Application of Twin-Screw Melt Granulation to Overcome the Poor Tabletability of a High Dose Drug.

Pharmaceutical tablet manufacturing has seen a paradigm shift toward continuous manufacturing and twin-screw granulation-based technologies have catalyzed this shift. Twin-screw granulator can simultaneously perform unit operations like mixing, granulation, and drying of the granules. The present study investigates the impact of polymer concentration and processing parameters of twin-screw melt granulation, on flow properties and compaction characteristics of a model drug having high dose and poor tabletability.

Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: part 2.

Melanin concentrating hormone receptor 1 (MCHR1) antagonists have potential for the treatment of obesity and several CNS disorders. In the preceding article, we have described a novel series of quinazolines as MCHR1 antagonists and demonstrated in vivo proof of principle with an early lead. Herein we describe the detailed SAR and SPR studies to identify an optimized lead candidate having good efficacy in a sub-chronic DIO model with a good cardiovascular safety window.

Efficient throughput method for hygroscopicity classification of active and inactive pharmaceutical ingredients by water vapor sorption analysis.

The conventional method of hygroscopicity determination proposed by Callahan and co-workers utilizes more sample and time, may not be precise in all the cases, and is a relatively broader classification system. The method of indicating degree of hygroscopicity as per European Pharmacopoeia considers equilibration of sample for 24 hours under single humidity condition and may not necessarily ensure equilibration in all the cases. Additionally, both these methods do not provide information on solid state changes occurring within the sample during the course of experiment.

Bioavailability enhancement of poorly water soluble and weakly acidic new chemical entity with 2-hydroxy propyl-beta-cyclodextrin: selection of meglumine, a polyhydroxy base, as a novel ternary component.

The purpose of the present study was to investigate the influence of a polyhydroxy base, N-acetyl glucamine (also know as Meglumine), as a ternary component on the complexation of DRF-4367, a poorly water-soluble and weakly acidic anti-inflammatory molecule, with 2-hydroxypropyl-beta-cyclodextrin (HPbetaCD). The molecular inclusion of DRF-4367 with HPbetaCD alone and in combination with ternary component was aimed at improvement in solubility and, subsequently, dissolution rate-limited oral bioavailability. The solid complexes of DRF-4367 and HPbetaCD with or without meglumine (binary and ternary systems, respectively) were prepared as coevaporated product in different stoichiometric ratios and compared against physical mixture.

Mannosylated liposomes for bio-film targeting.

Vesicular systems in general are investigated to achieve bacterial bio-film targeting as their architecture mimics bio-membranes in terms of structure and bio-behavior. This paper elaborates upon the role of the inherent characteristics of the carrier system and further envisages the role of anchored ligands in navigating the contents in the vicinity of bio-films. Vesicles in the present study were coated with hydrophobic derivatives of mannan (cholesteryl mannan and sialo-mannan).