Alteration of Warfarins Pharmacologic Properties in Clathrates with Glycyrrhizic Acid and Arabinogalactan

Abstract

The article describes the pharmacological examinations of clathrates of warfarin (WF) with glycyrrhizic acid (GA) and arabinogalactan (AG). A direct connection between the clathrate structure and the pharmacon's anticoagulative properties was observed. A 20 mg/kg (WF 2 mg/kg) dose of WF: GA 1:10 clathrate causes the increase in prothrombin time (PT) only in 54 hours, after 3 administrations. In contrast, a 20 mg/kg (WF 2 mg/kg) dose of WF: AG 1:10 clathrate leads to an increase in PT in 24 and 48 hours after a single administration, which corresponds to the effect of a comparator agent WF (2 mg/kg).

Effect of Complexation with Arabinogalactan on Pharmacokinetics of “Guest” Drugs in Rats: For Example, Warfarin

“…The complex formation was confirmed by differential scanning calorimetry and increased aqueous solubility of WF [ 9 ].…”

“…One of these successful examples is water-soluble AG complex with warfarin, which is widely used as an indirect oral anticoagulant prescribed for a long time to patients with different cardiovascular diseases and after complicated surgeries [ 7 , 8 ]. The new complex was found to be highly effective; however, its anticoagulant activity was not as sharp as that of warfarin [ 9 ]. These data suggested that the complex is safer as compared to blank warfarin, since smoother blood dilution can reduce the risk of bleeding, which is one of the major side effects of warfarin [ 7 , 8 , 10 , 11 ].…”

Synthesis of 4‐Aryl‐8‐fluoro‐3a,4,5,9b‐tetrahydro‐3H‐cyclopenta[c]quinolines and Their Ozonides

“…Ozonolytic cleavage of the cycloalkenyl C¼C bond in tetrahydroquinoline fused with cyclopentene affords the ozonides of aza-heterocycles [10]. To improve antimalaria or antiviral activity of synthetic peroxides and ozonides, their conjugates containing weakly basic functional groups and heterocycles were obtained [11].…”

“…This method opens a simple route to the synthesis of substituted tetrahydroquinolines [9].Ozonolytic cleavage of the cycloalkenyl C¼C bond in tetrahydroquinoline fused with cyclopentene affords the ozonides of aza-heterocycles [10]. To improve antimalaria or antiviral activity of synthetic peroxides and ozonides, their conjugates containing weakly basic functional groups and heterocycles were obtained [11].Within this context, we report here a one-pot three-component cyclocondensation of 4-fluoroaniline with aromatic aldehydes and cyclopentadiene to synthesize 6fluorotetrahydroquinoline annulated with cyclopentene for the following possibility to obtain their stable ozonides.…”

Complexes of Polysaccharides and Glycyrrhizic Acid with Drug Molecules − Mechanochemical Synthesis and Pharmacological Activity

“…Table 1 below shows solubility data reported in [22][23][24][25][26][27][28][29][30][31][32] as far as published for the first time in this review.…”