黄腐酸和羟丙基-β-环糊精对阿司匹林分解的影响比较  

Influence of Fulvic Acid and Hydroxyl Propyl-β-cyclodextrin on Aspirin Degradation

作　　者：Mohammad Khalid Anwer Suraj Prakash Agarwal Asgar Ali Yasmin Sultana 崔佳丽[3] 刘建珍[3] 游金坤[3] 李鹏[3] 李宝才[3] 

机构地区：[1]药学院药物制剂教研室,新德里999008 [2]沙特国王大学药学院药物制剂教研室,利雅得999088 [3]昆明理工大学生命科学与技术学院,昆明650224

出　　处：《腐植酸》2012年第3期36-38,共3页Humic Acid

摘　　要：研究了黄腐酸(FA)作为一种的新的络合剂,与羟丙基-β-环糊精络合物(Hp-β-CD)相比,对阿司匹林(ASA)分解的影响。ASA与FA以1:0.5、1:1、1:2(物质的量比)络合,并用冷冻干燥、溶剂蒸发和喷雾干燥三种方法进行干燥。ASA-羟丙基-β-环糊精(1:1)络合物通过喷雾干燥制备,并与最佳FA络合物进行比较。将所有的络合物和ASA放入贴好标签的铝塑小包中密封,在温度为40±2℃、相对湿度为75%±5%的稳定暗箱中存放120d。分别在0、30d、60d、90d和120d分析各样品的水杨酸含量。以物质的量比为1:1进行络合的ASA-FA喷雾干燥络合物中水杨酸含量为4.31%,该络合物在所有不同制备方法的络合物中具有最佳稳定性。然而,1:1的ASA-羟丙基-β-环糊精喷雾干燥络合物中测得水杨酸含量只有2.35%。与FA相比,ASA与羟丙基-β-环糊精络合,其稳定性更强。为提高阿司匹林的稳定性,对一种新型FA络合剂进行了研究。与1:1ASA-FA喷雾干燥络合物相比,ASA与羟丙基-β-环糊精1:1络合时,ASA的稳定性有显著改善。The degradation of aspirin（ASA） was investigated to reveal information about the influence of complexation with fulvic acid（FA）,as a new complexing agent and compared with hydroxy propyl-β-cyclodextrin complex.ASA was complexed with FA in the molar ratio 1：0.5,1：1,and 1：2 by different methods through lyophilization,solvent evaporation,and spray drying.Spray-dried（1：1） ASA-hydroxy propyl-β-cyclodextrin complex was prepared and compared with optimized complex of FA.All the complexes and ASA alone were packaged in well-labeled sealed polythene-lined aluminum pouches and stored in stability chamber at 40 ± 2 °C and 75 ± 5 % relative humidity for 120 days.Samples were analyzed for salicylic acid content at 0,30,60,90,and 120 days.Overall 4.31% salicylic acid was formed in 1：1 ASA-FA spray-dried complex,which was optimized stable complex among other complexes of FA prepared by different methods in different molar ratios.However,2.35% salicylic acid was measured with 1：1 spray-dried ASA-hydroxy propyl-β-cyclodextrin complex.Stability of ASA increased more when complexed with hydroxy propyl-β-cyclodextrin as compared to FA.A novel complexing agent in the form of FA was investigated to increase the stability of ASA.Amarked improvement in stability of ASA was observed when complexed with hydroxy propyl-β-cyclodextrin（1：1） by spray drying as compared to 1：1 spray-dried ASA-FA complex.

关 键 词：阿司匹林 络合作用 黄腐酸 羟丙基-Β-环糊精 斯拉洁特 稳定性 

分 类 号：TQ460.1[化学工程—制药化工]