缓控释微丸释药速率影响因素的研究与应用
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摘要
微丸作为一种多单元给药系统具有良好的释放调节性,其独特优势使它逐渐成为现代药物传递系统的重要组成部分。本文通过查阅近年来国内外相关文献,归纳总结了影响缓控释微丸释药速率的关键因素,包括药物溶解度、填充辅料和包衣材料等,并对调控微丸释药速率的一系列方法进行了概括,旨在为新型缓控释微丸的开发提供思路和科学依据。
Pellets as multi-unit drug delivery system has gradually become an important component of modern drug delivery systems due to its special superiority especially the good regulatory of the release. The recent progress of factors that affect the drug release rate from sustained-controlled release pellets including drug solubility,pharmaceutic adjuvant and coating technique were reviewed and series of methods to regulate the drug release rate of pellets were summarized in the article in order to provide new ideas and scientific evidence for further investigation and applications of the new patterns of sustained-controlled release pellets.
Pellets as multi-unit drug delivery system has gradually become an important component of modern drug delivery systems due to its special superiority especially the good regulatory of the release. The recent progress of factors that affect the drug release rate from sustained-controlled release pellets including drug solubility,pharmaceutic adjuvant and coating technique were reviewed and series of methods to regulate the drug release rate of pellets were summarized in the article in order to provide new ideas and scientific evidence for further investigation and applications of the new patterns of sustained-controlled release pellets.
引文
[1]国家药典委员会.中华人民共和国药典[S]. 2015年版.一部.北京:中国医药科技出版社,2015:附录ⅠA丸剂.
[2]陈兴荣,刘晓莎,方炳虎,等.缓控释微丸的研究进展[J].中国兽药杂志,2009,43(8):46-50.
[3]陆彬.药物新剂型与新技术[M].北京:人民卫生出版社,2005.
[4]唐星.口服缓控释制剂[M].北京:人民卫生出版社,2007:97.
[5] KIM KS,JIN SG,MUSTAPHA O,et al. Novel fenofibric acidloaded controlled release pellet bioequivalent to choline fenofibrate-loaded commercial product in beagle dogs[J]. Int J Pharm(Amsterdam,Neth),2015,490(1-2):273-280.
[6] YU H,PAN L,LI P,et al. Nitrofurantoin enteric pellets with high bioavailability based on aciform crystalline formation by wet milling[J]. Pharm Dev Technol,2014,20(4):433-441.
[7] MA J,WANG J,CHENG Z,et al. Sustained-release pellets of nifedipine using microcrystals combined with MCC-based matrix[J]. Drug Dev Ind Pharm,2015,41(2):307-314.
[8]陈振华,管咏梅,朱卫丰,等.白头翁总皂苷-羟丙基-β-环糊精包合物结肠靶向微丸的制备[J].中国中药杂志,2013,38(24):4292-4297.
[9] GUPTA NK,DIXIT VK. Bioavailability enhancement of curcumin by complexation with phosphatidyl choline[J]. J Pharm Sci(Philadelphia,PA,U. S.),2011,100(5):1987-1995.
[10] MA H,CHEN H,SUN L,et al. Improving permeability and oral absorption of mangiferin by phospholipid complexation[J]. Fitoterapia,2014,93(3):54-61.
[11] SANT VP,SMITH D,LEROUX JC. Enhancement of oral bioavailability of poorly water-soluble drugs by poly(ethylene glycol)-block-poly(alkyl acrylate-co-methacrylic acid)self-assemblies[J]. J Controlled Release,2005,104(2):289-300.
[12] SINGH C,BHATT TD,GILL MS,et al. Novel rifampicin-phospholipid complex for tubercular therapy:synthesis,physicochemical characterization and in-vivo evaluation[J]. Int J Pharm,2014,460(1-2):220-227.
[13] ZHANG S,YAN H,YU P,et al. Development of protocatechualdehyde proliposomes-based sustained-release pellets with improved bioavailability and desired pharmacokinetic behavior for angina chronotherapy[J]. Eur J Pharm Sci,2016,93:341-350.
