Formulation development and optimization: Encapsulated system of atenolol and Glyburide

Purpose: Objective of this study is to develop; tablet- in- a capsule system, to deliver Atenolol 25mg and Glyburide 5mg in the hard gelatin capsule. In order to improve patient compliance and reduce problems associated with complex therapeutic regimen Atenolol [cardio-selective beta-blocker] and Glyburide [anti-diabetic; sulfonylurea] are commonly, prescribed to the diabetic hypertensive patient

Method: In present work six different formulations of Atenolol [AF1-AF6] and Glyburide [GF1-GF6] were prepared by direct compression method using Avicel, Lactose DC, Crospovidone and Magnesium Stearate in different proportions and encapsulated in hard gelatin shells. Post compression parameters i.e. weight variation, diameter variation, thickness variation, hardness variation,% friability, disintegration,% drug release were determined at different pH 1.2, 4.5 and 6.8, and subjected to dissolution profile comparison through similarity factor [f[2]]

Results: Stability studies were performed and shelf lives were calculated by R-Gui Stab R console 2.15.2 and determined to be 15and 27 months for Atenolol and Glyburide respectively. The percentage drug contents of Atenolol and Glyburide were estimated spectrophotometerically at 286nm and 314.7nm respectively. Formulations CF1-CF6 [encapsulated] were subjected to weight variation, disintegration and dissolution tests and subjected to model dependant analysis for dissolution studies. The simultaneous quantitation of Atenolol and Glyburide for content assay was done by HPLC method of analysis

Conclusion: formulation CF6 is showing highest coefficient of correlation values for all models applied. So we can conclude that the proposed system can improve patient compliance by increasing the ease of administration of two drugs together

Formulation development and comparative in vitro study of metoprolol tartrate [IR] tablets

The objective of the present work was to develop Immediate Release [IR] tablets of Metoprolol Tartrate [MT] and to compare trial formulations to a reference product. Six formulations [F1-F6] were designed using central composite method and compared to a reference brand [A]. Two marketed products [brands B and C] were also evaluated. F1-F6 were prepared with Avicel PH101 [filler], Crospovidone [disintegrant] and Magnesium Stearate [lubricant] by direct compression. Pharmacopoeial and non-pharmacopoeial methods were used to assess their quality. Furthermore, drug profiles were characterized using model dependent and independent [f2] approaches. Brands B and C and F5 and F6 did not qualify the tests for content uniformity. Moreover, brand B did not meet weight variation criteria and brand C did not satisfy requirements for single point dissolution test. Of the trial formulations, F2 failed the test for uniformity in thickness while F4 did not disintegrate within time limit. Only F1 and F3 met all quality parameters and were subjected to accelerated stability testing without significant alterations in their physicochemical characteristics. Based on AIC and r2adjusted values obtained by applying various kinetic models, drug release was determined to most closely follow Hixson-Crowell cube root law. F1 was determined to be the optimized formulation