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2008| November-December | Volume 70 | Issue 6
Online since
April 4, 2009
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REVIEW ARTICLES
Microbial production and biomedical applications of lovastatin
A Seenivasan, S Subhagar, R Aravindan, T Viruthagiri
November-December 2008, 70(6):701-709
DOI
:10.4103/0250-474X.49087
PMID
:21369428
Lovastatin is a potent hypercholesterolemic drug used for lowering blood cholesterol. Lovastatin acts by competitively inhibiting the enzyme, 3-hydroxy-3-methylglutaryl coenzyme A reductase involved in the biosynthesis of cholesterol. Commercially lovastatin is produced by a variety of filamentous fungi including
Penicillium
species,
Monascus ruber
and
Aspergillus terreus
as a secondary metabolite. Production of lovastatin by fermentation decreases the production cost compared to costs of chemical synthesis. In recent years, lovastatin has also been reported as a potential therapeutic agent for the treatment of various types of tumors and also play a tremendous role in the regulation of the inflammatory and immune response, coagulation process, bone turnover, neovascularization, vascular tone, and arterial pressure. This review deals with the structure, biosynthesis, various modes of fermentation and applications of lovastatin.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
5,583
808
1
Current status of the regulation for medical devices
Anuja R Shah, RK Goyal
November-December 2008, 70(6):695-700
DOI
:10.4103/0250-474X.49085
PMID
:21369427
In the light of escalating use of medical devices, stringent regulatory standards are required to ensure that the devices are safe, well studied and have least adverse reactions. Recently introduced guidelines and the amendment in the law will provide adequate guidance for both the manufacturers and competent authorities to manage cases efficiently and appropriately. India has emerged as one of the leaders in pharmaceutical industry. Like many other amendments in Drugs and Cosmetics Act that have boosted the global confidence in pharmaceutical industry in India, guidelines for devices will encourage the much needed research in medical devices. Pharmacy personnel can certainly play an important role in the regulation of medical devices. Safety, risks, effectiveness and performance of the medial devices need to be well established and regulated properly. It is hoped that the guidelines are implemented and regulated properly with effective outcome.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
4,538
829
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RESEARCH PAPERS
Stability indicating RP-HPLC estimation of atorvastatin calcium and amlodipine besylate in pharmaceutical formulations
DA Shah, KK Bhatt, RS Mehta, SL Baldania, TR Gandhi
November-December 2008, 70(6):754-760
DOI
:10.4103/0250-474X.49117
PMID
:21369436
A simple, specific, accurate and stability indicating reversed phase high performance liquid chromatographic method was developed for the simultaneous determination of atorvastatin calcium and amlodipine besylate in tablet dosage forms. A phenomenex Gemini C-18, 5 mm column having 250´4.6 mm i.d. in isocratic mode, with mobile phase containing 0.02 M potassium dihydrogen phosphate:acetonitrile:methanol (30:10:60, v/v/v) adjusted to pH 4 using ortho phosphoric acid was used. The flow rate was 1.0 ml/min and effluents were monitored at 240 nm. The retention times of atorvastatin calcium and amlodipine besylate were 11.6 min and 4.5 min, respectively. The calibration curves were linear in the concentration range of 0.08-20 µg/ml for atorvastatin calcium and 0.1-20 µg/ml for amlodipine besylate. Atorvastatin calcium and amlodipine besylate stock solutions were subjected to acid and alkali hydrolysis, chemical oxidation and dry heat degradation. The degraded product peaks were well resolved from the pure drug peak with significant difference in their retention time values. The proposed method was validated and successfully applied to the estimation of atorvastatin calcium and amlodipine besylate in combined tablet dosage forms.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
4,498
642
9
SHORT COMMUNICATIONS
Antifungal activity of plant extracts against
candida
species from oral lesions
K Prabhakar, L Sathish Kumar, S Rajendran, M Chandrasekaran, K Bhaskar, AK Sajit Khan
November-December 2008, 70(6):801-803
DOI
:10.4103/0250-474X.49128
PMID
:21369447
Seventy five patients with oral lesions attending the different departments of Rajah Muthiah Medical College and Hospital, Annamalai University were screened for
Candida
. Forty six (61.3%)
Candida
strains were isolated from the oral lesions. Of the 46
Candida
strains,
Candida albicans
accounted for 35 (76.08%),
Candida glabrata
for 5 (10.86%),
Candida tropicalis
and
Candida krusei
for 2 (4.34%) each and
Candida parapsilosis
and
Candida guilliermondii
for one (2.17%) each. Antifungal activity of ethanol extracts of five plant species that included
Syzygium jambolanum, Cassia siamea, Odina wodier, Momordica charantia
and
Melia azedarach
and two algal species,
Sargassum wightii
and
Caulerpa scalpelliformis
