有序介孔二氧化硅FDU-12载非诺贝特双层渗透泵片的研究
|
摘要
目的利用FDU-12提高难溶性药物非诺贝特(FNB)的溶出速率,并结合双层渗透泵技术实现药物的恒速释放。方法用吸附法将FNB载入FDU-12的有序介孔孔道中形成载药体系FNB-FDU-12。通过粉末X射线衍射法(PXDR)和傅里叶红外光谱法(FTIR)对介孔孔道中FNB的存在状态进行表征。利用体外溶出实验对双层渗透泵片的处方组成进行筛选。结果通过表征结果证明,药物FNB是以无定型形式存在于载体FDU-12介孔孔道中。体外溶出实验表明,FDU-12能明显提高FNB溶出速率,双层渗透泵技术能使药物实现控释释放。结论有序介孔二氧化硅材料FDU-12和双层渗透泵技术的结合能显著改善FNB的溶出速率,并实现难溶性药物的恒速释放。
Objective To increase the dissolution of insoluble drug fenofibrate(FNB) by FDU-12 and achieve zero-level release of drug with dual-layer osmotic pump technology. Methods FNB was loaded into the ordered mesopores of FDU-12 via adsorption to obtain drug loading system(FNB-FDU-12). The existing state of FNB in the mesopores was characterized by powder X-ray diffraction and Fourier transform infrared spectroscopy. The prescription composition of dual-layer osmotic pump tablets was selected by the dissolution test. Results The characterization showed that the drug FNB was present in the mesopore of carrier FDU-12 at an amorphous state. In vitro dissolution tests showed that FDU-12 significantly increased the dissolution rate of FNB, and dual-layer osmotic pump technology controlled the drug release. Conclusion The combination of ordered mesoporous silica FDU-12 and dual-layer osmotic pump technology significantly improves the dissolution rate of FNB and achieve constant release of insoluble drugs.
Objective To increase the dissolution of insoluble drug fenofibrate(FNB) by FDU-12 and achieve zero-level release of drug with dual-layer osmotic pump technology. Methods FNB was loaded into the ordered mesopores of FDU-12 via adsorption to obtain drug loading system(FNB-FDU-12). The existing state of FNB in the mesopores was characterized by powder X-ray diffraction and Fourier transform infrared spectroscopy. The prescription composition of dual-layer osmotic pump tablets was selected by the dissolution test. Results The characterization showed that the drug FNB was present in the mesopore of carrier FDU-12 at an amorphous state. In vitro dissolution tests showed that FDU-12 significantly increased the dissolution rate of FNB, and dual-layer osmotic pump technology controlled the drug release. Conclusion The combination of ordered mesoporous silica FDU-12 and dual-layer osmotic pump technology significantly improves the dissolution rate of FNB and achieve constant release of insoluble drugs.
引文
[1]闰冬梅.非诺贝特作用机制的进展[J].中国医药指南,2012,21(10):467-469.
[2]Niu X,Wan L,Hou Z,et al.Mesoporous carbon as a novel drug carrier of fenofibrate for enhancement of the dissolution and oral bioavailability[J].Int J Pharm,2013,452(1-2):382-389.
[3]陈佳,平其能,陈盛君.非诺贝特微粉化片剂的研制[J].中国医药工业杂志,2003,34(3):130-132.
[4]葛蔓,全东琴.非诺贝特自微乳制剂的体内外评价[J].中国医院药学杂志,2009,29(14):1167-1169.
[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.
[6]时念秋,董钰婷,张秀荣,等.不同载体非诺贝特固体分散体的表征、溶出度和抑晶作用的对比研究[J].中国医药工业杂志,2016,47(8):1016-1021.
[7]邱阳,吴超,赵宗哲,等.SBA-15增溶非洛地平的双层渗透泵片的制备[J].中国新药杂志,2016,25(7):823-829.
[8]李艳芹,邱阳,吴超,等.介孔材料MCM-41与推拉式渗透泵技术联合制备尼群地平口服片的研究[J].中国现代应用药学,2016,33(7):907-912.
[9]邱阳,吴超,蒋杰,等.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[J].中国新药杂志,2016,25(17):2014-2020.
[10]徐杰,赵文明,吴超,等.有序介孔二氧化硅改善双嘧达莫的溶出速率[J].中国新药杂志,2015,24(17):2036-2040.
[11]郭庆明,张晖,苏晓峰,等.非诺贝特双层渗透泵片在Beagle犬体内的药动学研究[J].现代药物与临床,2014,29(6):594-598.
[12]凌静,戚虎昶,傅翔,等.难溶性药物渗透泵制剂制备工艺的研究进展[J].中国药房,2014,25(5):464-466.
[13]李佳,郭玲,宋旭,等.硝苯地平双层渗透泵控释片的制备[J].华西药学杂志,2015,30(1):18-21.
[14]邱阳,吴超,蒋杰,等.非诺贝特-淀粉源介孔碳载体固体分散体双层渗透泵控释片的研究[J].中国药学杂志,2017,52(16):1427-1433.
[15]翁敏劼,陈君琛,赖谱富,等.黄秋葵等外果粉末直接压片工艺研究[J].福建农业学报,2017,32(11):1263-1268.
[2]Niu X,Wan L,Hou Z,et al.Mesoporous carbon as a novel drug carrier of fenofibrate for enhancement of the dissolution and oral bioavailability[J].Int J Pharm,2013,452(1-2):382-389.
[3]陈佳,平其能,陈盛君.非诺贝特微粉化片剂的研制[J].中国医药工业杂志,2003,34(3):130-132.
[4]葛蔓,全东琴.非诺贝特自微乳制剂的体内外评价[J].中国医院药学杂志,2009,29(14):1167-1169.
[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.
[6]时念秋,董钰婷,张秀荣,等.不同载体非诺贝特固体分散体的表征、溶出度和抑晶作用的对比研究[J].中国医药工业杂志,2016,47(8):1016-1021.
[7]邱阳,吴超,赵宗哲,等.SBA-15增溶非洛地平的双层渗透泵片的制备[J].中国新药杂志,2016,25(7):823-829.
[8]李艳芹,邱阳,吴超,等.介孔材料MCM-41与推拉式渗透泵技术联合制备尼群地平口服片的研究[J].中国现代应用药学,2016,33(7):907-912.
[9]邱阳,吴超,蒋杰,等.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[J].中国新药杂志,2016,25(17):2014-2020.
[10]徐杰,赵文明,吴超,等.有序介孔二氧化硅改善双嘧达莫的溶出速率[J].中国新药杂志,2015,24(17):2036-2040.
[11]郭庆明,张晖,苏晓峰,等.非诺贝特双层渗透泵片在Beagle犬体内的药动学研究[J].现代药物与临床,2014,29(6):594-598.
[12]凌静,戚虎昶,傅翔,等.难溶性药物渗透泵制剂制备工艺的研究进展[J].中国药房,2014,25(5):464-466.
[13]李佳,郭玲,宋旭,等.硝苯地平双层渗透泵控释片的制备[J].华西药学杂志,2015,30(1):18-21.
[14]邱阳,吴超,蒋杰,等.非诺贝特-淀粉源介孔碳载体固体分散体双层渗透泵控释片的研究[J].中国药学杂志,2017,52(16):1427-1433.
[15]翁敏劼,陈君琛,赖谱富,等.黄秋葵等外果粉末直接压片工艺研究[J].福建农业学报,2017,32(11):1263-1268.