目的:考察3-乙酰基-11-羰基-b-乙酰乳香酸(AKBA)经血脑屏障的通透性.方法:采用MD-CK-MDR1细胞单层模型研究AKBA的双向跨膜转运,采用LC-MS/MS分析方法测定AKBA的浓度,计算其表观渗透系数(Papp).结果:咖啡因吸收方向Papp为(18.65±1.94)×10-6cm.s-1,罗丹明123外排率(RE)为19.96,接收室HBSS中可以检测到AKBA...
MDCK-MDR1细胞药物体外吸收模型的建立及验证
分别检测转运60min后接收侧及给药侧的浓度。计算60min后药物回收率,及表观通透系数(papp)和表观通透系数的比率(pappratio=papp[b→a]/papp[a→b]),据此来评判mdck细胞中犬p-gp细胞基因是否已敲除成功。 如表1、表2和表3所示,60min时digoxin在a→b方向给药和在b→a方向给药试验的papp值、pappratio及回收...
溶液中葛根素在MDCK-MDR1单层的吸收方向转运表观渗透系数(Papp)为1.04×10^-6 cm/s,外排方向转运Papp值为1.05×10^-6 cm/s,微乳中葛根素双侧转运Papp值均较溶液中葛根素显著增加(P〈0.05).微乳作用可以减少MDCK-MDR1紧密连接蛋白Claudin-1,Occludin,ZO-1,F-actin的表达,促进细胞膜流动,降低细胞膜电位.结论...
时,表现为中等渗透性;当Papp >200 nm·s -1 , 表现为高渗透性。如果Efflux >2,则认为GF120918 是Pgp 的作用底物。ML120B 的细胞膜渗透性检测 结果见表2。结果表明:ML120B 为高渗透性药物,但并不是Pgp 的作用底物。 Table 2 Passive permeability of ML120B MDCK-hMDR1 in the absence or presence of...
Hoodigogenin A was efficiently transported by passive diffusion across Caco-2 and MDR1-MDCK monolayers with Pappvalues in the range of 32脳106cm/sec ... VLM Madgula,B Avula,RS Pawar,... - 《Planta Medica》 被引量: 32发表: 2010年 Functional Dynamics of Myelin Lipids* Biological membranes...
In the MDCKII-MDR1 cells, berberine and berbamine inhibited both theefflux Papp of CSA and digoxin. Our data suggests that OGR extract, berberine,and berbamine can inhibit P-gp thereby may increase the bioavailability of drugsthat are substrates of P-gp....
In the MDCKII-MDR1 cells, berberine and berbamine inhibited both the efflux Papp of CSA and digoxin. Our data suggests that OGR extract, berberine, and berbamine can inhibit P-gp thereby may increase the bioavailability of drugs that are substrates of P-gp.;The first objective was to ...