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ZHANG Yajie, LIU Xiaoqing, CHEN Min, CHAI Fujuan, ZHENG Chunli, LIU Jianping. Preparation and in vitro evaluation of dabigatran etexilate nanoemulsion[J]. Journal of China Pharmaceutical University, 2016, 47(6): 688-693. DOI: 10.11665/j.issn.1000-5048.20160610
Citation: ZHANG Yajie, LIU Xiaoqing, CHEN Min, CHAI Fujuan, ZHENG Chunli, LIU Jianping. Preparation and in vitro evaluation of dabigatran etexilate nanoemulsion[J]. Journal of China Pharmaceutical University, 2016, 47(6): 688-693. DOI: 10.11665/j.issn.1000-5048.20160610
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Preparation and in vitro evaluation of dabigatran etexilate nanoemulsion

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  • The purpose of this study was to prepare dabigatran etexilate nanoemulsion to improve bioavailability of dabigatran etexilate, a poorly water-soluble drug. The physicochemical properties and the stability of dabigatran etexilate nanoemulsion were investigated. Equilibrium solubility of dabigatran etexilate in commonly used oil materials for nanoemulsion were determined for selection. Then, surfactant and co-surfactant were chosen based upon the plooted pseudo-ternary diagrams. The formulation and preparation process were further optimized with orthogonal design. As a result, the dabigatran etexilate nanoemulsion was formulated based on the system consisting of Oil Acid/Labrafac Lipophile WL1394/Cremophor RH40/Transcutol P/H2O. The dabigatran etexilate nanoemulsion was found to have a mean diameter of(57. 5±0. 2)nm, Zeta potential of -(20. 9±1. 4)mV, and the drug encapsulation efficiency of(85. 2±1. 0)%. Besides, the droplet size, stability constant and drug content of the nanoemulsion was found to have no significant changes in at least 3 months under room temperature. In conclusion, the uniform and stable dabigatran etexilate nanoemulsion with a clear and translucent appearance was obtained after the optimization of formulation and preparation process. Thus nanoemulsion could be a promising way for the improvement of bioavailability of dabigatran etexilate and other poorly water-soluble drugs.
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    • References (16)
  • [1]
    Bassiouny M,Saliba W,Rickard J,et al.Use of dabigatran for periprocedural anticoagulation in patients undergoing catheter ablation for atrial fibrillation[J].Circ Arrhythm Electrophysiol,2013,6(3):460-466.
    [2]
    Ishikawa T,Matsunaga N,Tawada H,et al. TAK-599,a novel N-phosphono type prodrug of anti-MRSA cephalosporin T-91825:synthesis,physicochemical and pharmacological properties[J].Bioorg Med Chem,2003,11(11):2427-2437.
    [3]
    Bellamy L,Rosencher N,Eriksson BI.Adherence to a new oral anticoagulant treatment prescription:dabigatran etexilate[J].Patient Prefer Adherence,2009,3:173-177.
    [4]
    Moreno GG,Salvatierra AA,Martin-Piedra MA,et al.Dabigatran and rivaroxaban,new oral anticoagulants.New approaches in Dentistry[J].J Clin Exp Dent,2010,2(1):1-5.
    [5]
    Yang M,He S,Fan Y,et al.Microenvironmental pH-modified solid dispersions to enhance the dissolution and bioavailability of poorly water-soluble weakly basic GT0918,a developing anti-prostate cancer drug:preparation,characterization and evaluation in vivo[J].Int J Pharm,2014,475(1/2):97-109.
    [6]
    Wang XR,Liu P,Wang SH,et al.Influence of pH on dissolution and oil-water partition coefficient of dabigatran etexilate[J].Chin New Drugs J(中国新药杂志),2013,22(24):2933-2937.
    [7]
    Carlert S,Lennernäs H,Abrahamsson B.Evaluation of the use of classical nucleation theory for predicting intestinal crystalline precipitation of two weakly basic BCS classⅡ drugs[J].Eur J Pharm Sci,2014,53(1):17-27.
    [8]
    Stillhart C,Dürr D,Kuentz M.Toward an improved understanding of the precipitation behavior of weakly basic drugs from oral lipid-based formulations[J].J Pharm Sci,2014,103(4):1194-1203.
    [9]
    Yang PF,Chen WD.Research progress of nanoemulsion applications in improving the bioavailability of poor water-soluble drugs[J].Chin Pharm J(中国药学杂志),2013,48(15):1238-1244.
    [10]
    Yao J,Lu Y,Zhou JP et al.Preparation of nobiletin-loaded self-microemulsifying system and its absorption kinetics in rat intestines[J].J China Pharm Univ(中国药科大学学报),2007,38(1):35-38.
    [11]
    Hu L,Wu H,Niu F,et al.Design of fenofibrate microemulsion for improved bioavailability[J].Int J Pharm,2011,420(2):251-255.
    [12]
    Li JL,Zheng CL,Liu JP,et al.Formulation and process optimization of doxorubicin-loaded PLGA nanoparticles and its in vitro release[J]. Acta Pharm Sin(药学学报),2013,48(5):759-766.
    [13]
    Liu Y,Tao SY,Guo WY.Determination of entrapment efficiency of oxaliplatin liposomes by sephadex microcolumn combined with HPLC[J].China J Mod Appl Pharm(中国现代应用药学),2014,1(31):74-77.
    [14]
    He SN.Preparation and characterization of docetaxel phospholipid complex submicron emulsion[J].Chin J Pharm(中国药剂学杂志),2010,8(1):9-16.
    [15]
    Zhao X,Liu JP,Zhu JB.Transdermal absorption and pharmacokinetics of theophylline microemulsion[J].J China Pharm Univ(中国药科大学学报),2006,37(1):28-32.
    [16]
    Chen J, Li B, Wu DW, et al. Preparation and evaluation of docetaxel nanoemulsion[J].Chin Pharm J(中国药学杂志),2010,45(7):534-538.
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