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2008| September-October | Volume 70 | Issue 5
Online since
February 12, 2009
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SHORT COMMUNICATIONS
Formulation and evaluation of nitrendipine buccal films
M Nappinnai, R Chandanbala, R Balaijirajan
September-October 2008, 70(5):631-635
DOI
:10.4103/0250-474X.45402
PMID
:21394260
A mucoadhesive drug delivery system for systemic delivery of nitrendipine, a calcium channel blocker through buccal route was formulated. Mucoadhesive polymers like hydroxypropylmethylcellulose K-100, hydroxypropylcellulose, sodium carboxymethylcellulose, sodium alginate, polyvinyl alcohol, polyvinyl pyrrolidone K-30 and carbopol-934P were used for film fabrication. The films were evaluated for their weight, thickness, percentage moisture absorbed and lost, surface pH, folding endurance, drug content uniformity,
In vitro
residence time,
In vitro
release and
ex vivo
permeation. Based on the evaluation of these results, it was concluded that buccal films made of hydroxylpropylcellulose and sodium carboxymethylcellulose (5±2% w/v; F-4), which showed moderate drug release (50% w/w at the end of 2 h) and satisfactory film characteristics could be selected as the best among the formulations studied.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
8,013
759
1
REVIEW ARTICLES
Key formulation variables in tableting of coated pellets
V.S.N Murthy Dwibhashyam, J Vijaya Ratna
September-October 2008, 70(5):555-564
DOI
:10.4103/0250-474X.45391
PMID
:21394249
Multiple unit controlled release dosage forms offer various advantages over their single unit counterparts. Most of these advantages are associated with the uniform distribution of multiparticulates throughout the gastrointestinal tract. Though coated pellets can be filled into hard gelatin capsules, tablet formulation is the preferred one because of various advantages associated with it. However, compression of coated pellets is a challenging task necessitating the optimization of various formulation and process variables. The key formulation variables include composition, porosity, size, shape and density of the pellets; type and amount of polymer coating; nature, size and amount of tableting excipients. The pellet core should be strong with some degree of plasticity. It should be highly porous, small, with an irregular shape. The critical density to achieve prolonged release was reported to lie between 2.4 and 2.8 g/cm
3
. Acrylic polymer films are more flexible and more suitable for the coating of pellets to be compressed into tablets. Thicker coatings offer better resistance to frictional forces. Solvent based coatings are more flexible and have a higher degree of mechanical stability than the aqueous based ones. The tableting excipients should have cushioning property. They should not be significantly different in size and density from those of the pellet cores in order to avoid segregation. Addition of 30%-60% of tableting excipients is necessary to avoid any damage to the polymer coat and to retain its functional property.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
5,393
1,571
1
RESEARCH PAPERS
RP-HPLC and spectrophotometric estimation of ambroxol hydrochloride and cetirizine hydrochloride in combined dosage form
Neela M Bhatia, SK Ganbavale, MS Bhatia, HN More, SU Kokil
September-October 2008, 70(5):603-608
DOI
:10.4103/0250-474X.45398
PMID
:21394256
Rapid, precise, accurate, specific and sensitive reverse phase liquid chromatographic and absorbance ratio spectrophotometric methods have been developed for the simultaneous analysis of ambroxol hydrochloride and cetirizine hydrochloride in their tablet formulation. The chromatographic methods were standardized using a HIQ SIL-C
18
column (250×4.6 mm i.d., 10 µm particle size) with UV detection at 229 nm and mobile phase consisting of methanol-acetonitrile-water (40:40:20, v/v/v). Ambroxol hydrochloride and cetirizine hydrochloride have absorbance maxima at 243 nm and 229 nm, respectively. The isoabsorptive wavelength for both the drugs was 236 nm. For absorbance ratio method developed, wavelengths selected were 243 nm and 236 nm. The proposed methods were successfully applied to the determination of ambroxol hydrochloride and cetirizine hydrochloride in tablets, with high percentage of recovery, good accuracy and acceptable precision. Different analytical performance parameters such as linearity, precision, accuracy, limit of detection, limit of quantitation and robustness were determined according to International Conference on Harmonization ICH Q2B guidelines. Results of analysis of the developed method were compared by performing ANOVA.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
4,346
614
2
REVIEW ARTICLES
