The present study involved preparation of solid dispersions of Olmesartan medoxomil by different solid dispersion techniques to improve the aqueous solubility and dissolution rate in order to enhance bioavailability. Olmesartan medoxomil is a BCS class II antihypertensive drug with low water solubility and bioavailability of 26%. In the present study solid dispersions of Olmesartan medoxomil with Poloxamer 407 in the ratio of 1:4 was prepared by five different techniques like melting method, Kneading method, solvent evaporation, Co-grinding method, and Lyophilization method. The Formulations were assessed for percentage yield, dissolution study, drug content, solubility study and stability study. In vitro release studies revealed that the solid dispersions prepared by solvent evaporation method showed faster drug release than other methods. Solid dispersion containing Poloxamer (1:4) prepared by solvent evaporation technique was considered as the best formulation because of its faster drug release among all formulations. Differential scanning calorimetry (DSC) and infrared spectroscopy (IR) studies revealed that no interactions exist between drug and polymer. In a nutshell, solid dispersions of Olmesartan medoxomil in Poloxamer 407 (1:4) by solvent evaporation have shown to be a promising approach to enhance the bioavailability of Olmesartan medoxomil.
A rapid, simple, sensitive and cost effective spectrofluorimetric method was developed for the estimation of Picroside II in pure pharmaceutical dosage form. The relative florescence intensity of Picroside II was measured in an at excitation wavelength of 269nm and emission wavelength 416nm. This reaction product was measured spectrofluorimetrically at 416nm after excitation at 269 nm under optimum conditions, linear relationship with best correlation coefficient 0.9999 and the linearity was detected in between the range of 25-10000ng/ml. The limits of detection (LOD) and limit of quantification (LOQ) were found in the range of 10.39 and 31.51ng/ml respectively. The validation of the developed spectrofluorimetric method was carried out by conducting linearity, accuracy, precision, and robustness and ruggedness, limit of detection and limit of quantitation studies. Developed spectrofluorimetric method was found to be precise for the intra-day and inter-day study and shows percent relative standard deviation in the range of 0.066 and 1.98 and 0.055 to 1.94 respectively. The total percent recovery of Picroside II was found to be 99.00 to 100.4.
The N- arylamines and its derivatives are an important class of organic and heterocyclic compounds. The chemistry of these compounds revised day by day because these are one of the most useful medicinal pharmacophore which appears as an important structural part in many naturally occurring and synthetically prepared medicinal drugs and heterocyclic compounds. Literature survey reveals that in the last few decades many chemists and researchers are engaged in the synthesis of various types N- arylamines by using various methods as they are having great biological and pharmacological activities.
Complexes of copper (II) with 4-chloro-2-(4-(hydroxymethyl)-1-phenyl-1H-pyrazol-3-yl)phenols (H2L1) and 2, 4-dichloro-6-(4-(hydroxymethyl)-1-phenyl-1H-pyrazol-3-yl) phenol (H2L2) ligands derived from reaction of 3-aryl-1-phenyl-1H-pyrazole-4- carbaldehyde with NaBH4 have been prepared. All the complexes have been characterized by elemental analyses, conductance measurement, magnetic moment, infrared, NMR, ESR and electronic spectral studies. The complexes were found to have stoichiometry (1:2), ML2. On the basis of spectral and magnetic studies square planar geometry has been assigned for these complexes. The formation of copper(II) complex with (H2L1) and (H2L2) has been studied spectrophotometrically at an absorption maximum of 658 nm at different temperatures. The data shows that copper(II) and (H2L1) and (H2L2) combine in the molar ratio of 1: 2 at pH 5.0. The stability constants of the complexes were calculated to be 14×104, 9.33×104 and 4.39×104 and 3.18x104, 3.36x104, 5.98x104 for (H2L1) and (H2L2) respectively by continuous variation method and 0.45×104, 0.58×104, and 0.51×104 and 0.62×104, 0.51×104, 0.48×104 for (H2L1) and (H2L2) respectively by mole ratio method at 30, 35 and 40°C, respectively.
S. G. Parvati*, Shweta M. Patil and Nirdosh Patil.
In this article, we have synthesised 5-bromo-7-methoxy-n'-[(3z)-2-oxo-1, 2-dihydro-3H-indol-3-ylidene]-1-benzofuran-2-carbohydrazide (1) from 5-bromo-7-methoxy-1-benzofuran-2-carbohydrazide and indole-2, 3-dione in the presence of ethanol and glacial acetic acid. Then 5-Bromo-7-Methoxy-N'-[(3z)-2-Oxo-1, 2-Dihydro-3h-Indol-3-Ylidene]-1-Benzofuran-2-Carbohydrazide (1) was treated with secondary amines in the presence of formaldehyde and DMF to yield Benzofuranyl Indolinones. All the synthesised compounds were characterised by IR and NMR spectral data. Also all the compounds were screened for antibacterial (Cup-plate method) and antifungal activity (MIC method).