were tested against 25 isolated strains by disc diffusion method. Antifungal activity was observed at 100 mg/ml for
Syzygium jambolanum, Cassia siamea
and
Caulerpa scalpelliformis
and at 10 mg/ml for
Sargassum wightii
.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
3,619
488
2
RESEARCH PAPERS
Synthesis and activity evaluation of 2-(1-naphtho[2,1-
b
]furan-2-yl-carbonyl)-3,5-disubstituted-2,3-dihydro-1H-pyrazoles
MN Kumaraswamy, C Chandrashekhar, H Shivakumar, DA Prathima Mathias, KM Mahadevan, VP Vaidya
November-December 2008, 70(6):715-720
DOI
:10.4103/0250-474X.49090
PMID
:21369430
Ethyl naphtho[2,1-
b
]furan-2-carboxylate (2) on reaction with hydrazine hydrate in presence of acid catalyst in ethanol medium affords naphtho[2,1-b]furan-2-carbohydrazide (3). The reaction of substituted acetophenones (4a-c) with aromatic aldehydes (5a-e) produces chalcones (6a-o) via the Claisen condensation. The reaction of naphtho[2,1-
b
]furan-2-carbohydrazide (3) with chalcones (6a-6o) in presence of acetic acid as catalyst in dioxane produces 1-(naphtho[2,1-
b
]furan-2-yl-carbonyl)-3,5-disubstituted-2,3-dihydro-1H-pyrazoles (7a-o). The structures of newly synthesized compounds have been established by elemental analysis and spectral studies. The compounds 7a-o have been evaluated for their antimicrobial activity and some selected compounds evaluated for antiinflammatory, analgesic, anthelmintic, diuretic and antipyretic activities.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
3,111
681
-
Formulation development and
in vitro
characterization of proliposomes for topical Delivery of aceclofenac
Vandana Gupta, Ashok K Barupal, Suman Ramteke
November-December 2008, 70(6):768-775
DOI
:10.4103/0250-474X.49119
PMID
:21369438
Non-steroidal antiinflammatory drugs are routinely prescribed for the patients with rheumatic disease and such patients are at increased risk of serious gastrointestinal complications, when non-steroidal antiinflammatory drugs administered by oral route. The aim of the present study was to develop and characterized a vesicular drug carrier system (proliposome) for topical delivery of aceclofenac to overcome the problems related with oral route. Aceclofenac proliposome were prepared by the film-deposition on carriers method and characterized for size and surface morphology, drug content in both proliposomes and liposomal system, percent yield,
in vitro
drug release studies and drug permeation studies. The prepared system was also characterized for drug-excipients interaction by Fourier transform infrared spectrophotometer and stability studies. The size and surface morphology were studied using optical microscopy, scanning electron microscopy and transmission electron microscopy. A spherical shape of reconstituted aceclofenac liposome with an average vesicular size of about 500 nm was observed in photomicrographs. The maximum entrapment efficiency of reconstituted liposomes was 80.31% whereas the drug content in proliposomes was found to be more than 90%.
In vitro
release of drug was significantly retarded indicating sustained release of aceclofenac from proliposomes. Stability study was performed at various temperatures indicating that aceclofenac proliposomes are stable at lower temperature.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
2,939
719
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SHORT COMMUNICATIONS
Design and evaluation of fast dissolving tablets of clonazepam
SB Shirsand, Sarasija Suresh, PV Swamy, D Nagendra Kumar, MV Rampure
November-December 2008, 70(6):791-795
DOI
:10.4103/0250-474X.49125
PMID
:21369444
In the present work, fast dissolving tablets of clonazepam were prepared by direct compression method with a view to enhance patient compliance. Three super-disintegrants, viz., crospovidone, croscarmellose sodium and sodium starch glycolate in different ratios with microcrystalline cellulose (Avicel PH-102) along with directly compressible mannitol (Pearlitol SD 200) to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity, wetting time, water absorption ratio and
in vitro
dispersion time. Based on
in vitro
dispersion time (approximately 13 s), three formulations were tested for the
in vitro
drug release pattern (in pH 6.8 phosphate buffer), short-term stability (at 40º/75% relative humidity for 6 mo) and drug-excipient interaction (IR spectroscopy). Among the three promising formulations, the formulation prepared by using 10% w/w of crospovidone and 35% w/w of microcrystalline cellulose emerged as the overall best formulation (t
50%
1.8 min) based on the
in vitro
drug release characteristics compared to conventional commercial tablet formulation (t
50%
16.4 min). Short-term stability studies on the formulations indicated that there were no significant changes in drug content and
in vitro
dispersion time (
P
<0.05).
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,710
792
2
Antioxidant and antiinflammatory activity of
Vitex negundo
RR Kulkarni, AD Virkar, Priscilla D'Mello
November-December 2008, 70(6):838-840
DOI
:10.4103/0250-474X.49140
PMID
:21369459
Reactive oxygen species are implicated in various inflammatory disorders.
