Mohammady, Mohsen published the artcileDesign of ultra-fine carvedilol nanococrystals: Development of a safe and stable injectable formulation, Synthetic Route of 1453-82-3, the publication is European Journal of Pharmaceutics and Biopharmaceutics (2021), 139-151, database is CAplus and MEDLINE.
Carvedilol (CAR) is a strategic beta-blocker agent which its application has been limited by its very low water solubility The present study describes a soluble form of drug based on nano-cocrystal (NCC) anti-solvent precipitation technique. The COSMOquick software was employed to select the optimum coformer (tartaric acid, TA) and organic solvent (acetone) relying on the enthalpy changes of cocrystn. and solubilization. Central Composite Design (CCD) considering the impact of CAR, TA, poloxamer 188 (stabilizer) concentrations, and anti-solvent/solvent ratio on CAR NCCs particle size (PS) could produce ultra-fine NCCs (about 1 nm). The lyophilization of NCCs investigating slow/fast freezing rates, various types and concentrations of cryprotectants and lyoprotectants indicated that PEG and trehalose (5% w/v concentration) under slow freezing rate could re-produce the initial PSs successfully. CAR NCCs indicated about 2000 fold increase in solubility compared with pure CAR. DSC and PXRD experiments proved that the formulations containing trehalose led to more crystalline and the ones comprising PEG led to more amorphous structures. Interestingly, the slow freezed PEG protected NCCs were phys. stable for at least 18 mo. In conclusion, the NCC technol. could produce the first safe soluble form of CAR for treating hypertension urgencies easy for industrial scale-up.
European Journal of Pharmaceutics and Biopharmaceutics published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Synthetic Route of 1453-82-3.
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