Current Issue : January - March Volume : 2014 Issue Number : 1 Articles : 7 Articles
Models for predicting solubility of drugs in solvent mixtures have an important practical relevance in drug\r\nformulation. Satranidazole, BCS class II, whose physicochemical properties in solution have not been studied enormously.\r\nExtended hildebrand solubility approach (EHSA) is effectively applied to assess the equilibrium solubility of satranidazole in\r\nbinary solvent mixtures at 298.15 K. The equilibrium solubility of satranidazole in various water-PEG 600 mixtures was\r\nexplored in terms of solute-solvent interactions using a modified version of hildebrand-Scatchard treatment for regular\r\nsolutions. The solubility equation employs term interaction energy (W) to replace the geometric mean (?1?2), where ?1 and ?2\r\nare the cohesive energy densities for the solvent and solute, respectively. The new equation provides an accurate prophecy of\r\nequilibrium solubility once the interaction energy, W, is obtained. In this case, the energy term is regressed against a polynomial\r\nin ?1 of the binary mixture. Quadratic, cubic and quartic expressions of ââ?¬Ë?Wââ?¬â?¢ in terms of solvent solubility parameters were found\r\nfor prognosticating the solubility of satranidazole in water-PEG 600 mixtures. A satisfactory correlation-performance of EHSA\r\nwas found using a standard polynomial model in order fourth of the W interaction energy vs. solubility parameter of the\r\nmixtures (Overall mean percentage error was ~-8.2%). Therefore, this empirical model has latent expediency in preformulation\r\nand formulation studies during which solubility prophecy is important for drug design processes....
Proniosomes are dry formulation of water soluble carrier particles that are coated with surfactant and can be\r\nmeasured out as needed and hydrated to form niosomal dispersion. Nevirapine is a non-nucleoside reverse transcriptase\r\ninhibitor (NNRTI). The pharmacokinetic profile and intracellular metabolism of nevirapine provide a strong rationale for the\r\ndevelopment of novel drug delivery system. A proniosome based drug delivery system of nevirapine was planned for\r\ndevelopment and evaluation of proniosomes for vesicle size analysis, encapsulation efficiency, drug diffusion profiles,\r\nmorphological and stability studies. Proniosomes loaded nevirapine were prepared by slurry method using maltodextrin,\r\nnonionic surfactant span 40, cholesterol and other ingredients at different concentrations. All the proniosome formulations\r\nwere converted to niosomal suspensions and evaluated for drug content, vesicle size, encapsulation efficiency, morphological\r\nand stability studies, FTIR studies and in-vitro release studies. The preliminary compatibility studies revealed that there were no\r\ninteractions between nevirapine and excipients which was evident from FTIR. Span 40 was chosen as the surfactant of choice for\r\nproniosomal formulation by preliminary screening study. The physical characteristics of proniosome were found to be within\r\nthe acceptable limits. The vesicle size was found to in a range 142 nm to 234 nm and entrapment efficiency was found in range\r\nof 69% to 88%. The proniosomes were spherical and homogenous in structure when observed under scanning electron\r\nmicroscopy. The release from the proniosomes was prolonged when compared to conventional formulation. The stability\r\nstudies showed that proniosomes were stable at 5�±3�°C and 30�°C�±2�°C....
The aim of this study was to prepare and characterize rifaximin nanosuspensions to mask bitter taste and enhance the solubility of this drug. Nanosuspensions were prepared by the precipitation ultrasonication method. The effects of two important process parameters, i.e. the concentration of PVA in the anti-solvent and the time length of ultrasonication on the particle size of nanosuspensions were investigated systematically and the optimal values were 0.15% and 15 min, respectively. The particle size and zeta potential of nanocrystals were 129 nm and −23.9 mV, respectively. The morphology of nanocrystals was found to be flaky and spherical in shape by scanning electron microscopy (SEM) observation. The X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) analysis indicated that there was no substantial crystalline change in the nanocrystals compared with raw crystals. The taste of rifaximin was significantly masked and its solubility increased by reducing the particle size....
