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.

116-119

Authors: S. L Sija*

Anacardic acids, a class of medicinally and industrially important phenolic compounds is found in a variety of dicotyledonous families chiefly in Cashew (Anacardium occidentale L). Phenylalanine ammonia-lyase (PAL) shows a dominant role in the biosynthesis of poly phenolic compounds, which are involved in the defense mechanism in harsh environments related to various stimuli. The current study was conducted to find out the presence of anacardic acid in ethyl acetate extract of young leaves of cashew using high performance thin layer chromatography (HPTLC) method and the presence of phenyl alanine ammonia lyase gene also plays a role in the biosynthesis of anacardic acid in young leaves was also confirmed by cDNA synthesis from a cellular mRNA template connected to the polymerase chain reaction (PCR).

126-128

Authors: J. Prathyusha*, N. S. Yamani, G. Santhosh, A. Aravind, B. Naresh

Cosmetics play a vital role for everyone to have a joyful and sanguine life. In present scenario herbal cosmeceuticals have more demand because they have no side effects. People having oily skin suffer from acne, whiteheads and blackheads quite often so scrubbing become more essential. In our present study we formulated 3 different formulations F1, F2, F3 in gel form for oily skin by using turmeric, aloe vera, cinnamon, potato starch, activated charcoal powder, honey, green tea, lemon juice, onion, walnut shell, coconut oil, beet root juice powder, sodium lauryl sulphate, water and evaluated by using various parameters such as physical appearance, viscosity, pH, Spreadability, irritability, washability, stability studies and got fruitful results with all the tests. The scrub F2 was found to show excellent effects on controlling oil secretion, and preventing formation of new pimples. The herbal formulation F2 was having characteristic odour, reddish brown in color having, light, non-irritant to the skin and quite elegant. The powder was smooth to touch and in gel form it spreads satisfactorily. Thus, the formulated scrub F2 can be utilized efficaciously without a side effect which exfoliates and makes glowing skin.

137-140

Authors: Shweta Shriwas1*, Raju Chouksey1, Sumeet Dwivedi2

Vaginal infection include irritation, itching and swelling are very frequent and common among women due to various un-hygienic issues including a major fungus causing infection is Candida species. According to Ayurveda several herbs are used to cure women disorders, though there proper documentation and validation need to be established. It has increasingly deserved a special attention among the medical community. In spite of the presence of Candida species as a human commensal, alarming rates of local and systemic infections have been observed, varying from moderate to severe impact. The present investigation aims to formulate and evaluate herbal tablet containing hydro-alcoholic extract of Achyranthes aspera Linn. (Roots). Various batches F1 to F8 were prepared using different ratio of ingredients and were evaluated as per IP. The data obtained indicate that F7 have excellent results when compared with other formulation codes.

147-151

Authors: P Gupta, V A Sethi, A W Siddiqui, L K Tyagi*

The objective of proposed work was to develop Ondansetron Hydrochloride (OND HCl) sustained release matrix tablets for the better treatment of vomiting for extended period of time. Sustained release matrix tablet is the drug delivery system that is designed to achieve a prolonged therapeutic effect by continuously releasing medication over an extended period of time after administration of single dose. The matrix tablets of OND HCl were prepared by direct compression method using varying ratio of hydroxy propyl methyl cellulose (HPMC) and ethyl cellulose. The bends of tablets were evaluated for bulk and tapped density, % compressibility index and angle of repose and powder of all formulations blend exhibited that low interparticle friction and excellent flow characteristics. The prepared matrix tablets were then assessed for different physical tests like consistency of weight, thickness, hardness, friability, drug content and in vitro drug release. Each batch of the OND HCl matrix tablets were of good quality as to hardness, thickness, friability and % medicament content. The in vitro drug release study was done for 2 hours by utilizing paddle technique in 0.1N HCl (pH 1.2) as dissolution media and 6 hours using phosphate buffer (pH 6.8) as dissolution media. The drug release study showed that all formulation FMT-1, FMT-2, FMT-3, FMT-4, FMT-5 and FMT-6 were provide the drug release on sustained manner up to 8 hrs. Amongst the developed matrix tablets formulations, FMT-2 containing ethyl cellulose (100 mg) was optimized as best because FMT-2 show highest drug release profile and promoting the sustained release of drug, which could potentially improve the patient compliance.

