摘要
目的考察微乳液递送吴茱萸碱(evodiamine loaded microemulsion,EDM)体外释放特征及大鼠的在体吸收情况。方法制备EDM,用透析法研究其在p H 1.2盐酸溶液和p H6.8磷酸缓冲溶液中的体外释放特征,计算其累积释放率。再用大鼠在体单向肠循环法研究其在十二指肠、空肠、回肠和结肠的吸收情况,以及在胃的吸收情况,计算其在各部位的吸收速率常数(absorption rate constant,K_a)与有效渗透率(effective permeability,P_(eff))。本实验用HPLC法测定吴茱萸碱(evodiamine,ED)的浓度。结果EDM和ED在p H 1.2盐酸溶液中的累积释放率分别为(64.76±0.73)%、(13.98±0.49)%,EDM的累积释放率为ED的4.63倍;在p H 6.8磷酸缓冲液中的累积释放率分别为(91.72±0.51)%、(18.34±0.20)%,EDM的累积释放率为ED的5.01倍。EDM在胃肠的K_a为ED的3倍以上,P_(eff)为ED的2倍以上。结论微乳液能使ED的体外释放以及大鼠胃肠吸收均得以改善。
AimTo study the characteristics of in vitro release and in situ absorption of evodiamine loaded microemulsion(EDM).MethodsEDM was prepared,its release in pH 1.2 HCl solution and pH 6.8 phosphate buffer solution were studied by dialysis,and the cumulative release rates were calculated.The single-pass intestinal perfusion was used to study the absorption of EDM in duodenum,jejunum,ileum and colon,the absorption in stomach was also studied,and the absorption rate constant(K_a)and effective permeability(P_(eff))of the drug were calculated.The concentration of ED was measured by HPLC.ResultsThe cumulative release rate of EDM and ED in pH 1.2 HCl solution was(64.76±0.73)%,(13.98±0.49)%,respectively,and that of EDM was 4.63 times of ED.In p H 6.8 phosphate buffer solution the cumulative release rate was(91.72±0.51)%,(18.34±0.20)%,respectively,which was 5.01 times of ED.The K_aof EDM was more than 3 times of ED,and P_(eff )was more than 2 times of ED.ConclusionMicroemulsion can improve in vitro release and in situ absorption of ED.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2018年第1期87-90,共4页
Chinese Pharmacological Bulletin
基金
重庆市科委项目(No cstc2015jcyj BX0027)
关键词
吴茱萸碱
微乳液
透析法
体外释放
单向肠灌流模型
在体吸收
高效液相色谱法
evodiamine
microemulsion
dialysis method
in vitro release
single-pass intestinal perfusion model
in situ absorption
high performance liquid chromatography
