title: Polysaccharide arabinogalactan from larch Larix sibirica as carrier for molecules of salicylic and acetylsalicylic acid: preparation, physicochemical and pharmacological study.
abstract: Inclusion complexes of salicylic acid (SA) and acetylsalicylic acid (aspirin, ASA) with polysaccharide arabinogalactan (AG) from larch wood Larix sibirica and Larix gmelinii were synthesized using mechanochemical technology. In the present study, we have investigated physicochemical properties of the synthesized complexes in solid state and in aqueous solutions as well as their anti-aggregation and ulcerogenic activity. The evidence of the complexes formation was obtained by nuclear magnetic resonance (NMR) relaxation technique. It was shown that in aqueous solution the molecules of SA and ASA are in fast exchange between the complex with AG macromolecules and solution. The stability constant of aspirin complex was calculated. It was shown that mechanochemically synthesized complexes are more stable when compared to the complex obtained by mixing solutions of the components. Complexes of ASA show two-fold increase of anti-platelet effect. It allows to reduce the dose of the antithrombotic drug and its ulcerogenic activity. These results substantiate the possibility to design new preparations on the basis of ASA with increased activity and safety.
authors: Institute of Solid State Chemistry and Mechanochemistry , Novosibirsk , Russia .
authors: Yulia S
authors: YS
authors: Chistyachenko
authors: Alexandr V
authors: AV
authors: Dushkin
authors: Nikolay E
authors: NE
authors: Polyakov
authors: Mikhail V
authors: MV
authors: Khvostov
authors: Tatyana G
authors: TG
authors: Tolstikova
authors: Genrikh A
authors: GA
authors: Tolstikov
authors: Nikolay Z
authors: NZ
authors: Lyakhov
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001241:Aspirin / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry* / Q000302:isolation & purification; D005685:Galactans / Q000737:chemistry* / Q000302:isolation & purification; D028221:Larix / Q000737:chemistry*; D008297:Male; D044367:Phase Transition; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood / Q000494:pharmacology; D017208:Rats, Wistar; D020156:Salicylic Acid / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000494:pharmacology; D012995:Solubility; D012996:Solutions; D013499:Surface Properties
chemical_list: D004337:Drug Carriers; D005685:Galactans; D010975:Platelet Aggregation Inhibitors; D012996:Solutions; D020156:Salicylic Acid; D001241:Aspirin; C005653:arabinogalactan
keywords: Complexation; NMR; mechanical activation; platelet aggregation; solid dispersion