当前位置： SCI文献检索 > EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS期刊下所有文献 > Supramolecular Complex of Ibuprofen with Larch Polysaccharide Arabinogalactan: Studies on Bioavailability and Pharmacokinetics.

Supramolecular Complex of Ibuprofen with Larch Polysaccharide Arabinogalactan: Studies on Bioavailability and Pharmacokinetics.

Abstract：

BACKGROUND AND OBJECTIVES:In the present work, pharmacological and pharmacokinetic properties of the supramolecular complex of non-steroid anti-inflammatory drug ibuprofen (IBU) with natural polysaccharide arabinogalactan (AG) were studied. The main goals of such complexation were the increase of ibuprofen's bioavailability and decrease its effective dose after oral administration. METHODS:The complex with mass ratio as IBU:AG 1:10 was obtained by mechanochemical synthesis and characterized by water solubility, electron microscopy, differential scanning calorimetry, X-ray powder diffraction analysis and 1H-nuclear magnetic resonance spectroscopy. Different animal models of pain and inflammation was used to investigate IBU:AG biological effects. Plasma concentration of IBU and its pharmacokinetic parameters were evaluated after oral introduction. RESULTS:It was found that ibuprofen's effective analgesic and anti-inflammatory dose decreased twofold after its introduction as a complex with AG. The reason of this difference is due to the increase of ibuprofen concentration in rats' plasma: C max of IBU at doses of 20 and 40 mg/kg was found as 0.088 and 0.132 μg/ml, whereas C max of IBU in the complex form was 0.103 and 0.160 μg/ml, respectively. CONCLUSIONS:Thus, we have shown that complexation of the IBU with AG results in its bioavailability increase, reduction of the effective dose and should decrease toxic side effects.

journal_name

Eur J Drug Metab Pharmacokinet

journal_title

European journal of drug metabolism and pharmacokinetics

authors

Khvostov MV,Borisov SA,Tolstikova TG,Dushkin AV,Tsyrenova BD,Chistyachenko YS,Polyakov NE,Dultseva GG,Onischuk AA,An'kov SV

doi

10.1007/s13318-016-0357-y

subject

Has Abstract

pub_date

2017-06-01 00:00:00

pages

431-440

issue

3

eissn

0378-7966

issn

2107-0180

pii

10.1007/s13318-016-0357-y

journal_volume

42

pub_type

杂志文章

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