基于热塑弹性体的辣椒素贴剂的制备及评价
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摘要
目的:以热塑弹性体为骨架材料,采用熔融共混法制备贴剂基质,制备辣椒素热熔压敏胶贴剂。方法:用红外光谱和偏振光显微镜考察药物在贴剂基质中的存在状态,同时以国外上市贴剂为对照,采用Franz扩散池考察贴剂中辣椒素的释放和体外透皮特性。以SD大鼠为模型动物,考察贴剂的体内透皮吸收行为。结果:辣椒素药物与热熔压敏胶基质相容性好,但贴剂的稳定性有待进一步提高。药物在两者种贴剂中的释放遵循Higuchi方程。实验室自制热熔胶贴剂的体内外透皮行为与国外市售贴剂相比无显著性差异。结论:热熔胶贴剂基质与皮肤和药物的相容性较好,具有良好的体外-体内透皮相关性。
OBJECTIVE Capsaicin patch based on hot-melt pressure sensitive adhesive were prepared by hot-melt methods.METHODS Fourier transform infrared spectroscopy and polarization light microscope were applied to investigate the interactions between drug and matrix.Patch adhesion profile,drug release,in vitro and in vivo penetration profiles were performed by comparing the lab-prepared patch with a commercial product as reference sample.HPLC was applied to performin vivo drug absorption using SD rat as model animals.RESULTS Capsaicin showed a great interaction with the prepared patch matrix,but the stability of the patch could be improved.Drug release profiles from patches followed Higuchi equation.Compared with Commercial patch,Lab-prepared patch possessed the same percutaneous permeability in vitro and in vivo.CONCLUSIONHot-melt pressure sensitive adhesive is suitable for preparation capsaicin patch for its good adhesion properties and good compatibility with drug and skin.It showed a well skin permeation ability without significant differences when comparing with commercial products.
OBJECTIVE Capsaicin patch based on hot-melt pressure sensitive adhesive were prepared by hot-melt methods.METHODS Fourier transform infrared spectroscopy and polarization light microscope were applied to investigate the interactions between drug and matrix.Patch adhesion profile,drug release,in vitro and in vivo penetration profiles were performed by comparing the lab-prepared patch with a commercial product as reference sample.HPLC was applied to performin vivo drug absorption using SD rat as model animals.RESULTS Capsaicin showed a great interaction with the prepared patch matrix,but the stability of the patch could be improved.Drug release profiles from patches followed Higuchi equation.Compared with Commercial patch,Lab-prepared patch possessed the same percutaneous permeability in vitro and in vivo.CONCLUSIONHot-melt pressure sensitive adhesive is suitable for preparation capsaicin patch for its good adhesion properties and good compatibility with drug and skin.It showed a well skin permeation ability without significant differences when comparing with commercial products.
引文
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[12]Gutschke E,Bracht S,Nagel S,et al.Adhesion testing of transdermal matrix patches with a probe tack test In vitro and in vivo evaluation[J].Eur J Pharm Biopharm,2010,75(3):399-404.
[13]汤秀珍,王承潇,张皓,等.星点设计-效应面法优化关节止痛膏贴剂处方[J].中草药,2012,43(1):86-90.
[14]Fang JY,Wu PC,Huang YB,et al.In vivo percutaneous absorption of capsaicin,nonivamide and sodium nonivamide acetate from ointment bases Pharmacokinetic analysis in rabbits[J].Int J Pharm,1996,128(1-2):169-177.
[15]Gibert FX,Marin G,Derail C,et al.Rheological properties of hot melt pressuresensitive adhesives based on styrene-isoprene copolymers.Part 1:A rheological model for[SIS-SI]formulations[J].J Adhesion,2003,79(8-9):825-852.
[16]Wang CX,Han W,Tang XZ,et al.Evaluation of drug release profile from patches based on styrene-isoprene-styrene block copolymer:the effect of block structure and plasticizer[J].AAPS Pharm Sci Tech,2012,13(2):556-567.
[2]Iwasaki Y,Ssaito O,Tanabe M,et al.Monoacylglycerols Active Capcaicin Recepter,TRPV1[J].Original Article,2008(43):471-483.
[3]刘营营,欧阳建勋,李忠海,等.辣椒素的抑菌活性研究现状[J].粮食科技与经济,2010,35(5):18-22.
[4]CHENG Yan-ping,WANG Yi-he,CHENG Li-ping.Electrophysiologic effects of capsaicin on pacemaker cells in sinoatrial nodes of rabbits[J].Acta Pharma-cologica Sinica,2003,24(8):826-830.
[5]Wahba NM,Ahmed AS,Ebraheim ZZ.Antimicrobial effects of pepper,parsley,and dill and their roles in the microbiological quality enhancement of traditi-onal Egyptian Kareish cheese[J].Foodborne Pathog Dis,2010,7(4):411-418.
[6]龙晓英,罗佳波,李立任,等.局部用辣椒碱传递体的制备及体外评价[J].中国中药杂志,2006,31(12).
[7]Li WL,Bouzidi L,Narine SS.Current research and development status and prospect of hot-melt adhesives:A review[J].Ind&Eng Chem Res,2008,47(20):7524-7532.
[8]王承潇,汤秀珍,沈平孃,等.热熔压敏胶应用于中药贴剂的研究进展[J].中草药,2010,41(3):466-499.
[9]俞振伟,梁漪,梁文权.经皮给药用热熔压敏胶的制备及其体外评价[J].中国药学杂志,2013,48(6):450-455.
[10]马建芳,罗华菲,朱壮志,等.透皮给药系统热熔压敏胶基质处方的优化与初步应用[J].中国医院工业杂志,2012,43(7):553-557.
[11]Wang C,Liu R,Tang X,et al.A Drug-in-Adhesive Matrix Based on Thermo plastic Elastomer:Evaluation of Percutaneous Absorption,Adhesion,and Skin Irritation[J].AAPS Pharm SciTech,2012,13(4):1179-1189.
[12]Gutschke E,Bracht S,Nagel S,et al.Adhesion testing of transdermal matrix patches with a probe tack test In vitro and in vivo evaluation[J].Eur J Pharm Biopharm,2010,75(3):399-404.
[13]汤秀珍,王承潇,张皓,等.星点设计-效应面法优化关节止痛膏贴剂处方[J].中草药,2012,43(1):86-90.
[14]Fang JY,Wu PC,Huang YB,et al.In vivo percutaneous absorption of capsaicin,nonivamide and sodium nonivamide acetate from ointment bases Pharmacokinetic analysis in rabbits[J].Int J Pharm,1996,128(1-2):169-177.
[15]Gibert FX,Marin G,Derail C,et al.Rheological properties of hot melt pressuresensitive adhesives based on styrene-isoprene copolymers.Part 1:A rheological model for[SIS-SI]formulations[J].J Adhesion,2003,79(8-9):825-852.
[16]Wang CX,Han W,Tang XZ,et al.Evaluation of drug release profile from patches based on styrene-isoprene-styrene block copolymer:the effect of block structure and plasticizer[J].AAPS Pharm Sci Tech,2012,13(2):556-567.