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2010| July-August | Volume 72 | Issue 4
Online since
December 14, 2010
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SHORT COMMUNICATIONS
Antidiabetic and free radicals scavenging potential of
Euphorbia hirta
flower extract
S Kumar, R Malhotra, D Kumar
July-August 2010, 72(4):533-537
DOI
:10.4103/0250-474X.73921
PMID
:21218075
The present study was carried out to evaluate antidiabetic and
in vitro
free radicals scavenging effects of flower extract of
Euphorbia hirta
. The ethanolic and petroleum ether extracts (250 and 500 mg/kg) were orally tested for 21 days in alloxan induced diabetic mice and blood glucose level was measured with glucometer. Administration of extract resulted in significant reduction in serum cholesterol, triglycerides, creatinine, urea, alkaline phosphatase levels but high density lipoprotein levels and total proteins were found to be increased after treatments. Free radicals scavenging effect of ethanolic extract was also evaluated by various antioxidant assays, including 1, 1-diphenyl-2-picryl hydrazyl free radical scavenging activity, superoxide anion radical scavenging, nitric oxide scavenging, and reducing power assay. It was compared with standard antioxidants compounds such as butylated hydroxyl anisole and ascorbic acid. All the extracts showed antioxidant activity in all the tested methods.
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1,503
177
Development and validation of HPLC method for the determination of pregabalin in capsules
GB Kasawar, MN Farooqui
July-August 2010, 72(4):517-519
DOI
:10.4103/0250-474X.73935
PMID
:21218069
A simple, precise, specific, and accurate reverse phase HPLC method has been developed for the determination of pregabalin in capsule dosage form. The chromatography was set on Hypersil BDS, C8, 150×4.6 mm, 5 μm column using photodiode array detector. The mobile phase consisting of phosphate buffer pH 6.9 and acetonitrile in the ratio of 95:05 with flow rate of 1 ml/min. The method was validated according to ICH guidelines with respect to specificity, linearity, accuracy, precision and robustness. Lower limit of quantification is 0.6 mg/l. The pregabalin sample solution was found to be stable at room temperature for about 26 h.
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RESEARCH PAPERS
Antiinflammatory, analgesic and antipyretic activities of
Mimusops elengi
Linn
A Purnima, BC Koti, A. H. M. Thippeswamy, MS Jaji, A. H. M. Vishwantha Swamy, YV Kurhe, A Jaffar Sadiq
July-August 2010, 72(4):480-485
DOI
:10.4103/0250-474X.73908
PMID
:21218059
In the present study, 70% ethanol extract of
Mimusops elengi
Linn. bark was assessed for antiinflammatory, analgesic and antipyretic activities in animals. The antiinflammatory activity of ethanol extract of
Mimusops elengi
(200 mg/kg, p.o) was evaluated using carrageenan-induced paw edema and cotton pellet-induced granuloma models. Analgesic effect was evaluated using acetic acid-induced writhing and Eddy's hot plate models and antipyretic activity was assessed by Brewer's yeast-induced pyrexia in rats. The ethanol extract of
Mimusops elengi
(200 mg/kg, p.o) significantly inhibited the carrageenan-induced paw oedema at 3rd and 4th h and in cotton pellet model it reduced the transudative weight and little extent of granuloma weight. In analgesic models the ethanol extract of
Mimusops elengi
decreases the acetic acid-induced writhing and it also reduces the rectal temperature in Brewer's yeast induced pyrexia. However,
Mimusops elengi
did not increase the latency time in the hot plate test. These results show that ethanol extract of
Mimusops elengi
has an antiinflammatory, analgesic and antipyretic activity.
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283
SHORT COMMUNICATIONS
Synthesis and antimicrobial screening of pyrazolo-3-aryl quinazolin-4(3h)ones
MB Deshmukh, S Patil, SS Patil, SD Jadhav
July-August 2010, 72(4):500-504
DOI
:10.4103/0250-474X.73934
PMID
:21218064
2-thio-3-aryl quinazolin-4(3H)one (1) was synthesized by reacting anthranilic acid with thiocarbamate salts of substituted aniline and carbon disulphide, which on reflux with excess of hydrazine hydrate to form 2-hydrazino quinazolin-4(3H)one derivatives (2). The reaction of (2) with variously substituted aryl aldehydes gave the corresponding hydrazones (3). Further, the cyclization of compound (3) in acetic anhydride gave tricyclic pyrazoloquinazolinones (4). All newly synthesized compounds have been tested for their antibacterial activity against gram +ve bacteria
B. substilis
,
S. aureus
and gram -ve bacteria
E. coli
,
P. vulgaris
. The species used for antifungal activity are
Aspergillus
niger and
Phytophora.
