Absorption Kinetics of Scutellarin-PEG Conjugates in Rat Intestine
ZHOU Qing-song，JIANG Xue-hua*，FAN Xin-xing
Author information+
West China School of Pharmacy，Sichuan University，Chengdu 610041，China
{{custom_zuoZheDiZhi}}
{{custom_authorNodes}}
{{custom_bio.content}}
{{custom_bio.content}}
{{custom_authorNodes}}
Collapse
History+
Received
Published
2005-05-11
2006-03-05
Issue Date
2006-03-05
Abstract
OBJECTIVE To investigate the absorption kinetics of scutellarin-PEG conjugates at different intestine segments of rats and the influence of different concentration and molecular weight of the drugs on the intestinal absorption after PEGylation.METHODS The intestine in rats was cannulated for in situ recirulation.RESULTS The absorption rate constant(Ka) at duodenum,jejunum and ileum were 0.132 6,0.079 9,0.081 9 h-1,respectively.The Ka of scutellarin at the concentrations of 30,100 and 200 mg·L-1 in intestine were 0.029 2,0.033 8,0.030 6 h-1 while the Ka of scutellarin-PEG400 conjugates at the concentrations of 40,130 and 260 mg·L-1 were 0.157 7,0.162 4 and 0.170 8 h-1,respectively.The Ka of scutellarin and its PEG200,400,1000 conjugates were 0.033 8,0.154 7,0.162 4 and 0.068 0 h-1,respectively.CONCLUSION The PEGylation enhances the absorption of scutellarin in rat intestine.However,among the PEG conjugates,with the increased PEG molecular weight,the absorption of conjugates decreases accordingly.The conjugates are well absorbed at the duodenum in rats.The concentration has no effect on the absorption kinetics.The absorption of scutellarin and its conjugates are a first-order process with the passive diffusion mechanism.
ZHOU Qing-song;JING Xue-hu;FN Xin-xing.
Absorption Kinetics of Scutellarin-PEG Conjugates in Rat Intestine [J]. Chinese Pharmaceutical Journal, 2006, 41(05): 375-378
{{custom_sec.title}}
{{custom_sec.title}}
{{custom_sec.content}}
References
[1] JIANG X H，LI S H，LAN K，et al. Study on the pharmacokinetics of scutellarin in dogs[J] .Acta Pharm Sin（药学学报），2003，38(5)：371-373.
[2] CHEN D W，ZOU Y S，LIANG Y Z，et al. Studies on the absorption kinetics of rosiglitazone maleate in rats’intestine[J] .Chin Pharm J（中国药学杂志），2002，37(6)：436-438.
[3] PIN Q N.Pharmaceutics Experiment and Guidance（药剂学实验与指导）[M] .Beijing：China Medicine Technology Press，1994：214-222.
[4] DING J S，ZHANG J S. Absorption of breviscapine in small intestine of rat[J] .J China Pharm Univ（中国药科大学学报），2003，34(1)：65-69.
[5] LIANG W Q.Biopharmaceutics and Pharmacokinetics（生物药剂学与药物动力学）[M] . Beijing： People’medical publishing house，2000：11.
[6] RICHARD B G，CHOE Y H，JEFFREY M，et al. Effective drug delivery by PEGylated drug conjugates[J] .Adv Drug Deliv Rev，2003，55：217-250.