Oral Submucous Fibrosis (OSMF) has been reported in 33% to 40% of Indian population due to an excessive usage of gutkha, tobacco, pan masalas and areca nut. Looking to the need of developing an oral formulation that would dissolve slowly in the oral cavity without causing any irritation, an attempt was made to formulate and evaluate Curcumin (Cu)-β-CD based medicated jelly and focus on improvement of its aqueous solubility. Inclusion complexes were prepared by common solvent evaporation method and were further evaluated for saturation, phase solubility, FTIR, DSC, in-vitro dissolution. Saturation solubility of Cu in DW and methanol (9:1) increased from (0.00027mg/ml) to (0.047mg/ml) respectively. At the end of 1 h, 9.2 ± 0.36 % and that for 7th h was 74.45±0.25% respectively. The inclusion complex was further formulated into Oral Medicated Jelly using 32 Factorial design pectin (X1) and propylene glycol (X2), selected as independent variables. (Y1) % drug release and (Y2) mucoadhesive strength were considered as dependent variables and were evaluated for Physical Appearance, pH, Viscosity, Consistency, Drug Content, Muchoadhesion, in-vitro Dissolution profiles and rheological studies. The optimized batch F6 exhibited 67.27% ±0.25 drug release in 7th h and mucoadhesive strength 14.81 ± 0.79g. Dynamic moduli can be used to measure gel strength and are significant for the interpretation of drug release. The results of stability studies of best formulation revealed no change in physical appearance, drug content, pH, viscosity thus indicating that formulation was stable....
During preformulation studies of pharmaceutical dosage forms, physical characterization and analysis techniques are\r\nvery useful to detect physical or chemical incompatibilities between the drug and excipients of interest that might interfere with\r\nefficacy and safety of the final drug product. In this study, an approach to possible physical interaction between olanzapine and\r\nguar gum is presented. For the investigation purpose; molecular level property, particulate level property and thermal methods\r\nof analysis have been assessed. Results of FTIR, XRD, DSC and TG analysis studies indicated that olanzapine had compatibility\r\nwith guar gum....
Glaucoma is the second leading cause of blindness in the world, according to the world health organization. Glaucoma\r\nwhen untreated leads to increased intra ocular pressure and possible loss of vision. Anti-glaucoma matrix type ocuserts of\r\nacetazolamide were designed using 32 factorial design to achieve prolonged therapeutic effect by improving residence time at\r\nthe site of the application. Independent variables selected were matrix forming polymer (X1) poly-?-caprolactone (PCL 37000)\r\nand polyethylene glycol (PEG 4000) as plasticizer (X2), dependent variables as cumulative drug release Q24hrs (Y1) and n value as\r\n(Y2). The central point (0, 0) was studied in quintuplicate. All other formulation and processing variables were kept in variant\r\nthroughout the study. Statistical optimization of polymer concentration by fitting it in factorial design was done. The main\r\npurpose of the study was to deliver the drug in zero order kinetics. Solvent casting technique was followed to prepare ocuserts.\r\nAll formulations were subjected to various physiochemical evaluations like thickness, uniformity of weight, swelling index,\r\nsurface pH, folding endurance, drug content, in-vitro drug release studies, release rate kinetics were investigated. One way\r\nanalysis of variance (ANOVA), regression analysis was performed. The ocular inserts were smooth and passed all the evaluation\r\ntests performed. The in-vitro kinetic treatment (zero order and korsemeyer�s regression value) and n values suggest that AB5\r\nwas the best formulation provided the desired in-vitro drug release for 48 hours....
Available topical antifungal agents face some limitations, to counter this novel, self-adhesive, flexible, thin and\r\ntransparent polymeric film-topical antifungal film for the topical delivery of antifungal agents was developed. Clotrimazole was\r\nselected as model antifungal agent. TAF consists of a very thin backing membrane of polyvinyl alcohol above which drug\r\ncontaining polymer layer was developed by solvent evaporation method. Polyvinyl pyrolidone K-30 a matrix forming polymer\r\nand propylene glycol (plasticizer) were used for the formulation of film. Betamethasone dipropionate a corticosteroid use of\r\nwhich in the treatment of fungal infection may lead to suppression of host inflammation, pain/itching associated with some\r\nfungal infection was also added in the film. Eucalyptus oil itself possessing antifungal activity was selected as permeation\r\nenhancer hence a synergistic antifungal activity was expected which was confirmed with the help of in-vitro antifungal test.\r\nEvaluation parameters like compatibility studies, physical appearance, thickness and weight variation, moisture uptake study,\r\ndrug content, tensile and adhesive strength was carried out. Adhesive strength and in-vitro drug release of both the drugs were\r\ndepended on optimum concentration of PVP K-30 and propylene glycol. FTIR spectra of final formulation reveal the presence of\r\nmajor spectra of eucalyptus oil in the fingerprint region. Drug release 88.24�±1.59% and 87.91�±1.72% for clotrimazole and\r\nbetamethasone dipropionate respectively, upto 10 h was established. SEM study depicts a very smooth area of film. Finally, no\r\nredness, inflammation or eschar formation during the observation period of 120 h/5 days was observed in the skin-irritancy test....
Loading....