微晶纤维素对巴洛沙星渗透性影响的研究  

The effect of microcrystalline cellulose on permeability of balofloxacin

作　　者：张丹丹 于明艳 张冬梅 赵海云 王松 刘文坤 李宁宁 陈德俊 Zhang Dan-dan;Yu Ming-yan;Zhang Dong-mei;Zhao Hai-yun;Wang song;Liu Wen-kun;Li Ning-ning;Chen De-jun(Shandong Institute for Food and Drug Control,Shandong Research Center of Engineering and Technology for Consistency Evaluation of Generic Drugs,NMPA Key Laboratory for Research and Evaluation of Generic Drugs,Ji'nan 250101)

机构地区：[1]山东省食品药品检验研究院,国家药品监督管理局仿制药研究与评价重点实验室,山东省仿制药一致性评价工程技术研究中心,济南250101

出　　处：《中国抗生素杂志》2023年第3期317-321,共5页Chinese Journal of Antibiotics

摘　　要：目的采用平行人工膜渗透性分析法(PAMPA)研究微晶纤维素的用量、来源、型号对巴洛沙星渗透性的影响,为巴洛沙星片处方中微晶纤维素的筛选及不同来源微晶纤维素的替代提供参考。方法采用μFLUXTM型药物渗透性测定系统,前30 min以胃模拟液(pH 1.6)为介质,而后介质转换成肠模拟液(pH 6.5),测定巴洛沙星在不同来源、型号、用量的微晶纤维素中的渗透性。通过对渗透性差异的比较,考察微晶纤维素对巴洛沙星渗透性的影响。结果随微晶纤维素(PH101型和PH102型)用量增加,巴洛沙星渗透性降低;不同型号的微晶纤维素对巴洛沙星渗透性的影响略有差异;同型号的进口微晶纤维素与国产品对巴洛沙星渗透性的影响没有显著性差异。结论微晶纤维素的用量和型号影响巴洛沙星的渗透性。在巴洛沙星片中,渗透性可作为重要指针,为选择不同来源的微晶纤维素进行相互替代。Objective To investigate the impact of sources,types,and ratios of microcrystalline cellulose on the permeability of balofloxacin using the parallel artificial membrane permeability analysis(PAMPA),and then to provide a reference for screening microcrystalline cellulose and the replacement of microcrystalline cellulose from different sources in balofloxacin tablet prescription.Methods TheμFLUXTM drug permeability test system was used to determinate the permeability of balofloxacin in samples which mixed balofloxacin with different sources,types,and ratios of microcrystalline cellulose.The experiment was carried out in the medium which was gastric simulated fluid(pH 1.6)at the beginning and then was converted into fasted-state simulated intestinal fluid(pH 6.5)after 30 min.Through comparing the differences in permeability,the impact of microcrystalline cellulose on the permeability of balofloxacin was investigated.Results With the increasing proportion of microcrystalline cellulose(PH101 and PH102),the permeability of balofloxacin decreased.The effect of different types of microcrystalline cellulose on the permeability of balofloxacin was slightly different.There was no significant difference between one domestic microcrystalline cellulose and another imported microcrystalline cellulose of the same model on the permeability of balofloxacin.Conclusion The proportion and type of microcrystalline cellulose can affect the permeability of balofloxacin.Permeability can be used as an important indicator to select different sources of microcrystalline cellulose for mutual substitution in balofloxacin tablet.

关 键 词：巴洛沙星 平行人工膜渗透性分析法 微晶纤维素 渗透性 辅料 替代 

分 类 号：R978.1[医药卫生—药品]