透皮贴剂质量控制与评价研究进展
|
摘要
透皮贴剂可将药物透过皮肤表面非侵入性递送到皮肤深部或循环系统,具有许多优于常规注射剂和口服制剂的优点,国内外已有多种透皮贴剂的上市产品。本文结合国内外透皮贴剂产品上市情况、质量控制现状、体外生物评价方法及皮肤吸收评价的数学模型等对透皮贴剂的质量控制与评价的研究进展进行综述。
Transdermal patches,which can deliver drugs from skin surface to the deep skin or circulatory system in a non-invasive way,have many advantages over conventional injection and oral methods. There are a variety of transdermal patches available in both domestic and overseas. In this review,the research progress of quality control and evaluation of transdermal patch products was expounded in following aspects,such as onsale-products situation,current situation of quality control,in vitro biological evaluation method research,skin absorption mathematical model evaluation and others.
Transdermal patches,which can deliver drugs from skin surface to the deep skin or circulatory system in a non-invasive way,have many advantages over conventional injection and oral methods. There are a variety of transdermal patches available in both domestic and overseas. In this review,the research progress of quality control and evaluation of transdermal patch products was expounded in following aspects,such as onsale-products situation,current situation of quality control,in vitro biological evaluation method research,skin absorption mathematical model evaluation and others.
引文
[1]国家药典委员会.中华人民共和国药典[S]. 2015年版.第四部.北京:中国医药科技出版社,2015:22-23.
[2] WIEDERSBERG S,GUY RH. Transdermal drug delivery:30+years of war and still fighting![J]. J Controlled Release,2014,190:150-156.
[3]平其能,方晓玲,吕高荣.薄层双波长扫描法测定东莨菪碱贴膜的化学稳定性[J].中国医院药学杂志,1992,12(6):246-248.
[4]魏雪芳.硝酸甘油贴膜的含量均匀度和体外释放度测定[J].广东药学院学报,2005,21(1):34-38.
[5]陈蓉,郁琦.半水合雌二醇贴片(松奇)临床应用指导建议[J].实用妇产科杂志,2011,27(3):236-237.
[6]杜亚松.可乐定透皮贴剂临床应用的研究进展[J].上海精神医学,2007,19(3):179-181.
[7]汪平,熊维政,武惠斌,等.芬太尼透皮贴剂的研究进展[J].中国药房,2015,26(32):4596-4598.
[8]马建芳,罗华菲,武余波,等.近期上市的经皮给药制剂[J].世界临床药物,2012,33(8):496-502.
[9] KOKUBO T,SUGIBAYASHI K,MORIMOTO Y. Interaction between drugs and pressure-sensitive adhesives in transdermal therapeutic systems[J]. Pharm Res,1994,11(1):104-107.
[10]胡婧,罗华菲,王浩.压敏胶骨架型透皮给药系统的生产工艺及设备概况[J].中国医药工业杂志,2010,41(1):46-50.
[11]国家药典委员会.中华人民共和国药典[S]. 2015年版.第二部.北京:中国医药科技出版社,2015:130.
[12]国家药典委员会.中华人民共和国药典[S]. 2015年版.第二部.北京:中国医药科技出版社,2015:121.
[13] EDQM. European Pharmacopoeia[M]. 9. 0,2016,873.
[14] EDQM. Guideline on Quality of Transdermal Patches[S]. 2013.
[15] EDQM. European Pharmacopoeia[M]. 9. 0,2016,309-311.
[16] U. S. Pharmacopeia[M]. 41th,2017,5926-5933.
[17] U. S. Pharmacopeia[M]. 41th,2017,8637-8644.
[18]日本厚生省,日本药局方[M].第十七改正版,2016,161-166.
[19]熊玲,张亿,陈红,等.妥洛特罗透皮贴剂的释放度测定及不同测定方法结果比较[J].中国现代应用药学,2017,34(12):1654-1657.
[20]李婧瑜,马云淑,杨子贤,等.克班宁透皮贴剂的制备及其体外经皮渗透实验研究[J].中国新药杂志,2017,26(21):2584-2589.
[21] SIMON GA,MAIBACH HI. The pig as an experimental animal model of percutaneous permeation in man:qualitative and quantitative observations-an overview[J]. Skin Pharmacol Appl Skin Physiol,2000,13(5):229-234.