[14] MIAO Y,CHEN G,REN L,et al. Preparation and evaluation of ziprasidone-phospholipid complex from sustained-release pellet formulation with enhanced bioavailability and no food effect[J].J Pharm Pharmacol,2016,68(2):185-194.
[15] SEMALTY A,SEMALTY M,SINGH D,et al. Development and physicochemical evaluation of pharmacosomes of diclofenac[J].Acta Pharm,2009,59(3):335-344.
[16] JOVANA J,LJILJANA D,VLADIMIR DI,et al. Evaluation of critical formulation parameters in design and differentiation of self-microemulsifying drug delivery systems(SMEDDSs)for oral delivery of aciclovir[J]. Int J Pharm(Amsterdam, Neth),2016,497(2):301-311.
[17] XU Y,WANG Q,FENG Y,et al. Enhanced oral bioavailability of[6]-Gingerol-SMEDDS:preparation,in vitro and in vivo evaluation[J]. J Funct Foods,2016,27:703-710.
[18] NESLIHAN GR,BENITA S. Self-emulsifying drug delivery systems(SEDDS)for improved oral delivery of lipophilic drugs[J].Biomed Pharmacother,2004,58(3):173.
[19] SELJAK KB,BERGINC K,TRONTELJ J,et al. A self-microemulsifying drug delivery system to overcome intestinal resveratrol toxicity and presystemic metabolism[J]. J Pharm Sci(Philadelphia,PA,U. S.),2014,103(11):3491-3500.
[20] MANNINA P,SEGALE L,GIOVANNELLI L,et al. Self-emulsifying excipient platform for improving technological properties of alginate-hydroxypropylcellulose pellets[J]. Int J Pharm(Amsterdam,Neth),2016,499(1-2):74-80.
[21] GU Z,SHI X,OMARI E,et al. Self-microemulsifying sustainedrelease pellet of Ginkgo biloba extract,preparation,in vitro drug release and pharmacokinetics study in beagle dogs[J]. J Drug Delivery Sci Technol,2017,37:184-193.
[22]赵呈雷,黄一平.葛根素固体自乳化微丸的制备研究[J].中成药,2012,34(4):653-657.
[23]王海霞.正交实验设计优化槲皮素自乳化微丸的制备[J].中国伤残医学,2011,19(3):90-91.
[24]刘丹,张露,张振海,等.银杏黄酮组分自微乳-微丸释药系统的构建[J].中草药,2017,48(16):3377-3383.
[25]杨静,韩静,孙铭,等.喷雾干燥法制备丹参酮ⅡA自乳化微丸[J].医药导报,2010,29(7):920-922.
[26] KENDRE PN,CHAUDHARI PD. Effect of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer on bioadhesion and release rate property of eplerenone pellets[J].Drug Dev Ind Pharm,2016,43(5):1-11.
[27] IOVANOV RSI,TIT,BARBU A,et al. Preparation and in vitro characterization of pellets containing felodipine solid dispersions[J]. Farmacia,2015,63(5):639-646.
[28] ZHANG Y,HUANG Z,OMARI E,et al. Preparation and in vitro-in vivo evaluation of sustained-release matrix pellets of capsaicin to enhance the oral bioavailability[J]. AAPS Pharm Sci Tech,2016,17(2):339-349.
[29]梅康康,胡容峰,罗志红,等.球晶技术固体自微乳法制备水飞蓟宾缓释微丸[J].中国医院药学杂志,2014,34(21):1826-1831.
[30]任君刚,邹梅娟,王悦,等.硝苯地平骨架缓释微丸的制备及在家犬体内的药物动力学[J].沈阳药科大学学报,2007,24(2):70-73.
[31]赖春花,邱天健,郑琴,等.丹参总酮缓释微丸的制备及处方工艺优化[J].中国实验方剂学杂志,2013,19(13):18-21.
[32]杨翎,毕瑞林.硫酸沙丁胺醇缓释微丸的制备[J].黑龙江医药,2000,13(6):339-340.
[33]陈斌,萧伟,贾晓斌,等.通脉复方微丸多元释药系统中丹参酮缓释单元的制备工艺[J].中国实验方剂学杂志,2012,18(4):39-42.
