鸦胆子油油水分配系数及其乳剂大鼠在体肠吸收特性
? 1669 ?
中华中医药杂志(原中国医药学报)2012年6月第27卷第6期 CJTCMP ,June 2012,Vol .27,No.6?研究报告?
通讯作者：陈钢，广州大学城外环东路280号广东药学院药科学院药剂系，邮编：510006，电话： 020-********，E -mail：cg753@https://www.wendangku.net/doc/4b10165092.html, 鸦胆子油油水分配系数及其乳剂大鼠在体
肠吸收特性研究
陈钢1，张晓1，卢刚2，刘广泉1，曾洁1，李晔3，魏少阳3
（1广东药学院药科学院，广州 510006；2上海博爱医院，上海 200031；3陕西省中医药研究院，
西安 710003）
摘要：目的：测定鸦胆子油的油水分配系数，并考察鸦胆子油乳在大鼠的肠吸收性质及机制。方法：采用经典摇瓶法测定鸦胆子油的油水分配系数（P）；采用在体单向肠灌流法模型研究不同浓度鸦胆子油乳在大鼠的十二指肠、空肠、回肠及结肠的吸收情况，并测定其吸收速率常数（Ka）、吸收率（Fa）和表观渗透系数（Papp）。结果：鸦胆子油疏水常数logP的平均值为1.193。鸦胆子油乳在小肠（十二指肠、空肠、回肠）吸收较好，在结肠吸收较少且不规则。其Ka、Fa和Papp按十二指肠、空肠、回肠依次下降且差异显著（P <0.05），不同浓度在同一肠段随着浓度增加，吸收也随之增加，高浓度与低浓度相比，Fa和Papp差异显著（P <0.05），Ka没有显著性差异。结论：鸦胆子油透过生物膜的能力较强。鸦胆子油乳在十二指肠吸收最佳，在小肠内的吸收为一级动力学过程，并无自身浓度抑制作用，可能主要为被动转运机制。
关键词：鸦胆子油；在体单向肠灌流模型；吸收机制；油水分配系数；乳剂；油酸
基金资助：广东省科技计划项目（No.2011B031700016），广东省大学生创新实验项目（No.1057310012），陕西省“13115”科技创新工程重大科技专项（No.2009ZDKG-82），广东药学院师资队伍建设经费资助
O/W partition coef ? cient of brucea javanica oil and absorption characteristics of
its emulsion in rat intestine in situ
CHEN Gang 1, ZHANG Xiao 1, LU Gang 2, LIU Guang-quan 1, ZENG Jie 1, LI Ye 3, WEI Shao-yang 3( 1School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China; 2Shanghai Humanity Hospital,
Shanghai 200031, China; 3Shaanxi Academy of Traditional Chinese Medicine, Xi’an 710003, China )
Abstract: Objective: To determine the O/W partition coef ?
cient of brucea javanica oil and investigate the absorption characteristics and mechanism of its emulsion in rat intestine. Methods: The shake-flask method was employed to determine the O/W partition coef ? cient （P ）of brucea javanica oil. The absorptions of six concentrations of brucea javanica oil emulsion in different intestinal segments were studied by in situ rats single pass perfusion model, and the absorption rate constant (Ka), absorption rate (Fa) and apparent permeability coef ? cients (Papp) were determined. Results: The logP of brucea javanica oil was
1.193. Brucea javanica oil emulsion was absorbed at all intestinal segments. However, the absorption of small intestine was better than that of colon. The Ka, Fa and Papp of various intestinal segments decreased in turns in duodenum, jejunum and ileum (P < 0.05). Drug concentration had little signi ? cant effect on the Ka in the same intestinal segment. The uptake of the drug increased when the concentration rose, and the Fa and Papp at the high concentration were signi ? cantly improved compared with those at the low concentration (P < 0.05). Conclusion: According to the logP, it was conjectured that brucea javanica oil could easily permeate the membrane. The absorption of the duodenum was the best at various segments of rat intestine. The absorption of small intestine was ? rst-order kinetics without highest saturated concentration and passive transport mechanism might be the major factor.
Key words: Brucea javanica oil; In situ rats single pass perfusion model; Absorption mechanism; O/W partition coef ? cient; Emulsion; Oleic acid
Fund assistance: Science and Technology Planning Project of Guangdong Province (No. 2011B031700016), College Students Innovative Experimental Project of Guangdong Province (No.1057310012), the Key Project of ‘13115’Technology Innovation Project of Shanxi Province (No.2009ZDKG-82), the Faculty Construction Funds of Guangdong Pharmaceutical University