[22] SINGH S,ZHAO K,SINGH J,In vitro permeability and binding of hydrocarbons in pig ear and human abdominal skin[J]. Drug Chem Toxicol,2002,25(1):83-92.
[23] SATO K,SUGIBAYASHI K,MORIMOTO Y. Species differences in percutaneous absorption of nicorandil[J]. J Pharm Sci,1991,80(2):104-107.
[24] SEKKAT N,KALIA YN,GUY RH,Porcine ear skin as a model for the assessment of transdermal drug delivery to premature neonates[J]. Pharm Res,2004,21(8):1390-1397.
[25] ROY SD,HOU SY,WITHAM SL,et al. Transdermal delivery of narcotic analgesics:comparative metabolism and permeability of human cadaver skin and hairless mouse skin[J]. J Pharm Sci,1994,83(12):1723-1728.
[26] RAVENZWAAY B,LEIBOLD E. A comparison between in vitro rat and human and in vivo rat skin absorption studies[J]. Human Exp Toxicol,2004,23(9):421-430.
[27] NETZLAFF F,LEHR CM,WERTZ PW,et al. The human epidermis models EpiSkin,SkinEthic and EpiDerm:an evaluation of morphology and their suitability for testing phototoxicity,irritancy,corrosivity,and substance transport[J]. Eur J Pharm Biopharm,2005,60(2):167-178.
[28] SCHMOOK FP,MEINGASSNER JG,BILLICH A. Comparison of human skin or epidermis models with human and animal skin in in-vitro percutaneous absorption[J]. Int J Pharm,2001,215(1-2)51-56.
[29] ROY SD,FUJIKI J,FLEITMAN JS. Permeabilities of alkyl paminobenzoates through living skin equivalent and cadaver skin[J]. J Pharm Sci,1993,82(12):1266-1268.
[30] BROWN MB,LAU CH,LIM ST,et al. An evaluation of the potential of linear and nonlinear skin permeation models for the prediction of experimentally measured percutaneous drug absorption[J]. J Pharm Pharmacol,2012,64(4):566-577.
[31] GRASSI M,LAMBERTI G,CASCONE S,et al. Mathematical modeling of simultaneous drug release and in vivo absorption[J].Int J Pharm,2011,418(1):130-141.
[32] LAM LT,SUN Y,DAVEY N,et al. The application of feature selection to the development of Gaussian process models for percutaneous absorption[J]. J Pharm Pharmacol,2010,62(6):738-749.
[33] YANG Z,TENG Y,WANG H,et al. Enhancement of skin permeation of bufalin by limonene via reservoir type transdermal patch:formulation design and biopharmaceutical evaluation[J].Int J Pharm,2013,447(210):231-240.
[34] NADINE G,MICHELE P,REGINA M,et al. The safety,immunogenicity,and acceptability of inactivated influenza vaccine delivered by microneedle patch(TIV-MNP 2015):a randomised,partly blinded,placebo-controlled,phase 1 trial[J]. Lancet,2017,390(10095):649-658.
[2] WIEDERSBERG S,GUY RH. Transdermal drug delivery:30+years of war and still fighting![J]. J Controlled Release,2014,190:150-156.
[3]平其能,方晓玲,吕高荣.薄层双波长扫描法测定东莨菪碱贴膜的化学稳定性[J].中国医院药学杂志,1992,12(6):246-248.
[4]魏雪芳.硝酸甘油贴膜的含量均匀度和体外释放度测定[J].广东药学院学报,2005,21(1):34-38.
[5]陈蓉,郁琦.半水合雌二醇贴片(松奇)临床应用指导建议[J].实用妇产科杂志,2011,27(3):236-237.
[6]杜亚松.可乐定透皮贴剂临床应用的研究进展[J].上海精神医学,2007,19(3):179-181.
[7]汪平,熊维政,武惠斌,等.芬太尼透皮贴剂的研究进展[J].中国药房,2015,26(32):4596-4598.
[8]马建芳,罗华菲,武余波,等.近期上市的经皮给药制剂[J].世界临床药物,2012,33(8):496-502.
[9] KOKUBO T,SUGIBAYASHI K,MORIMOTO Y. Interaction between drugs and pressure-sensitive adhesives in transdermal therapeutic systems[J]. Pharm Res,1994,11(1):104-107.
[10]胡婧,罗华菲,王浩.压敏胶骨架型透皮给药系统的生产工艺及设备概况[J].中国医药工业杂志,2010,41(1):46-50.