[34] ALVAREZ L,CONCHEIRO A,GMEZ JL,et al. Powdered cellulose as excipient for extrusion-spheronization pellets of a cohesive hydrophobic drug[J]. Eur J Pharm Biopharm,2003,55(3):291-295.
[35] STECKEL H,MINDERMANNNOGLY F. Production of chitosan pellets by extrusion/spheronization[J]. Eur J Pharm Biopharm,2004,57(1):107-114.
[36] SOUTO C,RODRGUEZ A,PARAJES S,et al. A comparative study of the utility of two superdisintegrants in microcrystalline cellulose pellets prepared by extrusion-spheronization[J]. Eur J Pharm Biopharm,2005,61(1-2):94-99.
[37] KRANZ H,JRGENS K,PINIER M,et al. Drug release from MCC-and carrageenan-based pellets:experiment and theory[J].Eur J Pharm Biopharm,2009,73(2):302-309.
[38] DREU R,IRCA J,PINTYE K,et al. Physicochemical properties of granulating liquids and their influence on microcrystalline cellulose pellets obtained by extrusion-spheronisation technology[J]. Int J Pharm(Amsterdam,Neth),2005,291(1-2):99-111.
[39] GAREKANI HA,NOKHODCHI A,RAYENI MA,et al. Preparation and characterization and release properties of Eudragit RS based ibuprofen pellets prepared by extrusion spheronization:effect of binder type and concentration[J]. Drug Dev Ind Pharm,2013,39(8):1238-1246.
[40] TAVAKOLI N,MINAIYAN M,TABBAKHIAN M,et al. Preparation and evaluation of a controlled drug release of repaglinide through matrix pellets:in vitro and in vivo studies[J]. J Microencapsulation,2014,31(6):529-534.
[41] BALAXI M,NIKOLAKAKIS I,KACHRIMANIS K,et al. Combined effects of wetting,drying,and microcrystalline cellulose type on the mechanical strength and disintegration of pellets[J].J Pharm Sci(Philadelphia,PA,U. S.),2009,98(2):676-689.
[42] SARKAR S,LIEW CV. Moistening liquid-dependent de-aggregation of microcrystalline cellulose and its impact on pellet formation by extrusion-spheronization[J]. AAPS Pharm Sci Tech,2014,15(3):753-761.
[43] GURRAM RK,GANDRA S,SHASTRI NR. Design and optimization of disintegrating pellets of MCC by non-aqueous extrusion process using statistical tools[J]. Eur J Pharm Sci,2016,84:146-156.
[44]陈盛君,朱家壁.缓控释微丸制剂的研究进展[J].国外医学(药学分册),2004,31(3):177-181.
[45]张丹参,梅艳飞,宋晓敏,等.大黄结肠靶向微丸的制备及处方优化[J].中草药,2016,47(8):1321-1326.
[46]高捷,朱淼,沃联群,等.多索茶碱脉冲控释微丸的研制[J].中国现代应用药学,2016,33(7):895-900.
[47]李闻涛,万科,杨莹,等.何首乌抗性淀粉促进靶向结肠微丸体外药物释放研究[J].中国药业,2017,26(17):6-9.
[48]汪忠军,赵月,王颖,等.琥珀酸去甲文拉法辛膜控与骨架结合型缓释微丸的制备及释放特性研究[J].华西药学杂志,2018,33(2):126-130.
[49]茹庆国,彭宇,马书伟,等.响应面分析法优化当归超临界提取物结肠定位微丸的制备工艺研究[J].中国中药杂志,2016,41(13):2442-2448.
[50]秦永丽,张宇,于莲,等.结肠靶向剂黄芪多糖微丸制备工艺研究[J].中国药学杂志,2016,51(1):35-39.
[51] BRUCE LD,PETEREIT HU,BECKERT T,et al. Properties of enteric coated sodium valproate pellets[J]. Int J Pharm(Amsterdam,Neth),2003,264(1-2):85-96.
[52] ENAYATIFARD R,MAHJOOB A,EBRAHIMI P,et al. Evaluation of the effect of physical variables on in vitro release of diclofenac pellets using Box-Behnken design[J]. Iran J Basic Med Sci,2015,18(7):710-714.
