布洛芬纳米微粉的制备、表征及体外透皮性研究
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篇名: | 布洛芬纳米微粉的制备、表征及体外透皮性研究 |
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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/mL、水相-有机相体积比40 ∶ 1、布洛芬质量浓度250 mg/mL、匀浆速度5 000 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 (IBU) nano-powder, and to investigate its transdermal ability in vitro. METHODS: Using chloroform-ethanol (7 ∶ 3, V/V) as organic phase, deionized water as aqueous phase and polysorbate 80 as surfactant, the emulsification method was used to prepare IBU nano-powder. Laser granulometric analysis, Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), differential scanning calorimetry (DSC) were used to characterize IBU nano-powder. IBU nano-powder was compared with bulk drug in respects of saturation solubility, dissolution rate and transdermal rate in vitro. RESULTS: The optimum condition was as follows that the concentration of polysorbate 80 was 5 mg/mL; the volume ratio of water phase-organic phase was 40 ∶ 1; the concentration of IBU was 250 mg/mL; homogenate speed was 5 000 r/min; homogenate time was 2 min. Prepared IBU nano-powder was polyporous crumbly coralliform, and its chemical structure kept stable; the nano-powder changed from crystal to amorphous state; the particle size was 179.6 nm, and drug-loading amount was 8.99%; saturation solubility, dissolution rate and transdermal rate of IBU nano-powder were 148, 1.23 and 4.08 times of bulk drug. CONCLUSIONS: The prepared IBU nano-powder shows good water-solubility and percutaneous permeability. |
期刊: | 2017年第28卷第1期 |
作者: | 邓怡平,赵修华,祖元刚,王璐 |
AUTHORS: | DENG Yiping,ZHAO Xiuhua,ZU Yuangang,WANG Lu |
关键字: | 布洛芬;乳化法;纳米微粉;表征;透皮 |
KEYWORDS: | Ibuprofen; Emulsion method; Nano-powder; Characterization; Transdermal |
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