Vitex negundo
is mentioned in Ayurveda as useful in treating arthritic disorders. The present work was undertaken to evaluate the antioxidant potential and anti-inflammatory activity of the plant. The total methanol extract of the plant was standardized in terms of total polyphenols. The standardized extract in a dose of 100 mg/kg caused a comparable reduction in edema with that of diclofenac sodium (25 mg/kg) when evaluated for antiinflammatory activity by carrageenan-induced rat paw edema method. The extract also exhibited a strong free radical scavenging activity by 1,1-diphenyl-2-picrylhydrazyl method and caused a significant reduction in the formation of thiobarbituric acid reacting substances when evaluated for its lipid peroxidation inhibitory activity. The results strongly suggest that radical quenching may be one of the mechanisms responsible for its antiinflammatory activity.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,824
600
3
Estimation of duloxetine hydrochloride in pharmaceutical formulations by RP-HPLC method
Sejal K Patel, NJ Patel, KM Patel, PU Patel, BH Patel
November-December 2008, 70(6):825-827
DOI
:10.4103/0250-474X.49136
PMID
:21369455
Simple, specific, accurate and precise method, namely, reverse phase high performance liquid chromatography was developed for estimation of duloxetine HCl in pharmaceutical formulations. For the high performance liquid chromatography method, Phenomenox C-18, 5 µm column consisting of 250×4.6 mm i.d. in isocratic mode, with mobile phase containing 0.01M 5.5 pH phosphate buffer: acetonitrile (60:40 v/v) and final pH adjust to 5.5±0.02 with phosphoric acid was used. The flow rate was 1.2 ml/min and effluent was monitored at 231 nm. The retention time was 5.61 min. The method was validated in terms of linearity, accuracy and precision. The linearity curve was found to be linear over 0.25-4 µg/ml. The limit of detection and limit of quantification were found to be 0.10 and 0.25 µg/ml respectively. The proposed method was successfully used to determine the drug content of marketed formulations.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,866
375
2
A reverse phase HPLC-UV and HPTLC methods for determination of plumbagin in
Plumbago indica
and
Plumbago zeylanica
KP Unnikrishnan, S Sudhakar Raja, Indira Balachandran
November-December 2008, 70(6):844-847
DOI
:10.4103/0250-474X.49142
PMID
:21369461
A reverse phase HPLC method with UV detection has been developed and validated in order to quantify plumbagin, the bioactive marker of the roots of
P. indica
and
P. zeylanica
. A quantitative HPTLC method was also developed using hexane: ethyl acetate (8:2) as the mobile phase. The plumbagin content in the roots were determined using both the methods.
P. indica
was found to contain significantly higher amount of plumbagin than
P. zeylanica
. The HPLC and HPTLC methods described here are simple, rapid, accurate and sensitive.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,636
563
1
Antidiabetic activity of
clerodendron phlomoidis
leaf extract in alloxan-induced diabetic rats
SP Dhanabal, MK Mohan Marugaraja, B Suresh
November-December 2008, 70(6):841-844
DOI
:10.4103/0250-474X.49141
PMID
:21369460
Ethanol extract of leaves of
Clerodendron phlomoidis
L. subjected to preliminary qualitative phytochemical investigations showed the presence of alkaloids, phytosterols, glycosides, saponins, phenolic compounds, proteins and flavonoids. The extract was screened for hypoglycemic activity in alloxan-induced diabetic rats (120 mg/kg, i.p.) at two dose levels, viz., 100 and 200 mg/kg. The ethanol extract at 200 mg/kg dose level exhibited significant (
p
<0.05) hypoglycemic activity and also correction of altered biochemical parameters viz., cholesterol and triglycerides (
p
<0.05).
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,498
598
2
RESEARCH PAPERS
Evaluation of hydrophobic nanoparticulate delivery system for insulin
PS Singnurkar, SK Gidwani
November-December 2008, 70(6):721-726
DOI
:10.4103/0250-474X.49091
PMID
:21369431
Insulin loaded hydrophobic nanoparticles were prepared by solvent diffusion followed by lyophilization. Nanoparticles were characterized for mean size by dynamic laser scattering and for shape by scanning electron microscopy. Insulin encapsulation efficiency,
in vitro
stability of nanoparticles in presence of proteolytic enzymes and
in vitro
release were determined by high pressure liquid chromatography analysis. The biological activity insulin from the nanopraticles was estimated by enzyme-linked immunosorbant assay and
in vivo
using Wister diabetic rats. Nanoparticles ranged 0.526±0.071 µm in diameter. Insulin encapsulation efficiency was 95.7±1.2%. Insulin hydrophobic nanoparticles suppressed insulin release promoted sustained release in pH 7.4 phosphate buffer and shown to protect insulin from enzymatic degradation
in vitro
in presence of chymotripsin. Nanoencapsulated insulin was bioactive, demonstrated through both in vivo and
in vitro
.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
2,334
489
-
SHORT COMMUNICATIONS
Antimicrobial activity of
Acanthus ilicifolius
(L.)
S Bose, Arti Bose
November-December 2008, 70(6):821-823
DOI
:10.4103/0250-474X.49134
PMID
:21369453
The antimicrobial activity of alcoholic, butanolic and chloroform extracts of leaves and roots of the plant
Acanthus ilicifolius
ware studied. Ampicillin and clotrimazole were used as standard antibacterial and antifungal agents respectively. The result of the study revealed that the alcoholic extract and chloroform extract of leaves exhibited strong inhibitory action against
Bacillus subtilis, Staphylococcus aureus, Candida albicans, Aspergillus fumigatus
and
Aspergillus niger
and moderate inhibitory action against
Pseudomonas aeruginosa
and
Proteus vulgaris.