[53]汪少,杨恒博,袁婷,等.溴吡斯的明包衣缓释微丸的研制[J].中国医药工业杂志,2019,50(1):84-92.
[54] KAN S,LI J,LIU J,et al. Preparation and IVIVC evaluation of salvianolic acid B micro-porous osmotic pump pellets[J]. Drug Dev Ind Pharm,2015,41(3):476-481.
[55] DEKYNDT B,VERIN J,NEUT C,et al. How to easily provide zero order release of freely soluble drugs from coated pellets[J].Int J Pharm(Amsterdam,Neth),2015,478(1):31-38.
[56] YANG Q,MA Y,ZHU J. Applying a novel electrostatic dry powder coating technology to pellets[J]. Eur J Pharm Sci,2015,97(Pt A):118-124.
[2]陈兴荣,刘晓莎,方炳虎,等.缓控释微丸的研究进展[J].中国兽药杂志,2009,43(8):46-50.
[3]陆彬.药物新剂型与新技术[M].北京:人民卫生出版社,2005.
[4]唐星.口服缓控释制剂[M].北京:人民卫生出版社,2007:97.
[5] KIM KS,JIN SG,MUSTAPHA O,et al. Novel fenofibric acidloaded controlled release pellet bioequivalent to choline fenofibrate-loaded commercial product in beagle dogs[J]. Int J Pharm(Amsterdam,Neth),2015,490(1-2):273-280.
[6] YU H,PAN L,LI P,et al. Nitrofurantoin enteric pellets with high bioavailability based on aciform crystalline formation by wet milling[J]. Pharm Dev Technol,2014,20(4):433-441.
[7] MA J,WANG J,CHENG Z,et al. Sustained-release pellets of nifedipine using microcrystals combined with MCC-based matrix[J]. Drug Dev Ind Pharm,2015,41(2):307-314.
[8]陈振华,管咏梅,朱卫丰,等.白头翁总皂苷-羟丙基-β-环糊精包合物结肠靶向微丸的制备[J].中国中药杂志,2013,38(24):4292-4297.
[9] GUPTA NK,DIXIT VK. Bioavailability enhancement of curcumin by complexation with phosphatidyl choline[J]. J Pharm Sci(Philadelphia,PA,U. S.),2011,100(5):1987-1995.
[10] MA H,CHEN H,SUN L,et al. Improving permeability and oral absorption of mangiferin by phospholipid complexation[J]. Fitoterapia,2014,93(3):54-61.
[11] SANT VP,SMITH D,LEROUX JC. Enhancement of oral bioavailability of poorly water-soluble drugs by poly(ethylene glycol)-block-poly(alkyl acrylate-co-methacrylic acid)self-assemblies[J]. J Controlled Release,2005,104(2):289-300.
[12] SINGH C,BHATT TD,GILL MS,et al. Novel rifampicin-phospholipid complex for tubercular therapy:synthesis,physicochemical characterization and in-vivo evaluation[J]. Int J Pharm,2014,460(1-2):220-227.
[13] ZHANG S,YAN H,YU P,et al. Development of protocatechualdehyde proliposomes-based sustained-release pellets with improved bioavailability and desired pharmacokinetic behavior for angina chronotherapy[J]. Eur J Pharm Sci,2016,93:341-350.
[14] MIAO Y,CHEN G,REN L,et al. Preparation and evaluation of ziprasidone-phospholipid complex from sustained-release pellet formulation with enhanced bioavailability and no food effect[J].J Pharm Pharmacol,2016,68(2):185-194.
[15] SEMALTY A,SEMALTY M,SINGH D,et al. Development and physicochemical evaluation of pharmacosomes of diclofenac[J].Acta Pharm,2009,59(3):335-344.
[16] JOVANA J,LJILJANA D,VLADIMIR DI,et al. Evaluation of critical formulation parameters in design and differentiation of self-microemulsifying drug delivery systems(SMEDDSs)for oral delivery of aciclovir[J]. Int J Pharm(Amsterdam, Neth),2016,497(2):301-311.
[17] XU Y,WANG Q,FENG Y,et al. Enhanced oral bioavailability of[6]-Gingerol-SMEDDS:preparation,in vitro and in vivo evaluation[J]. J Funct Foods,2016,27:703-710.
