ABSTRACT
Aims: This research investigated the thrombolytic, cytotoxic and antidiabetic effects of Paederia foetida leaf methanol extract. Place and Duration of Study: Department of Genetic Engineering and Biotechnology and Department of Biochemistry and Molecular Biology, University of Chittagong, Bangladesh, between April to December, 2012. Methodology: An in-vitro thrombolytic model was used to check the thrombolytic effect of Paederia foetida extract using streptokinase as a positive control. Cytotoxic effect was measured by Brine shrimp lethality bioassay. Antidiabetic effect of the extract was conducted in alloxan induced diabetic model of Swiss albino mice. Data were analyzed by one way ANOVA using statistical package for social science (SPSS) software. Results: In in-vitro thrombolysis, Paederia foetida extract (100μl) lysed 21.40 ± 1.39 %, Streptokinase (positive control) 81.42 ± 0.88 % and water (negative control) 4.63 ± 0.31% of the blood clots. These clot lysis values were statistically different (p<0.05) from each other. In Brine shrimp bioassay, lethal concentration (LC50) of Paederia foetida extract was found 65.31 μg/mL which was statistically significant compared to Vincristine sulfate (positive control, LC50=0.76 μg/mL). The extract showed a significant and dosedependent decrease in blood glucose level in alloxan induced diabetic mice. The effect of the extract was comparable to the reference antidiabetic drug metformin (150 mg/kg BW). Conclusion: The results demonstrated a moderate thrombolytic, cytotoxic and antidiabetic effect of Paederia foetida leaf extract to be analyzed further for prospective pharmaceutical preparation.
ABSTRACT
The aim of the study was to develop a formulation of Ticagrelor 90 mg tablets that is equivalent to the reference product using similar excipients to match the in-vitro dissolution profile. A compressed coated tablet was formulated consisting of Ticagrelor and excipients conforming to the USP/BP monograph and below maximum amount allowed per unit dose. The physical characteristics of powder blends were evaluated for bulk density, tapped density, compressibility index, hausner ratio, angle of repose and moisture content. The compressed core and coated tablets were evaluated for thickness, hardness, weight variation, friability, disintegration, dissolution, drug content and stability. The powder blends for all formulations showed satisfactory bulk density, tapped density, compressibility index, hausner ratio, angle of repose and moisture content. All the core and coated tablets showed acceptable pharmaco-technical properties in terms of thickness, hardness, weight variation, friability, disintegration. Dissolution performances were varied depending on the composition of matrix tablet. Finally a formulation batch B05 consisting of Ticagrelor (34.61%), mannitol (61.15%), sodium starch glycolate (2.69%), hypromellose (HPMC-2910, 5cps) (0.77%), purified talc (0.38%), magnesium stearate (0.38%) and opadry grey (21k57558) (2%) showed maximum similarity with the reference product. Using this formulation a pharmaceutical will be able to met regulatory compliance.
ABSTRACT
In the present study an attempt has been taken to develop Indapamide sustained release matrix tablet using Methocel K15M CR by direct compression method. Various amount of polymer was used in the five proposed formulations (F-1to F-5) for the study of release rate retardant effect at 26.47%, 29.41%, 32.35%, 35.29% and 38.24% of total weight of tablet matrix respectively. Then the tablets were evaluated in terms of their physical parameters (weight variation, hardness, friability and thickness), drug content and in vitro release studies. All the formulations showed compliance with pharmacopoeial standards. The in vitro dissolution study were conducted using USP 30 dissolution apparatus type I (Basket method) in 900 ml phosphate buffer (pH 6.8) at 100 rpm for a total period of 24 hours. The release mechanisms were explored and explained by Zero order, Higuchi, First order and Korsmeyer-Peppas equations. Based on the dissolution data comparison with innovator brand formulation F-3 (32.35% Methocel K15M CR w/w) was found as the best formulation. The drug release profile of this formulation was well controlled and uniform throughout the dissolution studies. The drug release of formulation F-3 followed First Order kinetic model (r2 = 0.99) and the mechanism was found to be non- Fickian/anomalous according to Korsmeyer-Peppas equation.