Introduction of -OCH3, -OH and -Cl groups to the heterocyclic frame work enhanced antibacterial and antifungal activities.
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1,332
164
Formulation and evaluation of omeprazole tablets for duodenal ulcer
A Choudhury, S Das, S Bahadur, S Saha, A Roy
July-August 2010, 72(4):491-494
DOI
:10.4103/0250-474X.73922
PMID
:21218061
Omeprazole pellets containing mucoadhesive tablets were developed by direct punch method. Three mucoadhesive polymers namely hydroxypropylemethylcellulose K4M, sodium carboxy methylcellulose, carbopol-934P and ethyl cellulose were used for preparation of tablets which intended for prolong action may be due to the attachment with intestinal mucosa for relief from active duodenal ulcer. Mucoadhesive tablets were coated with respective polymer and coated with Eudragit L100 to fabricate enteric coated tablets. The prepared tablets were evaluated for different physical parameters and dissolution study were performed in three dissolution mediums like 0.1N hydrochloric acid for 2h, pH 6.5 and pH 7.8 phosphate buffer solution for 12hr. Sodium carboxymethylcellulose showed above 95% release within 10 h where as carbopol-934P showed slow release about 88% to 92% over a period of 12 h. having excellent mucoadhesive strength but ethyl cellulose containing tablets showed less than 65% release. The release mechanism of all formulation was diffusion controlled confirmed from Higuchi's plot. Thus, the present study concluded that, carbopol-934P containing mucoadhesive tablets of omeprazole pellets can be used for local action in the ulcer disease as well as for oral controlled release drug delivery.
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2,531
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Development and validation of a rp-ultra performance liquid chromatographic method for quantification of topotecan hydrochloride in bulk and injection dosage form
PK Saini, CL Jain, RM Singh, SC Mathur, GN Singh
July-August 2010, 72(4):494-497
DOI
:10.4103/0250-474X.73925
PMID
:21218062
A simple, very fast, precise and accurate reverse phase ultra performance liquid chromatographic method was developed for the determination and validation of topotecan hydrochloride in bulk and injection dosage form. A Waters BEH C18, 50Χ2.1 mm, 1.7 μm particle size column in gradient mode was used with mobile phase comprising of 0.1% v/v orthophosphoric acid in water and acetonitrile. The analytical column was thermostated at 50° and flow rate was set at 0.4 ml per min, with photo diode array detection at 260 nm. The retention time of topotecan was found 1.38 min. The method was validated in terms of linearity, accuracy, precision and specificity. The calibration curve was found linear between 20 to 60 μg/ml. The limit of detection and limit of quantification were found 0.2353 and 0.7131 μg/ml, respectively. Percentage recoveries were obtained in the range of 98.91% and 99.17%. The proposed method is precise, accurate, selective and reproducible. The ultra performance liquid chromatographic assay procedure, which proved superior because of its greater sensitivity and relatively shorter (4 min) run time, should be an important tool for speedy future analysis of topotecan hydrochloride in bulk and its injection dosage form.
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912
97
Antimicrobial activity of α-(2-hydroxy-2-methylpropyl)-ω-(2-hydroxy-3-methylbut-2-en-1-yl) polymethylene from
caesalpinia bonducella
(L.) flem
Kavitha Sagar, GM Vidyasagar
July-August 2010, 72(4):497-500
DOI
:10.4103/0250-474X.73929
PMID
:21218063
The compound, α-(2-hydroxy-2-methylpropyl)-w-(2-hydroxy-3-methylbut-2-en-1-yl)polymethylene, isolated from ethyl acetate leaf extract of
Caesalpinia bonducella
(L.) Flem. was evaluated for antimicrobial activity against clinical isolates,
Proteus vulgaris
,
Pseudomonas aeruginosa
,
Klebsiella
sp.,
Staphylococcus citrus
,
Staphylococcus aureus
,
Escherichia coli
,
Candida albicans
and
Rhodotorula
sp. using agar diffusion method. The compound exerted inhibitory zone at all concentrations and revealed the concentration-dependent activity against all tested bacterial and yeast strains comparable to standards streptomycin sulphate and gentamycin for bacteria and fluconazole and griseofulvin for
Candida albicans
and Rhodotorula sp. The inhibition zones were wider and clear for
C. albicans
and
Rhodotorula
sp. (IZ >20 mm) and for Pseudomonas aeruginosa,
P. vulgaris
and
E. coli
zones were greater than standards tested, whereas, zones for
Klebsiella
sp. and
S. aureus
were similar to standards.
