International Journal of Pharmaceutical Sciences and Drug Research

157-163

Authors: N. O. Ezenobi*, H. I. Ogbu, G. O. Musa

A successful treatment of wound infection is determined by the proper identification and evaluation of the varied types of microorganisms that colonize the wound surface. Such evaluation will include an antimicrobial susceptibility profiling of the invading pathogen(s) in order to implement an effective and pathogen specific treatment. The antimicrobial susceptibility profile of the bacterial species isolated from wound infections was tested to provide basis for their prudent use as antimicrobials. The standard method of antibiotic sensitivity testing with single antibiotic disc was employed in the analysis. The bacterial isolates tested were Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumoniae. The organisms were isolated from samples collected from patients at different wards at the University of Port Harcourt Teaching Hospital, Port Harcourt, Nigeria. The number and percentage occurrence of each individual bacterium encountered varied among the isolates. Pseudomonas aeruginosa has the highest frequency of occurrence of 48.6% accounting for 36 of the 74 bacterial isolates. This was followed by Staphylococcus aureus and Escherichia coli accounting for 17 (23.0%) and 11 (14.9%) respectively. Klebsiella pneumoniae was the least prevalent bacteria species accounting for 10 (13.5%) of the total bacterial count. The study shows imipenem as the most potent antimicrobial agent against the isolates tested. The isolates were moderately sensitive to gentamicin, ciprofloxacin and levofloxacin, but highly resistance to ceftazidime, erythromycin, sulphamethoxazole/trimethoprim, cefepime, amoxicillin/clavulanic acid and aztreonam. The study further reiterates the need for prudent use and control of antimicrobials.

174-180

Authors: R. Govindharaju1*, P. Durairaj2, T. Maruthavanan3, M. Marlin Risana4, T. Ramachandramoorthy5

Cr(III) and Mn(II) metal complexes of Schiff base ligand derived from phenylacetylurea condensed with salicylaldehyde (SBPS) and thiocyanate(SCN-) ion were synthesized by using microwave irradiation. Microwave assisted synthesis gives high yield of the complexes within a very short time. The molecular formulae and the geometry of the complexes have been deduced from elemental analysis, metal estimation, electrical conductance, magnetic moment, electronic spectra, FT- IR, Far IR spectra, cyclic voltammetry, thermal analysis and powder-XRD techniques. The molar conductance values indicate that the complexes are non-electrolyte (1:0) type. FT-IR spectra show that Schiff base and thiocyanate ion are coordinated to the metal ion in a monodentate manner. The electronic spectra and the magnetic moment indicate the geometry of the complexes is found to be octahedral. The antimicrobial activities of ligands and their Cr(III) and Mn(II) complexes were studied against the microorganisms, viz., E. coli, Klebsiella Pneumonia, P. aeruginosa, S. aureus, Bacillus cereus, Aspergillus flavus, Aspergillus niger, Aspergillus oryzae, Aspergillus sojae and Candida albicans by agar well diffusion method. The complexes show moderate activity against the bacteria and enhanced activity against the fungi as compared to free SBPS ligand. The free radical scavenging activity of the complexes and the ligands has been determined by measuring their interaction with the stable free radical, DPPH. The complexes have larger antioxidant activity as compared to the ligand. DNA-binding properties have been studied by fluorescence-emissions method. The results suggest that the complexes strongly bind to DNA because of metal complexes are well-known to speed up the drug action and the ability of a therapeutic agent which can frequently be enhanced upon coordination with a metal ion.

187-193

Authors: Rajesh Desai1*, Suresh Koradia2

The objective of this study is to isolation and characterization of unknown degradation product of Atorvastatin calcium in combination formulation product with Ezetimibe by using modern techniques of separation and characterization. An unknown impurity is generating during a forced degradation study of Atorvastatin and Ezetimibe fixed-dose combination tablets. By using the gradient reversed-phase high-pressure liquid chromatographic method, unknown degradation impurity was detected and quantified in the range of 0.05% to 0.2% of Atorvastatin. The impurity was enriched by extreme oxidation degradation of Atorvastatin and isolated through preparative HPLC. The structure of the impurity was characterized by mass and NMR spectrum.

