Synthesis of 5-Substituted-1H-tetrazoles. -One-pot conversion of aryl iodides to nitriles and direct [2 + 3] cycloaddition with sodium azide offers a convenient synthesis of 5-aryl-1H-tetrazoles. The cyanation step is independently screened revealing nanosized CuO as optimal catalyst which can be easily recovered and reused at least four times without any significant loss of activity. -(YAPURI, U.; PALLE, S.; GUDAPARTHI, O.; NARAHARI, S. R.; RAWAT, D. K.; MUKKANTI, K.; VANTIKOMMU*, J.; Tetrahedron Lett. 54 (2013) 35, 4732-4734, http://dx.
In the treatment of hypertension fast onset of action is the major concern. The problem of slow onset of action of drugs can be overcome by development of appropriate dosage forms. Fast disintegrating tablets in mouth are best suited and have gained popularity in the oral antihypertensive drug therapy. These are advantageous over other conventional systems in terms of patient compliance, rapid onset of action, accurate dosing, good chemical stability, convenience of self-administration and compactness. Losartan potassium is widely used as an antihypertensive drug, which is a potent drug candidate for developing in to Fast Dissolving Tablets (FDT’s). It has low bioavailability due to first pass metabolism. Hence the main objective of the study was to formulate fast dissolving tablets of Losartan potassium to achieve a better dissolution rate and further improving the bioavailability of the drug. Fast dissolving tablet of Losartan potassium were formulated by using microcrystalline cellulose with different concentration of super disintegrants like sodium starch glycolate and Isabgol Mucilage. All the batches were prepared by direct compression.
API characterization studies were conducted to check the purity of API .The tablets were evaluated for Pre compression parameters and post compression parameters. Before the formulation of the tablets IR spectroscopic studies were also performed to check the compatibility with the excipients.
A 23 full factorial design was applied to investigate the combine effect of 3 formulation variables. Here the concentration of Isabgol mucilage, concentration of Sodium Starch Glycolate and concentration of Microcrystalline Cellulose were taken as independent variable X1, X2 & X3 respectively and their effect of disintegration time is studied as dependent parameter. To represent the data Design Expert software is used.
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