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957
82
RESEARCH PAPERS
Rapid and sensitive liquid chromatographic method for determination of paclitaxel from parenteral formulation and nanoparticles
S Kollipara, G Bende, RN Saha
July-August 2010, 72(4):465-470
DOI
:10.4103/0250-474X.73914
PMID
:21218057
A simple and fast reversed phase liquid chromatographic method was developed for estimation of paclitaxel in commercially available parenteral formulation and nanoparticles. Separations were carried out using mobile phase consisting of acetonitrile and 20 mM potassium dihydrogen phosphate (45:55, v/v) on Lichrocart
®
C
18
analytical column at a flow rate of 1 ml/min and detection wavelength of 230 nm. The developed method exhibited linearity over an analytical range of 50-2000 ng/ml with regression equation, mean peak area= 137.58 concentration (ng/ml)+1765.94, (R
2
=0.9999). The method demonstrated selectivity with no interfering peaks eluting near the vicinity of drug peak. The method was found to be sensitive with detection and quantification limits of 7.57 ng/ml and 22.94 ng/ml. The method has shown consistent and good recoveries from parenteral formulation (100.06±0.86%) and nanoparticles (100.43±0.91%). The method was successfully employed for the analysis of
in vitro
release study samples of nanoparticle formulation. The method was also applied for determination of paclitaxel content in various pharmaceutical formulations.
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1,325
126
Carbopol 934-sodium alginate-gelatin mucoadhesive ondansetron tablets for buccal delivery: Effect of PH modifiers
NR Kotagale, CJ Patel, AP Parkhe, HM Khandelwal, JB Taksande, MJ Umekar
July-August 2010, 72(4):471-479
DOI
:10.4103/0250-474X.73912
PMID
:21218058
The present work aims at developing mucoahesive tablets of ondansetron hydrochloride using bioadhesive polymers like carbopol-934, sodium alginate and gelatin. Tablets prepared by direct compression using different polymer with varying ratio were evaluated for hardness, friability, uniformity of weight, disintegration time, microenvironmental pH, bioadhesion and
in vitro
release. Hardness, friability disintegration time and drug release were found within pharmacopoeial limit. Microenvironmental pH decreased whereas bioadhesive strength, water uptake, and
in vitro
release increased with increase in carbopol-934. Increasing sodium alginate and gelatin increased the microenviromental pH and decreased bioadhesive strength, water uptake and
in vitro
release. With a view to investigate the modulation of drug release from formulation by addition of pH modifiers viz. citric acid and sodium bicarbonate, the tablets with carbopol-934 (2.0), sodium alginate (0.5) and gelatin (6.5) were used and the effect of pH modifiers on microenvironmental pH, bioadhesion, water uptake,
in vitro
permeation and
in vitro
release was studied. Microenvironmental pH, bioadhesive strength, water uptake,
in vitro
release and permeation decreased with increasing concentration of citric acid whereas microenvironmental pH, water uptake and release were enhanced and bioadhesive strength was lowered with increase in sodium bicarbonate. Present study demonstrates carbopol-934, sodium alginate, gelatin polymer system with added pH modifier can be successfully formulated for buccal delivery of ondansetron with desired release profile.
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1,901
291
A new validated HPLC method for the simultaneous determination of 2-phenoxyethanol, methylparaben, ethylparaben and propylparaben in a pharmaceutical gel
GA Shabir
July-August 2010, 72(4):421-425
DOI
:10.4103/0250-474X.73906
PMID
:21218050
A novel reversed-phase HPLC method has been developed and validated for the simultaneous determination of 2-phenoxyethanol, methylparaben, ethylparaben and propylparaben preservatives. The method uses a Lichrosorb C8 (150Χ4.6 mm, 5 μm) column and isocratic elution. The mobile phase consisted of a mixture of acetonitrile, tetrahydrofuran and water (21:13:66, v/v/v), pumped at a flow rate of 1 ml/min. The UV detection was set at 258 nm. The method was validated with respect to accuracy, precision (repeatability and intermediate precision), specificity, linearity and range. All the parameters examined met the current recommendations for bioanalytical method validation. The developed method was successfully applied to the determination of commercially available pharmaceutical gel products for these preservatives. The procedure describes here is simple, selective and reliable for routine quality control analysis and stability tests.
