Formulation and Evaluation of Escitalopram Oxalate Immediate Release Tablets

Escitalopram Oxalate is a class of drug with selective serotonin (5-HT) reuptake inhibitor (SSRIs). SSRIs are broad spectrum antidepressants that are effective for major depressive disorder and several anxiety disorders. The main objective of the present study was to develop a pharmaceutically equivalent, stable, cost effective and quality improved formulation of immediate release tablets of Escitalopram Oxalate using different concentration of superdisintegrants like croscarmellose sodium and sodium starch glycolate. Preformulation studies were performed prior to formulation. The tablets were compressed using microcrystalline cellulose, colloidal silicon dioxide, talc, magnesium stearate and opadry white was used for coating the tablets. The tablets were formulated by wet granulation with non aqueous binder and the fabricated tablets were evaluated for various micromeritic properties like bulk density, tapped density, compressibility index, Hausner’sratio, angle of repose and post compression characteristics like thickness, hardness, friability, disintegration time and drug release. Croscarmellose sodium was used as the disintegrant in the formulation of immediate release tablets of Escitalopram Oxalate. The stability studies were carried out for the optimized batch for six months. The results of the present study showed that among all the formulations, F12 was better in all terms of preformulation and post compression parameters and showed comparably a good dissolution profile like that of the marketed product(cipralex)

Exploitation of a Novel Binding Pocket in Human Lipoprotein-Associated Phospholipase A2 (Lp-PLA₂) Discovered through X‑ray Fragment Screening

Elevated levels of human lipoprotein-associated phospholipase A2 (Lp-PLA₂) are associated with cardiovascular disease and dementia. A fragment screen was conducted against Lp-PLA₂ in order to identify novel inhibitors. Multiple fragment hits were observed in different regions of the active site, including some hits that bound in a pocket created by movement of a protein side chain (approximately 13 Å from the catalytic residue Ser273). Using structure guided design, we optimized a fragment that bound in this pocket to generate a novel low nanomolar chemotype, which did not interact with the catalytic residues

Exploitation of a Novel Binding Pocket in Human Lipoprotein-Associated Phospholipase A2 (Lp-PLA₂) Discovered through X‑ray Fragment Screening

Elevated levels of human lipoprotein-associated phospholipase A2 (Lp-PLA₂) are associated with cardiovascular disease and dementia. A fragment screen was conducted against Lp-PLA₂ in order to identify novel inhibitors. Multiple fragment hits were observed in different regions of the active site, including some hits that bound in a pocket created by movement of a protein side chain (approximately 13 Å from the catalytic residue Ser273). Using structure guided design, we optimized a fragment that bound in this pocket to generate a novel low nanomolar chemotype, which did not interact with the catalytic residues