[18] NESLIHAN GR,BENITA S. Self-emulsifying drug delivery systems(SEDDS)for improved oral delivery of lipophilic drugs[J].Biomed Pharmacother,2004,58(3):173.
[19] SELJAK KB,BERGINC K,TRONTELJ J,et al. A self-microemulsifying drug delivery system to overcome intestinal resveratrol toxicity and presystemic metabolism[J]. J Pharm Sci(Philadelphia,PA,U. S.),2014,103(11):3491-3500.
[20] MANNINA P,SEGALE L,GIOVANNELLI L,et al. Self-emulsifying excipient platform for improving technological properties of alginate-hydroxypropylcellulose pellets[J]. Int J Pharm(Amsterdam,Neth),2016,499(1-2):74-80.
[21] GU Z,SHI X,OMARI E,et al. Self-microemulsifying sustainedrelease pellet of Ginkgo biloba extract,preparation,in vitro drug release and pharmacokinetics study in beagle dogs[J]. J Drug Delivery Sci Technol,2017,37:184-193.
[22]赵呈雷,黄一平.葛根素固体自乳化微丸的制备研究[J].中成药,2012,34(4):653-657.
[23]王海霞.正交实验设计优化槲皮素自乳化微丸的制备[J].中国伤残医学,2011,19(3):90-91.
[24]刘丹,张露,张振海,等.银杏黄酮组分自微乳-微丸释药系统的构建[J].中草药,2017,48(16):3377-3383.
[25]杨静,韩静,孙铭,等.喷雾干燥法制备丹参酮ⅡA自乳化微丸[J].医药导报,2010,29(7):920-922.
[26] KENDRE PN,CHAUDHARI PD. Effect of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer on bioadhesion and release rate property of eplerenone pellets[J].Drug Dev Ind Pharm,2016,43(5):1-11.
[27] IOVANOV RSI,TIT,BARBU A,et al. Preparation and in vitro characterization of pellets containing felodipine solid dispersions[J]. Farmacia,2015,63(5):639-646.
[28] ZHANG Y,HUANG Z,OMARI E,et al. Preparation and in vitro-in vivo evaluation of sustained-release matrix pellets of capsaicin to enhance the oral bioavailability[J]. AAPS Pharm Sci Tech,2016,17(2):339-349.
[29]梅康康,胡容峰,罗志红,等.球晶技术固体自微乳法制备水飞蓟宾缓释微丸[J].中国医院药学杂志,2014,34(21):1826-1831.
[30]任君刚,邹梅娟,王悦,等.硝苯地平骨架缓释微丸的制备及在家犬体内的药物动力学[J].沈阳药科大学学报,2007,24(2):70-73.
[31]赖春花,邱天健,郑琴,等.丹参总酮缓释微丸的制备及处方工艺优化[J].中国实验方剂学杂志,2013,19(13):18-21.
[32]杨翎,毕瑞林.硫酸沙丁胺醇缓释微丸的制备[J].黑龙江医药,2000,13(6):339-340.
[33]陈斌,萧伟,贾晓斌,等.通脉复方微丸多元释药系统中丹参酮缓释单元的制备工艺[J].中国实验方剂学杂志,2012,18(4):39-42.
[34] ALVAREZ L,CONCHEIRO A,GMEZ JL,et al. Powdered cellulose as excipient for extrusion-spheronization pellets of a cohesive hydrophobic drug[J]. Eur J Pharm Biopharm,2003,55(3):291-295.
[35] STECKEL H,MINDERMANNNOGLY F. Production of chitosan pellets by extrusion/spheronization[J]. Eur J Pharm Biopharm,2004,57(1):107-114.
[36] SOUTO C,RODRGUEZ A,PARAJES S,et al. A comparative study of the utility of two superdisintegrants in microcrystalline cellulose pellets prepared by extrusion-spheronization[J]. Eur J Pharm Biopharm,2005,61(1-2):94-99.
[37] KRANZ H,JRGENS K,PINIER M,et al. Drug release from MCC-and carrageenan-based pellets:experiment and theory[J].Eur J Pharm Biopharm,2009,73(2):302-309.