The rest of the extracts showed moderate activity.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,261
531
5
Study of the soil isolates for antimicrobial activity
AR Srividya, GS Saritha, B Suresh
November-December 2008, 70(6):812-815
DOI
:10.4103/0250-474X.49132
PMID
:21369451
During the process of screening for a potent antimicrobial compound, a new strain was isolated from the soil sample of Thalaikunda village in Ooty, Tamil Nadu. That organism was name as NK
2
. It was found to be antagonistic to both bacterial and fungal test organisms. Production of antibiotic was more in a newly formulated broth. Antibiotic production reached maximum at the end of the 70 h of fermentation by stirred flask culture. The antimicrobial compound was extracted in
n
-butanol, ethyl acetate and methanol. Antimicrobial compound, which was produced by the soil isolate NK
2
did not showed cytotoxic activity on Vero cell lines.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
2,411
323
-
REVIEW ARTICLES
Treatment of onychomycosis: An update
AA Shirwaikar, T Thomas, A Shirwaikar, R Lobo, KS Prabhu
November-December 2008, 70(6):710-714
DOI
:10.4103/0250-474X.49088
PMID
:21369429
Fungal infections of skin are one of the most common infections in human beings. The areas which are likely to get infected include the scalp, the hands and the feet. Dermatophytes, yeasts and moulds are the three major fungi responsible for skin infections. Earlier oral antifungal agents were used for treatment of fungal infection in finger and toe nails. The disadvantages of oral antifungal agents are toxicity and longer treatment period. Now medicated nail lacquers have been developed for the treatment of fungal infections i.e. onychomycosis, which has less toxicity and shorter treatment period.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
2,393
318
-
RESEARCH PAPERS
Pharmacological evaluation of bioactive principle of
Turnera aphrodisiaca
S Kumar, R Madaan, A Sharma
November-December 2008, 70(6):740-744
DOI
:10.4103/0250-474X.49095
PMID
:21369434
In the present investigation, pharmacological evaluation of apigenin, a bioactive principle of
Turnera aphrodisiaca
Ward (Turneraceae) was carried out. Apigenin was evaluated for antianxiety activity at a dose of 2 mg/kg using well established models of anxiety, the hole board test, light/dark test and mirrored chamber test. Apigenin significantly increased head dipping in hole board test. Further, apigenin increased latency to leave light zone and the time spent in light compartment of light/dark model of anxiety. Apigenin also decreased the latency time to enter the mirrored chamber, and increased the total time spent/number of entries in the mirrored chamber with respect to control. All these observations confirmed the anxiolytic activity of apigenin. At a higher dose (about 12 fold the anxiolytic dose), apigenin showed mild sedative activity in actophotometer as it decreased activity scores. It (2, 5 or 10 mg/kg) was found to be devoid of anticonvulsant, antidepressant and antistress activity in MES-induced convulsion test, despair swim test and cold swimming endurance test, respectively. In tail immersion test for six hours, apigenin exhibited excellent dose dependent analgesic activity, which was comparable to that of morphine sulphate (5 mg/kg). Maximum activity was observed 30 min after the administration of 10 mg/kg dose of apigenin.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,220
467
1
In situ
formed phase transited drug delivery system of ketoprofen for achieving osmotic, controlled and level a
in vitro
in vivo
correlation
AK Philip, Kamla Pathak
November-December 2008, 70(6):745-753
DOI
:10.4103/0250-474X.49096
PMID
:21369435
A dry process induced phase transited, non disintegrating, controlled release,
in situ
formed asymmetric membrane capsular system for poorly water soluble drug, ketoprofen, was developed and evaluated both
in vitro
and
in vivo
for osmotic and controlled release of the drug.
In situ
formed asymmetric membrane capsules were prepared using fabricated glass capsule holders via dry, phase inversion process. Effect of varying osmotic pressure of the dissolution medium on drug release was studied. Membrane characterization by scanning electron microscopy showed an outer dense region with less pores and an inner porous region for the prepared asymmetric membrane.
In vitro
release studies and statistical test for all the prepared and marketed formulation were done at
P
>0.05. The drug release was found to be independent of the pH, but dependent on the osmotic pressure of the dissolution medium.
