基于药效的氟康唑氯化钠注射液处方工艺筛选  

Screening of Preparation Process of Fluconazole and Sodium Chloride Injection Based on Pharmacodynamics

作　　者：侯海婷 路晓兵 赵方红 左亚茹 崔雪妹 杨娴 HOU Haiting;LU Xiaobing;ZHAO Fanghong;ZUO Yaru;CUI Xuemei;YANG Xian(Pharmaceutical Research Institute of Shijiazhuang No.4 Pharmaceutical Co.,Ltd.,Hebei Large Capacity Injection Engineering Technology Research Center,Shijiazhuang Hebei 050000,China;Postdoctoral Research station of Shijiazhuang No.4 Pharmaceutical Co.,Ltd.,Shijiazhuang Hebei 050000,China)

机构地区：[1]石家庄四药有限公司研发中心,河北省大容量注射剂工程技术研究中心,河北石家庄050000 [2]石家庄四药有限公司博士后科研工作站,河北石家庄050000

出　　处：《药品评价》2023年第5期558-561,共4页Drug Evaluation

摘　　要：目的建立系统性真菌感染模型,基于抗真菌活性筛选氟康唑氯化钠注射液的处方工艺,为其进一步处方工艺路线的确定和工艺参数的选择提供参考。方法通过ICR小鼠尾静脉注射白色念珠菌,制备系统性真菌感染小鼠模型;以上市氟康唑氯化钠注射液为阳性对照药,分别尾静脉注射给予不同剂量不同工艺的供试氟康唑氯化钠注射液Y1和Y2,通过观察系统性真菌感染小鼠在给药后的生存曲线和肾脏载菌量变化,比较供试品Y1、Y2的体内抗真菌活性,并比较其与上市氟康唑氯化钠注射液的活性差异。结果上市氟康唑氯化钠注射液、Y1、Y2在ICR小鼠体内具有抗白色念珠菌活性,且剂量依赖性地有效延长系统性真菌感染小鼠的存活时间,并提高小鼠的生存率(P<0.001);上市氟康唑氯化钠注射液、Y1、Y2均能有效减少系统性真菌感染小鼠肾脏载菌量(P<0.05),且呈剂量依赖性。结论Y1、Y2的体内抗真菌活性与阳性对照药相当,氟康唑氯化钠注射液不同处方工艺对其体内抗真菌活性无影响。Objective To establish a systemic fungal infection model and screen the prescription technology of fluconazole and sodium chloride injection based on antifungal activity,so as to provide reference for the determination of its further prescription process route and the selection of process parameters.Methods In this experiment,the mice model of systemic fungal infection was prepared by injecting candida albicans into the tail vein of ICR mice.fluconazole and sodium chloride injection was used as a positive control drug,and,different doses of test fluconazole and sodium chloride injection Y1 and Y2 were injected into the tail vein respectively.By observing the survival curve of mice with systemic fungal infection and the changes in kidney bacterial load after administration,the antifungal activity of the test product in vivo was verified,and the activity differences between them and fluconazole and sodium chloride injection were compared.Results fluconazole and sodium chloride injection,Y1 and Y2 injection had anti-candida albicans activity in ICR mice,and could effectively prolong the survival time of ICR mice infected with systemic fungal and improve the survival rate of ICR mice(P<0.001);fluconazole and sodium chloride injection,Y1 and Y2 injection could effectively reduce the renal bacterial load of ICR mice with systemic fungal infection(P<0.05).Conclusion In vivo antifungal activity of Y1 and Y2 are not significantly different from that of positive control drug.The different preparations of fluconazole and sodium chloride injection have no effect on the antifungal activity in vivo.

关 键 词：氟康唑 工艺学 制药 药效学 工艺筛选 真菌感染 小鼠 近交ICR 

分 类 号：R285.5[医药卫生—中药学]