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1
2,141
228
Formulation design and optimization of fast disintegrating lorazepam tablets by effervescent method
SB Shirsand, Sarasija Suresh, LS Jodhana, PV Swamy
July-August 2010, 72(4):431-436
DOI
:10.4103/0250-474X.73911
PMID
:21218052
Fast disintegrating tablets of lorazepam were prepared by effervescent method with a view to enhance patient compliance. A 3 full factorial design was applied to investigate the combined effect of two formulation variables: amount of crospovidone and mixture of sodium bicarbonate, citric acid and tartaric acid (effervescent material) on
in vitro
dispersion time. Crospovidone (2-8% w/w) was used as superdisintegrant and mixture of sodium bicarbonate, citric acid and tartaric acid (6-18% w/w) was used as effervescent material, along with directly compressible mannitol to enhance mouth feel. The tablets were evaluated for hardness, friability, thickness, drug content uniformity and
in vitro
dispersion time. Based on
in vitro
dispersion time (approximately 13 s); the formulation containing 8% w/w crospovidone and 18% w/w mixture of sodium bicarbonate, citric acid and tartaric acid was found to be promising and tested for
in vitro
drug release pattern (in pH 6.8 phosphate buffer), short-term stability and drug-excipient interaction. Surface response plots are presented to graphically represent the effect of independent variables (concentrations of crospovidone and effervescent material) on the
in vitro
dispersion time. The validity of the generated mathematical model was tested by preparing two extra-design check point formulations. The optimized tablet formulation was compared with conventional marketed tablet for drug release profiles. This formulation showed nearly eleven-fold faster drug release (t
50%
2.8 min) compared to the conventional commercial tablet formulation (t
50%
>30 min). Short-term stability studies on the formulation indicated that there were no significant changes in drug content and
in vitro
dispersion time (
P
<0.05).
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2,066
477
Bcl-2 expression alters the mitochondrial tri carboxyl acid pathway in hepatic ischemic and reperfusion induced necrosis and apoptosis in rat liver
P Chattopadhyay, P Chaudhury, AK Wahi
July-August 2010, 72(4):437-441
DOI
:10.4103/0250-474X.73913
PMID
:21218053
Ischemic and reperfusion injury leads to necrosis and apoptosis. Mitochondrial enzymes and antiapoptotic gene plays an important role in necrosis and apoptosis. The aim of this study was to investigate the role of Bcl-2 expression in alternations in mitochondrial energy regulation during hepatic ischemia and reperfusion and role in necrosis and apoptosis. Total 12 Wistar rats were divided into sham-operated control group (I) and ischemia and reperfusion group (II). Mitochondrial tri carboxylic acid cycles marker enzymes, respiratory marker enzymes, apoptotic cells, necrotic cells and Bcl-2 expression was measured. Number of necrotic and apoptotic cells were increased in ischemic and reperfusion group with reducing tri carboxylic acid cycles marker enzymes, respiratory marker enzymes and decreasing of Bcl-2 expression. On the basis of our findings it may be concluded that suppression of Bcl-2 gene, inhibition of tri carboxylic acid cycles and respiration rate, adenosine tri phosphate production in mitochondria is a pathophysiological consequences which provides a clue for necrosis and apoptosis in hepatic ischemic and reperfusion injury.
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1,076
66
Development and evaluation of inhalational liposomal system of budesonide for better management of asthma
JJ Parmar, DJ Singh, Darshana D Hegde, AA Lohade, PS Soni, A Samad, Mala D Menon
July-August 2010, 72(4):442-448
DOI
:10.4103/0250-474X.73916
PMID
:21218054
Budesonide is a corticosteroid used by inhalation in the prophylactic management of asthma. However, frequent dosing and adverse effects (local and systemic) remain a major concern in the use of budesonide. Liposomal systems for sustained pulmonary drug delivery have been particularly attractive because of their compatibility with lung surfactant components. In the present investigation, pulmonary liposomal delivery system of budesonide was prepared by film hydration method and evaluated for sustained release. Various parameters were optimized with respect to entrapment efficiency as well as particle size of budesonide liposomes. For better shelf life of budesonide liposomes, they were freeze dried using trehalose as cryoprotectant. The liposomes were characterized for entrapment efficiency, particle size, and surface topography;
in vitro
drug release was evaluated out in simulated lung fluid at 37° at pH 7.4. The respirable or fine particle fraction was determined by using twin stage impinger. The stability study of freeze dried as well as aqueous liposomal systems was carried out at 2-8° and at ambient temperature (28±40). The freeze dried liposomes showed better fine particle fraction and drug content over the period of six months at ambient as well as at 2-8° storage condition compared to aqueous dispersion of liposomes.
