期刊文献+

淀粉源介孔碳材料改善非诺贝特溶出速率及口服生物利用度研究 被引量:2

The research of improving the dissolution rate and oral bioavailability of fenofibrate by starch-derived mesoporous carbon materials
原文传递
导出
摘要 目的:用淀粉源介孔碳材料(SMC)改善非诺贝特(FNB)的溶出速率,并提高其口服生物利用度。方法:以介孔二氧化硅FDU作为模板制备SMC,通过吸附法将药物FNB载入SMC介孔孔道中制备固体分散体(FNB-SMC)。采用透射电镜(TEM)观察SMC的结构。采用差示扫描量热法(DSC)和X射线衍射法(XRD)对药物在介孔孔道中的存在状态进行表征。利用溶出试验考察FNB-SMC的溶出速率。通过体内实验考察自制片和市售片在家兔体内的血药浓度变化。结果:SMC能抑制FNB的结晶度,使药物以无定型形式存在。溶出试验表明SMC显著提高了FNB的溶出速率。体内试验表明自制片的口服生物利用度明显提高。结论:固体分散体改善难溶性药物的水溶性的同时,提高了口服生物利用度。 Objective: To improve the dissolution rate and the oral bioavailability of fenofibrate (FNB) by using starch-derived mesoporous carbon materials ( SMC). Methods : FDU of mesoporous silica material was used as template for preparing SMC, and FNB was loaded into the mesopores of SMC by adsorption method to prepare solid dispersion (FNB-SMC). The structure of SMC was observed by transmission electron microscopy (TEM). The existing state of FNB in mesoporous pores was characterized by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The dissolution rate of FNB-SMC was investigated by dissolution test. The plasma concentrations of FNB in self-made and commercial tablets were investigated by in vivo experiment in rabbits. Results: SMC could inhibit the crystallinity of FNB, and the drug existed in amorphous form. The dissolution test showed that SMC significantly increased the dissolution rate of FNB. The oral bioavailability of self-made tablets was significantly increased compared to commercial tablets. Conclusion: Solid dispersion technology can improve the water solubility of the insoluble drug. fenofibrate, and increase its oral bioavailahilitv
机构地区 锦州医科大学
出处 《中国新药杂志》 CAS CSCD 北大核心 2016年第17期2014-2020,共7页 Chinese Journal of New Drugs
关键词 非诺贝特 淀粉源介孔碳材料 固体分散体 溶出速率 生物利用度 fenofibrate starch derived mesoporous carbon material solid dispersion dissolution rate bioavailability
  • 相关文献

参考文献15

  • 1JIA ZR,LIN P,XIANG Y,et al.A novel nanomatrix system consisted of colloidal silica and pH-sensitive polymethylacrylate improves the oral bioavailability of fenofibrate[J].Biopharmaceutics,2011,79(1):126-134.
  • 2LI HC,SAKAMOTO Y,LI YS,et al.Synthesis of carbon replicas of SBA-1 and SBA-7 mesoporous silicas[J].Micropor Mesopor Mat,2006,95(1-3):193-199.
  • 3MOHAMMAD BJ,SAEED G,KHOSRO A,et al.Development and characterization of solid dispersion of piroxicam for improvement of dissolution rate using hydrophilic carriers[J].Bioimpacts,2014,4(3):141-148.
  • 4WU C,ZHAO ZZ,ZHAO Y,et al.Preparation of a push-pull osmotic pump of felodipine solubilized by mesoporous silica nanoparticles with a core-shell structure[J].Int J Pharm,2014,475(1-2):298-305.
  • 5高源源,谷福根.非诺贝特-羟丙基-β-环糊精包合物在大鼠体内的药动学及生物利用度研究[J].中南药学,2014,12(5):427-431. 被引量:5
  • 6LIU DF,BIMBO LM,MAKILA E,et al.Co-delivery of a hydrophobic small molecule and a hydrophilic peptide by porous silicon nanoparticles[J].J Control Release,2013,170(2):268-278.
  • 7SAREEN S,MUTREJA V,PAL B,et al.Homogeneous dispersion of Au nanoparticles into mesoporous SBA-15 exhibiting improved catalytic activity for nitroaromatic reduction[J].Micropor Mesopor Mat,2015,202(15):219-225.
  • 8MALEKI A,HAMIDI M.Dissolution enhancement of a model poorly water-soluble drug,atorvastatin,with ordered mesoporous silica:comparison of MSF with SBA-15 as drug carriers[J].Expert Opin Drug Del,2016,13(2):171-181.
  • 9ZHAO P,JIANG H,JIANG T,et al.Inclusion of celecoxib into fibrous ordered mesoporous carbon for enhanced oral bioavailability and reduced gastric irritancy[J].Eur J Pharm Sci,2012,45(5):639-647.
  • 10BOULEDJOUIDJA A,MASMOUDI Y,VAN SM,et al.Impregnation of fenofibrate on mesoporous silica using supercritical carbon dioxide[J].Int J Pharm,2016,499(1-2):1-9.