K. M. Basavaraja*, Manjunatha Harihara Mathada, H. M. Naveena Kumari, Mahesh Kumar, K. T. Sudha.
The in vitro antifungal potential of plant extracts prepared in ethanol of Catharanthus roseus and Calotropis procera were screened against fungal pathogens isolated from Aegle marmelos. Plant extracts have been used as an alternative bio-fungicide against commercial fungicides. Disc diffusion methodology has been used to examine the antifungal potential of the selected plant extracts. Leaf and flower extracts of C. roseus and C. procera have been studied against the fungal pathogens isolated from various parts of A. marmelos. Alternaria and Curvularia were the isolated fungi treated against the bio-fungicides and compared with the commercial fungicide considered as a control. C. roseus showed positive results in comparison to C. procera. In addition, flower extracts of C. roseus showed comparatively positive results than leaves and stem. The bio-fungicides showed a wide scope as an alternative to commercial fungicide for inhibition of fungal growth on Aegle marmelos.
This paper deals with study of inhibition of human carbonic anhydrase IV by benzene sulfonamides. QSAR and molecular modeling studies have been performed on a series of CA IV with benzene sulfonamides. The proposed prediction set includes 25 molecules of benzene sulfonamides. Statistically significant models were derived by correlation analysis. Quality of regression increases with variables. The model obtained by deleting outliers allow us to confirm that the six parametric model is the most significant model for modeling biological activity. The efficiency of the proposed model is around 92%. The predictive power has been examined by leave one out procedure.
Development of new food product is very difficult process because it requires the information of ingredients, methods and techniques, packaging materials, consumer demands and likes and dislikes. Product development is a method of trade research in its own right. It is a combination and application of nature with the food sciences and processing with the marketing and consumer science into one type of integrated research whose aim is the development of new products. Product development is the important part of the food industry; from clarify an establishing product range to developing completely new products. The challenge for product development is to develop a product which is acceptable to the consumer. The acceptability scores for five developed samples were Sample A had the most preferred taste based on the assessment with a rating of 8.75. Sample B was the next preferred having a score of 8.5. Sample E was next in the line with a score of 7.9. Samples C and Sample D were seen to have the least scores in the Taste category by the subjects who tested. The color category was led by Sample A with a rating of 8.8. This was followed by Sample B having an 8.5 rating and Sample E with 8.1. Sample C and D followed respectively with 7.75 and 7.6. Sample A was accepted to be developed best of all.
Solid lipid nanoparticles (SLN) developed in early 90’s was considered as an alternative and novel drug delivery systems to existing traditional drug delivery systems with auspicious delivery of active pharmaceutical substances with enhanced bioavailability, biocompatibility and reduced toxicity. SLN’s are solid colloidal carriers with spherical shape ranging from 10-1000 nm in diameter replacing liquid lipid with solid lipid which eventually developed into solid lipid nanoparticles. Solid lipids incorporated in SLN’s are solid at room temperature and resembles similar to physiological lipids with site specific and targeted drug delivery. The drug is dispersed and/or dissolved in solid lipid core matrix cable of carrying both hydrophilic and lipophilic drugs. This review article focuses on various methods of preparation of SLN’s, their characterizations. The analytical techniques for characterization of solid lipid nanoparticles like photon correlation spectroscopy, scanning electron microscopy (SEM), differential scanning calorimetry (DSC) were also highlighted. Current trends in SLN’s have great scope for targeted and controlled drug delivery in treating various diseases with improved bioavailability, reduced dose and fewer side effects. Hence, solid lipid nanoparticles are attracting a wide group of researchers around the globe for exploiting their benefits.
Plants derived bioactive compounds have been focused on recent research due to their health promoting effects. Medicinal Plants serve as the main source of medicine to poor communities that do not have access to modern medical services. The present Investigation has been carried out to assess the phytochemicals of leaves from crotalaria verrucosa medicinal plant. The solvents like Acetone, Chloroform and Hydro alcohol were used for phytochemical screening of plant extract. The results revealed the presence of alkaloids, flavonoids, phenols, saponin, streroids, tannin and carbohydrate.