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1,575
215
SHORT COMMUNICATIONS
Simultaneous estimation of metformin and pioglitazone by ultraviolet spectrophotometry
Laxmi Goswami, S Mukhopadhyay, S Durgapal
July-August 2010, 72(4):508-510
DOI
:10.4103/0250-474X.73940
PMID
:21218066
This work deals with the simultaneous estimation of metformin hydrochloride and pioglitazone hydrochloride in a bilayered tablet dosage form, without prior separation by two techniques. The methods employed are derivative spectrophotometery and Q analysis. The absorption maxima at 231 nm and 269 nm were used for the estimation of metformin and pioglitazone, respectively. Both the drugs and their mixture obey Beer-Lamberts law at selected wavelength at given concentration range. The result of analysis has been validated statistically and recovery studies confirmed the accuracy of the proposed method. The proposed procedures are simple, rapid, require no separation steps and can be used for the routine analysis of both drugs.
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2,134
234
Formulation and evaluation of mouth dissolving tablets of cinnarizine
BP Patel, JK Patel, GC Rajput, RS Thakor
July-August 2010, 72(4):522-525
DOI
:10.4103/0250-474X.73930
PMID
:21218071
The purpose of this research was to develop mouth dissolve tablets of cinnarizine by effervescent, superdisintegrant addition and sublimation methods. All the three formulations were evaluated for disintegration time, hardness and friability, among these superdisintegrant addition method showed lowest disintegration time; hence it was selected for further studies. Further nine batches (B1-B9) were prepared by using crospovidone, croscarmellose sodium and L-HPC in different concentrations such as 5, 7.5 and 10%. All the formulations were evaluated for weight variation, hardness, friability, drug content,
in vitro
disintegration time, wetting time,
in vitro
dissolution. Formulation with 10% L-HPC showed the less disintegration time (25.3 s) and less wetting time (29.1 s).
In vitro
dissolution studies showed total drug release at the end of 6 min.
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2,069
320
Simultaneous spectrophotometric estimation of tenofovir disoproxil fumarate and lamivudine in three component tablet formulation containing efavirenz
R Sharma, K Mehta
July-August 2010, 72(4):527-530
DOI
:10.4103/0250-474X.73926
PMID
:21218073
Three UV spectrophotometric methods have been developed, simultaneous equation method, multicomponent analysis (II) and derivative spectroscopy method (III). The absorption maxima of the drugs were found to be 247, 259 and 272 nm, respectively for efavirenz, tenofovir disoproxil fumarate and lamivudine in methanol:water (50:50) solvent system. Efavirenz, tenofovir disoproxil fumarate and lamivudine obeyed Beer's law in the concentration range of 10-60, 5-30 and 5-30 μg/ml, respectively. Results of analysis for all the three methods were analyzed and validated for various parameters according to ICH guidelines.