78-84

Authors: A R Shabaraya*, A S Parulkar, D Shripathy, P Shetty

Mucoadhesive microspheres are drug delivery system intended for drug targeting to a specific region. Etodolac is a Non-steroidal anti-inflammatory drug. Sustain released Etodolac loaded mucoadhesive microspheres were prepared to overcome the relatively short residence time of Etodolac in the GIT tract before elimination. Solvent evaporation method was used for preparation of mucoadhesive microspheres with the help of Carbopol 974P, HPMC K100M and HPMC K4M as the polymers. Central composite design was selected for the development of the formulation. The formulations were evaluated for their particle size, surface morphology, degree of swelling, entrapment efficiency, drug content and in-vitro drug release study was done. Based on the results obtained from the preliminary formulations three optimized formulations were designed. The percentage mucoadhesion and swelling index of these formulations were obtained in the range of 66-70% and 82.50-83.84% respectively. Optimized formulation releases 90.94% to 92.11% of drug after 10 hours and follows zero order kinetics.

91-97

Authors: Manas Ranjan Mishra*, Punam Agrawal, Surya Narayan Das

Capecitabine is a 'pro-drug' to the cytotoxic agent 5-fluorouracil (5-FU) intended to administered orally. Capecitabine is generally used as first line monotherapy for advanced colon cancer. Simple, rapid, accurate UV spectrophotometric methods were developed in the present study and validated for the estimation of Capecitabine in bulk and its formulations as per ICH guidelines. Three solvent systems viz., 0.1N NaOH, 0.1N HCl and Methanol: Water (1:3) was tried. The results suggest that the developed method shows linearity over the range of concentration 2-24μg/ml and a correlation coefficient of 0.9999. Accuracy, precision, linearity, robustness, and ruggedness were statistically validated as per ICH guidelines for all the developed methods. The % RSD values for validated methods were found to be less than 1.5 and methods will find application in routine analysis of drug formulations containing Capecitabine.

105-110

Authors: NM Lima1*, RS Silveira1, RR Ramos1, VNC Santos2, MP Nascimento3, Tjas Andrade4, AP Carli1, Mal Oliveira3, MV Almeida3

Three medicinal plants with recognized anti-inflammatory potential, identified as “erva de São João“ (Ageratum conyzoides), “Tanchagem“ (Plantago major) and “ Bardana“ (Arctium lappa L.) were obtained from a medicinal herbs company located in Teófilo Otoni city (Minas Gerais State, Brazil). The dry plant material obtained in packages was submitted to the chemical procedures to prepare the crude extracts by maceration according to the Brazilian pharmacopoeia legislation. After extraction, the samples were subjected to 1H NMR, TLC and Capillary Electrophoresis analysis by co-injection of authentic patterns of phenolic acids and flavonoids to identify the major compounds and classes of secondary metabolites present in each material and then their chemical and biological potential was assessed by DPPH free radical inhibition assay and antimicrobial against E. coli. The results obtained allow us to conclude that the phytopreparation was effective in the extraction of compounds with antioxidant potential and the three species presented a high concentration of flavonoids and other phenolics that is compatible with the chemosystematic data. The screening obtained by 1H NMR spectroscopy, TLC and Capillary Electrophoresis with ultraviolet detection analysis provided us a qualitative profile of the phytochemicals present in each material. None of the extracts were active against Escherichia coli by antibacterial disk diffusion assay at concentration of 1 mg/ml.

56-60

Authors: M Lakshmi Kanth*, B Raj Kamal

An accurate RP-HPLC method developed for the estimation of Neratinib in bulk and tablet dosage form. The method is and validated for parameters linearity, accuracy, suitability, specificity, precession, LOD, LOQ and robustness. An Altima column (150 mm × 4.6 mm × 5µ) used for chromatographic separation within a runtime of 6 min. The mobile phase buffer (monopotassium phosphate) and acetonitrile (60:40 v/v) with 0.1% formic acid is used. The flow rate maintained at 1.0 ml/min with the effluents monitored at 215 nm. The Neratinib analyzed at retention time of 4.001. The concentration linear over 30-180µg/ml with regression equation y = 6065.6x + 795.43 and regression co-efficient 0.999.