A detailed study of patent system for protection of inventions
G Krishna Tulasi, B Subba Rao
September-October 2008, 70(5):547-554
DOI
:10.4103/0250-474X.45390
PMID
:21394248
Creations of brain are called intellect. Since these creations have good commercial value, are called as property. Inventions are intellectual property and can be protected by patents provided the invention is novel, non-obvious, useful and enabled. To have fare trade among member countries, World Trade Organisation proposed TRIPS agreement. India had taken necessary initiation by signing the World Trade Organisation agreement and transformed to global needs. The aim of this article is to enlighten pharmaceutical professionals especially in the field of research and development about planning inventions by thorough review of prior-art, which saves time and money. A thorough understanding is made possible by providing details of origin; present governing bodies, their role along with the Act that is safeguarding the patent system.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
4,001
944
1
RESEARCH PAPERS
Design and evaluation of ethyl cellulose based matrix tablets of ibuprofen with pH modulated release kinetics
S Chandran, Laila F.A Asghar, Neelima Mantha
September-October 2008, 70(5):596-602
DOI
:10.4103/0250-474X.45397
PMID
:21394255
Controlled release preparations have been reported to reduce the gastro irritant and ulcerogenic effects of non steroidal antiinflammatory drugs. In the present study, an attempt was made to develop matrix tablet-based controlled release formulations of ibuprofen, using ethyl cellulose as the rate-controlling polymer. In order to prevent initial release of the drug in the acidic environment of the stomach, cellulose acetate phthalate was incorporated in the matrix in varying amounts. It was found that with increasing the proportion of ethyl cellulose in the matrix, the drug release was extended for 14-16 h. Incorporation of cellulose acetate phthalate in ethyl cellulose matrix provided very low initial release of the drug in the first 2-3 h followed by enhanced release rate in alkaline medium owing to the high solubility of cellulose acetate phthalate at basic pH which led to creation of a porous matrix. It was concluded that combination of cellulose acetate phthalate with ethyl cellulose in the matrix base can be an effective means of developing a controlled release formulation of ibuprofen with very low initial release followed with controlled release up to 14-16 h.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
3,505
981
4
SHORT COMMUNICATIONS
Estimation of paracetamol and aceclofenac in tablet formulation by ratio spectra derivative spectroscopy
AD Nikam, Sampada S Pawar, SV Gandhi
September-October 2008, 70(5):635-637
DOI
:10.4103/0250-474X.45403
PMID
:21394261
A new sensitive, simple, rapid and precise method for simultaneous estimation of paracetamol and aceclofenac in combined tablet dosage form has been developed. The method is based on ratio derivative spectrophotometry. The amplitude in first derivative of the ratio spectra at 256 nm and 268 nm (minima) were selected to determine paracetamol and aceclofenac in combined formulation. The method showed good linearity, accuracy and reproducibility. Results of analysis were validated statistically and by recovery studies.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
3,550
731
6
RESEARCH PAPERS
Use of solubility parameter to design dry suspension of cefaclor as a dual pack system
Kiran Kuksal, Kamla Pathak
September-October 2008, 70(5):609-613
DOI
:10.4103/0250-474X.45399
PMID
:21394257
One of the important methods to improve the solubility of a less water-soluble drug is by the use of co solvents. The solubility enhancement produced by two binary blends with a common co solvent (water-propylene glycol and propylene glycol-ethyl acetate) was studied against the solubility parameter of solvent blends (δ
1
) to evaluate the solubility parameter of drug (δ
2
). The binary blend water:propylene glycol (20:80) gave maximum solubility with an experimental δ
2
value of 16.52 (Cal/cm
3
)
0.5
that was comparable to the theoretical value of 16.52 (Cal/cm
3
)
0.5
determined by molar volume method and 16.35 (Cal/cm
3
)
0.5
when determined by method proposed by Lin and Nash. The solvent blend water:propylene glycol (20:80) in which the drug exhibited maximum solubility was used as the reconstituting medium for formulation of dry suspension of cefaclor. The percentage cumulative drug release of cefaclor from the formulation F7 was compared to the marketed formulation by calculating the
f
1 (dissimilarity factor) and
f
2 (similarity factor) factors. A higher
f
1 value and
f
2 value below 50 indicates difference between the two dissolution profiles.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
