Protective effect of Acampe praemorsa (Roxb.) Blatt. & McCann against oxidative stress

The current study was carried to make available phytochemical information and evaluation of antioxidant activity of Acampe praemorsa (Roxb.) Blatt. & McCann. The phytochemical analysis was carried out using procedures and quantified phenolic and alkaloid contents. The antioxidant activity was evaluated by in-vitro and in-vivo studies. The In-vitro antioxidant activity was carried on free radicals such as superoxide, hydroxyl DPPH, hydrogen peroxide, evaluation of reducing power. In-vivo study was carried on albino Wistar rats with different doses of extracts. The results provide that, A. praemorsa extracts have diversified phytochemicals in extracts like steroids, alkaloids, phenolics, glycosides, oils, quinones, tannins etc. The hydroalcoholic extract has more phenolic (26.80±0.51) and alkaloid (20.59±0.22) contents. The antioxidant activity results provide information that the extracts possess concentration dependent activity on tested free radicals. The hydroalcoholic extract has more protective nature against superoxide, DPPH, H2O2 free radicals and reducing power but ethyl acetate extract has more potential against hydroxyl free radical than hydroalcoholic extract. The extracts were found to be safe on toxic studies and In-vivo study results and they play significant role in controlling the oxidative enzymes such as catalase, superoxide dismutase, lipid peroxidation (malonaldehyde) in the body. Thus, it was determined that A. praemorsa have potential bioactive compounds and antioxidant activity

DMPK studies in rat model for comparative evaluation of bioavailability of alpha-mangostin and its formulated solid lipid nanoparticle using a validated LC-MS/MS method

Garcinia mangostana L., contains the xanthone ?-mangostin, which is a bioactive secondary metabolite. The Caco-2 cell line transport of ?-mangostin was explored to see whether it could be used to study oral uptake. There has been little in-vivo research on the drug metabolism and pharmacokinetics of solid lipid nanoparticles of ?-mangostin. The ?-mangostin content estimation in plasma of rat was accomplished using a validated LC-MS/MS technique. The Papp (permeability coefficient apparent) across the Caco-2 cell monolayer is used to predict the absorption of orally administered ?-mangostin and ?-mangostin solid lipid nanoparticles (AM-SLNP). In the presence of the solid lipid and emulsifiers, AM-SLNP had 3.72 times higher Papp than ?-mangostin after 4 hours of study across the Caco-2 cell line. In-vivo rat model study show that formulated AM-SLNP has a 3.3-fold higher bioavailability than pure ?-mangostin. High tissue distribution of the AM-SLNP is observed compared to ?-mangostin, which may improve the efficacy of the product when compared to pure extract, as the available drug at the site of distribution is high. Because both cell monolayer and animal studies demonstrate the same pattern of drug intake mechanism for SLNP’s and as it is almost identical, nanotechnology can be utilized in avoiding hepatic metabolism and improving bioavailability

The Effect of pH dependent and pH independent polymers on the drug release of anti-ischemic agent : Development and Characterization of Ranolazine ER Tablets

The objective of current study is to study the effects of combination of pH independent (HPMCK100M) and dependent (partially neutralized; Eudragit L 100-55) polymers on the drug release of Ranolazine form extended release tablet formulation. Ranolazine, an anti-ischemic or anginal agent. Mainly used for treating exercise induced; variant and stable chronic angina pectoris along with myocardial infarction. Anti-ischemic effect exhibited by Ranolazine is independent of haemodynamic effects, due to this benefit; it was useful for treating patients, who were not responded to other anti-anginals. Extended release tablets of Ranolazine were prepared using various proportions of  Eudragit L 100-55,HPMCK100M in by direct compression technique. 9 formulations were developed and characterized for pharmacopoeial limits.  Data obtained from the dissolution study fitted well to kinetic modeling, kinetic parameters were determined. EHR5 containing 31.25 mg of Eudragit L 100-55& 31.25 mg of HPMCK100M, is the best formulation showing similarity f2=85.77, f1= 2.31 with the marketed product (RANOLAZ). Formulation EHR5 follow zero order, whereas release mechanism found to be nonfickian type (n= 0.653)