Monday, 25 August 2014

Gravimetric Determination and Antimicrobial Studies of The Co (Ii) With Schiff Bases Derived From Sulphathiazole and 2-Hydroxy, 1-Napthaldehyde

Gravimetric Determination and Antimicrobial Studies of The Co (Ii) With Schiff Bases Derived From Sulphathiazole and 2-Hydroxy, 1-Napthaldehyde: Gravimetric determination of the Co(II) with the 2-hydroxy,1-napthaldehyde Sulphathiazole. The synthesis of metal sulfanilamide compounds has received much attention due to the effective chemotherapeutic agents to be employed for the prevention and cure of bacterial infections in humans. The present works deals with the synthesis and preliminary characteristics of various Schiff bases as ligands. Schiff bases derived by the condensation 2-hydroxy,1-napthaldehyde with Sulphathiazole. After synthesis of such Schiff bases as ligands, Co+2 ion introduced with them by chelation. The chemical and physical properties of metal chelates evaluated. Antimicrobial properties the ligands and metal chelate of 2-hydroxy,1-napthaldehyde Sulphathiazole also evaluated.

Studies of Newly Synthesized Octahedral Copper Complexes Based on Coumarins Along With Their Antioxidant, Anti-Tubercular And Antimicrobial Activity Evaluation

Studies of Newly Synthesized Octahedral Copper Complexes Based on Coumarins Along With Their Antioxidant, Anti-Tubercular And Antimicrobial Activity Evaluation: Some newly heterochelates synthesized by reflux of 3-acetyl 4-hydroxy coumarin, Enrofloxacin and transition metal. 1H, 13C, IR and ESI Mass confirm the formation of ligand. The heterochelates were characterized on the basis of different spectroscopic techniques like IR studies and elemental analysis while the geometry of complexes was octahedral which is confirmed by electronic spectra analysis. The compounds were subjected to antimicrobial, antioxidant and anti-tubercular activity viewing using serial broth dilution method and Minimum Inhibitory Concentration (MIC) is determined.

Effect of Different Viscosity Grade of HPMC on Cefixime Trihydrate Sustained Release Matrix Tablet

Effect of Different Viscosity Grade of HPMC on Cefixime Trihydrate Sustained Release Matrix Tablet: The present work aims to study effect of different viscosity grade of HPMC on cefixime trihydrate sustained release matrix tablet with a view to prolong drug release in vivo and reduce frequency of dosing. Cefixime Trihydrate is an orally active third generation cephalosporin. It has plasma half-life of 3-4 hrs. It is active against Gram+ve as well as Gram-ve bacteria. The Sustained release matrix tablets were prepared by wet granulation method using various release retardant polymers like different grade of HPMC, Lactose, MCC, and PVP K-30. The granules were subjected to pre-compression and post-compression parameters and they were in the acceptable limits. The in vitro retardation of drug release from HPMC matrices in accordance with its different proportion and viscosity grade was HPMC K-100M>HPMC K-15M >HPMC K-4M with ratio of (1, 1.5, 2) individually in formulation F1-F9 and (0.5, 0.75, 1) ratio in F10-F12. Among various kinetic models drug release was found to best fit the case – II transport, Zero order release model. A drug-excipient interaction was performed by DSC and FTIR; results were shown that there was no interaction between drug and excipients used. After 3 months stability study at 400C/75% RH, formulations found to be stable. So as the viscosity and proportion of HPMC increases release rate from sustained release cefixime trihydrate matrix tablet decreases.

Stability Indicating HPLC Method Development for Estimation of Montelukast Sodium and Acebrophylline in Combined Dosage Form

Stability Indicating HPLC Method Development for Estimation of Montelukast Sodium and Acebrophylline in Combined Dosage Form: Analysis of pharmaceutical product is very important as it concerned with life. Combination of Montelukast sodium and Acebrophylline is used in bronchial asthama and allergic rhinitis. In this Research work, Montelukast sodium and Acebrophylline stock solution was subjected to acid and alkali hydrolysis, oxidation, thermal photolytic and thermal degradation. In this Stability-Indicating method sample was analyzed by reverse phase C18 column (Hibar Lichrospher® 100, RP-18e 5 μm, 250 mm L × 4.6 mm diameter in size) as stationary phase and Acetonitrile:Methanol (60:40 %v/v, pH 3.2 adjusted with O-phosphoric acid) as a mobile phase at a flow rate of 0.8ml/min. Quantification was achieved at 260 nm with PDA detector. Method was validated according to ICH Q2 R1 guideline. The retention time for Montelukast sodium and Acebrophylline was found to be 15.49 minute and 3.45 minute, respectively. The linearity for Montelukast sodium and Acebrophylline was obtained in the concentration range of 5-25 µg/ml and 100-500 µg/ml with mean accuracies of 99.49-100.81% and 99.45-100.51% respectively. Values of %RSD for Precision Study and Robustness was found < 2%. % label claim was found to be 99.23% for MTKT and 100.83% for ACBR. The developed method meets all the acceptance criteria for the validation of analytical method as per the ICH Q2 R1 guideline. The degraded product peaks were well resolved from the pure drug peak with significant difference in their retention-time values. A simple, precise and accurate stability indicating RP-HPLC method was developed for estimation of Montelukast sodium and Acebrophylline in combined Dosage form.

