微孔淀粉对2,4-二硝基苯酚的负载与缓释

杨慧; 樊艳叶; 赵佩莹; 黄红梨; 钟旋铭; 林日辉; 廖安平

doi:10.13386/j.issn1002-0306.2019.17.003

微孔淀粉对2,4-二硝基苯酚的负载与缓释

Loading and Sustained Release of 2,4-Dinitrophenol from Microporous Starch

摘要

摘要: 为降低2,4-二硝基苯酚(DNP)的毒副作用,延长药效时间,本文以α-淀粉酶催化水解玉米淀粉制备的微孔淀粉作为载体,负载DNP制成缓释制剂,并考察了其体外释放性能。结果表明:微孔淀粉对DNP的吸附平衡时间为1 h,增加DNP的初始浓度及降低负载过程温度有利于增加吸附量。在DNP初始浓度为500 mg/L、吸附温度为25℃、吸附时间为1 h时,微孔淀粉对DNP吸附量可达3.4369 mg/g。动力学及热力学模型拟合结果表明,微孔淀粉对DNP的吸附是范德华力和氢键共同作用的表面物理吸附,为可自发进行的放热过程。在模拟胃液和模拟肠液释放介质的体外释放实验中,0.50 g的DNP-微孔淀粉缓释制剂(载药量为3.3085 mg/g)的释放时间可达12 h,释药量分别为91.18%和89.29%;而原料药在模拟胃液和模拟肠液中完全释放时间分别为4、3 h,DNP累积释放量分别为91.01%、92.23%。DNP-微孔淀粉缓释剂的释放动力学分析表明,DNP-微孔淀粉在模拟胃液中为扩散和溶蚀协同作用释药,符合Peppas动力学方程;在肠液中遵循Fickian的扩散符合一级动力学模型。因此,微孔淀粉对DNP具有良好的吸附和缓释性能,本研究可为DNP缓释制剂开发与应用提供基础。

Abstract: In this paper,in order to reduce the toxic side effects of 2,4-dinitrophenol(DNP)and prolong its efficacy time,corn microporous starch was prepared by α-amylase catalyzed hydrolysis of corn starch,and used as a carrier for DNP-loaded sustained release agent preparation,the release performance in vitro was also investigated. The experimental results showed that the adsorption equilibrium of DNP onto microporous starch was reached at 1 h in the loading process. Increasing the initial concentration of DNP and decreasing the temperature were beneficial to increase the adsorption capacity. With the condition of initial DNP concentration of 500 mg/L,the adsorption temperature at 25℃ and adsorption for 1 h,the adsorption amount of DNP onto microporous starch could reach 3.4369 mg/g. The fitting results of kinetic and thermodynamic model showed it was a surface physical adsorption by Van der Waals force and hydrogen bonding force,and it was also a spontaneous exothermic process. In the release experiment in vitro,the gastric juice and intestinal fluid release medium were simulated,the complete release time of 0.5 g DNP-microporous starch sustained release agent(1.6543 mg DNP was loaded)was up to 12 h,the release amount was 91.18% and 89.29%,respectively;However,the complete release time of raw material medicine in simulated gastric juice and simulated intestinal fluid was 4 and 3 h,and the cumulative release of DNP was 91.01% and 92.23%,respectively. The release kinetics of DNP-microporous starch sustained release agent analysis showed that,the DNP released form microporous starch in simulated gastric juice was the synergistic result of diffusion and dissolution,the process was consistent with Peppas kinetic equation;the release process followed Fickian diffusion in intestinal juice,which was consistent with the first-order kinetic model. The microporous starch had good adsorption and sustained release properties for DNP. This study would provide a basis for the development and application of DNP sustained-release preparations.