The relative bioavailability of 2 prototype fixed-dose combination formulations for amlodipine and rosuvastatin in healthy white and Chinese subjects.

A fixed-dose combination (FDC) may improve patient compliance and clinical outcomes in the management of cardiovascular risk in hypertensive and dyslipidemic patients. The study (NCT02075619) evaluated the bioavailability of 2 prototype FDC tablet formulations (FDC1 and FDC2) of amlodipine/rosuvastatin (10 mg/20 mg) compared with coadministered reference tablets. It was a randomized, single-dose, 3-way crossover pilot study in healthy white (n = 12) and Chinese (n = 12) adults.

Analytical characterization of an orally-delivered peptide pharmaceutical product.

The characterization of orally-delivered peptide pharmaceuticals presents several challenges to analytical methods in comparison to characterization of conventional small-molecule drugs. These challenges include the analysis and characterization of difficult-to-separate impurities, secondary structure, the amorphous solid-state form, and the integrity of enteric-coated drug delivery systems. This work presents the multidisciplinary analytical characterization of a parathyroid hormone (PTH) peptide active pharmaceutical ingredient (API) and an oral formulation of this API within enteric-coated sucrose spheres.

Processing factors in development of solid solution formulation of itraconazole for enhancement of drug dissolution and bioavailability.

This study investigated solid solutions of itraconazole, a water insoluble antifungal, for improved dissolution and improved bioavailability. Influence of processing factors on drug and carrier properties in solid solution and subsequently on drug dissolution behavior was also studied. An optimized solid solution formulation was compared with marketed product in healthy human subjects under fasted and fed conditions for bioequivalency.

Synthesis, analgesic and anti-inflammatory activities of some 1-acyl/aracyl-5-aminopyrazole derivatives.

A series of 1-acyl/aracyl-3, 4-disubstituted-5-aminopyrazoles (IV) were synthesized by the reaction of 1-acyl/aracylhydrazines (I) with an appropriately substituted ketenedithioacetal (II/III). Compounds IV were tested for their analgesic activity by rat caudal immersion test and anti-inflammatory activity by carrageenin induced edema in rat paw test. 1-Benzoyl-3-mercapto-4-carboxamido-5-aminopyrazole (IVk) proved to be the most active compound of the series in both tests.