A.R.Shabaraya

The present investigation focuses on the Optimization and formulation of medicated nail lacquer containing Fluconazole for transungual drug delivery system using ethyl cellulose as polymer and two different penetration enhancers. Fluconazole is a tri azole antifungal drug having broad spectrum activity. It acts by inhibiting 14 – α demethylase, a cytochrome P450 enzyme which converts lanosterol to ergosterol. Ergosterol inhibition causes increase in permeability of cellular membrane of fungi and hence leakage of cellular components. In present study Formulations were designed according by the design expert software 8.0.7.1 and the central composite design was selected for designing of experiments. The prepared formulations were evaluated for the different parameters such as drying time, smoothness of flow, gloss, water resistance, non – volatile content, drug content, in – vitro diffusion studies, in – vitro permeation studies, drug release kinetic studies. By applying the available information from the evaluation of nail lacquer 35 optimized formulations were obtained and out of which three were selected for further studies. Three optimized products were subjected to different evaluation parameters, drug release kinetics, anti – fungal testing and stability studies. Key words: transungual drug delivery, Fluconazole, optimization, penetration enhancers, in – vitro permeation studies, ethyl cellulose.

Fast dissolving tablets are the tablets which dissolves rapidly and shows higher bioavailability than conventional tablets. The concept of formulating Fast dissolving tablets of Carvedilol (antihypertensive drug) offer suitable and practical approach in serving the desired objective of faster disintegration and dissolution characteristic with increase bioavailability and to know the effects of two natural superdisintegrants (Hibiscus Rosa, Linseed Mucilage). In the present work solid dispersion were prepared by solvent evaporation method for improving the bioavailability with beta cyclodextrin as a carrier to increase the solubility of the drug. And after compressing the tablet , heat is applied to create pores in tablet as it contain camphor as subliming agent which increase the porosity and cause faster release of drug from the tablet. Comparison between these two natural superdisintegrants was done by taking different ratios individually and in combination. Combination of these two superdisintegrants shows synergistic effect when it is compared to individually. Prepared tablets were subjected to different evaluation parameters such as hardness, friability, weight variation, drug content uniformity, in vitro disintegration time, wetting time, in vitro dissolution studies and stability studies are carried out by using the best formulation. From all the formulations prepared and tested, F11 was found to be the best formulation.

A new series of novel substituted Gallic acid derivatives were synthesized by reacting methylated Gallic acid with hydrazine hydrate and then with various substituted aromatic aldehyde in mild and facile synthetic route to form various Schiff base derivatives.  Melting points of the synthesized compounds were determined by open capillary and are uncorrected. The purity of the compounds was checked using precoated TLC plates (MERCK, 60F) using chloroform: methanol (8:2) solvent system. The developed chromatographic plates were visualized under UV at 254nm. IR spectra were recorded using KBr on Josco FTIR model 8400 spectrophotometer, 1H NMR spectra in DMSO on a BRUKER FT-NMR instrument using TMS as internal standard. FAB mass spectra were recorded on JEOL SX 102 (DA-6000 mass Spectrometer) Data system using Argon (6KV.10MA) as the FAB gas. The designed compounds were screened for Antibacterial activity against Staphylococcus aureus and Escherichia coli and Antifungal activity against Aspergillus Niger in comparison with Ofloxacin and Fluconazole as standard to reveal the potency of synthesized derivatives. In accordance with the data obtained from antimicrobial activity, all the synthesized Schiff bases of substituted gallic acid have shown good activity against the tested microbes. Among these Schiff bases, compound bearing p-chloro group, o-chloro group, p-nitro group and m-nitro group has shown good activity against all the tested bacteria and fungi.