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The purpose of this work was to apply approach of salt formation for improvement of solubility and dissolution rate of Ketoconazole, a water insoluble antifungal drug. Ketoconazole dihydrochloride was synthesized by simple bubbling anhydrous hydrogen chloride gas into the acetonic suspension of ketoconazole. According to previous reports, the technique produced clustures of nanoparticles during crystallization, which contributes to solubility enhancement. The elemental analysis elaborated the molecular formula of C26H28Cl2N4O4 ·2HCl and its structure was confirmed by gas chromatography-mass spectroscopy (GC-MS), Fourier transform infrared (FTIR), UV- spectroscopic characterization and differential scanning calorimetry (DSC). The morphological study by scanning electron microscopy (SEM) showed that the salt particles were as clusters of dispersible nanoparticles. Aqueous solubility measurements showed that aqueous solubility of the salt was extremely greater than its base. The percent dissolution of ketoconazole out of the salt after 15 min was also found more than 90%. The stability studies for 6 months were carried out for assay and dissolution which indicated that the salt remained stable. The present results depict that hydrochloride formation can significantly improve solubility and dissolution rate of ketoconazole and the method would be an easy, economical and practical alternative to the commercially available ketoconazole formulations. [ABSTRACT FROM AUTHOR]

The purpose of this research was to study mucoadhesive microspheres of tramadol hydrochloride compressed into tablet along with a loading dose. Microspheres containing tramadol hydrochloride were prepared by employing sodium alginate in combination with a mucoadhesive polymer, i.e., Carbopol 971P. An orifice-ionic gelation method was used to prepare the microspheres. A 32 factorial design was used to investigate the combined effect of two independent formulation variables in the preparation of microspheres. The concentration of sodium alginate (X1) and Carbopol 971P (X2) were selected as independent variables. Nine batches were used in the experimental design and evaluated for swelling index, mucoadhesion, and drug entrapment efficiency. A surface plot is presented to graphically represent the effect of the independent variables on the evaluation parameters. The best batch exhibited drug entrapment efficiency of 70.12%, swelling index of 2.3 and mucoadhesion of 95.42%. Microspheres showing maximum drug entrapment were compressed with the loading dose and subjected to in vitro dissolution studies. Drug release from tablets was found to follow a matrix model. Initial burst release from these tablets indicated the release of the loading dose and then a sustained effect over the time. This modified approach to formulation of tablets was found to be effective in sustaining drug release. [ABSTRACT FROM AUTHOR]

The purpose of the present study was to develop ophthalmic gel formulations of fluconazole. Intraocular delivery of topically applied drugs such as fluconazole is hampered by elimination of the solution due to tear turnover, so an in situ gelling thermoreversible mucoadhesive gel was formulated. Thermoreversible mucoadhesive gels were prepared using the cold method along with poloxamer 407 and different mucoadhesive polymers such as hydroxy ethyl cellulose (HEC), hydroxy propyl methyl cellulose (HPMC) K4M, and polyvinyl pyrrolidone (PVP) K30. Gels were evaluated for physical parameters like appearance, gelation temperature, pH, spreadability, drug content, gel strength, bioadhesion, and in vitro permeation. A modified device (modified K-C diffusion cell with a sheep's eye corneal membrane as a diffusion membrane) was used for evaluation of drug permeation through a sheep's corneal membrane. The formulated gels were transparent, uniform in consistency, and had spreadability with a pH range of 6.8 to 7.3. Satisfactory bioadhesion on the sheep's corneal surface and good gel strength were also observed. Diffusion studies have shown that a matrix is the best-fit model. As the concentration of mucoadhesive agent increases, the rate of permeation decreases. The order of drug permeation through the membrane was HEC > PVP K30 > HPMC K4M. This study found that a thermoreversible polymer and mucoadhesive polymers can be effectively used to prolong residence time. [ABSTRACT FROM AUTHOR]

Eco-friendly acid base indicators (anthocyanins) are always a center of attention in quantitative volumetric analysis as substitute for synthetic dye indicators. The purpose of the study is to promote utilization of Punica granatum (pomegranate) peel biomass by developing a novel eco-friendly acid–base indicator for titrimetric analysis. Pomegranate peel extract (PPEx) was prepared by ultrasonic probe sonication, a green method for extraction. The obtained extracts were evaluated for total phenol, anthocyanin content and the color change ability analysis (CIEL*a*b* analysis). The pKa of PPEx was determined, the effectiveness of PPEx as indicator was established in different acid–base titrations and compared with conventional synthetic indicators phenolphthalein and methyl orange. The aspirin powder and tablet (Ecosprin) were analyzed by using PPEx as indicator. An attempt was also made to develop PPEx pH indicator paper. The aqueous and ethanolic PPEx prepared by ultrasonic probe sonication contains 657.1 ± 21 and 718.1 ± 21 mg/LGAE of total phenols and 38.49 ± 0.83 and 42.91 ± 2.10 mgC3G/100gm of anthocyanins, respectively.The PPEx and pH indicator paper shows color change with the pH of solution. The pKa of PPEx was 7.14. PPEx was served as eco-friendly substitute for phenolphthalein and methyl orange indicators. PPEx was effective to analyze aspirin. The statistical analysis ensures the reliability and effectiveness of PPEx as an eco-friendly indicator in acid base titrations as substitute for the synthetic dye indicator. [ABSTRACT FROM AUTHOR]

