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This research work is designed to overcome the problems associated with the poorly aqueous soluble drug. Fenofibrate (FENO) being a BCS Class II drug shows low solubility with high permeability. Compatibility of the drug and polymer studies was done by FTIR. Physical mixtures (PM) of the drug and polymer HPMCAS were prepared by the trituration method. Fenofibrate solid dispersions (SD) were prepared by a common solvent technique ascribed to feasibility on a laboratory scale. The physical state of formulations was characterized by powder XRD and TGA. Solubility of a pure drug (FENO), Physical mixture, and SD were found to be 0.3, 0.78±0.15 to 1.15±0.28, and 2.17±0.37 to 3.25±0.14 mg/ml respectively. Percentage yield and percentage drug content were determined and found within a satisfactory range. The maximum cumulative percentage of drug release from the pure drug (FENO), Physical mixture, and SD was found to be 34.5%, 72.1 and 97.2% respectively at 60 minutes. A microscopy (SEM) study found that the prepared solid dispersion has porous morphology. The present study establishes the increased bioavailability of the optimized batch when compared with the pure FENO. There was a significant (50%) increase in absorption of Fenofibrate observed from the in vitro everted gut sac model. SD of FENO was developed successfully. The solubility of FENO was ameliorated significantly while compared with API (pure FENO). This research work found the formulation of SD preferable technique to enhance solubility and enhance dissolution of lipophilic drugs. [ABSTRACT FROM AUTHOR]

This research work designed to overcome the problems associated with poorly aqueous soluble drug. Fenofibrate (FENO) being BCS Class II drug shows low solubility but permeability is high. Compatibility of the drug and polymer studies was done by FTIR. Physical mixtures (PM) of the drug and polymer HPMCAS were prepared by trituration method. Fenofibrate solid dispersions (SD) were prepared by common solvent technique ascribed feasibility in laboratory scale. Physical state of formulations was characterized by powder XRD, TGA. Solubility of pure drug (FENO), Physical mixture and SD found to be 0.3, 0.78±0.15 to 1.15±0.28 and 2.17±0.37 to 3.25±0.14 mg/ml respectively. Percentage yield and percentage drug content were determined and found within satisfactory range. The maximum cumulative percentage of drug release from pure drug (FENO), Physical mixture and SD found to be 34.5%, 72.1 and 97.2% respectively at 60 minutes. Microscopy (SEM) study was found that the prepared solid dispersion has porous morphology. The present study establishes the increased bioavailability of the optimized batch when compared with the pure FENO. There was significant (50%) increase in absorption of Fenofibrate observed from the in vitro everted gut sac model. SD of FENO was developed successfully. The solubility of FENO was ameliorated significantly while compared with API (pure FENO). This research work found formulation of SD preferable technique to enhance solubility and enhance dissolution of lipophilic drugs. [ABSTRACT FROM AUTHOR]

Abstract: Reaction of [(η5-C5Me5)MCl4], 1–2 (1: M=Mo and 2: W) with six fold excess of [LiBH4·thf] followed by thermolysis with excess chalcogen powders (S, Se and Te) yielded dichalcomolybda- and tungstaboranes, [(η5-C5Me5M)2B4H4E2], 5–8 (5: M=Mo, E=S; 6: M=Mo, E=Se; 7: M=Mo, E=Te; 8: M=W, E=Se) in modest yields. The geometry of 5–8 resembles a hexagonal bipyramid with a missing connectivity of two chalcogen vertices and a very short cross cage metal–metal bonding. All these new dichalcometallaboranes have been characterized by mass, 1H, 11B, 13C NMR spectroscopy, and the structural types were unequivocally established by crystallographic analysis of compound 6. [Copyright &y& Elsevier]

Abstract: Reaction of (η5-C5Me5)MoCl4 with 6-fold excess of LiBH4·thf followed by pyrolysis with BHCl2·SMe2 in toluene at 90°C yielded known (η5-C5Me5Mo)2B5H9 (1) and B-Cl inserted (η5-C5Me5Mo)2B5H8Cl (2), (η5-C5Me5Mo)2B5H7Cl2 (3–5, three isomers) and (η5-C5Me5Mo)2B5H5Cl4 (6). In addition, reaction of (η5-C5Me5Mo)2B5H9 with 5-fold excess of n-BuLi followed by excess of MeI in THF yielded B-Me inserted metallaboranes (η5-C5Me5Mo)2B5H7(CH3)2 (7, 8 two isomers) and (η5-C5Me5Mo)2B5H6(CH3)3 (9, 10 two isomers). Isolated yields of 2–6 are poor but 7–10 are modest to good. Compounds 2–10 can be viewed as bicapped closo trigonal bipyramidal geometry. All the new compounds have been characterized in solution by IR, 1H, 11B, 13C NMR and mass spectroscopy as simple substitution derivatives of (η5-C5Me5Mo)2B5H9 and the structural types were unequivocally established by crystallographic analysis of compounds 2, 3, 5 and 6. [Copyright &y& Elsevier]

The present work describes the synthesis of a new class of glycolipids with systematic variations in the linkage region, as well as in the aglycon part using Cu(I) catalyzed click reaction. The linkage region between sugar and the aglycon part was diversified using amide, amido-triazole and 5-benzoyl triazole moieties. The structural diversity of glycolipids was further amplified by incorporating several polar peptide foldamer groups such as triazole, amide, peptide, or N-aryl peptoid in the aglycon part. The newly designed glycolipids were derived from the amalgamation of different peptide bond mimics. This work reports the first use of N-aryl peptoid in the synthesis of glycolipids. The newly synthesized glycolipids were characterized using different spectroscopic and spectrometric analyses. The impact of the amide bond as well as the triazole ring in the linkage region on the morphology of the glycolipids was analysed by comparing their self-assemblies using SEM analysis. The geometries of the glycolipids were also optimized using density functional theory and the optimized structures were found to be minima in the potential energy surfaces. [ABSTRACT FROM AUTHOR]

A series of novel 1,3-difunctionalized glycoconjugates were synthesized using a sequence of regioselective functionalization and stereoselective glycosidation of D-glucose and D-GlcNAc. Regioselective C-3 functionalization of sugar molecules was achieved by chemical functionalization of isopropylidene or oxazoline protected sugar derivatives. The structural diversity at the anomeric carbon was explored by stereoselective chemical glycosidation. The oxazoline protected D-GlcNAc derivative gave either pyranose or furanose derivatives on glycosidation depending on the amount of Lewis acid used. The diversely functionalized glycoconjugates with azide or alkyne groups are potentially useful for the synthesis of multifunctionalized complex glycoconjugates via click reactions. [ABSTRACT FROM AUTHOR]