In vivo
pharmacokinetic studies showed a level A correlation (R
2
>0.99) with 39.24 % relative bioavailability compared to immediate release tablet of ketoprofen. Excellent correlation achieved suggested that the
in vivo
performance of the phase transited
in situ
formed AMCs could be accurately predicted from their
in vitro
release profiles and could a means for controlled delivery of drugs with varying solubility.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,191
452
5
Evidences for the involvement of monoaminergic and GABAergic systems in antidepressant-like activity of
Tinospora cordifolia
in mice
D Dhingra, PK Goyal
November-December 2008, 70(6):761-767
DOI
:10.4103/0250-474X.49118
PMID
:21369437
The present study was taken up to investigate the effect of petroleum ether extract of
Tinospora cordifolia
(Wild.) Miers, on depression in mice. The extract (50, 100 and 200 mg/kg, p.o.) was administered for 14 successive days to Swiss young albino mice (either sex) and evaluated for antidepressant-like activity using tail suspension test and forced swim test. Petroleum ether extract at all three doses produced significant antidepressant-like effect in tail suspension test as well as in forced swim test and their efficacies were found to be comparable to imipramine (15 mg/kg, p.o.) and sertraline (20 mg/kg, p.o.). The extract at a dose of 50 mg/kg showed most potent effect and did not show any significant change in locomotor functions of mice as compared to control. The antidepressant-like effect of the extract was significantly reversed by pretreatment of animals with prazosin (a α
1
-adrenoceptor antagonist), sulpiride (a selective dopamine D
2
-receptor antagonist), p-CPA (a serotonin synthesis inhibitor) and baclofen (GABA-B agonist), when tested in tail suspension test. Moreover, petroleum ether extract also reduced the mouse whole brain monoamine oxidase (MAO-A and MAO-B) activities as compared to control, resulting in increase in the levels of brain monoamines. Therefore, the extract may have potential therapeutic value for the management of depressive disorders.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
2,172
417
-
Insulin-egg yolk dispersions in self microemulsifying system
PS Singnurkar, SK Gidwani
November-December 2008, 70(6):727-732
DOI
:10.4103/0250-474X.49092
PMID
:21369432
Formulation of insulin into a microemulsion very often presents a physicochemical instability during their preparation and storage. In order to overcome this lack of stability and facilitate the handling of these colloidal systems, stabilization of insulin in presence of hydrophobic components of a microemulsion appears as the most promising strategy. The present paper reports the use of egg yolk for stabilization of insulin in self microemulsifying dispersions. Insulin loaded egg yolk self microemulsifying dispersions were prepared by lyophilization followed by dispersion into self microemulsifying vehicle. The physicochemical characterization of selfmicroemulsifying dispersions includes such as insulin encapsulation efficiency,
in vitro
stability of insulin in presence of proteolytic enzymes and
in vitro
release. The biological activity of insulin from the dispersion was estimated by enzyme-linked immunosorbant assay and
in vivo
using Wistar diabetic rats. The particle size ranged 1.023±0.316 µm in diameter and insulin encapsulation efficiency was 98.2±0.9 %. Insulin hydrophobic self microemulsifying dispersions suppressed insulin release in pH 7.4 phosphate buffer and shown to protect insulin from enzymatic degradation
in vitro
in presence of chymotripsin. Egg yolk encapsulated insulin was bioactive, demonstrated through both
in vivo
and
in vitro
.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
2,233
335
-
A novel metered dose transdermal spray formulation for oxybutynin
A Bakshi, A Bajaj, G Malhotra, M Madan, N Amrutiya
November-December 2008, 70(6):733-739
DOI
:10.4103/0250-474X.49094
PMID
:21369433
The objective of the present work was to develop a metered dose spray formulation for transdermal delivery of oxybutynin and to carry out the in vitro characterization of the optimized formulation. Oxybutynin release from a series of ethanol/acetone/methylal based formulations was assessed
in vitro
and the developed formulation was used for delivery from a metered dose spray. Various qualitative and quantitative parameters like spray pattern, particle size distribution, pH, evaporation time, pump seal efficiency test, average weight per metered dose, content per spray and content uniformity were evaluated. The different film forming agents were assessed and carbopol (0.5%) and lutrol (0.1%) were found to give good clarity of solution, evaporation rate, spray pattern and tackiness of the film. Diffusion studies of the optimized formulations through the semipermeable membrane showed the release of drug to the extent of almost 50% over a period of 24 h. Stability studies were conducted as per ICH guidelines and indicated that formulations were stable. Skin irritation studies were performed using rabbit as an animal model. The results obtained show that the metered dose transdermal spray formulation can be a promising and innovative therapeutic system for the transdermal administration of oxybutynin.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,159
393
2
SHORT COMMUNICATIONS
Design, synthesis and antiHIV activity of novel isatine-sulphonamides
N Murugesh, M Chandramohan, Z Debyser, M Witvrouw, P Selvam
November-December 2008, 70(6):779-782
DOI
:10.4103/0250-474X.49121
PMID
:21369440
A series of novel isatine-sulphonamide derivatives have been synthesized by combining isatin derivatives with sulphonamides. The structure of the synthesized compounds were elucidated by spectral analysis (IR, NMR and Mass). Investigation of anti-HIV activity was done against HIV-1(IIIB) in MT-4 cells and HIV integrase inhibitory activity. 4-(1-acetyl-5-methyl-2-oxoindolin-3-ylideneamino)-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide (SPIII-5ME-AC) inhibits the HIV Integrase enzymatic activity as both over all and strand transfer reaction and 4-(1-benzoyl-5-chloro-2-oxoindolin-3-ylideneamino)-N-(4,6-dimethylpyrimidin-2-yl)benzene sulfonamide (SPIII-5Cl-BZ) exhibits 36 percent maximum protection against HIV-1 at sub toxic concentration.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,200
345
1
Spectrofluorimetric estimation of scopoletin in
Evolvulus alsinoides
linn. and
Convulvulus pluricaulis
choisy.
