期刊文献+

热熔挤出技术制备硝苯地平固体分散体 被引量:8

Preparation of Nifedipine Solid Dispersion by Hot-melt Extrusion Technology
原文传递
导出
摘要 目的利用热熔挤出技术制备难溶性药物硝苯地平固体分散体,提高其溶出度,并进一步制成控释片剂。方法以丙烯酸树脂Ⅳ号、醋酸羟丙甲基纤维素琥珀酸酯、聚乙烯吡咯烷酮共聚物、高取代羟丙基纤维素为载体,采用同向双螺杆热熔挤出机制备硝苯地平固体分散体,考察不同载体挤出物在不同介质中的累积溶出度,为筛选合适的固体分散体,进一步制备控释片做准备。结果利用热熔挤出技术制备的固体分散体均显著提高了硝苯地平的溶出度,通过羟丙基甲基纤维素骨架材料的控制作用,制成了符合零级释放的控释制剂。结论热熔挤出技术制备固体分散体能够提高难溶性药物硝苯地平的溶出度,并能进一步制成符合零级释放的控释片。 OBJECTIVE Hot-melt extrusion technology was used to prepare solid dispersion of nifedipine for improving its dissolution, and moreover controlled-release tablets were prepared based on the solid dispersion. METHODS Acrylic resin IV, hydroxypropylmethylcellulose acetate succinate (HPMCAS), polyethylene pyrrole copolymer(PVP-VA64) and high replace hydroxypropyl cellulose(H-HPC) were selected as carriers. The homonymous double screw extrusion method was used for prepare nifedipine solid dispersion. The dissolution of various extrudates in different mediums were studied. Furthermore, nifedipine tablets were prepared. RESULTS The dissolution of nifedipine was improved significantly by solid dispersion technology and the tablets made by hydroxypropyl methyl cellulose matrix showed the zero order release controlled-release. CONCLUSION Solid dispersion using hot-melt extrusion technology can improve the dissolution of poorly water soluble drug nifedipine, and further form the controlled-release formulation.
出处 《中国现代应用药学》 CAS CSCD 2012年第11期1002-1006,共5页 Chinese Journal of Modern Applied Pharmacy
关键词 热熔挤出 硝苯地平 固体分散体 hot-melt extrusion nifedipine solid dispersion
  • 相关文献

参考文献11

  • 1杨睿,唐星,黄惠锋.热熔挤出技术及其在药物传递系统中的应用[J].中国新药杂志,2007,16(4):279-284. 被引量:26
  • 2HOLSMANN S, BACKENSFELD T, KEITEL S, et al. Melt extrusion-an alternative method for enhancing the dissolution rate of 17β-estradiol hernihydrate [J]. Eur J Pharrn Biopharm, 2000, 49(3): 237-242.
  • 3FORSTER A, HEMPENSTALL J, TUCKER I, et al. Selection of excipients for melt extrusion with two poorly water-soluble drugs by solubility parameter calculation and thermal analysis [J]. Int J Pharm, 2001, 226(1/2): 147-161.
  • 4VERRECK G, SIX K, MOOTER G V, et al .Characterization of solid dispersions of itraconazole and hydroxypropyl- methylcellulose prepared by melt extrusion-partI [J]. Int J Pharm, 2003, 251(1/2): 165-174.
  • 5MEHUYS E, REMON J P, VERVAET C. Production of enteric capsules by means of hot-melt extrusion [J]. Eur J Pharm Sci, 2005, 24(2/3): 207-212.
  • 6GHEBREMESKEL A N, VEMAVARAPU C, LODAYA M. Use of surfactants as plasticizers in preparing solid dispersions of poorly soluble API: Selection of polymer surfactant combinations using solubility parameters and testing the processability [J]. Int J Pharm, 2007, 328(2): 119-129.
  • 7REPKA M A, MCGINITY J W. Bioadhesive properties of hydroxypropylcellulose topical films produced by hot-melt extrusion [J]. J Control Release, 2001, 70(3): 341-351.
  • 8CROWLEY M M, FREDERSDORF A, SCHROEDER B, et al. The influence of guaifenesin and ketoprofen on the properties of hot-melt extruded polyethylene oxide films [J]. Eur J Pharm Sci, 2004, 22(5): 409-418.
  • 9朱海彦,方增军,孙杰,张曼红.热熔制粒在口服固体制剂中的应用[J].中国现代应用药学,2011,28(7):622-629. 被引量:10
  • 10FORSTER A, HEMPENSTALL J, TUCKER I, et al.Selection of excipients for melt extrusion with two poorly water-soluble drugs by solubility parameter calculation and thermal analysis[J].Int J Pharm, 2001, 226(1/2): 147-161.

二级参考文献35

  • 1杨睿,唐星,黄惠锋.热熔挤出技术提高水飞蓟素溶出度的初步研究[J].中国新药杂志,2005,14(11):1305-1308. 被引量:25
  • 2Nakamichi K, Nakano T, Yasuura H. The role of the kneading paddle and the effects of screw revolution speed and water content on the preparation of solid dispersions using a twin-screw extruder[J]. Int J Pharm ,2002,241(2) :203 - 211.
  • 3Hulsmann S, Backensfeld T, Keitel S, et al. Melt extrusion-an alternative method for enhancing the dissolution rate of 17β-estradiol hemihydrate [J]. Eur J Pharm Biopharm, 2000,49(3) :237 - 242.
  • 4Perissutti B, Michael B, Newton JM, et al. Preparation of extruded carbamazepine and PEG4000 as a potential rapid release dosage form [J]. Eur J Pharm B iopharm, 2002,53 (1): 125 - 132.
  • 5Verreck G, Six K, Mooter GV, et al. Characterization of solid dispersions of itraconazole and hydroxypropylmethylcellulose prepared by melt extrusion-partI [ J ]. lnt J Pharm, 2003,251 (1-2): 165 - 174.
  • 6Crowley MM, Schroeder B, Fredersdorf A, et al. Physicochemical properties and mechanism of drug release from ethyl cellulose matrix tablets prepared by direct compression and hot-melt extrusion[J]. Int J Pharm, 2004,269(2): 509 - 522.
  • 7Mehuys E, Vervaet C, Remon JP. Hot-melt extruded ethylcellulose cylinders containing a HPMC-Gelucire(R) core for sustained drug delivery [ J ]. J Controlled Release, 2004, 94 (2-3): 273 - 280.
  • 8Repka MA, Gutta K, Prodduturi S, et al. Characterization of cellulosic hot-melt extruded films containing lidocaine [ J ]. Eur J Pharm Biopharm ,2005,59( 1 ): 189 - 196.
  • 9Crowley MM, Fredersdorf A, Schroeder B, et al. The influence of guaifenesin and ketoprofen on the properties of hot-melt extruded polyethylene oxide films[ J]. Eur J Pharm Sci, 2004,22 ( 5 ): 409 -418.
  • 10Forster A, Hempenstall J, Tucker I, et al. Selection of excipients for melt extrusion with two poorly water-soluble drugs by solubility parameter calculation and thermal analysis [ J ]. Int J Pharm, 2001,226(1-2): 147 - 161.

共引文献52

同被引文献79

引证文献8

二级引证文献25

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