Drug delivery systems are becoming increasingly sophisticated as pharmaceutical scientists acquire a better understanding of the physicochemical and biochemical parameters pertinent to their performance. Over the past three decades, orally disintegrating tablets (ODTs) have gained considerable attention as a preferred alternative to conventional tablets and capsules due to better patient compliance. ODTs are solid dosage forms containing medicinal substances which disintegrate rapidly, usually in a matter of seconds, when placed on the tongue. Products of ODT technologies entered the market in the 1980s, have grown steadily in demand, and their product pipelines are rapidly expanding. New ODT technologies address many pharmaceutical and patient needs, ranging from enhanced life-cycle management to convenient dosing for paediatric, geriatric, and psychiatric patients with dysphagia. This has encouraged both academia and industry to generate new orally disintegrating formulations and technological approaches in this field. The aim of this article is to review the development of ODTs, challenges in formulation, new ODT technologies and evaluation methodologies, suitability of drug candidates, and future prospects.
M ain aim of this study was to develop controlled release (CR) floating multiparticulate drug delivery system of tolperisone hydrochloride. Microspheres were prepared by nonaqueous solvent evaporation technique consisting of porous calcium silicate (Florite or FLR) as porous carrier, tolperisone hydrochloride (API), Ethyl cellulose (EC), and HPMC 15 cPs as rate controlling polymers. 2 3 full factorial design was applied for optimization of formulation. The effect of various formulation and process variables on the particle morphology, micromeritic properties, in vitro floating behavior, entrapment efficiency, and in vitro drug release were studied. The size of microspheres was varied from 300 to 500 μm. The microspheres were found to be highly porous and regular in shape. All the formulations showed excellent flow properties. The percentage entrapment efficiency of all batches was greater than 80%. The percentage buoyancy varied from 85% to 98% at the end of 12 h. The release rate was determined in simulated gastric fluids. The formulation demonstrated favorable in vitro floating and release characteristics. Different kinetic models were applied to study the release mechanism. All formulations followed Higuchi model, which indicates the diffusion control release of water soluble drug from polymer matrix. Multiple regression analysis was applied for study of the effect of independent variables on the dependent variables. Optimized content for mobile and hand-held devicesHTML pages have been optimized of mobile and other hand-held devices (such as iPad, Kindle, iPod) for faster browsing speed. Click on [Mobile Full text] from Table of Contents page. This is simple HTML version for faster download on mobiles (if viewed on desktop, it will be automatically redirected to full HTML version)
Objectives:The aim of the present work was to synthesize a novel series of pyrazolo[3,4-d]pyrimidin-4(5H)-one derivatives and evaluate their in vitro antimicrobial activity.Methods:Cyclization of an ortho-amino ester of 1-(2,4-dinitrophenyl)pyrazole with various aliphatic/aromatic nitriles under different reaction conditions such as conventional and microwave assisted synthesis, provided pyrazolo[3,4-d] pyrimidin-4(5H)-one derivatives. All the synthesized compounds were evaluated in vitro for their antimicrobial activity against selected bacteria and fungi by agar well diffusion method.Results:All newly synthesized compounds were characterized using spectral and elemental analysis. Compounds 2e, 2f, and 2g showed significant antimicrobial activity as compared to standard drugs used.Conclusion:The newly synthesized compounds could be useful templates for the design and optimization of more active analogs as a possible antimicrobial agent.
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