3,297
415
1
SHORT COMMUNICATIONS
Ionic gelation controlled drug delivery systems for gastric-mucoadhesive microcapsules of captopril
MA Altaf, Sreedharan , N Charyulu
September-October 2008, 70(5):655-658
DOI
:10.4103/0250-474X.45410
PMID
:21394268
A new oral drug delivery system was developed utilizing both the concepts of controlled release and mucoadhesiveness, in order to obtain a unique drug delivery system which could remain in stomach and control the drug release for longer period of time. Captopril microcapsules were prepared with a coat consisting of alginate and a mucoadhesive polymer such as hydroxy propyl methyl cellulose, carbopol 934p, chitosan and cellulose acetate phthalate using emulsification ionic gelation process. The resulting microcapsules were discrete, large, spherical and free flowing. Microencapsulation efficiency was 41.7-89.7% and high percentage efficiency was observed with (9:1) alginate-chitosan microcapsules. All alginate-carbopol 934p microcapsules exhibited good mucoadhesive property in the
in vitro
wash off test. Drug release pattern for all formulation in 0.1 N HCl (pH 1.2) was diffusion controlled, gradually over 8 h and followed zero order kinetics.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
3,073
630
2
A validated RP-HPLC method for simultaneous estimation of nebivolol and hydrochlorothiazide in tablets
SN Meyyanathan, S Rajan, S Muralidharan, Arunadevi S Birajdar, B Suresh
September-October 2008, 70(5):687-689
DOI
:10.4103/0250-474X.45420
PMID
:21394278
A simple, selective, rapid, precise and economical reverse phase high pressure liquid chromatographic method has been developed for the simultaneous estimation of nebivolol and hydrochlorthiazide from pharmaceutical formulation. Phenomenex Gemini C
18
(25 cm×4.6 mm i.d., 5 µ) column with a mobile phase consisting of acetonitrile: 50mM ammonium acetate (adjusted to pH 3.5 using orthophosphoric acid) (70:30 v/v) at a flow rate of 1.0 ml/min was used. Detection was carried out at 254 nm. Probenecid was used as an internal standard. The retention times of probenecid, nebivolol and hydrochlorthiazide were 13.05, 3.32 and 4.25 min, respectively. The developed method was validated in terms of accuracy, precision, linearity, limit of detection, limit of quantitation and solution stability. The proposed method can be used for the estimation of these drugs in combined dosage forms.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
3,094
480
-
RESEARCH PAPERS
Evaluation of gum of
Moringa oleifera
as a binder and release retardant in tablet formulation
DS Panda, N.S.K Choudhury, M Yedukondalu, S Si, R Gupta
September-October 2008, 70(5):614-618
DOI
:10.4103/0250-474X.45400
PMID
:21394258
The present study was undertaken to find out the potential of gum from
Moringa oleifera
to act as a binder and release retardant in tablet formulations. The effect of calcium sulphate dihydrate (water insoluble) and lactose (water soluble) diluent on the release of propranolol hydrochloride was studied. The DSC thermograms of drug, gum and mixture of gum/drug indicated no chemical interaction. Tablets (F1, F2, F3, and F4) were prepared containing calcium sulphate dihydrate as diluent, propranolol hydrochloride as model drug using 10%, 8%, 6% and 4% w/v of gum solution as binder. Magnesium stearate was used as lubricant. Physical and technological properties of granules and tablets like flow rate, Carr index, Hausner ratio, angle of repose, hardness, friability and disintegration time were determined and found to be satisfactory. Tablets were prepared by wet granulation method containing calcium sulphate dihydrate as excipient, propranolol hydrochloride as model drug using 10%, 20% and 30% of gum as release retardant, magnesium stearate was used as lubricant. Similarly tablets were prepared replacing lactose with calcium sulphate dihydrate. Despite of the widely varying physico-chemical characteristics of the excipients, the drug release profiles were found to be similar. The drug release increased with increasing proportions of the excipient and decreased proportion of the gum irrespective of the solubility characteristics of the excipient. The values of release exponent 'n' are between 0.37 and 0.54. This implies that the release mechanism is Fickian. There is no evidence that the dissolution or erosion of the excipient has got any effect on the release of the drug. The t
50%
values for tablets containing calcium sulphate dihydrate were on an average 10%-15% longer than the tablets containing lactose as excipient. These relatively small differences in t
50%
values suggest that the nature of excipient used appeared to play a minor role in regulating the release, while the gum content was a major factor.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,912
