This study highlights the improved biopharmaceutical properties of quercetin with therapeutically active coformers: picolinic acid and nicotinamide, using cocrystallization, well supported by antioxidant, antihaemolytic and pharmacokinetic activities.

Cocrystallization by the solvent drop grinding technique has been employed successfully to generate highly water-soluble cocrystals of a poorly soluble nutraceutical hesperetin with different coformers, picolinic acid, nicotinamide, and caffeine. The miniscule amount of solvent (ethanol here), added during grinding, expectedly imparts high molecular mobility and efficiency to the method. On the basis of preliminary indication of the phase transformation by differential scanning calorimetry, these cocrystals were further characterized by Fourier transform-infrared and solid state NMR spectroscopy. However, the final structural confirmation of these distinct cocrystalline forms was provided by either single crystal X-ray diffraction (XRD) for HESP-PICO or powder XRD data in Material Studio software to generate the crystal structure of HESP-NICO and HESP-CAFF. The data revealed the existence of supramolecular synthons established by novel hydrogen bonds between hydroxyl groups of hesperetin with acid or amide carbonyl (CO), and/or amidic NH 2 , and/or pyridine/aromatic nitrogen (N aromatic ) of coformers. Dissolution studies of cocrystals in aqueous buffer showed maximum concentration of hesperetin to be nearly 4−5 times higher than the pure substance. This has led to optimized pharmacokinetics as exhibited by improved relative bioavailability (HESP-PICO:1.36, HESP-NICO:1.57, HESP-CAFF:1.60). Furthermore, the enhanced antioxidant and antihemolytic effect, coupled with the protective action against inflammation, signifies the development of a clinically useful and a pharmaceutically acceptable form of hesperetin.

The above results showed all the three plants possess nootropic, anxiolytic and CNS-depressant activity. The results of memory-enhancing activity suggest C. pluricaulis to be used as true source of shankhpushpi.

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For the studied period, an annual average growth rate (AAGR) of 2.4% in volumes and 9.2% in values of export was observed. Nearly 30% of the global trade is made up by top two countries of the import and export. China and India from Asia; Egypt and Morocco from Africa; Poland, Bulgaria and Albania from Europe; Chile and Peru from South America are important supply sources. The USA, Japan and Europe are the major consumers of the world.

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The methanol extract of Swertia chirata was evaluated for antihepatotoxic activity against carbon tetrachloride induced liver toxicity in experimental rats. The extract was found to be active and on fractionation into butanol soluble and chloroform soluble fractions, the activity was traced and found more profound in the chloroform soluble fraction. The butanol soluble bitter rich fraction showed marginal activity. The results based on biochemical estimations have been expressed statistically and are additionally supported by histopathological examination of the liver of experimental rats and pentobarbitone induced sleep time studies in mice. Copyright © 1999 John Wiley & Sons, Ltd.

The extracts of Swertia chirata were evaluated for antihepatotoxic activity using paracetamol and galactosamine models. The methanol extract of the whole plant was found active at a dose of 100 mg/kg i.p. On fractionating this extract into chloroform soluble and butanol soluble fractions, the activity was retained in the chloroform soluble fraction which was most active at a dose level of 25 mg/kg i.p. with overall protection of 81% and 78% against paracetamol and galactosamine, respectively. The butanol soluble fraction, rich in bitter secoiridoids, was devoid of significant activity. The protective effect observed against these two hepatotoxins which are different in their mechanisms of inducing hepatotoxicity, suggests broader and non-specific protection of the liver against these two toxins by non-bitter components of Swertia chirata.