ABSTRACT Aminopropyloxy derivatives of 1,8-naphthyridines have been synthesized using the principle of Conrad-Limpach synthesis of quinolines. The hydroxy group at 2- position of the naphthyridine ring was converted to the corresponding epoxypropane ether derivative by etherification with epichlorhydrin. The epoxy ether was then aminated in presence of KOH with the corresponding amines to obtain the aminopropyloxy derivatives. The compounds were tested for anti convulsant action at dose of 150mg/Kg relative to diazepam (5mg/Kg) by prevention of PTZ-induced seizures in mice.
Issue:1, Volume : 1, Page No. 1-8
ABSTRACT The current paper describes a reversed phase high performance liquid chromatographic method for the simultaneous estimation of Etoricoxib and Paracetamol in formulations. The separation was achieved on the LUNA C18 column 5µ (250 x 4.6 mm id), using methanol - water in the ratio 63 - 37 as the mobile phase at 1 ml/min flow rate and 237 nm as detection wavelength. The retention time of Etoricoxib and Paracetamol were 1.6 and 2.9 min respectively. The method was validated in terms of linearity, accuracy, precision, as per ICH Guidelines. The calibration curve was linear in the concentration range from 10-60 µg/ml for etoricoxib and 100-600 µg/ml for paracetamol. Percentage recovery obtained for etoricoxib and paracetamol were 99.60 % and 99.04 % respectively.
Issue:1, Volume : 1, Page No. 9-14
The present study was focused to develop floating microspheres of Lamivudine in order to achieve an extended retention in the upper gastrointestinal tract, which may result in enhanced absorption and thereby improved bioavailability. The present study involves preparation and evaluation of floating microspheres using Lamivudine as a model drug for prolongation of the gastric retention time. As Lamivudine is mainly absorbed from stomach, thus using floating microspheres as a mode of drug delivery helps in increasing its residence time and hence increasing the bioavailability of drug. The microspheres were prepared by the Ionic gelation method. The average diameter and surface morphology of the prepared microspheres were characterized by optical microscope and scanning electron microscopic methods respectively. The prepared microspheres were evaluated for particle size, micromeritic study, drug entrapment efficiency, in vitro buoyancy, swelling index and in vitro release. The effect of various formulation variables on the size and drug release was also investigated. All the formulated microspheres were found to possess good flow properties. Scanning electron microscopy confirmed spherical structure of the prepared microspheres. The best formulation F3 drug release kinetics were evaluated using Zero order, First order, Higuchi model, Korsmeyer - Peppas model. After the interpretation of data that was based on the value of a resulting regression coefficient, it was observed that the Korsmeyer- Peppas model has a highest regression coefficient values indicating that the drug release was based on the erosion of polymeric chain matrix system.
Issue:1, Volume : 1, Page No. 15-29