欧前胡素柔性脂质体凝胶的制备及质量评价(1)
中图分类号 R944.9 文献标志码 A 文章编号 1001-0408(2020)09-1074-06
DOI 10.6039/j.issn.1001-0408.2020.09.10
摘 要 目的：制备欧前胡素柔性脂质体凝胶(IMP-UDLs-Gel)，并对其进行质量评价。方法：在单因素考察的基础上，以12 h累积透过量(Q12 h)为评价指标，采用正交试验法对IMP-UDLs-Gel处方中的卡波姆940比例、甘油比例和丙二醇比例进行考察，筛选最优处方，并对最优处方所制备的IMP-UDLs-Gel进行质量评价。结果：IMP-UDLs-Gel最优处方为卡波姆940比例1%、甘油比例15%、丙二醇比例10%。所制得的IMP-UDLs-Gel的Q12 h为(11.543±0.241) μg/cm2;外觀为乳白色、半透明状;粒径为(93.13±1.68) nm，多分散系数为0.268±0.012，Zeta电位为(-24.96±1.99) mV;pH为7.32±0.03;黏度为(45.37±1.27) g·s;稳态流量为(0.727±0.002) μg·h/cm2，滞后时间为(4.358±0.175) h，表观渗透系数为1.392×10-3 cm/h，且具有良好的物理稳定性和光稳定性。结论：建立的制备方法稳定可行，所制备的IMP-UDLs-Gel具有良好的黏附性、稳定性和透皮性。
关键词 欧前胡素;柔性脂质体;凝胶;处方优化;制备;质量评价;透皮性
Preparation and Quality Evaluation of Imperatorin Ultradeformable Liposomes Gel
CUI Xuehui1，2，CHEN Shihong1，2，QIU Jindi1，2，BAN Junfeng1，2，YANG Nannan1，2，NI Qingchun3，PAN Zhaoyan4，XIE Qingchun1，2，CHEN Yanzhong1，2，LYU Zhufen1，2(1.Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems/New Drug R&D Center， Guangdong Pharmaceutical University， Guangzhou 510006， China;2.R&D Innovation Team for Controlled-release Microparticle Drug Delivery System/Guangdong Provincial Engineering Center of Topical Precision Drug Delivery System， Guangdong Pharmaceutical University， Guangzhou 510006， China;3.Guangzhou General Pharmaceutical Research Institute Co.， Ltd.， Guangzhou 510240， China;4.Xinhua College of Sun Yat-sen University， Guangzhou 510520， China)
ABSTRACT OBJECTIVE： To prepare Imperatorin ultradeformable liposomes gel (IMP-UDLs-Gel)， and to evaluate its quality. METHODS： Based on single factor test， using 12 h accumulative penetration amount (Q12 h) as evaluation index， the proportion of carbomer 940， glycerol and propyl glycol in formulation of IMP-UDLs-Gel were investigated by orthogonal test. The optimal formulation was screened. The quality of IMP-UDLs-Gel prepared with the optimal formulation was evaluated. RESULTS： The optimal formulation of IMP-UDLs-Gel included carbomer 940 proportion of 1%， glycerol proportion of 15% and propyl glycol proportion of 10%. Q12 h of IMP-UDLs-Gel was (11.543±0.241) μg/cm2; the appearance was milky white and translucent; the particle size was (93.13±1.68) nm， PDI was 0.268±0.012， Zeta potential was (-24.96±1.99) mV; pH was 7.32±0.03; viscosity was (45.37±1.27) g·s; steady flow was (0.727±0.002) μg·h/cm2， lag time was (4.358±0.175) h， apparent permeability coefficient was 1.392×10-3 cm/h， and it has good physical and optical stability. CONCLUSIONS： The preparation method is stable and feasible， and the prepared IMP-UDLs-Gel has good adhesion， stability and transdermal property., 百拇医药(崔雪惠 陈世洪 邱金娣 班俊峰 杨楠楠 倪庆纯 潘钊言 谢清春 )