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1,617
181
Simultaneous determination of ofloxacin and ornidazole in solid dosage form by RP-HPLC and HPTLC techniques
Manisha Puranik, DV Bhawsar, Prachi Rathi, PG Yeole
July-August 2010, 72(4):513-517
DOI
:10.4103/0250-474X.73937
PMID
:21218068
The objective of this work was to develop and validate simple, rapid and accurate chromatographic methods for simultaneous determination of ofloxacin and ornidazole in solid dosage form. The first method was based on reversed phase high performance liquid chromatography, on Intersil C
18
column (250 mm, 4.6 i.d.), using acetonitrile:methanol: 0.025M phosphate buffer, pH 3.0 (30:10:60 % v/v/v) as the mobile phase, at a flow rate of 1 ml/min at ambient temperature. Quantification was achieved with UV detection at 318 nm over a concentration range of 2-40 μg/ml for ofloxacin and 5-100 μg/ml for ornidazole. The mean retention time of ofloxacin and ornidazole was found to be 4.04 min and 5.83 min, 6.77 min (isomers), respectively. The amount of ofloxacin and ornidazole estimated as percentage of label claimed was found to be 100.23 and 99.61%, with mean percent recoveries 100.20 and 100.93%, respectively. The second method was based on TLC separation of these drugs using silica gel 60F
254
aluminium sheets and dichloromethane:methanol:25% ammonia solution (9.5:1:3 drops v/v) as mobile phase. Detection was carried out at 318 nm over the concentration range of 20-100 ng/spot for ofloxacin and 50-250 ng/spot for ornidazole. The mean R
f
value of ofloxacin and ornidazole was found to be 0.16 and 0.56, 0.78 (isomers), respectively. The amount of ofloxacin and ornidazole estimated as percentage of label claimed was found to be 100.23 and 99.61% with mean percent recoveries 100.47 and 99.32%, respectively. Both these methods were found to be simple, precise, accurate, selective and rapid and could be successfully applied for the determination of pure laboratory prepared mixtures and tablets.
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1,645
156
Synthesis and antibacterial activity of triphenyltinbenzoate
MK Choudhury, B Zewdie
July-August 2010, 72(4):531-533
DOI
:10.4103/0250-474X.73923
PMID
:21218074
Triphenyltinbenzoate was synthesized using triphenyltinchloride and silver benzoate prepared from sodium benzoate. The structure of the synthetic compound was elucidated by spectral and C, H analysis. The antibacterial activities of the organotin compound were determined against four bacteria namely
Escherichia coli
(ATCC 25922),
Staphylococcus aureus
(ATCC 25923),
Streptococcus pyogenes
(clinical isolate) and
Pseudomonas aeruginosa
(ATCC 27853)
in vitro
experiment. All the bacteria were inhibited at a concentration of 200 μg/ml and 20 μg/ml in dimethylsulphoxide solution and the minimum inhibitory concentration was found to be same, 7.5 μg/ml for
Escherichia coli, Staphylococcus aureus, Streptococcus pyogenes
and 10 μg/ml for
Pseudomonas aeruginosa
.
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845
82
Spectrophotometric assay of mefenamic acid in tablets using 1,4-dioxane as solvent for extraction
G Mathai, JT Moolayil, KB Jose, VS Sebastian
July-August 2010, 72(4):525-526
DOI
:10.4103/0250-474X.73928
PMID
:21218072
A spectrophotometric method of assay of mefenamic acid in tablets involving, dissolving the tablet powder in 1,4-dioxane and measuring the absorbance at 353.2 nm. The concentration of mefenamic acid is determined using the previously prepared calibration curve using standard solution of mefenamic acid in dioxane. The method was tested by assay of six different commercial tablets containing mefenamic acid.
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1,080
92
Antibacterial and antifungal potential of some arid zone plants
SC Jain, B Pancholi, R Singh, R Jain
July-August 2010, 72(4):510-513
DOI
:10.4103/0250-474X.73939
PMID
:21218067
Sequential extracts of some medicinally important arid zone plants of Rajasthan, viz.
Lepidagathis trinervis
Nees.,
Polycarpea corymbosa
Lam. and
Sericostoma pauciflorum
Stocks. ex Wight. were tested against six bacterial (Gram +ve and Gram -ve) and five fungal strains using agar well diffusion method. Ethyl acetate extract of
L. trinervis
showed maximum activity against
Bacillus subtilis, Enterobactor aerogenes, Pseudomonas aeruginosa, Aspergillus flavus
and
Trichophyton rubrum
(inhibition zone 16.00±0.81, 13.33±0.66, 14.33±1.85, 14.30±0.34 and 23.00±0.00 mm) at varied minimum inhibitory concentrations of 82, 20, 41, 41 and 20 μg/ml, respectively.
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953
93
In vitro
evaluation of anthelmintic activity of
Nauclea orientalis
leaves
S. T. V. Raghavamma, N Rama Rao
July-August 2010, 72(4):520-521
DOI
:10.4103/0250-474X.73932
PMID
:21218070
Antianthelmintic activity of successive extracts (chloroform, acetone, ethanol and aqueous) of
Nauclea orientalis
leaves were evaluated separately on adult Indian earthworm (
Pheretima posthuma
) and compared with that of albendazole. It was found that the extracts exhibited, respectively dose-dependent action and inhibition of spontaneous motility (paralysis) and death of earthworms. The results indicated that the chloroform, ethyl acetate and ethanol extracts were more potent.