二级参考文献65

  • 1邱枫,肇丽梅,何晓静,孙亚欣.人血浆中非诺贝特酸的测定及其药动学研究[J].华西药学杂志,2008,23(3):308-309. 被引量:2
  • 2WANG Xin-yu, CAI Shou-guang, WU Yi-fen, LI Jun-ying, YANG Wen-xiu, HU Fen Key Laboratory of Bioactive Materials of Education Ministry, School of Physics, Nankai University, Tianjin 300071, China.Inhibition of Emodin on LPS-induced Nitric Oxide Generation by Suppressing PLC-γ Phosphorylation in Rat Peritoneal Macrophages[J].Chinese Herbal Medicines,2010,2(3):189-194. 被引量:8
  • 3徐帆,冯恩富,余昉.HPLC法测定血浆中非诺贝特活性代谢物非诺贝酸的浓度[J].中国药师,2007,10(6):530-532. 被引量:9
  • 4郑杨,张志丽,王立红,等.非诺贝特固体分散体制备工艺研究及比较[J].中国药剂学杂志,2012,10(2):26-34.
  • 5Guay DR. Micronized fenofibrate: a new fibric acid hypolipidemic agent [J]. Ann Pharmacother, 1999, 33 (10) : 1083-1103.
  • 6Patel AR, Vavia PR. Preparation and in vivo evaluation of SMEDDS ( self-microemulsifying drug delivery system ) con- taining fenofibrate [J]. AAPS J, 2007, 9 ( 3 ) : 344-352.
  • 7Vogt M, Kunath K, Dressman JB. Dissolution enhance- ment of fenofibrate by micronization, cogrinding and spray- drying: comparison with commercial preparations [J]. Eur J PharmBiopharm, 2008, 68 (2) : 283-288.
  • 8Ehen YP, Lu Y, Chen JM, et al. Enhanced bioavailability of abe poorly water-soluble drug fenofibrate by using liposomes containing abile salt [J]. Int J Pharm, 2009, 376 ( 1-2 ) : 153-160.
  • 9Sant VP, Smith D, Leroux JC. Enhancement of oral bioavai- lability of poorly water-soluble drugs by poly ( ethylene glycol ) -block-poly ( alkylacrylate-co-methacrylic acid ) self- assemblies [J]. J Control Rel, 2005, 104 ( 2 ) : 289-300.
  • 10Hanafy A, Spahn-Langguth H, Vergnault G, et al. Pharma- cokinetic evaluation of oral fenofibrate nanosuspensions and SLN in comparison to conventional suspensions of micronized drug [J]. Adv Drug Deliv Rev, 2007, 59 ( 6 ) : 419-426.

共引文献41

同被引文献29

引证文献2

二级引证文献3

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部