Preparation and Evaluation of Controlled Release Matrix Pellets of Ketoprofen

Preparation and Evaluation of Controlled Release Matrix Pellets of Ketoprofen: Pellets are well accepted technique to control the drug release from the dosage form to improve bioavailability, reduce absorption difference in patients, reduce the dosing frequency and adverse effects during prolong treatment. The main objective of the present study is to prepare and evaluate controlled release pellets of Ketoprofen by extrusion sheronization method, with release rate retarding polymers using as carrier for oral administration in view to achieve oral controlled release of the drug and to protect the gastric mucous membrane from drug irritation. Ketoprofen is potent NSAID having anti-inflammatory, analgesic, antipyretic properties. It is readily absorbed from the gastrointestinal tract and peak plasma concentrations occur about 0.5–2 h after a dose, but it causes a certain irritation in the gastrointestinal mucous membrane and possesses a bitter taste and aftertaste. The half-life in plasma is about 2–3 hr. Preformulation studies performed were comply with the standards. Compatibility studies revealed there was no interaction between the drug and polymers. The various evaluation parameters were given the positive results. In-vitro dissolution studies were showed that the release of drug from pellets was optimum. It was also observed that drug release increases sharply as well as the release best fit to the zero order release kinetics.All the pellets were stable with respective storage condition.

Development and Evaluation of Fast Dissolving Tablets of Flurbiprofen

Development and Evaluation of Fast Dissolving Tablets of Flurbiprofen: The aim of the investigation is to prepare the fast dissolving tablet of flurbiprofen. Flurbiprofen, a widely prescribed anti inflammatory analgesic drug belongs to BCS class II and exhibit low and variable oral bioavailability due to its poor solubility and dissolution rate. The objective of the present study is to develop flurbiprofen fast dissolving tablet formulations by direct compression method by forming its inclusion complex with β-cyclodextrin. The 9 batches were prepared by using super disintegrants. The tablet weight is 350mg.The clathrate is having 1:1 proportion. Inclusion complex of BCD with drug enhance its dissolution and also improve the taste Different super disintegrating agent like cross carmellose sodium, kyron T-314 and SSG in different proportion to enhance solubility of flurbiprofen. The method used was direct compression and directly compressible vehicle used was avicel PH 102, Mannitol was used to fill up the tablet volume and was also acts as sweetener. All the evaluations were performed to check the efficacy and effectiveness of tablet like disintegration time, hardness, friability, wetting time and in-vitro dissolution test. From all the evaluations data batch B6 which contain kyron T-314 as superd isintegrating agent with 15mg in each tablet was evaluated as optimized formula for the preparation of fast dissolving tablet of flurbiprofen.

Formulation and Evaluation of Sustained Release Matrix Tablets of Diltiazem Hydrochloride

Formulation and Evaluation of Sustained Release Matrix Tablets of Diltiazem Hydrochloride: The purpose of present investigation was to develop sustained release matrix tablet of highly water soluble drug diltiazem hydrochloride by wet granulation method by using different hydrophilic (HPMC K4M, HPMC K1M, HPMC K100 M, Na CMC, Na alginate) and different hydrophobic (Eudragit RSPO, Eudragit RLPO, Eudragit RS-100, Eudragit RL-100, Ethyl cellulose) polymers. A 32 full factorial design was applied. The concentration of HPMC K15M in mg (X1) and concentration of Eudragit RSPO in mg (X2) were selected as independent variables. The %CDR at the end of 3 hrs (Q3) and %CDR at the end of 12 hrs (Q12) were selected as dependent variables. The prepared tablets were evaluated for hardness, friability, drug content, In vitro drug release. FT-IR, DSC and physical compatibility study were conducted for drug, and drug excipient mixture for interactions if any. The results indicated that concentration of HPMC K15M (X1) and concentration of Eudragit RSPO (X2) significantly affected the %CDR at the end of 3 hrs (Q3) and %CDR at the end of 12 hrs (Q12). Regression analysis and numerical optimization were performed to identify the best formulation. Formulation F11 prepared with HPMC K15M (70 mg) & Eudragit RSPO (10 mg) was found to be the best formulation with % CDR 20.32% and 96.59% at the end of 3 hrs and 12 hrs respectively. Optimized batch F11 showed similarity factor f2 value 69.14.