199-203

Authors: B. Usha Sri1*, G. Arjun2

The current research deals with formulation and evaluation of Benazepril hydrochloride transdermal films, by varying ratios of polymers Eudragit RL100, Eudragit RS100 by film casting technique. Preformulation studies were conducted to check the solubility, melting point and partition coefficient. The eleven formulations were analyzed for physicochemical parameters and drug dissolution potential of transdermal films. All the formulations are transparent with minimum weight variation and uniform thickness. The drug content uniformity of all the formulations vary between 96.84 ± 3.7% to 96.98 ± 1.6% indicate uniform drug distribution. The low water vapour transmission values indicate good water vapour permeation. The folding endurance is between 246 ± 4.60 to 315 ± 4.13 indicates that the transdermal films can withstand rupture. In vitro drug dissolution study indicates maximum amount of drug 96.8% (F2) released in 24 h when compared with marketed formulation 84.81%. The release order follows Fickian diffusion. The formulation F2 was optimized based on drug flux, permeability coefficient and enhancement ratio.

210-220

Authors: Monica RP Rao*, Mayuri K. Magar

Drug solubility poses numerous challenges in design of formulations for drugs with poor aqueous solubility. Ethionamide is an antitubercular drug belonging to biopharmaceutical classification system class II drug having less aqueous solubility. Nanosuspensions were prepared by using various solvents such as methanol, ethanol, acetone and chloroform and it was prepared using anti-solvent precipitation technique by using probe sonication. Various stabilizers such as tocopherolpolythytlene glycol succinate, polyvinylpyrrolidone and tween 80 singly or in combination were studied. A 32 factorial design was employed to study the effect of independent variables, concentration of stabilizers and stirring speed on particle size and cumulative percent drug release. The particle size of the optimized batch was 97.54 ± 8.47 nm with polydispersity index of 0.36 and zeta potential -10.1 ± 2.3 mV. The cumulative percent drug release of optimized batch was found to be 95.01 ± 1.16% in 60 min. Optimized batch was ultracentrifuged and evaluated for saturation solubility studies, stability and powder X-ray Diffraction studies. Optimized nanosuspension was loaded on Espheres by spraying in a coating pan and then coating of Eudragit controlled release polymers. The coated Espheres were evaluated for drug content, friability, scanning electron microscopy, ex-vivo permeation studies and drug release kinetics studies. The friability value for primary coated sphere was found to be 0.8 ± 0.12% and for secondary was 1% and the best fit model was found to be Korsmeyer-Peppas model which is indicative of diffusion controlled release. Ex vivo diffusion studies revealed a moderate increase in permeability.

226-230

Authors: Abhishek Biswal R, Vivek Pazhamalai*

The bioactive compounds of Gracilaria edulis were determined by using Gas Chromatography Mass spectroscopy. The drug compounds were screened for analyzing the inhibition potential against the virulent bacterial enzyme. In this research, the protein responsible for bacterial infection was docked against the drug compounds of Gracilaria edulis. The data of the virulent enzymes are studied and retrieved from PDB. The bioactive compounds were screened by Lipinski rule of five and ADMET properties. Using Autodock 4.2.6 the molecular docking analysis were done against virulent enzymes and was visualized by discovery studio 3.1. The bioactive compound eugenol with binding energy -4.42 Kcal/mol followed by 2 Heptene, 2,4,4,6 tetramethyl -3.89 Kcal/mol and 1, 2-Propanediol 2.77 Kcal/mol. The hydrogen and vanderwaals interaction of amino acids were studied. This research work mainly focuses on targeting the virulent enzymes that can reduce clinical costs by designing novel drug.

241-244

Authors: B. C. Joshi1, Vinod Kumar2*, Bhuwan Chandra2, N. D. Kandpal2

The components present in the essential oils extracted from Anaphalis margaritacea (L.) Benth., Salvia leucantha Cav. and Thymus linearis Benth. were identified by GC and GC/MS analysis. The main compounds present in the oils were aromadendrene (20.0%) in S. leucantha, Phellandrene (12.5%), α-thujene (12.0%) in A. margaritacea and thymol (50.0%) in T. linearis. The antibacterial activity of all the three oils against E. coli, P. aeruginosa, S. aureus and S. typhi, has been studied. In the antibacterial activity S. typhi is the most resistant bacteria to all the tested oils whereas essential oil of T. linearis showed highest antibactericidal activity against S. aureus in diffusion method.

