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Preparation of two poor water soluble drugs - nanoporous ZnO solid dispersions and the mechanism of drug dissolution improvement

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Author:: No author available

Journal Title:: Acta Pharmaceutica Sinica

Issue:: 11

DOI:: No doi available

Key Word:: 纳米多孔ZnO;吲哚美辛;西洛他唑;固体分散体;溶出度;无定型

Abstract：以自制的纳米多孔ZnO为载体制备药物固体分散体,并研究固体分散体提高药物溶出度的机制.采用熔融法分别制备吲哚美辛和西洛他唑固体分散体,扫描电镜、比表面分析仪、傅立叶红外光谱、差示扫描量热法和X-射线粉末衍射法表征结果显示纳米多孔ZnO与药物仅存在物理吸附作用,药物以无定型形式高度分散于ZnO纳米孔穴中且ZnO纳米孔穴可以抑制固体分散体中无定型药物于45℃、75％ RH条件下的重结晶.体外溶出度测定结果表明,吲哚美辛固体分散体5 min时的累积溶出度可达到90％左右,西洛他唑固体分散体30min时的累积溶出度可达到80％左右.研究探讨两种药物溶出度提高的机制与纳米多孔ZnO可增加药物分散性、控制药物以无定型形式存在并能抑制药物重结晶有关.

Reference

[1]Augsburger L,Pan X,Julian T.Increasing the dissolution rate of a low-solubility drug through a crystalline-amorphous transition: a case study with indomethacin (correction of indomethicin).[J].2008,34(2).
[2]Zhang P,Liu W.ZnO QD@PMAA-co-PDMAEMA nonviral vector for plasmid DNA delivery and bioimaging.[J].2010,31(11).
[3]Mukai T,Yamada K,Jinno J,etc.Effect of particle size reduction on dissolution and oral absorption of a poorly water-soluble drug, cilostazol, in beagle dogs[J].2006,111(1).
[4]Wang,F.,Hui,H.,Barnes,T.J.,etc.Oxidized mesoporous silicon microparticles for improved oral delivery of poorly soluble drugs[J].2010,7(1).
[5]Kawashima Y,Takeuchi H,Yasuji T.Particle design of poorly water-soluble drug substances using supercritical fluid technologies.[J].2008,60(3).
[6]Surya Singh.Nanomedicine-Nanoscale Drugs and Delivery Systems[J].2010,10(12).
[7]Nohynek GJ,Antignac E,Re T,etc.Safety assessment of personal care products/cosmetics and their ingredients.[J].2010,243(2).
[8]C.S.Andrews,V.L.Kett,D.Q.M.Craig,etc.Identification of Crystalline and Amorphous Regions in Low Molecular Weight Materials Using Microthermal Analysis[J].2001,105(29).
[9]Sun Y,Zhang GG,Yu L,etc.Solubility of small-molecule crystals in polymers: D-mannitol in PVP, indomethacin in PVP/VA, and nifedipine in PVP/VA.[J].2009,26(4).
[10]Agüeros, M.,Irache, J.M.,Zabaleta, V.,etc.Increased oral bioavailability of paclitaxel by its encapsulation through complex formation with cyclodextrins in poly(anhydride) nanoparticles[J].2010,145(1).
[11]Xiaosheng Tang,Eugene Shi Guang Choo,Ling Li.Synthesis of ZnO Nanoparticles with Tunable Emission Colors and Their Cell Labeling Applications[J].2010,22(11).
[12]Zografi G.,Andronis V..Crystal nucleation and growth of indomethacin polymorphs from the amorphous state[J].2000,271(3).
[13]Stowell JG,Morris KR,Chen X,etc.Analysis of the acid-base reaction between solid indomethacin and sodium bicarbonate using infrared spectroscopy, X-ray powder diffraction, and solid-state nuclear magnetic resonance spectroscopy.[J].2005,38(4).
[14]Zhang, J.,Jiang, T.,Wang, Z.,etc.Spherical mesoporous silica nanoparticles for loading and release of the poorly water-soluble drug telmisartan[J].2010,145(3).
[15]Zhang HJ,Chen JP,Ni YW,etc.Porous nanosheet-based ZnO microspheres for the construction of direct electrochemical biosensors[J].2008,24(1).
[16]Yliruusi J,Savolainen M,Strachan C,etc.Better understanding of dissolution behaviour of amorphous drugs by in situ solid-state analysis using Raman spectroscopy.[J].2009,71(1).
[17]Gordon KC,Heinz A,Sandler N,etc.Screening for differences in the amorphous state of indomethacin using multivariate visualization.[J].2007,30(2).
[18]Huang CC,Aronstam RS,Chen D.Oxidative stress, calcium homeostasis, and altered gene expression in human lung epithelial cells exposed to ZnO nanoparticles.[J].2010,24(1).
[19]Kim, JC,Kang, YS,Qiao, R,etc.Fabrication of Hierarchical ZnO Nanostructures via a Surfactant-Directed Process[J].2009,9(6).
[20]Hui Jiang,Chunhui Wu,Dadong Guo.Synergistic cytotoxic effect of different sized ZnO nanoparticles and daunorubicin against leukemia cancer cells under UV irradiation[J].2008,93(3).
[21]Stella VJ,Nti-Addae KW.Prodrug strategies to overcome poor water solubility.[J].2007,59(7).