RESEARCH PAPER
Year : 2013 | Volume : 75 | Issue : 1 | Page : 67-75
Improvement in Dissolution Rate of Cefuroxime Axetil by using Poloxamer 188 and
Neusilin US2
J Sruti1, Ch N Patra1, SK Swain1, S Beg1, HR Palatasingh1, SC Dinda2, M.E Bhanoji Rao1
1
Department of Pharmaceutics, Roland Institute of Pharmaceutical Sciences, Ambapua,
Khodasingi, Berhampur 760 010, India
2
School of Pharmaceutical Education and Research, Berhampur University, Bhanja Bihar,
Berhampur 760 007, India
Correspondence Address:
J Sruti
Department of Pharmaceutics, Roland Institute of Pharmaceutical Sciences, Ambapua,
Khodasingi, Berhampur 760 010
India
DOI: 10.4103/0250-474X.113551
PMID: 23901163
A combination of fusion and surface adsorption techniques was used to enhance the
dissolution rate of cefuroxime axetil. Solid dispersions of cefuroxime axetil were prepared
by two methods, namely fusion method using poloxamer 188 alone and combination of
poloxamer 188 and Neusilin US2 by fusion and surface adsorption method. Solid
dispersions were evaluated for solubility, phase solubility, flowability, compressibility,
Kawakita analysis, Fourier transform-infrared spectra, differential scanning
calorimetry, powder X-ray diffraction study, in vitro drug release, and stability study.
Solubility studies showed 12- and 14-fold increase in solubility for solid dispersions by
fusion method, and fusion and surface adsorption method, respectively. Phase solubility
studies showed negative values for poloxamer 188 at various concentrations (0, 0.25, 0.5,
0.75 and 1%) indicating spontaneous nature of solubilisation. Fourier transform-infrared
spectra and differential scanning calorimetry spectra showed that drug and excipients are
compatible with each other. Powder X-ray diffraction study studies indicated that presence
of Neusilin US2 is less likely to promote the reversion of the amorphous cefuroxime axetil
to crystalline state. In vitro dissolution studies, T50% and mean dissolution time have shown
better dissolution rate for solid dispersions by fusion and surface adsorption method.
Cefuroxime axetil release at 15 min (Q15) and DE15 exhibited 23- and 20-fold
improvement in dissolution rate. The optimized solid dispersion formulation was stable for 6
months of stability study as per ICH guidelines. The stability was ascertained from drug
content, in vitro dissolution, Fourier transform-infrared spectra and differential scanning
calorimetry study. Hence, this combined approach of fusion and surface adsorption can be
used successfully to improve the dissolution rate of poorly soluble biopharmaceutical
classification system class II drug cefuroxime axetil.
[FULL TEXT] [PDF]*
RESEARCH PAPER
Year : 2013 | Volume : 75 | Issue : 1 | Page : 83-88
Antiinflammatory, Analgesic and Antipyretic Activities of Aerial Parts of Costus speciosus
Koen
Shruti Srivastava1, P Singh1, KK Jha1, Garima Mishra1, S Srivastava1, RL Khosa2
1
Department of Pharmacognosy, Teerthanker Mahaveer College of Pharmacy, Teerthanker
Mahaveer University, Moradabad 244 001, India
2
Department of Pharmacy, Bharat Institute of Technology, Partapur Bypass, Delhi Road,
Meerut-250 103, India
Correspondence Address:
P Singh
Department of Pharmacognosy, Teerthanker Mahaveer College of Pharmacy, Teerthanker
Mahaveer University, Moradabad 244 001
India
DOI: 10.4103/0250-474X.113532
PMID: 23901165
In the present study, methanol extracts of Costus speciosus Koen. aerial parts were assessed
for antiinflammatory, analgesic and antipyretic activities in experimental animals. The
antiinflammatory activity of methanol extract of Costus speciosus (400 and 800 mg/kg, p.o.)