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978
203
RESEARCH PAPERS
Molecular dynamics of sialic acid analogues and their interaction with influenza hemagglutinin
T Femlin Blessia, VS Rapheal, D. J. S. Sharmila
July-August 2010, 72(4):449-457
DOI
:10.4103/0250-474X.73919
PMID
:21218055
Synthetic sialic acid analogues with multiple modifications at different positions(C-1/C-2/C-4/C-8/C-9) are investigated by molecular mechanics and molecular dynamics to determine their conformational preferences and structural stability to interact with their natural receptors. Sialic acids with multiple modifications are soaked in a periodic box of water as solvent. Molecular mechanics and a 2 nanosecond molecular dynamics are done using amber force fields with 30 picosecond equilibrium. Direct and water mediated hydrogen bonds existing in the sialic acid analogues, aiding for their structural stabilization are identified in this study. The accessible conformations of side chain linkages of sialic acid analogues holding multiple substituents are determined from molecular dynamics trajectory at every 1ps interval. Transitions between different minimum energy regions in conformational maps are also noticed in C-1, C-2, C-4, C-8 and C-9 substituents. Docking studies were done to find the binding mode of the sialic acid analogues with Influenza hemagglutinin. This finding provides stereo chemical explanation and conformational preference of sialic acid analogues which may be crucial for the design of sialic acid analogues as inhibitors for different sialic acid specific pathogenic proteins such as influenza toxins and neuraminidases.
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96
Efficient electrochemical synthesis, antimicrobial and antiinflammatory activity of 2-amino-5-substituted-1,3,4-oxadiazole derivatives
S Kumar, DP Srivastava
July-August 2010, 72(4):458-464
DOI
:10.4103/0250-474X.73917
PMID
:21218056
An efficient electrochemical method for the preparation of 2-amino-5-substituted-1,3,4-oxadiazoles (4a-k) at platinum anode through the electrooxidation of semicarbazone (3a-k) at controlled potential electrolysis has been reported in the present study. The electrolysis was carried out in the acetic acid solvent and lithium perchlorate was used as supporting electrolyte. The products were characterized by IR,
1
H-NMR,
13
C-NMR, mass spectra and elemental analysis. The synthesized compounds were screened for their
in vitro
growth inhibiting activity against different strains of bacteria viz.,
Klebsilla penumoniae, Escherichia coli, Bassilus subtilis
and
Streptococcus aureus
and antifungal activity against
Aspergillus niger
and
Crysosporium pannical
and results have been compared with the standard antibacterial streptomycin and antifungal griseofulvin. Compounds exhibits significant antibacterial activity and antifungal activity. Compounds 4a and g exhibited equal while 4c, d, i and j slightly less antibacterial activity than standard streptomycin. Compounds 4a and g exhibited equal while 4b, c, d, f and i displayed slightly less antifungal activity than standard griseofulvins.
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1,549
131
Soyabean powder as a novel diluent in tablet formulation of simvastatin
G Swami, Khushboo Gupta, KM Kymonil, Shubhini Saraf
July-August 2010, 72(4):426-430
DOI
:10.4103/0250-474X.73909
PMID
:21218051
The present research paper introduces soyabean nuggets powder, as a novel excipient with nutraceutical value for tablets containing cholesterol lowering drug, simvastatin. Experiments were carried out to evaluate the suitability of soyabean nuggets powder as a diluent by incorporating in tablet formulation of simvastatin. The formulation was compared with the marketed product to determine its relative efficacy. Soyabean nuggets powder was found to be a promising diluent for tablets for both pharmaceutical and nutraceutical purposes. Simavastatin soya tablet showed acceptable pharmacotechnical properties and assay requirement.
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2,056
285
REVIEW ARTICLE
Lifestyle drugs: Concept and impact on society
SZ Rahman, V Gupta, Anupama Sukhlecha, Y Khunte
July-August 2010, 72(4):409-413
DOI
:10.4103/0250-474X.73902
PMID
:21218048
Lifestyle has changed from being an indicator of the overall well being of an individual to a cause of disease and now "lifestyle" has itself become an object of medical attention. Alcohol has been used enormously as one of the oldest 'lifestyle' drugs, and currently sildenafil citrate (Viagra), the drug of choice for erectile dysfunction, exemplifies a turning point in the era of modern lifestyle drugs. This drug has transformed the lifestyles of millions and greatly increased the revenue of many pharmaceutical companies. With the Indian economy growing rapidly at an annual rate of 8-9%, a new era of drug discovery and development coupled with an enormous increase in the marketing of new drugs is being seen. This has certainly made the Indian public vulnerable to issues related to lifestyle drugs. There is a need to study this concept deeply and the impact of these drugs on Indian society, particularly since this topic has already been the centre of many discussions in other developed nations.
