title: Supramolecular Complex of Ibuprofen with Larch Polysaccharide Arabinogalactan: Studies on Bioavailability and Pharmacokinetics.
abstract: OBJECTIVE
  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 and1H-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: Cmaxof IBU at doses of 20 and 40 mg/kg was found as 0.088 and 0.132 μg/ml, whereas Cmaxof 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.
authors.affiliation: Laboratory of Pharmacological Research, N.N. Vorozhtsov Institute of Organic Chemistry SB RAS, 9, Lavrentjeva Prospect, 630090, Novosibirsk, Russia. mihail.hvostov@gmail.com.
authors.forename: Mikhail V
authors.initials: MV
authors.lastname: Khvostov
authors.affiliation: Laboratory of Pharmacological Research, N.N. Vorozhtsov Institute of Organic Chemistry SB RAS, 9, Lavrentjeva Prospect, 630090, Novosibirsk, Russia.
authors.forename: Sergey A
authors.initials: SA
authors.lastname: Borisov
authors.affiliation: Laboratory of Pharmacological Research, N.N. Vorozhtsov Institute of Organic Chemistry SB RAS, 9, Lavrentjeva Prospect, 630090, Novosibirsk, Russia.|Novosibirsk State University, Novosibirsk, 630090, Russia.
authors.forename: Tatjana G
authors.initials: TG
authors.lastname: Tolstikova
authors.affiliation: Institute of Solid State Chemistry and Mechanochemistry SB RAS, Novosibirsk, 630090, Russia.
authors.forename: Alexander V
authors.initials: AV
authors.lastname: Dushkin
authors.affiliation: Institute of Solid State Chemistry and Mechanochemistry SB RAS, Novosibirsk, 630090, Russia.
authors.forename: Biligma D
authors.initials: BD
authors.lastname: Tsyrenova
authors.affiliation: Institute of Solid State Chemistry and Mechanochemistry SB RAS, Novosibirsk, 630090, Russia.
authors.forename: Yulia S
authors.initials: YS
authors.lastname: Chistyachenko
authors.affiliation: Voevodsky Institute of Chemical Kinetics and Combustion, SB RAS, Novosibirsk, 630090, Russia.
authors.forename: Nikolay E
authors.initials: NE
authors.lastname: Polyakov
authors.affiliation: Voevodsky Institute of Chemical Kinetics and Combustion, SB RAS, Novosibirsk, 630090, Russia.|Novosibirsk State University, Novosibirsk, 630090, Russia.
authors.forename: Galina G
authors.initials: GG
authors.lastname: Dultseva
authors.affiliation: Voevodsky Institute of Chemical Kinetics and Combustion, SB RAS, Novosibirsk, 630090, Russia.|Novosibirsk State University, Novosibirsk, 630090, Russia.
authors.forename: Andrey A
authors.initials: AA
authors.lastname: Onischuk
authors.affiliation: Laboratory of Pharmacological Research, N.N. Vorozhtsov Institute of Organic Chemistry SB RAS, 9, Lavrentjeva Prospect, 630090, Novosibirsk, Russia.
authors.forename: Sergey V
authors.initials: SV
authors.lastname: An'kov
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics*; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning / Q000379:methods; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004338:Drug Combinations; D005685:Galactans / Q000493:pharmacokinetics*; D007052:Ibuprofen / Q000493:pharmacokinetics*; D028221:Larix / Q000737:chemistry*; D008297:Male; D051379:Mice; D011134:Polysaccharides / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004338:Drug Combinations; D005685:Galactans; D011134:Polysaccharides; C005653:arabinogalactan; D007052:Ibuprofen