7-15

Authors: Gourishyam Pasa*, Prasanta Kumar Choudhury, Ghanshyam Panigrahi, Biswajeet Maharana

The oral floating matrix tablets of Ciprofloxacin Hydrochloride were formulated by Experimental design by using HPMC K100M and Ethyl Cellulose as the retardant polymers each with three different levels with an approach to increase gastric residence and thereby improve drug bioavailability. From FTIR results it was confirmed that there is no chemical interaction between the drug with the excipients used in tablet formulations. Also, there was no shift in the endotherm of in the drug- excipients mixtures indicating compatibility of drug with all the excipients. All the tablets were prepared by effervescent approach in which Sodium bicarbonate was added as a gas generating agent. Floating Matrix tablets were prepared by direct compression method and prepared tablets were evaluated for weight variation, percentage friability, hardness and drug content studies. All the formulations showed compliance with pharmacopeia standards (I.P. 1996). Floating lag times of all the formulations were within 1 minute and Total floating time of all the formulations were more than 12 hours. In vitro release studies revealed that the release rate decreased with increase polymer proportion of retarding polymers. The formulation CHE9 sustained release of drug for 12 hours with 21% release of drug after 1 hour and more than 97% at the end of 12 hours. From the Kinetic model it was found that the optimized formulation CHE9 showed linearity in case of Zero order (R2: 0.938) and Higuchi model (R2: 0.954). By fitting data to Korsmeyer-Peppas model and ‘n’ value lying above 0.5 indicating non Fickian release.

22-30

Authors: Kamla Pathak1*, Anil Kumar2, Ekta Yadav2

The aim of the investigation was to develop and evaluate thermoreversible in situ nasal gel formulations of repaglinide (REP) and to establish correlation between its in vitro release and ex vivo permeation profiles. The solubility of REP was enhanced by preparing solid dispersions (SDs) with hydrophilic carriers (PVP K30/ PEG 6000/ poloxamer 188) in different weight ratios. REP: PVP K30 (1:5) was selected as the optimized SD as it showed highest enhancement in solubility (405%). The optimized SD was characterized by SEM and DSC and incorporated into a blend of thermoreversible and mucoadhesive polymers (poloxamer 407 and carbopol 934 P) by cold technique to form in situ gels (F1-F6). The prepared in-situ gels were evaluated for various pharmacotechnical features and the formulation F3 exhibited least gelling time of 6.1± 0.20, good mucoadhesive property to ensure sufficient residence time at the site of application and a %CDR of 82.25%. The ex vivo permeation characteristics across goat mucosa can be summarized as CDP of 78.7%, flux = 6.80 mg/cm2/h; permeability coefficient of 2.02 mg/h and zero order kinetics. On correlating the CDR profile of F3 with that of its CDP profile, a R2 value of 0.991 (slope= 0.921) was observed. The value of slope approximating one, suggested that almost entire amount of drug released from F3 was capable of permeating across the nasal mucosa, ex-vivo indicating that in-situ nasal gels of REP for systemic action can be successfully developed for the management non-insulin dependent type-II diabetes mellitus.

35-44

Authors: Hafsa Mohammadi*, V Hemanath Kumar

The aim of the present work is to develop fast dissolving tablets from the solid dispersion of Tenoxicam for enhancement of solubility. The solid dispersions of Tenoxicam were prepared with Kollidon CL, PVP K30 and Poloxamer 127, in 1:1:1, 1:2:1 and 1:3:1 by using solvent evaporation method. The prepared solid dispersions were analyzed for all the physical parameters, drug: carrier interactions like FTIR, SEM, XRD. Solid dispersions showed a better dissolution compared to the pure drugs and among all the other formulations SD9 shows high percentage drug release i.e. 99.11 ± 5.17% for 90 min and selected as an optimized formulation for the preparation of fast disintegrating tablets of Tenoxicam. Gellan Gum, Fenugreek Seed Mucilage and L-HPC (low, middle and high concentrations) used in the preparation of fast disintegrating tablets prepared by direct compression method using 33 Response surface method. The post compression parameters of all the prepared tablets were within the limits. TF13 was selected as optimized formulation based on its highest disintegration time 36 sec and drug release 99.68 ± 1.52% for 10 min. Drug-excipients characterization also revealed that there is no interaction. Hence it concluded that solid dispersions incorporated fast disintegrating tablets is very useful approach for immediate release of Tenoxicam in the efficient management of inflammation and pain.