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/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。
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 polysorbate80 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/m L;the volume ratio of water phase-organic phase was 40∶1;the concentration of IBU was 250 mg/m L;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.
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 polysorbate80 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/m L;the volume ratio of water phase-organic phase was 40∶1;the concentration of IBU was 250 mg/m L;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.
引文
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[3]王玉杰,胡剑,赵凯.布洛芬混悬液口服治疗儿童急性发热退热的疗效观察[J].临床合理用药杂志,2013,6(7C):47-48.
[4]Wang JJ,Dai DY,Qiu QQ,et al.Evaluation of anti-inflammatory and analgesic effects of synthesized derivatives of ibuprofen[J].Chemical Biology&Drug Design,2015,85(5):623-632.
[5]杨国瑛,阮淑芳.儿童使用布洛芬致不良反应15例回顾性分析[J].中国药房,2014,25(8):727-728.
[6]周晓梅,兰玉梅.布洛芬的不良反应33例文献分析[J].中国医药科学,2013,3(9):76-77.
[7]张莉,齐刚,朱辉.布洛芬透皮吸收制剂的家兔体内药代动力学研究[J].中国药学杂志,2000,35(3):47-49.
[8]赵修华,刘影,王卫国,等.微粉化反式肉桂酸的反溶剂重结晶法制备与表征[J].中草药,2014,45(15):2165-2171.
[9]刘楠,王卫京,赵启成,等.利用超临界CO2制备聚合物载药微粒的研究进展[J].化工新型材料,2015,43(10):212-214、217.
[10]刘克.超临界二氧化碳技术制备纳米药物颗粒的研究[D].北京:北京化工大学,2015.
[11]闫俊锋.布洛芬微粉化的研究[D].天津:天津大学,2010.
[12]Li Y,Zhao XH,Zu YG,et al.Preparation and characterization of paclitaxel nanosuspension using novel emulsification method by combining high speed homogenizer and high pressure homogenization[J].Int J Pharm,2015,490(1/2):324-333.
[13]Zu YG,Meng L,Zhao XH,et al.Preparation of 10-hydroxycamptothecin-loaded glycyrrhizic acid-conjugated bovine serum albumin nanoparticles for hepatocellular carcinoma-targeted drug delivery[J].Int J Nanomedicine,2013:10.2147/IJN.S40493.
[14]肖志方.美洛昔康固体脂质纳米粒的制备及体外透皮研究[J].中国药师,2015,18(9):1512-1515.