A Nahata, VK Dixit
November-December 2008, 70(6):834-837
DOI
:10.4103/0250-474X.49139
PMID
:21369458
A simple sensitive spectrofluorimetric method was developed for the analysis of total coumarins calculated as scopoletin in the plants
Evolvulus alsinoides
and
Convulvulus pluricaulis
. The fluorescent nature of scopoletin proved to be of immense value in the development of the spectrofluorimetric method. The excitation and emission wavelengths for scopoletin were 430 nm and 460 nm respectively and the instrument was Shimadzu RF 5301 PC spectrofluorophotometer. The method was validated in terms of linearity, accuracy and precision. The proposed spectrofluorimetric method provides a faster and cost effective qualitative and quantitative control for routine analysis of scopoletin in
Evolvulus alsinoides
and
Convulvulus pluricaulis
and their formulations.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,130
294
5
Antiinflammatory activity of a polyherbal formulation
SR Deorukhakar, A Dethe, RR Vohra, R Ghosh, J Chaudhary, V Kadam
November-December 2008, 70(6):785-787
DOI
:10.4103/0250-474X.49123
PMID
:21369442
The antiinflammatory activity of the polyherbal formulation Entox
®
was investigated in rats for acute and sub acute models of inflammation using carrageenan-induced rat paw edema and cotton pellet granuloma methods respectively at a dose of 300 mg/kg and 600 mg/kg administered orally. The formulation in doses of 300 mg/kg and 600 mg/kg showed 51.61% and 54.84% inhibition of paw edema, respectively at the end of 3 h. The percent inhibition of granuloma by cotton pellet method was 27.92% and 53.17%, respectively. The formulation showed a significant antiinflammatory activity in both the experimental models and the activity was comparable to that of the standard drug, indomethacin.
[ABSTRACT]
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[PubMed]
1,840
577
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Formulation and evaluation of gelatin micropellets of aceclofenac: Effect of process variables on encapsulation efficiency, particle size and drug release
SK Sahoo, MK Jena, S Dhala, BB Barik
November-December 2008, 70(6):795-798
DOI
:10.4103/0250-474X.49126
PMID
:21369445
In the present study aceclofenac-gelatin micropellets were prepared by the cross linking technique using gluteraldehyde as cross linking agent and characterized by X-ray diffractometry, differential scanning calorimetry and scanning electron microscopy. The effect of drug: polymer ratio, temperature of oil phase, amount of gluteraldehyde and stirring time was studied with respect to entrapment efficiency, micropellet size and drug release characteristics. Spherical micropellets having an entrapment efficiency of 57% to 97% were obtained. Differential scanning calorimetric analysis confirmed the absence of any drug-polymer interaction. The micromeritic studies of micropellets show improved flow property. The entrapment efficiency, micropellet size and drug release profile was altered significantly by changing various processing parameters.
[ABSTRACT]
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[CITATIONS]
[PubMed]
1,817
519
1
Evaluation of CNS depressant activity of different plant parts of
Nyctanthes arbortristis
linn.
Sanjita Das, D Sasmal, SP Basu
November-December 2008, 70(6):803-806
DOI
:10.4103/0250-474X.49129
PMID
:21369448
The present study was carried out with the water-soluble portion of the ethanol extracts of flowers, barks, seeds and leaves of
Nyctanthes arbortristis
Linn. to confirm their CNS depressant activity. The ethanol extracts of the plant parts were obtained by soxhlet extraction. After performing the gross behavioral study, the CNS depressant activity was evaluated by observing the prolongation of sleeping time induced by pentobarbital sodium in mice. Attempts have been made to explore the possible mechanism behind this activity by determining their effect on brain monoamine neurotransmitters like dopamine and serotonin. The gross behavioral study showed that ethanol extracts of the leaves, flowers and seeds possess significant CNS depressant activity. The leaves, flowers, seeds and barks (600 mg/kg) showed significant and dose-dependent prolongation of onset and duration of sleep and so found to cause decrease dopamine and increase serotonin level. From which it can be concluded that the CNS depressant activity of the ethanol extracts of seeds, leaves and flowers may be due to the decrease in dopamine and increase in serotonin level.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
1,948
378
2
Flow of formulation granules through a conical hopper
B Mazumder, R Rajan, Jasmina Khanam, A Nanda
November-December 2008, 70(6):816-821
DOI
:10.4103/0250-474X.49133
PMID
:21369452
Gravity flow characteristics of various pharmaceutical granules through static conical hoppers of different cone angles were studied. Mass flow rate depends on properties of granules and cone angles when environmental conditions such as temperature and relative humidity are kept within a fixed range. The granules were made with active pharmaceutical ingredients as per Indian pharmacopoeia with other additives like binders and diluents. Lubricants were added with the granules to observe their effects on mass flow rate. Magnesium stearate and colloidal silicon dioxide of different proportions were used as lubricants after granulation. A new dimensionally analyzed equation was developed to predict flow rate of the granules. The developed equation agreed well with the experimental data with a percentage deviation of ±10%.
