基于药物与羟丙甲纤维素凝胶相互作用的缓释特征参数研究

发布时间：2018-05-29 05:50

本文选题：羟丙甲纤维素 + 亲水凝胶　；参考：《中国新药杂志》2017年09期

【摘要】：目的:通过研究羟丙甲纤维素(HPMC)凝胶对不同药物的阻滞作用,考察HPMC缓释性征参数的适用性,从相互作用的角度阐明亲水凝胶的缓释机理。方法:选择不同性质的5种模型药物(托拉塞米、盐酸洛美利嗪、布洛芬、盐酸氨溴索、盐酸二甲双胍),用三室渗透模型测定药物透过亲水凝胶的速度,取点时间为1,3,7,10和24 h,计算药物的渗透率及阻滞率,利用Material Studio的blend模块计算药物与HPMC的相互作用能,考察试验结果与计算结果的相关性。结果:HPMC的存在对不同的药物影响不同,以3个浓度(5,10,20 mg·mL~(-1))的阻滞率作为表征HPMC对药物的缓释特征参数可以发现:HPMC对二甲双胍和氨溴索的阻滞能力较弱,对布洛芬和托拉塞米具有较强的吸附作用,对洛美利嗪也有较大的吸收作用,存在饱和现象。理论计算的HPMC与药物相互作用能与24 h阻滞率之间存在明显的相关性。结论:缓释特征参数可以通过高浓度和低浓度的阻滞率,明确药物和辅料的相互作用的方式,帮助药物选择适当的缓释材料,还可以用于保证辅料的本身质量的一致性。
[Abstract]:Aim: to study the inhibition effect of HPMC gel on different drugs, to investigate the applicability of HPMC sustained-release characteristic parameters, and to elucidate the slow-release mechanism of hydrophilic gel from the point of view of interaction. Methods: five different kinds of model drugs (Tora, lomerizine hydrochloride, ibuprofen, ambroxol hydrochloride, metformin hydrochloride) were selected. The permeation rate of the drug through hydrophilic gel was determined by a three-compartment osmotic model. The drug permeability and blocking rate were calculated for 10 and 24 hours, and the interaction energy between the drug and HPMC was calculated by blend module of Material Studio. The correlation between the experimental results and the calculated results was investigated. Results the effects of the presence of 1: HPMC on different drugs were different. The blocking rate of 3 concentrations of 5 10 ~ 10 ~ (10) mg / L ~ (-1) of HPMC was used as the characteristic parameter to characterize the sustained release of HPMC to the drug. It was found that the inhibition ability of the two groups to metformin and ambroxol was weak. Ibuprofen and Tora were adsorbed strongly, and lomerizine was also adsorbed and saturated. There was a significant correlation between the calculated HPMC and drug interaction energy and 24 h block rate. Conclusion: the characteristic parameters of slow release can be used to ensure the consistency of the quality of excipients by determining the way of interaction between drugs and excipients at high and low concentration.
【作者单位】：天津医科大学;天津中医药大学;天津药物研究院释药技术与药动学国家重点实验室;天津药物研究院天津市药物设计与发现重点实验室;
【分类号】：R943

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