02161nas a2200193 4500008004100000245010900041210006900150260000800219490000800227520145000235100002201685700002201707700002801729700001901757700001901776700002401795700002401819856012401843 2019 eng d00aCo amorphous valsartan nifedipine system: Preparation, characterization, in vitro and in vivo evaluation0 aCo amorphous valsartan nifedipine system Preparation characteriz cNOV0 v1393 a

Co amorphous systems are supersaturated drug delivery systems which offer a basic platform for delivery of multicomponent adducts (combination of more than one active pharmaceutical ingredient (API)) and/or as a fixed dose combination therapy, in addition to their potential to improve the apparent solubility, dissolution rate and ultimately bioavailability of poorly water soluble APIs. In the present work, a new drug-drug co amorphous system namely valsartan-nifedipine was prepared by quench cooling technique. Prepared co amorphous system was characterized for its solid state behavior with the help of Fourier Transform Infrared spectroscopy (FTIR), Differential Scanning Calorimetry (DSC) and Powder X Ray Diffractometry (PXRD). The optimized co amorphous system was stable for 1 month when exposed to accelerated stability condition (40 +/- 2 degrees C and 75 +/- 5% RH). The improved stability of amorphous nifedipine in co amorphous system was attributed to improved miscibility and intra and intermolecular non-covalent interactions mainly due to presence of hydrogen bonding between valsartan and nifedipine which was studied by FTIR analysis. Co amorphous systems were evaluated by mainly in vitro dissolution and in vivo benefit. In vitro dissolution study showed nearly 5.66 folds and 1.61 folds improvement which was translated to 3.63 and 2.19 times enhancement in vivo C-max for nifedipine and valsartan respectively.

1 aLodagekar, Anurag1 aChavan, Rahul, B.1 aMannava, M., K. Chaitan1 aYadav, Balvant1 aChella, Naveen1 aNangia, Ashwini, K.1 aShastri, Nalini, R. uhttps://library.ncl.res.in/content/co-amorphous-valsartan-nifedipine-system-preparation-characterization-vitro-and-vivo02217nas a2200181 4500008004100000245011400041210006900155260000800224300001400232490000700246520154700253100001901800700002201819700002601841700002401867700002401891856012001915 2019 eng d00aHepatoprotective cocrystals of isoniazid: synthesis, solid state characterization, and hepatotoxicity studies0 aHepatoprotective cocrystals of isoniazid synthesis solid state c cSEP a5161-51720 v193 a

Isoniazid (INH) is one of the first line drugs used in combination with pyrazinamide and rifampicin for the management of tuberculosis. Idiosyncratic hepatotoxicity is one of the most common side effects of antitubercular therapy worldwide. The current study explores solid phase modification of INH by cocrystallization with various hepatoprotective coformers, namely chrysin, hesperetin, silibinin, syringic acid (SYRA), and quercetin (QUE) to address hepatotoxicity concerns. Cocrystals were obtained with SYRA and QUE. Supramolecular synthons based on pyridine-carboxyl and pyridine-hydroxyl synthon enabled the formation of cocrystals. INHSYRA and INHQUE cocrystals were characterized by FT-IR, DSC, and PXRD. Single crystal X-ray analysis of INHSYRA revealed that it crystallized in triclinic system with the P (1) over bar space group. Intrinsic dissolution rate studies (IDR) showed slow drug release from both the cocrystals. Hepatoprotective effects of INHSYRA and INHQUE cocrystals were evaluated by a single toxic dose study and a subchronic study for 28 days. Results from the subchronic study indicated significant increase in ALT, AST, and ALP enzyme levels in the INH-treated group whereas the enzyme levels in INHSYRA and INHQUE cocrystal treated group were comparable to that of the untreated group. This study demonstrates the in vivo hepatoprotective effects of coformers SYRA and QUE provide promising evidence for utility of nutraceutical based coformers, to tackle hepatotoxicity associated with various drugs.

1 aYadav, Balvant1 aGunnam, Anilkumar1 aThipparaboina, Rajesh1 aNangia, Ashwini, K.1 aShastri, Nalini, R. uhttps://library.ncl.res.in/content/hepatoprotective-cocrystals-isoniazid-synthesis-solid-state-characterization-and01201nas a2200193 4500008004100000022001400041245009700055210006900152260000900221300001400230490000700244520052300251100001900774700002200793700001900815700002400834700002400858856012500882 2020 eng d a1528-748300aGeneration and evaluation of pharmacologically relevant drug-drug cocrystal for gout therapy0 aGeneration and evaluation of pharmacologically relevant drugdrug cJUN  a3577-35830 v203 a

The present study reports a novel drug-drug cocrystal of febuxostat and piroxicam for the treatment of gout. Single crystal X-ray diffraction revealed a monoclinic system with P2(1)/c space group. The prepared cocrystal enhanced the solubility of febuxostat and piroxicam and improved the dissolution rate of piroxicam in pH 6.8 as compared to the pure drug. Further, the compressibility assessment of cocrystal by Aulton and Wells method confirmed its plastic behavior and suitability for direct compression.

1 aModani, Sheela1 aGunnam, Anilkumar1 aYadav, Balvant1 aNangia, Ashwini, K.1 aShastri, Nalini, R. uhttps://library.ncl.res.in/content/generation-and-evaluation-pharmacologically-relevant-drug-drug-cocrystal-gout-therapy