DOI 10.6039/j.issn.1001-0408.2020.09.10
摘 要 目的：制备欧前胡素柔性脂质体凝胶(IMP-UDLs-Gel)，并对其进行质量评价。方法：在单因素考察的基础上，以12 h累积透过量(Q12 h)为评价指标，采用正交试验法对IMP-UDLs-Gel处方中的卡波姆940比例、甘油比例和丙二醇比例进行考察，筛选最优处方，并对最优处方所制备的IMP-UDLs-Gel进行质量评价。结果：IMP-UDLs-Gel最优处方为卡波姆940比例1%、甘油比例15%、丙二醇比例10%。所制得的IMP-UDLs-Gel的Q12 h为(11.543±0.241) μg/cm2;外觀为乳白色、半透明状;粒径为(93.13±1.68) nm，多分散系数为0.268±0.012，Zeta电位为(-24.96±1.99) mV;pH为7.32±0.03;黏度为(45.37±1.27) g·s;稳态流量为(0.727±0.002) μg·h/cm2，滞后时间为(4.358±0.175) h，表观渗透系数为1.392×10-3 cm/h，且具有良好的物理稳定性和光稳定性。结论：建立的制备方法稳定可行，所制备的IMP-UDLs-Gel具有良好的黏附性、稳定性和透皮性。
关键词 欧前胡素;柔性脂质体;凝胶;处方优化;制备;质量评价;透皮性
Preparation and Quality Evaluation of Imperatorin Ultradeformable Liposomes Gel
CUI Xuehui1，2，CHEN Shihong1，2，QIU Jindi1，2，BAN Junfeng1，2，YANG Nannan1，2，NI Qingchun3，PAN Zhaoyan4，XIE Qingchun1，2，CHEN Yanzhong1，2，LYU Zhufen1，2(1.Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems/New Drug R&D Center， Guangdong Pharmaceutical University， Guangzhou 510006， China;2.R&D Innovation Team for Controlled-release Microparticle Drug Delivery System/Guangdong Provincial Engineering Center of Topical Precision Drug Delivery System， Guangdong Pharmaceutical University， Guangzhou 510006， China;3.Guangzhou General Pharmaceutical Research Institute Co.， Ltd.， Guangzhou 510240， China;4.Xinhua College of Sun Yat-sen University， Guangzhou 510520， China)
ABSTRACT OBJECTIVE： To prepare Imperatorin ultradeformable liposomes gel (IMP-UDLs-Gel)， and to evaluate its quality. METHODS： Based on single factor test， using 12 h accumulative penetration amount (Q12 h) as evaluation index， the proportion of carbomer 940， glycerol and propyl glycol in formulation of IMP-UDLs-Gel were investigated by orthogonal test. The optimal formulation was screened. The quality of IMP-UDLs-Gel prepared with the optimal formulation was evaluated. RESULTS： The optimal formulation of IMP-UDLs-Gel included carbomer 940 proportion of 1%， glycerol proportion of 15% and propyl glycol proportion of 10%. Q12 h of IMP-UDLs-Gel was (11.543±0.241) μg/cm2; the appearance was milky white and translucent; the particle size was (93.13±1.68) nm， PDI was 0.268±0.012， Zeta potential was (-24.96±1.99) mV; pH was 7.32±0.03; viscosity was (45.37±1.27) g·s; steady flow was (0.727±0.002) μg·h/cm2， lag time was (4.358±0.175) h， apparent permeability coefficient was 1.392×10-3 cm/h， and it has good physical and optical stability. CONCLUSIONS： The preparation method is stable and feasible， and the prepared IMP-UDLs-Gel has good adhesion， stability and transdermal property., 百拇医药(崔雪惠 陈世洪 邱金娣 班俊峰 杨楠楠 倪庆纯 潘钊言 谢清春 )
参见：首页 > 中医药 > 中药专业 > 中草药汇编 > 中药大典 > 根类 > 前胡