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Table of Contents
January-March 2014
Volume 5 | Issue 1
Page Nos. 1-58
Online since Thursday, February 13, 2014
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EDITORIAL
Nanomedicine: Revolutionary trends in drug delivery and diagnostics
p. 1
Upendra Nagaich
DOI
:10.4103/2231-4040.126977
PMID
:24695465
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GUEST EDITORIAL
Pharmacovigilance: Curriculum and career
p. 2
Bhaswat S Chakraborty
DOI
:10.4103/2231-4040.126978
PMID
:24696810
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REVIEW ARTICLE
Bhasma
: The ancient Indian nanomedicine
p. 4
Dilipkumar Pal, Chandan Kumar Sahu, Arindam Haldar
DOI
:10.4103/2231-4040.126980
PMID
:24696811
Ayurveda and other Indian system of medicine use metals, but their use is also amply described in Chinese and Egyptian civilization in 2500 B.C.
Bhasma
are unique ayurvedic metallic/minerals preparation, treated with herbal juice or decoction and exposed for Ayurveda, which are known in Indian subcontinent since 7
th
century A.D. and widely recommended for treatment of a variety of chronic ailments. Animal's derivative such as horns, shells, feathers, metallic, nonmetallic and herbals are normally administered as
Bhasma
. A
Bhasma
means an ash obtained through incineration; the starter material undergoes an elaborate process of purification and this process is followed by the reaction phase, which involves incorporation of some other minerals and/or herbal extract. There are various importance of
Bhasma
like maintaining optimum alkalinity for optimum health, neutralizing harmful acids that lead to illness; because
Bhasma
do not get metabolized so they don't produce any harmful metabolite, rather it breakdowns heavy metals in the body. Methods including for
Bhasma
preparation are parpati, rasayoga, sindora, etc.,
Bhasma
which contain Fe, Cu, S or other manufacturing process plays a specific role in the final product(s). Particle size (1-2 μ) reduced significantly, which may facilitate absorption and assimilation of the drug into the body system. Standardization of
Bhasma
is utmost necessary to confirm its identity and to determine its quality, purity safety, effectiveness and acceptability of the product. But the most important challenges faced by these formulations are the lack of complete standardization by physiochemical parameters.
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ORIGINAL ARTICLES
Determination of uric acid level by polyaniline and poly (allylamine): Based biosensor
p. 13
Nasrul Wathoni, Aliya Nur Hasanah, Dolih Gozali, Yeni Wahyuni, Lia Layusa Fauziah
DOI
:10.4103/2231-4040.126981
PMID
:24696812
The uric acid biosensor has been much developed by immobilizing uricase enzyme into the membrane of conductive polymer and the membrane of polyelectrolyte such as polyaniline (PANI) and poly (allylamine) (PAA) respectively. The purpose of this research was to create a new amperometric uric acid biosensor by immobilization of uricase in combination between PANI and PAA membranes. The working electrode was Pt plate (0.5 mm). The auxiliary and the reference electrode were Pt wire 0.4 mm and Ag/AgCl respectively. Uricase, uric acid, PAA, pyrrole and glutaraldehyde were supplied from Sigma. All other chemical was obtained from Merck. The biosensor was created by immobilizing of uricase by a glutaraldehyde crosslinking procedure on PANI composite film on the surface of a platinum electrode while the polyelectrolyte layer of PAA were prepared via layer-by-layer assembly on the electrode, functioning as H
2
O
2
-selective film. Standard of deviation, coefficient of variation (CV) and coefficient of correlation (
r
) analysis were used in this study. The biosensor had a good linearity with a correlation coefficient of 0.993 and it could be used up to 27 times with the CV value of 3.97%. The presence of other compounds such as glucose and ascorbic acid gave 1.3 ± 1.13% and 3.27 ± 2.29% respectively on the interference effect toward the current response of uric acid biosensor. The polymer combination of PANI and PAA can be used as a selective matrix of uric acid biosensor.
