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Objective: The rationale for the study was to develop a once-daily dose of immediate as well as a gastro-retentive form of carvedilol phosphate by compression coating floating technique. Methods:In the presented study the core tablet was containing half the quantity of the drug formulated as floating drug delivery using different controlled release polymers blend in various proportions like ethyl cellulose, carbopol, hydroxypropyl methylcellulose (HPMC) K4, K15, and K100 by direct compression method. Outer coat layer was formulated with rest of the drug with the blend of different super disintegrants in various proportions like crospovidone, croscarmellose sodium (CCS), sodium starch glycolate (SSG) for the immediate release of the drug. Both the immediate and controlled formulation was separately formulated from sf1 to sf9 and f1 to f9 respectively. Based on the evaluation parameters finally, formulation F1 to F9 were formulated by applying compression coating floating method. These formulations were characterized for their tablet density, disintegration time, floating lag time, in vitro drug release, drug-excipients interaction and accelerated stability studies etc. Results:The result revealed formulation sf9 containing SSG of 15% was able to 97.2% of drug release within 15 min towards the achievement of immediate release. Similarly, the formulation f9 containing 0.5:0.5:4.5 ratios of ethyl cellulose, carbopol and HPMC K15 was able to 95.3% of drug release within 16h. From compressed coat tablets batches of F1 to F9, based on the dissolution data F9 was considered as an optimized formulation which was able to release 48.6% of drug release within 15 min and cumulatively controlled the release up to 96.4% for 16 h, followed zero-order kinetics and Higuchi pattern. Conclusion:The results obtained in this research work clearly indicated that the compression coating floating tablet of carvedilol phosphate was the best dosage form for the treatment of hypertension. Results of the evaluation of prepared batches indicate that the batch F9 is a promising formulation for both a quick onset of action as well as gastro-retentive dosage form to maintain the constant drug action which would improve the maximum therapeutic efficacy and patient compliance.

Synthesis of pyrazole-3-carboxylic acid was progressed via two different protocols, one of which is solid state. Pyrazole-3-carboxylic acid was converted into different derivatives such as ester, urea, amide and nitrile. The amide compound was converted to nitrile using SOCl2 and DMF. Solid state heating of carboxylic acid gave decarboxylated product. Cyclization of tetra-substituted pyrazole with hydrazines resulted in pyrazolopyridazinones. The antimicrobial activities of the synthesized pyrazole derivatives against Bacillus cereus, Escherichia coli, Micrococcus luteus, Staphylococcus aureus, and Saccharomyces cerevisiae were evaluated. One of the pyrazole derivatives which possess nitro group showed antimicrobial activity in only B. cereus, a Gram-positive bacteria, with an MIC of 128 μg/mL.

The present investigation is concerned with formulation and evaluation of Transdermal gels of Tacrolimus, anti-psoriasis drug, to circumvent the first pass effect and to improve its bioavailability with reduction in dosing frequency and dose related side effects. Twelve formulations were developed with varying concentrations of polymers like Carbopol 934P, HPMCK4M and Sodium CMC. The gels were tested for clarity, Homogeneity, Spreadability, Extrudability, Viscosity, surface pH, drug Content uniformity, in-vitro drug diffusion study and ex-vivo permeation study using rat abdominal skin. FTIR studies showed no evidence on interactions between drug, polymers and excipients. The best in-vitro drug release profile was achieved with the formulation F4 containing 0.5 mg of exhibited 6 hr drug release i.e. 98.68 % with desired therapeutic concentration which contains the drug and Carbopol 934p in the ratio of 1:2. The surface pH, drug content and viscosity of the formulation F4 was found to be 6.27, 101.3% and 3, 10,000cps respectively. The drug permeation from formulation F4 was slow and steady and 0.89gm of tacrolimus could permeate through the rat abdominal skin membrane with a flux of 0.071 gm hr-1 cm-2. The in-vitro release kinetics studies reveal that all formulations fit well with zero order kinetics followed by non-Fickian diffusion mechanism. Keywords: Transdermal gel, Viscosity, In-vitro drug release, In-vitro drug release kinetics study, Ex-vivo permeation study

Aim:The aim of the present research work is to develop buccal tablets of Lercanidipine hydrochloride to reduce dosage frequency; obtain optimized and controlled therapy, better patient compliance. Materials and Methods: Lercanidipine HCl was obtained as a gift sample from Sun Pharma, Baroda, India. Other ingredients like Na-alginate, Carbopol 934 P, Micro Crystalline Cellulose, Mannitol, Magnesium stearate, Ethyl cellulose and Hydroxy Propyl Methyl CelluloseK4M were purchased from various sources. All other ingredients used were of analytical grade. Attempt was made by using mucoadhesive polymers HPMC K4 M, sodium alginate and carbopol 934 P in combination with Ethyl Cellulose as an impermeable backing layer. Results: Combination of polymer HPMC K4 M and sodium alginate release of drug was found in desired manner than other combinations. On the basis of the preliminary trials a 3 2 full factorial design was employed to study the effect of independent variables such as concentration of sodium alginate: HPMC K4M (X1) and type of filler (X2) on dependent variables. Factorial batches of F1 to F9 were formulated. HPMC K4M exhibited a much greater sustained effect on the release rate compared with sodium alginate. F4 shown the highest f2 value 70.46 and also all the h drug release was within the specified range. Based on the f2 value and targeted release profile the F4 batch was considered as optimized batch. Formulation F4 was subjected to an in vitro buccal permeation study. The results showed drug permeation of 99.04% in 12 h. The correlation between in vitro drug release rate and in vitro drug permeation across the chicken mucosa was found to be positive, with a correlation coefficient (R 2 ) of 0.9921. Conclusion: From kinetic modelling of the dissolution profile of the optimized formulation, it was concluded that there is erosion-controlled release of Lercanidipine from the buccal adhesive drug delivery system.