聚卡波菲/泊洛沙姆407为基质的姜黄素眼用凝胶研究
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摘要
目的:探讨以聚卡波菲(AA-1)和泊洛沙姆407(P407)为胶凝材料,制备姜黄素眼用凝胶。方法:考察姜黄素在不同溶剂中的溶解性和稳定性,以AA-1和P407为胶凝材料制备姜黄素眼用凝胶,考察其动态黏度及体外药物释放。结果:5.0%P407和0.9%AA-1为凝胶基质、滴眼液pH5.0、氯化钠和甘露醇为渗透压调节剂、羟苯乙酯为防腐剂,制备的姜黄素眼用凝胶,其动态黏度具有剪切变稀的特点,药物稳定、体外缓慢释放。结论:泊洛沙姆407和聚卡波菲AA-1联合使用作为凝胶基质,用于姜黄素眼用凝胶的制备具有良好的应用前景。
Objective:To study the using of poloxamer 407 and polycarbophil as the gelator for the ophthalmic gels of curcumin.Methods:The equilibrium solubility and stability of curcumin in different solvents were studied to select the formulation compositions and the pH value of ophthalmic gels.The in vitro release and dynamic viscosity of the gels prepared were investigated.Results:Curcumin ophthalmic gels were prepared with 5.0% poloxamer 407 and 0.9% polycarbophil as the matrix materials,sodium chloride and mannitol as the osmotic pressure regulator,ethylparaben as preservative.The obtained gels indicated shear-thinning and extended release properties in vitro.Conclusion:Poloxamer 407 and polycabophil used as the matrix of curcumin ophthalmic gels has great potential applications.
Objective:To study the using of poloxamer 407 and polycarbophil as the gelator for the ophthalmic gels of curcumin.Methods:The equilibrium solubility and stability of curcumin in different solvents were studied to select the formulation compositions and the pH value of ophthalmic gels.The in vitro release and dynamic viscosity of the gels prepared were investigated.Results:Curcumin ophthalmic gels were prepared with 5.0% poloxamer 407 and 0.9% polycarbophil as the matrix materials,sodium chloride and mannitol as the osmotic pressure regulator,ethylparaben as preservative.The obtained gels indicated shear-thinning and extended release properties in vitro.Conclusion:Poloxamer 407 and polycabophil used as the matrix of curcumin ophthalmic gels has great potential applications.
引文
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[2] 李翔,刘亚丽,张鹏,等.姜黄素眼用纳米混悬凝胶剂对大鼠硒性白内障的治疗作用[J].中国实验方剂学杂志,2017,23(22):9-13.
[3] 徐雷,刘刚,刘朝.选姜黄素对前列腺癌PC-3细胞HSP27 mRNA表达及凋亡的影响[J].中国现代中药,2015,17(9):927-930.
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[12] MARGIT H,WIM W,ANNICK L,et al.Mucoadhesive ocular insert based on thiolated poly(acrylic acid):development and in vivo evaluation in humans[J].J Controlled Release,2003,89(3):419-428.
[13] YANG Y L,WANG S N,XU H,et al.Properties of topically applied organogels:rheology and in vitro drug release[J].Asian J pharm SCI,2008,3(4):175-183.
[14] 周巧云,张朝晖,潘俊芳,等.泊洛沙姆为载体的疏水性药物新剂型研究进展[J].中国现代应用药学,2011(4):315-319.
[15] 李鸿滨,丁平田,徐晖,等.处方因素对黄体酮缓释凝胶体外释放性质和黏度的影响[J].中国新药杂志,2004,13(2):133-136.
[16] 陆伟,蒋新国.卡波姆和聚卡波菲在药剂学中应用的新进展[J].中国医院药学杂志,2002,22(8):491-493.
[17] KULICKE W M.Polymers in aqeueous media:performance through associationAdvances in Chemistry Series 223[M].Washington DC:American Chemiscal Society,1989:15-44.
[18] 宋玉琴.离子敏感眼用原位凝胶的制备及体内外评价[D].兰州:兰州大学,2008.
[19] 丁明和,娄杰,洪春雪,等.氯化钠强化硫酸吗啡缓释液体栓制备及其性能[J].武汉大学学报:理学版,2011,57(4):277-282.
[2] 李翔,刘亚丽,张鹏,等.姜黄素眼用纳米混悬凝胶剂对大鼠硒性白内障的治疗作用[J].中国实验方剂学杂志,2017,23(22):9-13.
[3] 徐雷,刘刚,刘朝.选姜黄素对前列腺癌PC-3细胞HSP27 mRNA表达及凋亡的影响[J].中国现代中药,2015,17(9):927-930.
[4] 崔晶,翟光喜,娄红祥.姜黄素的研究进展[J].中南药学杂志,2005,3(2):108-111.
[5] MITRA S K,SUNDARAM R,VENKATARANGANNA M V.Anti-inflammatory,Antioxidant and Antimicrobial Activity of Ophthacare Brand,an Herbal Eye Drops[J].Phytomedicine,2000,7(2):123-127.
[6] 余美荣,蒋福升,丁志山.姜黄素的研究进展[J].中草药,2009,40(5):828-931.
[7] WANG L L,SUN Y,HUANG K,et al.Curcumin,a potential therapeutic candidate for retinal diseases[J].Mol Nutr & Food Res,2013,57(9):1557-1568.
[8] PESCOSOLIDO N,Giannotti R,Plateroti,et al.Curcumin:Therapeutical Potential in Ophthalmology[J].Planta Med,2014,80(4):249-254.
[9] 倪斌,李翔,罗云,等.姜黄素眼用脂质体的制备及晶状体抗氧化作用考察[J].中国实验方剂学杂志,2014,20(6):5-9.
[10] 关辉,欧阳梅,梁娇旸,等.姜黄素固体分散体的制备和溶出度考察[J].沈阳药科大学学报,2009,26(12):945-955.
[11] MARIA D N,MISHRA S R,WANG L,et al.Water-soluble Complex of Curcumin with Cyclodextrins:Enhanced Physical Properties For Ocular Drug Delivery[J].Curr Drug Deliv,2017,14(6):875-886.
[12] MARGIT H,WIM W,ANNICK L,et al.Mucoadhesive ocular insert based on thiolated poly(acrylic acid):development and in vivo evaluation in humans[J].J Controlled Release,2003,89(3):419-428.
[13] YANG Y L,WANG S N,XU H,et al.Properties of topically applied organogels:rheology and in vitro drug release[J].Asian J pharm SCI,2008,3(4):175-183.
[14] 周巧云,张朝晖,潘俊芳,等.泊洛沙姆为载体的疏水性药物新剂型研究进展[J].中国现代应用药学,2011(4):315-319.
[15] 李鸿滨,丁平田,徐晖,等.处方因素对黄体酮缓释凝胶体外释放性质和黏度的影响[J].中国新药杂志,2004,13(2):133-136.
[16] 陆伟,蒋新国.卡波姆和聚卡波菲在药剂学中应用的新进展[J].中国医院药学杂志,2002,22(8):491-493.
[17] KULICKE W M.Polymers in aqeueous media:performance through associationAdvances in Chemistry Series 223[M].Washington DC:American Chemiscal Society,1989:15-44.
[18] 宋玉琴.离子敏感眼用原位凝胶的制备及体内外评价[D].兰州:兰州大学,2008.
[19] 丁明和,娄杰,洪春雪,等.氯化钠强化硫酸吗啡缓释液体栓制备及其性能[J].武汉大学学报:理学版,2011,57(4):277-282.