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Study on diuretic activity of saffron (stigma of
Crocus sativus
L.) Aqueous extract in rat
p. 17
Nabi Shariatifar, Shahram Shoeibi, Moslem Jaferi Sani, Amir Hossein Jamshidi, Ali Zarei, Abbas Mehdizade, Manouchehr Dadgarnejad
DOI
:10.4103/2231-4040.126982
PMID
:24696813
Saffron is the most expensive spice in the world and consists of the dried stigmas of
Crocus sativus
L. It is used as food coloring and flavoring in food industry and traditional cooking and also in folk medicine as antispasmodic, carminative, stomachic, expectorant, aphrodisiac and cardiotonic. The present study has evaluated the diuretic activity of aqueous extract of dried saffron (stigma of
Crocussativus
) in rat. Aqueous extracts of saffron were administered to experimental rats orally as doses of 60, 120 and 240 mg/kg body weight (BW) and compared with hydrochlorothiazide (10 mg/kg B.W., intraperitoneally), a potent diuretic as positive control and normal saline solution as placebo for control group. The measured parameters for diuretic activity were total urine volume, urine electrolytes concentration such as sodium and potassium, creatinine and urea concentration. The treated rats with aqueous extract of saffron as doses of 120 and 240 mg/kg BW showed higher urine output when compared to the control group. Also, it has shown a significant dose-dependent increase in the excretion of electrolytes when compared to the control group. Our findings proved the diuretic activity of saffron which is used in traditional medicine, it can be an effective and safe strategy for related dysfunction. Also further studies are needed to identify the mechanisms of action, probably other effects and interactions with other medicines.
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Synthesis, characterization and antimicrobial activity of some novel benzimidazole derivatives
p. 21
Immadisetty Sri Krishnanjaneyulu, Govindaraj Saravanan, Janga Vamsi, Pamidipamula Supriya, Jarugula Udaya Bhavana, Mittineni Venkata Sunil Kumar
DOI
:10.4103/2231-4040.126983
PMID
:24696814
A series of novel
N
-((1
H
-benzoimidazol-1-yl) methyl)-4-(1-phenyl-5-substituted-4, 5-dihydro-1-benzoimidazol-1-yl) methyl)-4-(1-phenyl-5-substituted-4, 5-dihydro-1
H
-pyrazol-3-yl) benzenamine were synthesized by treating various 1-(4-((1
H
-benzoimidazol-1-yl) methylamino) phenyl)-3-substitutedprop-2-en-1-one with phenyl hydrazine in the presence of sodium acetate through a simple ring closure reaction. The starting material, 1-(4-((1
H
-benzoimidazol-1-yl) methylamino) phenyl)-3-substitutedprop-2-en-1-one,-benzoimidazol-1-yl) methylamino) phenyl)-3-substitutedprop-2-en-1-one, was synthesized from
o
-phenylenediamine by a multistep synthesis. All the synthesized compounds were characterized by spectroscopic means and elemental analyses. The title compounds were investigated for
in vitro
antibacterial and antifungal properties against some human pathogenic microorganisms by employing the agar streak dilution method using Ciprofloxacin and Ketoconazole as standard drugs. All title compounds showed activity against the entire strains of microorganism. Structural activity relationship studies reveal that compounds possessing an electron-withdrawing group display better activity than the compounds containing electron-donating groups, whereas the unsubstituted derivatives display moderate activity. Based on the results obtained,
N
-((1
H
-benzoimidazol-1-yl) methyl)-4-(1-phenyl-5-(4-(trifluoromethyl) phenyl)-4,5-dihydro-1
H
-pyrazol-3-yl) benzenamine 5i was found to be very active compared with the rest of the compounds and standard drugs that were subjected to antimicrobial assay.
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Plumbagin analogs-synthesis, characterization, and antitubercular activity
p. 28
Nishi Nayak, Meenakshi Bajpai, Balkishen Razdan
DOI
:10.4103/2231-4040.126984
PMID
:24696815
Considering the emerging problem of drug resistance in tuberculosis, there is an urgent need of development of new analogs that are useful in curing drug resistant tuberculosis. In India, tuberculosis continues to remain one of the most pressing health problems. India is the highest tuberculosis burden country in the world, accounting one fifth of global incidence - estimated 2.0-2.5 million cases annually. In 2011, approximately 8.7 million new cases of tuberculosis and 1.4 million people die from tuberculosis each year worldwide. Current antitubercular therapies are successful against normal tuberculosis but it is not suitable for drug resistant tuberculosis. In this study Plumbagin analogs, obtained from
Plumbago zeylanica
(Family-
Plumbaginaceae
), have been synthesized. Out of the various synthesized analogs, the antitubercular activity of compound a and b was evaluated using standard H
37
Rv and S, H, R, and E sensitive M tuberculosis strains using LRF assay method. Compound a showed strong activity against both standard H
37
Rv and S, H, R and E sensitive
M. tuberculosis
strains as compared to standard Rifampicin. The other compounds are proved to be more active against standard H
37
Rv and S, H, R and E sensitive
M. tuberculosis
strain as compared to Rifampicin.