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3,590
858
RESEARCH PAPERS
Interchangeability of two 500 mg amoxicillin capsules with one 1000 mg amoxicillin tablet after a single oral administration
AN Zaid, R Cortesi, J Kort, W Sweileh
July-August 2010, 72(4):414-420
DOI
:10.4103/0250-474X.73904
PMID
:21218049
The aim of the study was to evaluate if two capsules (Amoxil
®
capsules, 500 mg/capsule) and one tablet (Amoxicare
®
tablets, 1000 mg/tablet) of amoxicillin have similar bioequivalence parameters. For this purpose a randomized, two-way, crossover, bioequivalence study was performed in 24 healthy, male volunteers, divided into two groups of 12 subjects each. One group was treated with the reference standard (Amoxil
®
) and the other one with the generic tablet Amoxicare
®
, with a crossover after a wash-out period of 7 days. Blood samples were collected at fixed time intervals and amoxicillin was determined by a validated HPLC method. The pharmacokinetic parameters AUC
0-8
, AUC
0-͵
, C
max
, T
max
, K
e
and T
1/2
were determined for both formulations and statistically compared to evaluate the bioequivalence between the two brands of amoxicillin, using the statistical model recommended by the FDA. C
max
and AUC
0-͵
were statistically analyzed using analysis of variance (ANOVA); no statistically significant difference was observed between the two formulations. The 90% confidence intervals between the mean values of C
max
and AUC
0-͵
fall within the FDA specified bioequivalent limits (80-125%) suggesting that the two products are bioequivalent and the two formulations are interchangeable. Based on these findings it was concluded that the practice of interchangeability between the above formulations to achieve better patient compliance could be followed without compromising the extent of amoxicillin absorption.
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3,034
712
Molecular docking studies with rabies virus glycoprotein to design viral therapeutics
NR Tomar, V Singh, SS Marla, R Chandra, R Kumar, A Kumar
July-August 2010, 72(4):486-490
DOI
:10.4103/0250-474X.73905
PMID
:21218060
The genome of rabies virus encodes five proteins; the nucleoprotein, the phosphoprotein, the matrix protein, the glycoprotein, and the RNA-dependent RNA polymerase. Among these, the glycoprotein is the most important as it is the major contributor to pathogenicity and virus neutralizing antibody response. Keeping in mind that glycoprotein is the only protein exposed on the surface of virus and is thought to be responsible for the interaction with the cell membrane, it was attempted to target glycoprotein by a ligand polyethylene glycol 4000, which blocks its active site, as seen by molecular operating environment software, so that it may be possible to prevent the spread of virus into the host. The ligand polyethylene glycol 4000 was retrieved from Research Collaboratory for Structural Bioinformatics protein data bank by providing the glycoprotein sequence to the databank. In this study it was observed that the ligand was successfully docked on a major portion of antigenic site II of glycoprotein by mimicking the virus neutralizing antibodies. This knowledge may be important for the development of novel therapies for the treatment of rabies and other viral diseases in the future.
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180
SHORT COMMUNICATIONS
Triterpenoids from
Psidium guajava
with biocidal activity
P Ghosh, A Mandal, P Chakraborty, MG Rasul, Madhumita Chakraborty, A Saha
July-August 2010, 72(4):504-507
DOI
:10.4103/0250-474X.73936
PMID
:21218065
In continuation of our studies on the phytochemical investigation of medicinal plants available in the foothills of Darjeeling and Teri, we report herein the isolation of two triterpenoids betulinic acid and lupeol from the leaf extract of
Psidium guajava
and their potential antimicrobial and phytotoxic activities. All the structures of the isolated compounds were confirmed by spectral (IR, NMR) analysis and by comparison with the literature reports.
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1,329
96
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© 2006 - Indian Journal of Pharmaceutical Sciences | Published by
Medknow
Online since 20
th
April, 2006