This work aimed to prepare a formulation for fenofibrate a poor water soluble drug characterized by incomplete oral bioavailability, bitter taste, and tendency to destabilize in aqueous media. Regarding to the good solubility of fenofibrate in lipid materials, lipid nanoparticles seemed to be an excellent way to overcome these issues. In an attempt to prevent eventual stability problems linked to lipid nanoparticles, we dried the prepared nanosuspensions into redispersible powder, in association with adapted drying carriers such as aerosol 200. The comparison took into account quality of the obtained powder and its redispersibility, palatability, drug stability during the process and the effect of the drying method on particle size, entrapment efficiency. The morphology of dried nanoparticles was found to be 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 spray dried nanoparticles compared with pure drug. The in vitro dissolution rate of fenofibrate was significantly increased by reducing the particle size. The amorphous fenofibrate nanoparticles showed dramatic improvement in rate as well as extent of in-vitro drug dissolution. [ABSTRACT FROM AUTHOR]

The aim of the present work was to prepare and evaluate sustained release liquisolid compact formulations of tramadol hydrochloride. The dissolution profile of the prepared compacts was also compared to that of a marketed preparation. Liquisolid sustained release formulations were prepared by using HPMC K4M as a sustained release agent. Precompression studies of characteristics such as flow properties were also carried out. Liquisolid compacts were evaluated by hardness, friability, and in vitro dissolution studies. Comparison of dissolution profiles was carried out by using a modelindependent, model-dependent, and statistical approach. The prepared liquisolid compacts are new dosage forms with better sustained release behavior compared to a marketed sustained formulation. The dissolution profile followed the Peppas model as "best fit" model. Two-way ANOVA results revealed a significant difference in dissolution profiles. This systematic approach to producing a formulation was found to help with analyzing the sustained release of tramadol hydrochloride. The use and evaluation of model-dependent methods is more complicated. These methods provide an acceptable model approach that indicates the true relationship between percent drug release and time variables, including statistical assumptions. [ABSTRACT FROM AUTHOR]

The aim of present work was preparation and evaluation of sustained release liquisolid compact formulations of tramadol hydrochloride. Comparison of dissolution profiles of prepared compacts with marketed preparation was also done. Liquisolid sustained release formulations were prepared by using HPMC K4M as adjuvant for sustaining release. Precompression studies such as flow properties were also carried out. Liquisolid compacts were evaluated by hardness, friability, and in vitro dissolution studies. Comparison of dissolution profiles was carried out by using model independent, model dependent and statistical approach. The prepared liquisolid compacts are new dosage forms showing more sustained release behavior as compared to marketed sustained formulations. Dissolution profile followed Peppas model as "best fit" model. Two Way ANOVA results showed significant difference in dissolution profiles. This systematic approach to the formulation was found to be useful in analyzing sustained release of tramadol hydrochloride. The application and evaluation of model dependent methods are more complicated. These methods give acceptable model approach which is indication of true relationship between percent drug release and time variables, including statistical assumptions. [ABSTRACT FROM AUTHOR]

The purpose of present study is to develop a new, simple, single step melt solidification technique for hypolipidemic agent fenofibrate. The melt solidified beads were prepared by two techniques. The first method involves melting the drug and cooling the melt. In second method, the drug melt was poured in the water stirred at optimum speed to obtain beads. The beads were evaluated by Differential Scanning Calorimetry, Thin Layer Chromatography, Fourier Transform -Infrared Spectroscopy, X-ray powder diffraction, and stereomicroscopic analysis. Flow properties such as angle of repose, Carr's index and Hausner's ratio were also determined. The melt solidified beads were excipient free, nondisintegrating and of irregular shape. DSC, FTIR spectra showed no changes in drug properties. Flow properties of the beads were found to be acceptable. In vitro dissolution studies of melt solidified beads showed slower dissolution rate which might be due to compactness and higher bond strength of the beads. The present technique of melt solidification of Fenofibrate serves to effective as it takes low processing time, convenient methodology, as compared to conventional particle size enlargement techniques. [ABSTRACT FROM AUTHOR]

The aim of this research was to develop different ophthalmic gels of gatifloxacin using mucoadhesive polymers. To improve intraocular delivery of topically applied drugs such as gatifloxacin, gel formulations were prepared since solutions have a shorter ocular residence time because of tear turnover. A 32 factorial design was used to investigate the combined effect of two independent formulation variables in the preparation of the gels. Nine batches were prepared as per experimental design and evaluated for gelation temperature, gel strength, bioadhesion, viscosity, permeation, and antimicrobial efficacy. A surface plot was also created to graphically represent the effect of the independent variables on the evaluation parameters. Drug polymer compatibility was evaluated by differential scanning calorimetry and Fourier transform infrared spectroscopy. The prepared gels were observed to have a satisfactory gelation temperature, gel strength, and bioadhesion. Rheological study of the formulations indicated that gels exhibited pseudoplastic rheology. A modified device was used to evaluate drug permeation through a sheep's corneal membrane. In vitro permeation studies showed that a Peppas model was the best-fit model. Antimicrobial studies also indicated efficacy comparable to that of a marketed formulation. This systematic approach to formulation design should help in investigating the effect of variables in formulation processing. [ABSTRACT FROM AUTHOR]