Improvement of pharmacological values of the nifedipine by means of mechanochemical complexation with glycyrrhizic acid

Abstract

A new water-soluble form of the calcium blocker nifedipine (NF) with glycyrrhizic acid (GA) (with molecular ratio 1:4) has been obtained by mechanochemical synthesis. Its pharmacological advantages in comparison with nifedipine were determined. An effective dose of nifedipine in complex reduced to 10 times as compared to its therapeutic dose while high antihypertensive activity preservation and pleiotropic antiarhythmic activity enhancement. This new antihypertensive and antiarhythmic agent (complex of NF:GA = 1:4) is chemically stable and safe for parenteral administration.

Supramolecular assemblies based on natural small molecules: Union would be effective

“…The process of complexation was attributed to the multiple noncovalent interactions. After entering the body, glycyrrhizic acid might affect the ordering of lipids and enhance the fluidity and permeability of cell membrane via incorporating and/or extracting the membrane cholesterol, thus promoting the active ingredients penetration into the cell [ [108] , [109] , [110] , [111] , [112] ].…”

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.…”

Formulation and evaluation of novel glycyrrhizic acid micelles for transdermal delivery of podophyllotoxin

“…If so, whether could this new POD delivery system attenuate the side effects of POD? It has been reported that GA could form the ''host-guest'' type (Polyakov et al, 2006) with some medicines such as nifedipine (Tolstikova et al, 2010), buspirone (Fomina et al, 2014), carotenoids (Polyakov et al, 2006), simvastatin (Vavilin et al, 2008), and lappaconitine (Polyakov et al, 2005), of which GA is the host while the medicine is the guest. Interestingly, it was demonstrated that applications of GA together with these medicines could strengthen their therapeutic actions (Selyutina et al, 2015) and reduce their side effects.…”