[38] DREU R,IRCA J,PINTYE K,et al. Physicochemical properties of granulating liquids and their influence on microcrystalline cellulose pellets obtained by extrusion-spheronisation technology[J]. Int J Pharm(Amsterdam,Neth),2005,291(1-2):99-111.
[39] GAREKANI HA,NOKHODCHI A,RAYENI MA,et al. Preparation and characterization and release properties of Eudragit RS based ibuprofen pellets prepared by extrusion spheronization:effect of binder type and concentration[J]. Drug Dev Ind Pharm,2013,39(8):1238-1246.
[40] TAVAKOLI N,MINAIYAN M,TABBAKHIAN M,et al. Preparation and evaluation of a controlled drug release of repaglinide through matrix pellets:in vitro and in vivo studies[J]. J Microencapsulation,2014,31(6):529-534.
[41] BALAXI M,NIKOLAKAKIS I,KACHRIMANIS K,et al. Combined effects of wetting,drying,and microcrystalline cellulose type on the mechanical strength and disintegration of pellets[J].J Pharm Sci(Philadelphia,PA,U. S.),2009,98(2):676-689.
[42] SARKAR S,LIEW CV. Moistening liquid-dependent de-aggregation of microcrystalline cellulose and its impact on pellet formation by extrusion-spheronization[J]. AAPS Pharm Sci Tech,2014,15(3):753-761.
[43] GURRAM RK,GANDRA S,SHASTRI NR. Design and optimization of disintegrating pellets of MCC by non-aqueous extrusion process using statistical tools[J]. Eur J Pharm Sci,2016,84:146-156.
[44]陈盛君,朱家壁.缓控释微丸制剂的研究进展[J].国外医学(药学分册),2004,31(3):177-181.
[45]张丹参,梅艳飞,宋晓敏,等.大黄结肠靶向微丸的制备及处方优化[J].中草药,2016,47(8):1321-1326.
[46]高捷,朱淼,沃联群,等.多索茶碱脉冲控释微丸的研制[J].中国现代应用药学,2016,33(7):895-900.
[47]李闻涛,万科,杨莹,等.何首乌抗性淀粉促进靶向结肠微丸体外药物释放研究[J].中国药业,2017,26(17):6-9.
[48]汪忠军,赵月,王颖,等.琥珀酸去甲文拉法辛膜控与骨架结合型缓释微丸的制备及释放特性研究[J].华西药学杂志,2018,33(2):126-130.
[49]茹庆国,彭宇,马书伟,等.响应面分析法优化当归超临界提取物结肠定位微丸的制备工艺研究[J].中国中药杂志,2016,41(13):2442-2448.
[50]秦永丽,张宇,于莲,等.结肠靶向剂黄芪多糖微丸制备工艺研究[J].中国药学杂志,2016,51(1):35-39.
[51] BRUCE LD,PETEREIT HU,BECKERT T,et al. Properties of enteric coated sodium valproate pellets[J]. Int J Pharm(Amsterdam,Neth),2003,264(1-2):85-96.
[52] ENAYATIFARD R,MAHJOOB A,EBRAHIMI P,et al. Evaluation of the effect of physical variables on in vitro release of diclofenac pellets using Box-Behnken design[J]. Iran J Basic Med Sci,2015,18(7):710-714.
[53]汪少,杨恒博,袁婷,等.溴吡斯的明包衣缓释微丸的研制[J].中国医药工业杂志,2019,50(1):84-92.
[54] KAN S,LI J,LIU J,et al. Preparation and IVIVC evaluation of salvianolic acid B micro-porous osmotic pump pellets[J]. Drug Dev Ind Pharm,2015,41(3):476-481.
[55] DEKYNDT B,VERIN J,NEUT C,et al. How to easily provide zero order release of freely soluble drugs from coated pellets[J].Int J Pharm(Amsterdam,Neth),2015,478(1):31-38.
[56] YANG Q,MA Y,ZHU J. Applying a novel electrostatic dry powder coating technology to pellets[J]. Eur J Pharm Sci,2015,97(Pt A):118-124.
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