250-254

Authors: Gouranga Nandi*

Recently, worldwide extensive attention is being paid in exploration and exploitation of pharmaceutical excipients from natural resource. Various natural polysaccharides have been significantly reported as prospective drug delivery carriers. These natural gums are preferred over synthetic polymers because of their biocompatibility, low cost, free availability and biodegradability. But due to variable chemical composition, microbial load, microbial growth and change in viscosity upon aging, acceptability is low compared to commercial synthetic products. Tailoring or modification may be an approach to make them smart as drug carriers specially in order to modulate the site of drug release and it’s kinetic. The chemical modification of okra gum (OG) was the main objective of the present study in order to make it potential mucoadhesive for the application in mucoadhesive drug delivery. In this study, methacrylic acid was grafted onto okra gum. At first, okra gum has been isolated from the fruits of Hibiscus esculentus. Poly (methacrylic acid)-grafted-okra gum (PMAc-g-OG) was synthesized employing a microwave-promoted and redox-initiated method. Potassium persulphate was used as free- radical-initiator. Methacrylic acid was mixed to 1% solution of OG and then 30 ml of potassium per sulphate aqueous solution was added to the previous mixture along with continuous stirring. The mixture was exposed to microwave in a domestic micro-oven. The mixture was kept overnight and the copolymer was collected and purified using acetone and aqueous methanol (30% v/v) subsequently. The copolymer was characterized by elemental analysis, FTIR, DSC-TGA, and 13C NMR study. Ex-vivo mucoadhesion test was performed using goat stomach. A highest % grafting of 448.32% was found in the synthetic procedure employed in the study. The characterization studies also substantiate the successful grafting. Ex-vivo mucoadhesion study also showed excellent mucoadhesive capacity over a period of 16 hours. The study exhibited that the method employed was very simple, less time consuming, one-pot and without N2 atmosphere. The copolymer also exhibited excellent mucoadhesivity which might be applied in different mucoadhesive drug delivery systems such as prolonged release gastroretentives, buccal gels, etc.

263-271

Authors: Kajal Kamalso Malgave*, Nilofar Shahnwaj Naikwade, Padma Laxmikant Ladda, Tabbasum S. Shikalgar, Sudhir S. Patil

Adansonia digitata (AD) Linn has been used to cure PU in Ayurveda but its efficacy has not been validated. The current study was so carried out to evaluate the antiulcer activity of ethanolic extract of Adansonia digitata fruit pulp (ADFP), n hexane extract of Adansonia digitata seed oil (ADSO) & their combination (ADFP+ADSO) in rats. The effect of AD on gastric ulcer in pylorus ligation induced and ethanol induced models was studied using doses [ADFO (500 mg/kg), ADSO (300 mg/kg) & combination of ADFP & ADSO] for 10 days. Omeprazole (10 mg/kg) were used as the standard drug. Depending on the model, outcomes measures were gastric volume, pH, free acidity, total acidity, ulcer index, percentage inhibition of ulcer index, protein, pepsin, mucus, antioxidant marker enzyme level (Superoxide dismutase, Catalase, Lipid peroxidation), morphological & Histopathological study. The result obtained with combination was set up near to the standard drug and consequence showed that the combination of ADFP & ADSO was found to be more effective than the individual extract of AD. The outcomes were statistically evaluated with the one-way ANOVA followed by the test of Dennett’s‘t’. The secondary-metabolites such as flavonoids, proteins, saponins, tannins, phenols, terpenoids, alkaloids and Fatty acids (palmitic acid, oleic acid, linoleic acid) are potent as antioxidant, antiulcer and anti-inflammatory. The finding of this reading confirmed that AD has antiulcer activity due to 1 or more of the secondary-metabolites present in it. Therefore, this study validates its antiulcer use in Ayurveda. Future investigation on separation of specific phytochemicals and elucidate MOA are needed.