[11]国家药典委员会.中华人民共和国药典[S]. 2015年版.第二部.北京:中国医药科技出版社,2015:130.
[12]国家药典委员会.中华人民共和国药典[S]. 2015年版.第二部.北京:中国医药科技出版社,2015:121.
[13] EDQM. European Pharmacopoeia[M]. 9. 0,2016,873.
[14] EDQM. Guideline on Quality of Transdermal Patches[S]. 2013.
[15] EDQM. European Pharmacopoeia[M]. 9. 0,2016,309-311.
[16] U. S. Pharmacopeia[M]. 41th,2017,5926-5933.
[17] U. S. Pharmacopeia[M]. 41th,2017,8637-8644.
[18]日本厚生省,日本药局方[M].第十七改正版,2016,161-166.
[19]熊玲,张亿,陈红,等.妥洛特罗透皮贴剂的释放度测定及不同测定方法结果比较[J].中国现代应用药学,2017,34(12):1654-1657.
[20]李婧瑜,马云淑,杨子贤,等.克班宁透皮贴剂的制备及其体外经皮渗透实验研究[J].中国新药杂志,2017,26(21):2584-2589.
[21] SIMON GA,MAIBACH HI. The pig as an experimental animal model of percutaneous permeation in man:qualitative and quantitative observations-an overview[J]. Skin Pharmacol Appl Skin Physiol,2000,13(5):229-234.
[22] SINGH S,ZHAO K,SINGH J,In vitro permeability and binding of hydrocarbons in pig ear and human abdominal skin[J]. Drug Chem Toxicol,2002,25(1):83-92.
[23] SATO K,SUGIBAYASHI K,MORIMOTO Y. Species differences in percutaneous absorption of nicorandil[J]. J Pharm Sci,1991,80(2):104-107.
[24] SEKKAT N,KALIA YN,GUY RH,Porcine ear skin as a model for the assessment of transdermal drug delivery to premature neonates[J]. Pharm Res,2004,21(8):1390-1397.
[25] ROY SD,HOU SY,WITHAM SL,et al. Transdermal delivery of narcotic analgesics:comparative metabolism and permeability of human cadaver skin and hairless mouse skin[J]. J Pharm Sci,1994,83(12):1723-1728.
[26] RAVENZWAAY B,LEIBOLD E. A comparison between in vitro rat and human and in vivo rat skin absorption studies[J]. Human Exp Toxicol,2004,23(9):421-430.
[27] NETZLAFF F,LEHR CM,WERTZ PW,et al. The human epidermis models EpiSkin,SkinEthic and EpiDerm:an evaluation of morphology and their suitability for testing phototoxicity,irritancy,corrosivity,and substance transport[J]. Eur J Pharm Biopharm,2005,60(2):167-178.
[28] SCHMOOK FP,MEINGASSNER JG,BILLICH A. Comparison of human skin or epidermis models with human and animal skin in in-vitro percutaneous absorption[J]. Int J Pharm,2001,215(1-2)51-56.
[29] ROY SD,FUJIKI J,FLEITMAN JS. Permeabilities of alkyl paminobenzoates through living skin equivalent and cadaver skin[J]. J Pharm Sci,1993,82(12):1266-1268.
[30] BROWN MB,LAU CH,LIM ST,et al. An evaluation of the potential of linear and nonlinear skin permeation models for the prediction of experimentally measured percutaneous drug absorption[J]. J Pharm Pharmacol,2012,64(4):566-577.
[31] GRASSI M,LAMBERTI G,CASCONE S,et al. Mathematical modeling of simultaneous drug release and in vivo absorption[J].Int J Pharm,2011,418(1):130-141.
[32] LAM LT,SUN Y,DAVEY N,et al. The application of feature selection to the development of Gaussian process models for percutaneous absorption[J]. J Pharm Pharmacol,2010,62(6):738-749.
[33] YANG Z,TENG Y,WANG H,et al. Enhancement of skin permeation of bufalin by limonene via reservoir type transdermal patch:formulation design and biopharmaceutical evaluation[J].Int J Pharm,2013,447(210):231-240.
[34] NADINE G,MICHELE P,REGINA M,et al. The safety,immunogenicity,and acceptability of inactivated influenza vaccine delivered by microneedle patch(TIV-MNP 2015):a randomised,partly blinded,placebo-controlled,phase 1 trial[J]. Lancet,2017,390(10095):649-658.