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A validated stability-indicating liquid chromatographic method for determination of process related impurities and degradation behavior of Irbesartan in solid oral dosage
p. 33
Nishant Goswami
DOI
:10.4103/2231-4040.126985
PMID
:24695518
The present work describes the development and validation of a stability-indicating RP-HPLC method for the estimation of degradation and process related impurities of Irbesartan, namely Impurity-1, Impurity-2, Impurity-3 and Impurity-4. The developed LC method was validated with respect to specificity, limit of detection and quantification, linearity, precision, accuracy and robustness. The chromatographic separation was achieved on Hypersil Octadecylsilyl (4.6 mm Χ 150 mm, 3 ΅m) column by using mobile phase containing a gradient mixture of solvent A (0.55% v/v ortho-phosphoric acid, pH adjusted to 3.2 with triethyl amine) and B (95:5 v/v mixture of acetonitrile and solvent A) at a flow rate of 1.2 mL/min. The detection was carried out at a wavelength of 220 nm. During method validation parameter such as precision, linearity, accuracy, specificity, limit of detection and quantification were evaluated, which remained within acceptable limits. HPLC analytical method is linear, accurate, precise, robust and specific, being able to separate the main drug from its degradation products. The degradation products were well-resolved from the main peak and its impurities, thus proving the stability-indicating power of the method. The method is stability-indicating in nature and can be used for routine analysis of production samples and to check the stability of the Irbesartan HCl tablets.
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Synthesis and antinociceptive activity of novel mannich base derivatives of some new fused 3,5-pyrazolidinedione
p. 41
Abhishek Tiwari, Anita Singh
DOI
:10.4103/2231-4040.126993
PMID
:24696816
In the present study, a novel series of mannich bases 1-((1-substituted ethyl-1H-benzo[d] imidazol-2-yl) methyl)-2-substituted phenylpyrazolidine-3,5-dione 3(a-l) were synthesized and evaluated as antinociceptive agents in mice by Eddy's hot plate and acetic acid-induced writhing models. The structures attributed to compounds 3a-3l were elucidated by using IR, 1H-NMR, and Mass spectroscopic techniques. Some compounds showed promising analgesic activity when compared with the standard drug Diclofenac sodium. Results of analgesic activity via hot plate model showed that compounds 3d and 3f were found to be more active than standard drug. Results of analgesic activity via acetic acid-induced writhing model showed that compounds 3a, 3c, 3k, and 3l showed activity which is comparable with the standard drug.
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Mucoadhesive microparticulate drug delivery system of curcumin against Helicobacter pylori infection: Design, development and optimization
p. 48
Mohd Sajid Ali, Vinay Pandit, Mahendra Jain, Kanhiya Lal Dhar
DOI
:10.4103/2231-4040.126996
PMID
:24696817
The purpose of the present research was to develop and characterize mucoadhesive microspheres of curcumin for the potential use of treating gastric adenocarcinoma, gastric and duodenal ulcer associated with
Helicobacter pylori.
Curcumin mucoadhesive microspheres were prepared using ethyl cellulose as a matrix and carbopol 934P as a mucoadhesive polymer by an emulsion-solvent evaporation technique. Response surface methodology was used for optimization of formulation using central composite design (CCD) for two factors at three levels each was employed to study the effect of independent variables, drug:polymer:polymer ratio (curcumin:ethylcellulose:carbopol 934P)(X
1
) and surfactant concentration (X
2
) on dependent variables, namely drug entrapment efficiency (DEE), percentage mucoadhesion (PM),
in vitro
drug release and particle size (PS). Optimized formulation was obtained using desirability approach of numerical optimization. The experimental values of DEE, PM, % release and PS after 8 h for the optimized formulation were found to be 50.256 ± 1.38%, 66.23%±0.06, 73.564 ± 1.32%, and 139.881 ± 2.56 μm, respectively, which were in close agreement with those predicted by the mathematical models. The drug release was also found to be slow and extended more than 8 h and release rates were fitted to the Power law equation and Higuchi model to compute the diffusional parameters. The prolonged stomach residence time of curcumin mucoadhesive microspheres might make a contribution to
H. pylori
complete eradication in combination with other antimicrobial agents.
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COMMENTARY
An important player in brine shrimp lethality bioassay: The solvent
p. 57
Chao Wu
PMID
:24696818
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