544
4
Solid-state characterization of nevirapine
Mahua Sarkar, OP Perumal, R Panchagnula
September-October 2008, 70(5):619-630
DOI
:10.4103/0250-474X.45401
PMID
:21394259
The purpose of this investigation is to characterize nevirapine from commercial samples and samples crystallized from different solvents under various conditions. The solid-state behavior of nevirapine samples was investigated using a variety of complementary techniques such as microscopy (optical, polarized, hot stage microscopy), differential scanning calorimeter, thermogravimetric analysis, Fourier transform infrared spectroscopy and powder X-ray diffractometry. The commercial samples of nevirapine had the same polymorphic crystalline form with an anhedral crystal habit. Intrinsic dissolution of nevirapine was similar for both the commercial batches. Powder dissolution showed pH dependency, with maximum dissolution in acidic pH and there was no significant effect of particle size. The samples recrystallized from different solvent systems with varying polarity yielded different crystal habits. Stirring and degrees of supersaturation influenced the size and shape of the crystals. The recrystallized samples did not produce any new polymorphic form, but weak solvates with varying crystal habit were produced. Recrystallized samples showed differences in the x-ray diffractograms. However, all the samples had the same internal crystal lattice as revealed from their similar melting points and heat of fusion. The intrinsic dissolution rate of recrystallized samples was lower than the commercial sample. It was found that the compression pressure resulted in desolvation and partial conversion of the crystal form. After compression, the recrystallized samples showed similar x-ray diffractograms to the commercial sample. Amorphous form showed slightly higher aqueous solubility than the commercial crystalline form.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,903
520
4
Response surface methodology for the optimization of celecoxib self-microemulsifying drug delivery system
Jessy Shaji, Shital Lodha
September-October 2008, 70(5):585-590
DOI
:10.4103/0250-474X.45395
PMID
:21394253
The aim of the present study was to prepare, evaluate and optimize, self micro emulsifying drug delivery system of celecoxib. A 3 factor, 3 level factorial design was used for the optimization procedure with different amounts of Labrafil 2609 WL, Labrasol, and Cremophor EL as the independent variables. The response variable was selected on particle size (nm) of the droplets after dilution in 0.1N HCl. Particle size of the self micro-emulsifying drug delivery system depends on the quantity of above three independent variables. Three different levels of each independent variable were selected for the optimization. Mathematical equation and response surface plots were used to relate the dependent and independent variables. The regression equation generated for the particle size after dilution was, Particle size (Y)= +27.83+76.07×A-23.62×B-43.83×C+52.72×A2+9.82×B2+27.20×C2-14.52×A×B-32.38×A×C+12.1×B×C, where, A=Labrafil 2609 WL, B= Labrasol, C= Cremophor EL, Y= particle size. The optimized model predicted a particle size of 28.33 nm with 0.16ml of labrafil 2609 WL, 0.17ml Labrasol and 0.22 ml of Cremophor EL.The observed response were in close agreement with the predicted values of the optimized formulation. This demonstrates the reliability of the optimization procedure in predicting particle size of self microemulsifying delivery system for celecoxib.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,691
707
1
SHORT COMMUNICATIONS
Simultaneous estimation of andrographolide and wedelolactone in herbal formulations
MB Patel, VM Kadakia, SH Mishra
September-October 2008, 70(5):689-693
DOI
:10.4103/0250-474X.45421
PMID
:21394279
Andrographolide and wedelolactone are active components of
Andrographis paniculata
and
Eclipta alba,
respectively. The extracts of these plants are used in many traditional hepatoprotective formulations. An attempt has been made to develop an accurate, precise and specific HPTLC method to quantify simultaneously both these chemical markers of diversified chemical structures in different dosage forms like tablet and syrup. Precoated silica 60F
254
plates with toluene:acetone:formic acid (9:6:1) as mobile phase and detection wavelength of 254 nm were used. The method was validated in terms of linearity, accuracy, precision and specificity. The calibration curve was found to be linear between 200 to 400 ng/spot for andrographolide and 100 to 200 ng/spot for wedelolactone. The limit of detection and the limit of quantification for andrographolide were 26.16 and 79.28 ng/spot, respectively and for wedelolactone 5.06 and 15.32 ng/spot, respectively.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,724
