pH依赖-时滞型核桃肽结肠定位微丸的制备
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摘要
采用挤出滚圆/流化床包衣技术制备p H依赖-时滞型核桃肽结肠定位微丸。通过单因素试验,以体外释放度为评价指标,对包衣处方进行优化,优化的包衣处方为:以小伦包衣材料为pH依赖材料,乙基纤维素为时滞层材料,小伦包衣材料/乙基纤维素比例4︰6,包衣增重15%。优化处方制备的核桃肽微丸在模拟胃液中2 h、模拟肠液中3 h核桃肽不释放,在模拟结肠液中4 h核桃肽释放完全,具有明显结肠定位性能。抗氧化活性试验结果表明微丸制备过程对核桃肽活性影响不大。
The pH-based and time-lag type pellets of walnut peptides(WPs) for colon-specific delivery were prepared by extrusion/spheronization and film coating. The preparation parameters of the film coating process were optimized by independent single factor experiments, and dissolution profile was selected as dependent variable. The results of optimum preparation parameters were as follows: Xiaolun chosen as pH-dependent material, ethyecellulose chosen as sustained-release material, the ratio of Xiaolun and ethylcellulose 4︰6 and the coating weight gain 15%. The results of in vitro release revealed that the optimum pellets showed no WP release in the simulated gastric fluid and intestinal fluid, while a complete WP released in the simulated colon fluid, which indicated the obvious features of colon-specific delivery. The results of antioxidant experiments showed that the formulation process held less influence on the bioactivity of walnut peptides.
The pH-based and time-lag type pellets of walnut peptides(WPs) for colon-specific delivery were prepared by extrusion/spheronization and film coating. The preparation parameters of the film coating process were optimized by independent single factor experiments, and dissolution profile was selected as dependent variable. The results of optimum preparation parameters were as follows: Xiaolun chosen as pH-dependent material, ethyecellulose chosen as sustained-release material, the ratio of Xiaolun and ethylcellulose 4︰6 and the coating weight gain 15%. The results of in vitro release revealed that the optimum pellets showed no WP release in the simulated gastric fluid and intestinal fluid, while a complete WP released in the simulated colon fluid, which indicated the obvious features of colon-specific delivery. The results of antioxidant experiments showed that the formulation process held less influence on the bioactivity of walnut peptides.
引文
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[2]赵谋明,陈卉平,任娇艳.核桃粕、核桃仁酶解物抗氧化活性的研究[J].现代食品科技,2013(10):2335-2339.
[3]毛晓英,华欲飞,卢伟.核桃蛋白质的研究进展[J].食品工业科技,2009(9):328-331.
[4]CHEN H,ZHAO M,LIN L,et al.Identification of antioxidative peptides from defatted walnut meal hydrolysate with potential for improving learning and memory[J].Food Res Int,2015(78):216-223.
[5]林燕,陈计峦,胡小松,等.酶解核桃蛋白制备抗氧化肽的研究[J].食品工业科技,2011(4):204-207.
[6]胡鑫,刘成柏,林相友,等.酶解核桃仁制备低分子肽[J].吉林大学学报(理学版),2003,41(4):526-530.
[7]喻峰,熊华,吕培蕾,等.核桃粕酶解工艺研究[J].食品与发酵工业,2006,32(5):89-91.
[8]CHEN N,YANG H,SUN Y,et al.Purification and identification of antioxidant peptides from walnut(Juglans regia L)protein hydrolysates[J].Peptides,2012,38(2):344-349.
[9]RENUKUNTLA J,VADLAPUDI A D,PATEL A,et al.Approaches for enhancing oral bioavailability of peptides and proteins[J].Int J Pharm,2013,447(1/2):75-93.
[10]BRAYDEN D J,ALONSO M J.Oral delivery of peptides:Opportunities and issues for translation[J].Adv Drug Deliv Rev,2016,106(Pt B):193-195.
[11]CHOONARA B F,CHOONARA Y E,KUMAR P,et al.A review of advanced oral drug delivery technologies facilitating the protection and absorption of protein and peptide molecules[J].Biotechnol Adv,2014,32(7):1269-1282.
[12]詹璐璐,尹东东,王杏林,等.结肠靶向给药制备技术的研究进展[J].中国新药杂志,2014(16):1868-1874.
[13]周洁,朱小宁,张艺,等.口服结肠定位释药系统研究新进展[J].中国新药杂志,2015(4):390-394.
[14]金剑,李伟宁,李琦,等.口服结肠定位给药系统的研究进展[J].中国临床药学杂志,2011(3):184-187.
[15]LI Y,JIANG B,ZHANG T,et al.Antioxidant and free radical-scavenging activities of chickpea protein hydrolysate(CPH)[J].Food Chemistry,2008,106(2):444-450.
[16]LAN W,ZHAOJUN Z,ZESHENG Z.Characterization of antioxidant activity of extracts from Flos Lonicerae[J].Drug Development and Industrial Pharmacy,2007,33(8):841-847.
[17]任飞亮,裴元英.口服结肠定位释药系统的研究进展[J].中国药学杂志,2005,40(17):1288-1291.
[18]李国锋,陈建海,陈志良.结肠定位给药技术研究进展[J].中国药房,2005,16(1):182-185.
[19]张建伟,刘力,徐德生.结肠定位释药系统的研究进展[J].中国医院药学杂志,2013,33(21):1802-1804.
[20]郭波红,程怡.乙基纤维素在缓控释制剂中的应用[J].广东药学,2003,13(1):14-16.