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 Full article

Journal

European Journal of Drug Metabolism and Pharmacokinetics
ISSN: 0378-7966 , E-ISSN: 2107-0180

Output data

Year: 2017, Volume: 42, Number: 3, Pages: 431-440 Pages count : 10 DOI: 10.1007/s13318-016-0357-y

Authors

Khvostov Mikhail V. ¹ , Borisov Sergey A. ¹ , Tolstikova Tatjana G. ^1,4 , Dushkin Alexander V. ² , Tsyrenova Biligma D. ² , Chistyachenko Yulia S. ² , Polyakov Nikolay E. ³ , Dultseva Galina G. ^3,4 , Onischuk Andrey A. ^3,4 , An'kov Sergey V. ¹

Affiliations

1	(Данные Web of science) RAS, SB, NN Vorozhtsov Inst Organ Chem, Lab Pharmacol Res, 9,Lavrentjeva Prospect, Novosibirsk 630090, Russia
2	(Данные Web of science) RAS, SB, Inst Solid State Chem & Mechanochem, Novosibirsk 630090, Russia
3	(Данные Web of science) RAS, SB, Voevodsky Inst Chem Kinet & Combust, Novosibirsk 630090, Russia
4	(Данные Web of science) Novosibirsk State Univ, Novosibirsk 630090, Russia

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 H-1-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 mu g/ml, whereas C-max of IBU in the complex form was 0.103 and 0.160 mu g/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.

Khvostov M.V. , Borisov S.A. , Tolstikova T.G. , Dushkin A.V. , Tsyrenova B.D. , Chistyachenko Y.S. , Polyakov N.E. , Dultseva G.G. , Onischuk A.A. , An'kov S.V.
Supramolecular Complex of Ibuprofen with Larch Polysaccharide Arabinogalactan: Studies on Bioavailability and Pharmacokinetics
European Journal of Drug Metabolism and Pharmacokinetics. 2017. V.42. N3. P.431-440. DOI: 10.1007/s13318-016-0357-y WOS Scopus

Published online:	Jun 28, 2016
Published print:	Jun 1, 2017

Web of science	WOS:000400988000008
Scopus	2-s2.0-84976407537
OpenAlex	W2468017369