was evaluated using carrageenan-induced paw oedema test. 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 methanol extract of aerial parts of
Costus speciosus in a dose of 400 and 800 mg/kg showed significant antiinflammatory
activity (19.36 and 40.05% reduction) at 5 h postmedication. In analgesic models extract
treated animals at (400 and 800 mg/kg) inhibited writhing's caused by acetic acid by 14.24
and 31.90%, respectively, and it also increased the latency period at both high and low doses
which showed the mean reaction time at 16.60±0.355 s and 14.12±0.355 s, respectively,
when compared to control in hot-plate test. It also reduces the rectal temperature of the
animals at low and high doses significantly 37.03±0.108° and 36.63±0.098°, respectively, in
Brewer's yeast induced pyrexia. The obtained results of the present investigation revealed that
methanol extract of Costus speciosus has significant antiinflammatory, analgesic and
antipyretic activities.
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SHORT COMMUNICATION
Year : 2013 | Volume : 75 | Issue : 1 | Page : 122-125
Antimicrobial Activity and Phytochemical Constituents of Leaf Extracts of Cassia
auriculata
T Murugan1, J Albino Wins2, M Murugan3
1
Microbilogy Unit, Kamini Research Foundation, Thuckalay 629 175, India
2
Department of Biotechnology, Holy Cross College, Nagercoil 629 003, India
3
Department of Biomedical Engineering, Noorul Islam Centre for Higher Education,
Kumaracoil 629 180, India
Correspondence Address:
M Murugan
Department of Biomedical Engineering, Noorul Islam Centre for Higher Education,
Kumaracoil 629 180
India
DOI: 10.4103/0250-474X.113546
PMID: 23901174
Plants produce a wide variety of phytochemical constituents, which are secondary
metabolites and are used either directly or indirectly in the pharmaceutical industry. 'For
centuries, man has effectively used various components of plants or their extracts for the
treatment of many diseases, including bacterial infections. In the present study methanol,
chloroform and aqueous extracts of Cassia auriculata leaf were subjected for antimicrobial
activity by well-diffusion method against six bacterial strains namely Bacillus cereus,
Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa
and Proteus mirabilis. The results revealed that the methanol and chloroform extracts
exhibited strong inhibitory activity against all the tested organisms (zone of inhibition of 1220 mm), except Pseudomonas aeruginosa (zone of inhibition 10 mm or nil). The aqueous
extracts showed moderate activity by 'Zone of inhibition ≤12 or nil). The extracts were
screened for their phytochemical constituents by standard protocols' and were shown to
contain carbohydrates, proteins, alkaloids, flavonoids, steroids, saponins and tannins. The
antibacterial activity of these extracts is possibly linked to the presence of flavonoids,
steroid, saponins and/or tannins. Further studies are needed to determine the precise active
principles from Cassia auriculata.
IEW ARTICLE
Year : 2012 | Volume : 74 | Issue : 6 | Page : 487-497
Nitric oxide modulators: An emerging class of medicinal agents
SR Deshpande1, K Satyanarayana2, M. N. A. Rao3, KV Pai4
1
Department of Medicinal and Pharmaceutical Chemistry, HSK College of Pharmacy,
Bagalkote-587 101, India
2
Natco Research Center, Natco Pharma Ltd., Hyderabad-500 018, India
3
R and D Center, Divi's Laboratories Ltd., Hyderabad-500 016, India
4
Department of Industrial Chemistry, Kuvempu University, Shankaraghatta-577 451, India
Correspondence Address:
S R Deshpande
Department of Medicinal and Pharmaceutical Chemistry, HSK College of Pharmacy,
Bagalkote-587 101
India
PMID: 23798773
Nitric oxide, a unique messenger in biological system, is ubiquitously present virtually in all
tissues revealing its versatile nature of being involved in diverse physiological functions such
as vascular tone, inhibition of platelet aggregation, cell adhesion, neurotransmission and
enzyme and immune regulation. The tremendous advancements made in the past few decades
in this area suggests that the nitric oxide modulation either by its exogenous release through
nitric oxide donors or inhibition of its synthesis by nitric oxide synthase inhibitors in
physiological milieu may provide newer clinical strategies for the treatment of some diseases.
In this review, an attempt is made to document and understand the biological chemistry of
different classes of nitric oxide modulators that would prove to be a fruitful area in the years
to come.