绿原酸表观油水分配系数测定及在体肠吸收动力学研究

毕肖林; 李瑶瑶; 杜秋; 狄留庆

绿原酸表观油水分配系数测定及在体肠吸收动力学研究

毕肖林^1,2,3,,
李瑶瑶¹,
杜秋¹,
狄留庆^1,2,3

1.
南京中医药大学药学院，江苏南京 210023
2.
江苏省中药高效给药系统工程技术研究中心，江苏南京 210023
3.
南京市中药微丸产业化工程技术研究中心，江苏南京 210023

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出版历程
- 收稿日期: 2013-08-07
- 修回日期: 2013-09-16
- 刊出日期: 2013-11-10

Study on O/W Partition Coefficient of Chlorogenic Acid and Rats Intestinal Absorption Kinetics

BIXiao-lin^{1,2,3
,},
LIYao-yao¹,
DUQiu¹,
DILiu-qing^1,2,3

1.
School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China
2.
Jiangsu Engineering Research Center for Efficient Delivery System of TCM, Nanjing, 210023, China
3.
Nanjing Engineering Research Center for Industrialization of Chinese Medicine Pellets, Nanjing, 210023, China

摘要

摘要: 目的测定绿原酸的油水分配系数，研究绿原酸在体肠吸收机制。方法采用摇瓶法测定绿原酸在正辛醇-水/缓冲盐溶液中的表观油水分配系数；采用在体单向肠灌流实验，HPLC测定灌流液中绿原酸的浓度，考察吸收部位、药物浓度对绿原酸吸收的影响。结果 25℃下，绿原酸的表观油水分配系数为26.07（logP1.42）；绿原酸浓度为10、20和40 μg/mL 3个浓度时，各肠段不同浓度间的部分Ka值无显著性差异，同一浓度条件下不同肠段的吸收参数无显著性差异。结论在酸性和近中性条件下，绿原酸正辛醇/缓冲液分配系数受缓冲液的pH值影响不大；绿原酸在大鼠肠道内的吸收除被动扩散外，可能还存在其他吸收机制。绿原酸在大鼠小肠各个肠段均有吸收。
- 绿原酸 /
- 油水分配系数 /
- 在体肠单向灌流模型
Abstract: OBJECTIVE To determine apparent partition coefficients of chlorogenic acid and to investigate its absorption kinetics in the whole small intestine and different intestinal segments of rats. METHODS The shake-flask method was employed to determine the O/W partition coefficient of chlorogenic acid， and rat single-pass intestinal perfusion technique was employed to investigate the absorptive kinetics of chlorogenic acid. RESULTS The partition coefficient(P) of chlorogenic acid was 26.07（logP1.42）；There were a little significant difference (P<0.05) between the value of Peff of chlorogenic acid at three concentrations (10， 20 and 40 μg/mL)， and no significant difference between different intestinal segment. CONCLUSION There is little difference in apparent partition on coefficient in acidic and neutral phosphate buffer solution. Besides passive diffusion mechanism， other transports methods also worked， and chlorogenic acid could be absorbed in rats' every intestinal segment.
- chlorogenic acid /
- O/W partition coefficient /
- rat single-pass intestinal perfusion technique model

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参考文献(10)

[1]	金玉燕，张钧寿，张瑛，等．西红花苷大鼠小肠吸收研究及油水分配系数的测定[J]．中国药科大学学报，2004，35（3）：283-284．
[2]	Jin YY， Zhang JS， Zhang Y， et al. Studies on the intestinal absorption of crocin in rats and determination of the partition coefficient[J]. J Chin Pharm Univ， 2004， 35(3): 283-284.
[3]	李珂佳．靛玉红口服吸收机理研究[D]．成都：四川大学，2007．
[4]	Li KJ. Mechanism research on the oral absorption of Dianyuhong[D]. Chengdu: Sichuan university， 2007.
[5]	翟永松，杜守颖，徐冰，等．三七总皂苷油水分配系数及大鼠在体肠吸收动力学研究[J]．中国中药杂志，2010， 35（8）：984-988．
[6]	Zhai YS， Du SY， Xu B， et al. O/W partition coefficient of PNS and absorption kinetics of it in rat intestine[J].China J Chin Mater Med， 2010， 35(8): 984-988.
[7]	Tan XB， Jia XB. Absorptive property of eleutheroside B in rat intestine[J]. Chin Tradit Pat Med， 2008， 30: 346-349.
[8]	Gao Q， Shan J， Di L， et al. Therapeutic effects of daphnetin on adjuvant-induced arthritic rats[J]. J Ethnopharmacol， 2008， 120(2): 259-263.
[9]	Dressman JB， Lennernas H. Oral drug absorption:prediction and assessment[J]. Marcel Dekker Ihc， 2000: 51-72.
[10]	Ren J， Jiang XH， LI CR. Investigation on the absorption kinetics of chlorogenic acid in rats by HPLC[J]. Arch Pharm Res， 30（7）， 2007: 911-916.