[ABSTRACT]
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[PubMed]
2,070
177
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pH-Induced
in situ
gel for periodontal anesthesia
H Gupta, RM Singh, GN Singh, D Kaushik, A Sharma
November-December 2008, 70(6):776-778
DOI
:10.4103/0250-474X.49120
PMID
:21369439
A pH mediated
in situ
gelling system was developed using prilocaine hydrochloride for periodontal anesthesia using combination of chitosan and hydroxypropylmethylcellulose. The gel so developed can be used as anaesthetic in lengthy dental surgery. The gel was evaluated for many parameters like gelation pH, viscosity, physicochemical properties,
in vitro
release, sterility and stability. Gel with chitosan (0.25% w/v) and hydroxypropylmethylcellulose (0.25% w/v) was found to have good gelation near pH 7.4 (pH of mucous) with prolonged action.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
1,760
328
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Analysis of bulk sample of salicylic acid by application of hydrotropic solubilization method
RK Maheshwari, V Chavada, S Varghese, K Shahoo
November-December 2008, 70(6):823-825
DOI
:10.4103/0250-474X.49135
PMID
:21369454
In the present investigation, the poorly water-soluble drug, salicylic acid has been solubilized using 0.5 M ibuprofen sodium and 2.0 M sodium salicylate solution as hydrotropic agents for the titrimetric analysis precluding the use of organic solvents. Both hydrotropes are economic and pollution-free. The mean percent estimation of salicylic acid estimated in bulk sample by Indian Pharmacopoeial method is 98.78%. The mean percent estimation by ibuprofen sodium method and sodium salicylate method are 99.25% and 98.82%, respectively. The results of analysis by the proposed method are very close to the results of analysis by the standard method. This confirms the accuracy of the proposed method. The proposed method was validated statistically by low values of statistical parameters viz. standard deviation, percent coefficient of variation and standard error. The proposed method is new, accurate, simple and economic.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
1,685
304
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Fingerprinting of plumbagin in
Drosera burmannii
vahl using high performance thin layer chromatography
V Madhavan, Hema Basnett, A Cendil Kumar, SN Yoganarasimhan
November-December 2008, 70(6):798-800
DOI
:10.4103/0250-474X.49127
PMID
:21369446
HPTLC fingerprinting profile of the alcohol and aqueous extracts of
Drosera burmannii
is described. Seven components have been detected in the alcohol extract. Further, plumbagin, an useful antifertility agent, was also detected by comparison with the reference standard. The aqueous extract revealed two spots with no spot corresponding to plumbagin.
[ABSTRACT]
[FULL TEXT]
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[CITATIONS]
[PubMed]
1,601
333
1
In vitro
evaluation of
Eclipta alba
against serogroups of
Leptospira interrogans
N Prabhu, Joseph Pushpa Innocent, P Chinnaswamy, K Natarajaseenivasan, Lakshmi Sarayu
November-December 2008, 70(6):788-791
DOI
:10.4103/0250-474X.49124
PMID
:21369443
Leptospirosis is now acknowledged as the most widespread zoonoses in the world. Hundreds of cases occur in India every year accounting for considerable morbidity and sizable mortality. Several studies have delineated the epidemiology, pathology and variable clinical features of this condition. The present study comprises the importance and utilization of traditional based medicines to overcome the adverse reaction by conventional drugs and standardize the technology. The antileptospiral activity of
Eclipta alba
L. was well studied by both tube dilution and micro dilution techniques and the result showed better inhibitory action against various serogroups of
Leptospira interrogans. L. australis, L. autumnalis
and
L. grippotyphosa
are inhibited by both water and ethanol extract by tube dilution technique. The MIC level observed are 50 µg and 100 µg respectively. Similarly acetone extract, Icterohaemorrhagiae was responded to 200 µg/ml as MIC whereas in petroleum ether extract, no inhibition was observed. In the case of micro dilution technique, the entire inhibition rates are supported to the tube dilution technique. It showed that the micro dilution technique is the best method where we obtained the results within 30 minutes; at the same time tube dilution technique takes minimum of 7 days to provide the result.
[ABSTRACT]
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[PubMed]
1,690
219
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Effect of
Withania somnifera
on sleep-wake cycle in sleep-disturbed rats: Possible GABAergic mechanism
A Kumar, H Kalonia
November-December 2008, 70(6):806-810
DOI
:10.4103/0250-474X.49130
PMID
:21369449
Sleep deprivation disrupts significantly sleep pattern and cause poor quality of sleep. The aim the present study was to explore role of
Withania somniferra
root extract in sleep-disturbed rats. Male wistar rats (n=5-6/group) were sleep deprived for 24 h using grid suspended over water method.
Withania somniferra
extract (100 mg/kg) was administered intraperitoneally (i.p.) 30 min before actual recording (EEG and EMG) recording and electrophysiological recordings are further classified as- sleep latency, slow wave sleep, paradoxical sleep, total sleep, wakefulness. One day (24 h) sleep deprivation delayed latency sleep, reduced duration of slow wave sleep, rapid eye movement sleep, total sleep time and increased total waking as compared to animals placed on saw dust (P<0.05). Pretreatment with
Withania somniferra
extract (100 mg/kg) and diazepam (0.5 mg/kg) significantly improved electrophysiological parameters, which was further reversed by picrotoxin (2 mg/kg) and potentiated by muscimol (0.05 mg/kg). Flumazenil (2 mg/kg) did not produce any significant effect on the sleep parameters of
Withania somnifera
root extract. Present study suggests the involvement of GABAergic mechanism in the sleep promoting effect of
Withania somniferra
in sleep-disturbed state.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
1,631
228
2
Development and validation of a HPTLC method for the estimation of sumatriptan in tablet dosage forms
CR Shah, BN Suhagia, NJ Shah, RR Shah
November-December 2008, 70(6):831-834
DOI
:10.4103/0250-474X.49138
PMID
:21369457
A simple, precise, accurate and rapid high performance thin layer chromatographic method has been developed and validated for the estimation of sumatriptan in tablet dosage forms. The stationary phase used was precoated silica gel 60F254. The mobile phase used was a mixture of methanol:water:glacial acetic acid (4.0:8.0:0.1, v/v/v). The detection of spots was carried out at 230 nm. The method was validated in terms of linearity, accuracy, precision and specificity. The calibration curve was found to be linear between 200 to 800 ng/spot. The limit of detection and the limit of quantification for the sumatriptan were found to be 63.87 and 193.54 ng/spot, respectively. The proposed method can be successfully used to determine the drug content of marketed formulation.