Formulation Optimization and Evaluation of Orodispersible Tablets of an Antipsychotic Drug Using Solubility Enhancement Technique

Formulation Optimization and Evaluation of Orodispersible Tablets of an Antipsychotic Drug Using Solubility Enhancement Technique: The main objective of this study is to formulate oro dispersible tablets of Olanzapine and to complex Olanzapine with β-cyclodextrin (β-CD) and PVP K 30. Olanzapine is second generation atypical antipsychotic drug. Phase solubility studies demonstrated that addition of water soluble polymer PVP K 30 with β-CD further enhanced solubility of drug compared to β-CD without PVP K 30. Complex was characterized using infrared spectroscopy, differential scanning calorimetry, % drug release study, % drug content and saturated solubility study. A 32 full factorial design was applied to systematically optimize the drug disintegration time. The concentration of Croscarmellose Sodium (X1) and concentration of Kyron T 314 (X2) were selected as independent variables. The disintegration time (Y1) and wetting time (Y2) were selected as dependent variables. The prepared tablets were evaluated for hardness, friability, disintegration time, wetting time and In-vitro drug release. The different formulations showed disintegration time between 19 to 48 seconds. The results indicated that concentration of croscarmellose Sodium (X1) and concentration of Kyron T 314 (X2) significantly affected the disintegration time (Y1) and wetting time (Y2).Regression analysis and numerical optimization were performed to identify the best formulation. Formulation F18 prepared with Croscarmellose Sodium (4.47 %) & Kyron T 314 (3.73 %) was found to be the best formulation with disintegration time 20 sec, wetting time 26 sec and % drug release in 10 min 99.49%.

Development and Characterization of Transdermal Patch for Controlled Release of Fluocinolone Acetonide

Development and Characterization of Transdermal Patch for Controlled Release of Fluocinolone Acetonide: The purpose of this research was to design matrix type of transdermal patch of Fluocinolone acetonide. Polyvinyl pyrrolidone K-30 (PVP K-30) and polyvinyl alcohol (PVA) was used in fixed ratio of 2:5 throughout the study and was concluded from preliminary study. Single layer matrix was chosen for providing 24 hrs. of continuous release. Solvent casting method was used for preparation of patches. 3 level 2 factor full factorial designs was applied for optimization of batch for optimising amount of poly ethylene oxide ( Polyox WSR 1105) and Propylene Glycol (PG). The effects of polymer type, polymer ratio, permeation enhancer, plasticiser on drug release were evaluated by in-vitro release using treated cellophane paper by using Franz diffusion cell. In addition various other characterizations like appearance, folding endurance, tensile strength, % moisture content, % drug content, thickness, flatness was done. ANOVA for Response Surface Quadratic Model for % cumulative drug release and % moisture content responses applied and found significant for optimization. From the contour plot and over lay plot range of various amounts of PG and Polyox found to provide desired responses. Validity of equation was checked by checkpoint batch was true for present work.

Solubility Enhancement of Carbamazepine by Using Various Solubility Enhancement Techniques

Solubility Enhancement of Carbamazepine by Using Various Solubility Enhancement Techniques: Carbamazepine, structurally similar to dibenzine derivative is used in the treatment of Epilepsy and pain associated with trigeminal neuralgia. The drug is practically insoluble in water, so the rate of dissolution and bioavailability is less. In this investigation an attempt was made to enhance solubility of carbamazepine by solubility enhancement techniques like Solid dispersion, Inclusion complexation and Crystallization. For solid dispersion phase solubility studies were carried out using Mannitol, PEG 4000 and PVP K 30 and for Inclusion complexation Phase solubility studies were carried out using Complexol-HPTM and HPMC E 3. The solid dispersions, Inclusion complexes and Crystals were prepared by solvent evaporation method and characterized by FT-IR and differential scanning calorimetry (DSC) and evaluated for different parameters. The highest percent cumulative drug release was observed for CBI-2 batch of inclusion complex (97.38% in 60 min.)