摘要
盐酸小檗碱是临床治疗胃肠道细菌感染等疾病的有效药物。但由于脂溶性差等问题,造成其口服生物利用度较低,难以充分发挥药效。本研究旨在利用磷脂复合技术提高盐酸小檗碱的脂溶性。通过溶剂-旋转蒸发法,以复合率(AE)为筛选指标,采用单因素筛选及正交设计,筛选得到制备盐酸小檗碱-磷脂复合物的最佳处方。优选处方下,盐酸小檗碱-磷脂复合率达到90%以上,4℃下可稳定保存3个月。该研究为盐酸小檗碱-磷脂复合物的后期应用奠定了物质基础。
Berberine hydrochloride is effective medicine for gastrointestinal bacterial infection treatment clinically. However, as for its poor lipophilicity, oral bioavailability of beriberine hydrochloride is relatively low. This study was designed to increase the lipophilicity of berberine hydrochloride using phospholipid complexation technology. In this study, associative efficiency(AE)was set as screening parameter and optimal formulation of berberine hydrochloride phospholipid complex was obtained using solvent evaporation method based on single factor screening and orthogonal design. Under the selected formulation, AE of berberine hydrochloride phospholipid complex could reach 90% and storage stability remained in 6 months under 4 ℃, which provided the basis for practical application.
作者
王庆
刘黎瑶
王庆奎
WANG Qinga;LIU Li-yao;WANG Qing-kuib(Tianjin Agricultural University,Department of Biopharmaceuticals, College of Basic Science;Tianjin Agricultural University,Tianjin Key Lab of Aqua-Ecology and Aquaculture, Tianjin 300384, China)
出处
《天津农学院学报》
CAS
2019年第2期64-68,共5页
Journal of Tianjin Agricultural University
基金
天津市教委科研计划项目(2017KJ181)
天津市水产产业技术体系创新团队项目(ITTFRS2017004)
国家自然科学基金面上项目(31170442)
关键词
盐酸小檗碱
磷脂复合物
正交设计
处方筛选
berberine hydrochloride
phospholipid complex
orthogonal screening
formulation optimization