[ABSTRACT]
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[CITATIONS]
[PubMed]
1,507
351
4
Spectrophotometric estimation of bicalutamide in tablets
PP Sancheti, VM Vyas, Manali Shah, Poonam Karekar, YV Pore
November-December 2008, 70(6):810-812
DOI
:10.4103/0250-474X.49131
PMID
:21369450
A simple, sensitive, rapid, accurate and precise spectrophotometric method has been developed for the estimation of bicalutamide in bulk and pharmaceutical dosage forms. Bicalutamide shows maximum absorbance at 272 nm with molar absorptivity of 2.3399×10
4
l/mol/cm. Beer's law was obeyed in the concentration range of 1.5-18 µg/ml. The limit of detection and limit of quantification were found to be 0.1 and 0.4 µg/ml, respectively. Results of analysis were validated statistically and by recovery studies.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
1,472
334
1
Estimation of apigenin, an anxiolytic constituent, in
Turnera aphrodisiaca
S Kumar, R Madaan, A Sharma
November-December 2008, 70(6):847-851
DOI
:10.4103/0250-474X.49143
PMID
:21369462
An HPTLC densitometric method has been developed to estimate apigenin in
Turnera aphrodisiaca
aerial and its segregated parts (leaves, stems, flowers and fruits) so that plant can be standardized on the basis of its bioactive marker. The apigenin content in methanol extract of
T. aphrodisiaca
aerial parts was found to be about fourteen times less than acid hydrolyzed methanol extract of the plant indicating the presence of most of apigenin in glycosidic form. Amongst different plant parts, flowers possessed maximum content of apigenin followed by leaves. The apigenin content was also determined in three marketed formulations of
T. aphrodisiaca
viz., NLK, DWSG and SBL. DWSG contained higher content of apigenin. Aerial parts of the plant were collected at bimonthly intervals over a period of one year in the months of January, March, May, July, September and November. The plant material collected in September showed maximum content of apigenin.
[ABSTRACT]
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[CITATIONS]
[PubMed]
1,490
243
1
Amitriptyline pharmacokinetics in experimental spinal cord injury in the rabbit
H Reihanikermani, M Ansari, A Soltani, MS Meymandi
November-December 2008, 70(6):782-785
DOI
:10.4103/0250-474X.49122
PMID
:21369441
Previous studies have demonstrated that pharmacokinetic behavior of several drugs such as paracetamol, theophylline, and aminoglycosides are significantly altered in spinal cord injured patients. No pharmacokinetic study of amitriptyline has been performed in patients and experimental models of spinal cord injury. Pharmacokinetic parameters of amitriptyline in orally treated rabbits subjected to laminectomy and spinal cord injury compared with those underwent laminectomy alone. Among twenty four male rabbits were included in this study, nine of them subjected to spinal cord injury at the 8
th
thoracic level by knife severance method and six rabbits underwent laminectomy alone (sham group) and nine rabbits treated as control. All received a single oral dose of amitriptyline (20 mg/kg) 24 h after injury. Blood sampling were done at predetermined times to 36 h after drug administration. Amitriptyline concentration in serum samples was determined by high-performance liquid chromatography. Pharmacokinetic parameters including maximum concentration (C
max
), time to reach maximum concentration (T
max
), half life, and the area under the curve to last detectable concentration time point (AUC
0-t
) were directly determined from the concentration-time curve. Maximum concentration was observed at 6.5 h after administration in sham group with a concentration of 439.6 ng/ml, whereas in SCI group T
max
was at 2.7 h with a concentration of 2763.9 ng/ml. In control group it was 3.3 h and 396 ng/ml, respectively. In SCI group, AUC was 9465.6 ng.h/ml and half life was 6 h and for control group it was 2817.4 ng.h/ml and 6.4 h, respectively. Statistical analysis of data showed that SCI didn't induce significant changes in amitriptyline pharmacokinetic parameters.
[ABSTRACT]
[FULL TEXT]
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[CITATIONS]
[PubMed]
1,342
147
1
Synthesis and biological evaluation of delavayin-C
Nirmala V Shinde, M Himaja, SK Bhosale, MV Ramana, DM Sakarkar
November-December 2008, 70(6):827-831
DOI
:10.4103/0250-474X.49137
PMID
:21369456
The synthesis of a cyclic heptapeptide, delavayin-C, cyclo(gly-tyr-tyr-tyr-pro-val-pro) is described. The structure of this compound was established on the basis of analytical IR,
1
H NMR and FAB mass spectral data. The antibacterial and antifungal activities of this peptide are also described.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
1,259
146
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© 2006 - Indian Journal of Pharmaceutical Sciences | Published by
Medknow
Online since 20
th
April, 2006