Design and synthesis of a new class of inhibitors for the treatment of osteoporosis and its comparative h17β-HSD2 and m17β-HSD2 SAR study are described. 17a is the first compound to show strong inhibition of both h17β-HSD2 and m17β-HSD2, intracellular activity, metabolic stability, selectivity toward h17β-HSD1, m17β-HSD1 and estrogen receptors α and β as well as appropriate physicochemical prop...

The plasma concentrations of ranitidine after oral and intravenous administration have been measured in 10 healthy young adults, nine cirrhotic patients, and eight healthy elderly people. In the first of these bioavailability was 51 +/- 4% and half life 161 +/- 11 minutes after oral and 124 +/- 5 minutes after intravenous administration. In the cirrhotics bioavailability was increased to 70 +/-...

Alendronate sodium, a bisphosphonate drug, is used to treat osteoporosis and other bone diseases. The present study was designed to conduct comparative bioavailability analysis of oral formulations of alendronate sodium through an open-label, randomized, 2-sequence, 2-period crossover study. Healthy adult male Pakistani volunteers received a single 70mg dose of the test or reference formulation...

oenzyme Q10 (CoQ10) plays an essential role in mitochondrial electron transport, and as such it is fundamental for energy production in cells. Further, CoQ10 is an antioxidant whose activity is particularly important in regenerating vitamin E. Its ability to quench free-radicals also helps maintain the structural integrity and stability of mitochondrial and cellular membranes—including intracel...

In a three-way cross-over study the bioavailability of cefuroxime was determined in 12 healthy volunteers after oral administration of 250 mg as cefuroxime axetil (Elobact; CAS 64544-07-6) in a plain aqueous suspension and as tablets from different batches. The tablet formulations showed nearly identical pharmacokinetic parameters and were bioequivalent. The mean maximum serum concentration was...

Fluoxetine drops and marketed fluoxetine capsules had quite the same Cmax (50.25 +/- 4.43 vs 47.55 +/- 5.29 ng/ml), but significantly different AUC0-t (717.27 +/- 71.29 vs 644.91 +/- 78.91 ng/ml/h). Furthermore the drops were characterised by a very early Tmax (4.61 +/- 0.85 hours) with a highly significant difference in comparison to the capsules reference compound (6.72 +/- 1.23 hours). After...

The cyclooxygenase (COX)-2 enzyme appears to be an important target for cancer chemoprevention. Given the recent emergence of potentially serious cardiovascular toxicity associated with selective COX-2 inhibitors, nonsteroidal antiinflammatory drugs (NSAIDs), which inhibit both COX-1 and COX-2, have received renewed attention as candidate chemoprevention agents. Sulindac has shown consistent ch...