Design and development of gastro retentive drug delivery System of tramadol hydrochloride

The present investigation concerns the development of floating tablets of tramadol hydrochloride, which after oral administration are designed to prolong the gastric residence time; improves the drug bioavailability, reduces drug waste and diminish the side effects of drug. The D-optimal experimental design was employed to evaluate contribution of hydroxypropyl methyl cellulose (HPMC) K4M concentration, lactose concentration and kollidone SR concentration on drug release from floating tablets. Tablets were prepared using direct compression technique. Formulations were evaluated for in vitro buoyancy and drug release study using United States Pharmacopoeia (USP) 24 paddle type dissolution apparatus using 0.1 N HCl as dissolution medium. Multiple regression analysis was performed for factorial design batches to evaluate the response. All formulation had floating lag time below 2 min and constantly floated on dissolution medium for more than 24 h. It was found that optimized HPMC K4M (100 mg), kollidone SR (25 mg) and lactose (17.5 mg) have shown the release of 98.4 % in 22 h which was better as compare to marketed product (i.e. Tramazac-SR). Kinetic treatment to dissolution profiles revealed the diffusion mechanism so called as Fickian diffusion (Case I transport) which was mainly dependent on all the independent variables.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Anxiolytic Potency of Cardamonin Mediated through Brain GABAergic System

Anxiety is an ailment causing personal, social and economic burden. Some drugs are available to provide symptomatic assistance for the treatment of anxiety and attempts are being made to find new therapeutic entities and subside associated adverse effects. Approaching natural sources, the current study aims to investigate the anxiolytic effects of cardamonin and its effect on the brain GABAergic system. The anxiolytic effects of various dose of cardamonin were investigated using the elevated plus maze apparatus and possible motor disabilities were evaluated trough open field test. Possible impact on GABAergic system was investigated using the ELISA. Fourteen days treatment with cardamonin (5.0 and 10.0 mg/kg, i.p.) in mice significantly (p < 0.0001) increased and the percentages of open arm entry and open arm time compared to respective vehicle control group. Cardamonin show no influence on gross locomotor movement in open field test. Treatment with cardamonin significantly (p < 0.0001) increased levels of GABA in brain of treated mice compared to control mice. This study provided evidence on the anxiolytic potency of the cardamonin and revealed its action mechanism of regulating the GABA level in mouse brain

QbD-Based Development and Evaluation of Pazopanib Hydrochloride Extrudates Prepared by Hot-Melt Extrusion Technique: In Vitro and In Vivo Evaluation

Background: Pazopanib hydrochloride (PZB) is a protein kinase inhibitor approved by the United States Food and Drug Administration and European agencies for the treatment of renal cell carcinoma and other renal malignancies. However, it exhibits poor aqueous solubility and inconsistent oral drug absorption. In this regard, the current research work entails the development and evaluation of the extrudates of pazopanib hydrochloride by the hot-melt extrusion (HME) technique for solubility enhancement and augmenting oral bioavailability. Results: Solid dispersion of the drug was prepared using polymers such as Kollidon VA64, hydroxypropylmethylcellulose (HPMC), Eudragit EPO, and Affinisol 15LV in a 1:2 ratio by the HME process through a lab-scale 18 mm extruder. Systematic optimization of the formulation variables was carried out with the help of custom screening design (JMP Software by SAS, Version 14.0) to study the impact of polymer type and plasticizer level on the quality of extrudate processability by measuring the torque value, appearance, and disintegration time as the responses. The polymer blends containing Kollidon VA64 and Affinisol 15LV resulted in respective clear transparent extrudates, while Eudragit EPO and HPMC extrudates were found to be opaque white and brownish, respectively. Furthermore, evaluation of the impact of process parameters such as screw rpm and barrel temperature was measured using a definitive screening design on the extrude appearance, torque, disintegration time, and dissolution profile. Based on the statistical outcomes, it can be concluded that barrel temperature has a significant impact on torque, disintegration time, and dissolution at 30 min, while screw speed has an insignificant impact on the response variables. Affinisol extrudates showed less moisture uptake and faster dissolution in comparison to Kollidon VA64 extrudates. Affinisol extrudates were evaluated for polymorphic stability up to a 3-month accelerated condition and found no recrystallization. PZB–Extrudates using the Affinisol polymer (Test formulation A) revealed significantly higher bioavailability (AUC) in comparison to the free Pazopanib drug and marketed formulation