布洛芬纳米微粉的制备、表征及体外透皮性研究

发布时间：2018-01-19 19:10

本文关键词： 布洛芬乳化法纳米微粉表征透皮　出处：《中国药房》2017年01期 　论文类型：期刊论文

【摘要】：目的:制备布洛芬纳米微粉并对其进行表征,考察其体外透皮作用。方法:采用乳化法,以氯仿-乙醇(7∶3,V/V)为有机相、超纯水为水相、聚山梨酯80为表面活性剂制备布洛芬纳米微粉。利用激光粒度分析方法、扫描电镜、傅里叶变换红外光谱、X射线衍射、差示扫描对制备的布洛芬纳米微粉进行表征。比较布洛芬纳米微粉与原料药的饱和溶解度、体外溶出度和体外透皮率。结果:确定的处方及制备工艺为聚山梨酯80 5 mg/m L、水相-有机相体积比40∶1、布洛芬质量浓度250 mg/m L、匀浆速度5000 r/min、匀浆时间2 min。所制布洛芬纳米微粉为多孔疏松珊瑚状,其化学结构未改变,由原来的晶体态变为无定形态,粒径为179.6 nm,载药量为8.99%;其饱和溶解度、溶出度和透皮率分别是原料药的148、1.23、4.08倍。结论:所制布洛芬纳米微粉具有良好的水溶性和体外透皮性。
[Abstract]:Objective: to prepare and characterize ibuprofen nano-powder and investigate its transdermal effect in vitro. Methods: the emulsification method was used with chloroform-ethanol 7: 3 V / V) as organic phase and ultrapure water as aqueous phase. The ibuprofen nano-powder was prepared by using polysorbate 80 as surfactant. Laser particle size analysis, scanning electron microscope, Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (FTIR) were used to prepare ibuprofen nanocrystalline powder. The prepared ibuprofen nano-powder was characterized by differential scanning and the saturation solubility of ibuprofen nano-powder and raw material was compared. Results: the formulation and preparation process were determined as follows: the polysorbate 805 mg/m / L, the volume ratio of aqueous phase to organic phase 40: 1. The ibuprofen nanocrystalline powder prepared by ibuprofen concentration 250 mg/m / L, homogenate speed 5000rmin, homogenate time 2 mins, is porous and loose coral, and its chemical structure remains unchanged. From the original crystal state to the amorphous form, the particle size is 179.6 nm, and the drug load is 8.99 nm; The saturated solubility, dissolution and transdermal rate of ibuprofen were 1.234.08 times of that of the raw drug, respectively. Conclusion: the prepared ibuprofen nano-powder has good water solubility and in vitro transdermal properties.
【作者单位】：东北林业大学森林植物生态学教育部重点实验室;
【基金】：国家自然科学基金资助项目(No.21473023)
【分类号】：R943
【正文快照】： 布洛芬(异丁苯丙醇,Ibuprofen)是一类非甾体抗炎药,具有抗炎、镇痛、解热作用。临床上用于轻到中度的偏头痛发作期治疗和预防性治疗,及各类关节和肌肉病变,同时也用于躯体疼痛、手术及外伤后的镇痛[1-3]。但是,由于布洛芬水溶性差,而且口服时会引起溃疡、出血等胃肠道反应[4-6

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