19 research outputs found
AN OVERVIEW: POLYMORPHISM AND ITS APPLICATIONS IN DRUG DEVELOPMENT PROCESS
The physical properties, characterization, and uses of polymorphism are highlighted in this article. Polymorphism is important in pharmaceutical compounds and it's important to research and development of drug and drug discovery. Polymorphism in pharmacological substances is well known for its prevalence and relevance. During medication discovery and development, it is critical to plan and pick the appropriate form from the start. This review introduces the basic concepts of Polymorphism in pharmaceutical compounds and also vibrational spectroscopy in polymorphism applications and study of crystal polymorphism, cocrystals, physicochemical characteristics and uses, polymorphism research methods, Chemical stability and polymorphism, polymorphisms effect on drug substance and drug administration product polymorphism's impact on bioavailability, solubility, and dissolution bioequivalence (BA) and bioequivalence (BE) polymorphism's impact on drug product manufacturing, etc. Hence this study topic is undertaken for detail insights of phenomena of polymorphism and its relevance in drug development process.
Key words: Polymorphism, Crystallization, Bioavilability ,API, Polymorph
A NEW CESTODE COTUGNIA LIVIAE N.SP. (EUCESTODA : DAVAINEDIAE DIAMARE, 1893) FROM COLUMBA LIVIA AT AMBAJOGAI, MAHARASHTRA
The present form deals with description of new species of genus Cotugnia Diamare. 1893 as a type species C. digonopora (Pasquale, 1890) from domestic fowl in Africa, in having testes number 120-125 (123), comes closer to C. dignopora (Pasquale, 1890), Diamare 1893, C. rimondoi Tubangui et al. (1937). C. aurangabadensis Shinde. 1968 and C. kamatiensis Kharade et al. 1995. C. alii Shinde et al. 2002 and C. lohaensis Jadhav et al. 2004 but differs from them in size of Scolex, size of rostellum, number of rostellar hooks, number of testes and length of cirrus pouch
A NEW CESTODE ALIEZIA KAIJENSIS N.S.P. (CESTODA : AVITELLINEIDAE) FROM OVIS BHARAL AT KAIJ, MAHARASHTRA
The present form deals with description of new species of genus Aliezia as a type species Aliezia indica Shinde 1968 from sheep, Ovis bharal and having many distinct characters than all reported species such as in size of scolex, testes number, breadth of mature proglottids, position of cirrus pouch and a report from host
Design of selective TACE inhibitors using molecular docking studies: Synthesis and preliminary evaluation of anti-inflammatory and TACE inhibitory activity
<div><p>Tumor necrosis factor-α (TNF-α) converting enzyme (TACE) has been considered one of the principal therapeutic targets for the treatment of TNF-dependent pathologies. Several TACE inhibitors have been reported, but none of them has been successfully passed to phase II clinical trials. In the present work, we attempted to design highly selective new non-hydroxamate sulfonamide TACE inhibitors. The docking study was performed on one of the crystal structures of TACE, selected based on its resolution and R value, to tackle the flexibility issue of the active site. The results allowed us to distinguish the analogues with a higher binding affinity toward the active site of TACE and to identify the substituent of analogues needed for binding with the surrounding site of the enzyme. Finally the analogues were docked on crystal structures of six different matrix metalloproteinases (MMPs) for a selectivity study of TACE over MMPs. Some of these analogues were synthesized and subjected to preliminary testing for <i>in vivo</i> anti-inflammatory activity and TACE inhibitory activity.</p></div