Drugs with lower bioavailability need repeated dosing to reach the minimum effective therapeutic concentration in plasma. In order to retain the drug in upper part of gastro intestinal tract (GIT) which is the major absorption window for majority of drugs and also to have localized effect many advances in drug delivery were made. Researchers mainly emphasize on to get patient compliance by formulating single dose, targeted and minimal side effects dosage form. The design must give constant drug release for longer time period that could be achieved through proper selection of polymers. These approaches in dosage design may also be advantageous for local action, to prevent drug degradation, delivery of gastro-irritant, narrow absorption window drugs and to get pH dependent release throughout the GIT. Polymethacrylate polymers in different ratios are available for the above objective as they are inert materials, could stay for longer time and are resistant to body fluids. This review also discusses the physicochemical properties of different available grades along with their glass transition temperatures (Tg).
Protein tyrosine phosphatase 1B (PTP 1B), a negative regulator of insulin receptor signaling system, has emerged as a highly validated, attractive target for the treatment of non-insulin dependent diabetes mellitus (NIDDM) and obesity. As a result there is a growing interest in the development of potent and specific inhibitors for this enzyme. This quantitative structureactivity relationship (QSAR) study for a series of formylchromone derivatives as PTP 1B inhibitors was performed using genetic function approximation (GFA) technique. The QSAR models were developed using a training set of 29 compounds and the predictive ability of the QSAR model was evaluated against a test set of 7 compounds. The internal and external consistency of the final QSAR model was 0.766 and 0.785. The statistical quality of QSAR models was assessed by statistical parameters r 2 , r ) and lack of fit (LOF) measure. The results indicate that PTP 1B inhibitory activity of the formylchromone derivatives is strongly dependent on electronic, thermodynamic and shape related parameters.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.