乙基纤维素的质量属性对美沙拉嗪缓释胶囊体外释放行为的影响
|
摘要
目的:考察乙基纤维素(ethyl cellulose,EC)作为包衣,控制释放速率,其质量属性对薄膜包衣型缓释制剂体外释放行为的影响。方法:以美沙拉嗪为模型药物,不同质量属性的EC为包衣材料,分别制备缓释胶囊,考察EC的质量属性对模型药物的释放速率和释放动力学的影响。结果:EC包衣增厚和增加EC黏度,都会使得模型药物的释放速率降低,高乙氧基含量的EC也有利于药物释放。此外,EC的来源不同对药物释放也有较大影响。结论:EC质量属性与缓控释制剂释药行为间相关性的研究,将有利于EC质量评价方法的建立。
Objective: To investigate the influence of quality attributes of ethyl cellulose( EC),as rate controlling polymer,on the in vitro drug release behaviors of film-coated extended-release preparations. Methods:Mesalazine was chosen as the model drug and sustained-release capsules were prepared by using different attributes of EC as coating materials,and then in vitro dissolution testing was performed to investigate the effects of different quality attributes of EC on the release rate and release kinetics of mesalazine. Results: Increasing the weight of the EC coating and the EC viscosity could reduce the release rate of mesalazine. Besides,EC with a high ethoxy content was beneficial for drug release. In addition,the release rate of mesalazine was obviously influenced by the sources of EC. Conclusion: The study of the correlation between EC quality attributes and the behavior of drug release from extended-release formulations will facilitate the establishment of EC quality assessment system.
Objective: To investigate the influence of quality attributes of ethyl cellulose( EC),as rate controlling polymer,on the in vitro drug release behaviors of film-coated extended-release preparations. Methods:Mesalazine was chosen as the model drug and sustained-release capsules were prepared by using different attributes of EC as coating materials,and then in vitro dissolution testing was performed to investigate the effects of different quality attributes of EC on the release rate and release kinetics of mesalazine. Results: Increasing the weight of the EC coating and the EC viscosity could reduce the release rate of mesalazine. Besides,EC with a high ethoxy content was beneficial for drug release. In addition,the release rate of mesalazine was obviously influenced by the sources of EC. Conclusion: The study of the correlation between EC quality attributes and the behavior of drug release from extended-release formulations will facilitate the establishment of EC quality assessment system.
引文
[1] ARCA HC,MOSQUERA-GIRALDO LI,BI V,et al. Pharmaceutical applications of cellulose ethers and cellulose ether esters[J].Biomacromolecules,2018,19(7):2351-2376.
[2] MABOOS M,YOUSUF RI,SHOAIB MH,et al. Effect of lipid and cellulose based matrix former on the release of highly soluble drug from extruded/spheronized,sintered and compacted pellets[J]. Lipids Health Dis,2018,17(136):2351-2376.
[3]万东华,林滔,汤丽容,等.盐酸克林霉素微囊的体外释药及其影响因素的考察[J].海峡药学,2003,15(6):17-19.
[4]龚炜,赵磊磊,朱盛山.辅料性质对缓控释制剂体外释药特性的影响[J].中国药学杂志,2006,41(18):1370-1373.
[5] MEHSUD S,RAUF M,OBAIDULLAH,et al. To study the influence of different grades of ethylcellulose ether derivative polymer ethocel(r)and co-excipient on drug release profile of controlled release matrix tablet of acarbose[J]. Pak J Pharm Sci,2015,28(6):2259-2265.
[6] REKHI GS,JAMBHEKAR SS. Ethylcellulose-a polymer review[J]. Drug Dev Ind Pharm,1995,21(1):61-77.
[7]王晋,王红琰,张汝华.乙基纤维素理化性质的研究[J].中国药学杂志,2000,35(4):249-251.
[2] MABOOS M,YOUSUF RI,SHOAIB MH,et al. Effect of lipid and cellulose based matrix former on the release of highly soluble drug from extruded/spheronized,sintered and compacted pellets[J]. Lipids Health Dis,2018,17(136):2351-2376.
[3]万东华,林滔,汤丽容,等.盐酸克林霉素微囊的体外释药及其影响因素的考察[J].海峡药学,2003,15(6):17-19.
[4]龚炜,赵磊磊,朱盛山.辅料性质对缓控释制剂体外释药特性的影响[J].中国药学杂志,2006,41(18):1370-1373.
[5] MEHSUD S,RAUF M,OBAIDULLAH,et al. To study the influence of different grades of ethylcellulose ether derivative polymer ethocel(r)and co-excipient on drug release profile of controlled release matrix tablet of acarbose[J]. Pak J Pharm Sci,2015,28(6):2259-2265.
[6] REKHI GS,JAMBHEKAR SS. Ethylcellulose-a polymer review[J]. Drug Dev Ind Pharm,1995,21(1):61-77.
[7]王晋,王红琰,张汝华.乙基纤维素理化性质的研究[J].中国药学杂志,2000,35(4):249-251.