 ,刘孝天

中国药学杂志 ›› 2016, Vol. 51 ›› Issue (15) : 1308-1311.

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中国药学杂志 ›› 2016, Vol. 51 ›› Issue (15) : 1308-1311. DOI: 10.11669/cpj.2016.15.013
论 著

橙皮素纳米晶体制备中药物结晶度、微结构对粒径减小效率的影响

  • 刘涛1 ,尹海鹏2 ,刘孝天1
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Preparation of Hesperetin Nanocrystals:Effect of Solid State and Particle Morphology on the Particle Size Reduction Efficiency

  • LIU Tao1,YIN Hai-peng2,LIU Xiao-tian1
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摘要

目的 药物本身的物理性质在药物纳米混悬液/药物纳米晶体的制备中起着重要作用,决定了最终的粒径和生产效率。目前已发表的研究大量集中在过程参数(如稳定剂筛选等),而药物本身对粒径减小的影响尚不清楚。方法 本实验采用中药活性物橙皮素为研究对象,不同于以往的研究,初始药物物理性质通过喷雾干燥、旋转蒸发、淬火冷却进行改造,改造后的药物和初始药物物理性质(药物结晶度、颗粒微结构等)将进行对比并分别用于高压均质机制备纳米混悬液。结果 喷雾干燥后的橙皮素能被高压均质得到最小的粒径。结论 药物颗粒微结构的改变应为影响高压均质过程粒径减小效率的重要原因。同时,药物在最终的纳米混悬液中均为晶体,重结晶现象发生。

Abstract

OBJECTIVE Drug properties have important effect on the drug nanosuspenions/nanocrystal production and can determine the final particle size and production efficiency. A number of papers have referred to the optimizations of processes expecting the smaller achievable particle sizes as well as increased production efficiency. Aspects such as stabilizer selection are those most commonly described in the literature. The aims of this study are to systematically investigate the mechanism of nanocrystal formation and identify the physical properties that can affect the particle size reduction process. METHODS The influence of drug properties such as degree of crystallinity and particle morphology on particle size reduction was systematically investigated by producing hesperetin as a model drug. Processes ie spray-drying, rotavapor, and quench-cooling were applied to modify the physical properties of hesperetin. Both unmodified drugs and modified drugs were used for production of nanosuspension. RESULTS The nanosuspension with the smallest particle size was obtained from spray-dried hesperetin. CONCLUSION An improved crystal morphology of modified starting material obtained through spray-drying may lead to a more efficient homogenization process. The drug exists in the nanosuspensions as crystalline, which means recrystallization has occurred as a result of the high pressure homogenization process.

关键词

药物物理性质 / 纳米混悬液 / 药物结晶度 / 药物颗粒形态 / 橙皮素

Key words

drug property / nanosuspension / drug crystallinity / particle morphology / hesperetin

引用本文

导出引用
刘涛 ,尹海鹏 ,刘孝天. 橙皮素纳米晶体制备中药物结晶度、微结构对粒径减小效率的影响[J]. 中国药学杂志, 2016, 51(15): 1308-1311 https://doi.org/10.11669/cpj.2016.15.013
LIU Tao,YIN Hai-peng,LIU Xiao-tian. Preparation of Hesperetin Nanocrystals:Effect of Solid State and Particle Morphology on the Particle Size Reduction Efficiency[J]. Chinese Pharmaceutical Journal, 2016, 51(15): 1308-1311 https://doi.org/10.11669/cpj.2016.15.013
中图分类号: R944   

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基金

山东省自然科学基金资助项目(ZR2014HP023)
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