665
3
Quantitative estimation of itopride hydrochloride and rabeprazole sodium from capsule formulation
S Pillai, I Singhvi
September-October 2008, 70(5):658-661
DOI
:10.4103/0250-474X.45411
PMID
:21394269
Two simple, accurate, economical and reproducible UV spectrophotometric methods and one HPLC method for simultaneous estimation of two component drug mixture of itopride hydrochloride and rabeprazole sodium from combined capsule dosage form have been developed. First developed method involves formation and solving of simultaneous equations using 265.2 nm and 290.8 nm as two wavelengths. Second method is based on two wavelength calculation, wavelengths selected for estimation of itopride hydrochloride was 278.0 nm and 298.8 nm and for rabeprazole sodium 253.6 nm and 275.2 nm. Developed HPLC method is a reverse phase chromatographic method using phenomenex C
18
column and acetonitrile: phosphate buffer (35:65 v/v) pH 7.0 as mobile phase. All developed methods obey Beer's law in concentration range employed for respective methods. Results of analysis were validated statistically and by recovery studies.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,871
395
2
Antioxidant, heavy metals and elemental analysis of
Holoptelea integrifolia
planch
A Saraswathy, S Nandini Devi, D Ramasamy
September-October 2008, 70(5):683-576
DOI
:10.4103/0250-474X.45419
PMID
:21394277
The ethanol crude extract of stem bark of
Holoptelea integrifolia
Planch. traditionally used in Indian system of medicine was screened for its antioxidant activity using a-tocopherol as standard antioxidant. The free radical scavenging potential of the extract was evaluated by two different antioxidant methods; ferric thiocyanate and thiobarbituric acid method. The ethanol extract was found to exhibit good antioxidant property. Further physico-chemical constants, elemental and heavy metal analysis of stem bark have been described.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,780
462
1
RESEARCH PAPERS
Development of mesophasic microreservoir-based transdermal drug delivery system of propranolol
LK Omray, S Kohli, AJ Khopade, S Patil, Asmita Gajbhiye, GP Agrawal
September-October 2008, 70(5):578-584
DOI
:10.4103/0250-474X.45394
PMID
:21394252
The mesophasic microreservoir comprises lyotrophic liquid crystals. The liquid crystals were prepared of Brij-35, cetosteryl alcohol and propranolol and evaluated for parameters viz. anisotropy, size and size distribution and drug entrapment efficiency. Subsequent to this liquid crystals based transdermal drug delivery system (TDS) was prepared by incorporating liquid crystals in previously prepared matrix based transdermal patch and evaluated for stability studies like temperature, humidity and aging. The system was also studied for tensile strength, moisture content, water vapor transmission, drug content, anisotropy and
In vitro
drug release studies.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
2,598
537
-
SHORT COMMUNICATIONS
Concurrent estimation of clopidogrel bisulfate and aspirin in tablets by validated RP-HPLC method
PK Shrivastava, PK Basniwal, Deepti Jain, SK Shrivastava
September-October 2008, 70(5):667-669
DOI
:10.4103/0250-474X.45414
PMID
:21394272
A simple, rapid, precise RP-HPLC method was developed for simultaneous estimation of aspirin and clopidogrel bisulphate in tablet dosage form used in the treatment of cardiovascular diseases. To achieve the maximum resolution, acetonitrile:50 mM potassium dihydrogen phosphate buffer:methanol, solution pH adjusted to 3, in the ratio 50:30:20; v/v was selected as mobile phase. This mixture was found to be appropriate allowing good separation of both the components at a flow rate of 1.5 ml/min and detection wavelength 240 nm. In these conditions clopidogrel bisulfate and aspirin were eluated at the 7.47 and 2.2 min. The linearity was found in the concentration range 1.5-7.5 and 3.5-15.0 µg/ml, respectively. All the analytical validation parameters were determined and found with in the limit as per ICH guideline, which indicates the validity of method.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,653
426
3
RESEARCH PAPERS
Synthesis and pharmacological evaluation of azetidin-2-ones and thiazolidin-4-ones encompassing benzothiazole
BM Gurupadayya, M Gopal, B Padmashali, YN Manohara
September-October 2008, 70(5):572-577
DOI
:10.4103/0250-474X.45393
PMID
:21394251
Various 7-chloro-6-fluoro-2-arylidenylaminobenzo(1,3)thiazole (2a-h) have been synthesized by the condensation of 7-chloro-6-fluoro-2-aminobenzo(1,3)thiazole (1) with different aromatic aldehydes. The Schiff's bases on reaction with acetyl chloride, chloroacetyl chloride and phenyl acetyl chloride yielded 1-(7-chloro-6-fluorobenzothiazol-2-yl)-3,4-substituted-aryl-azetidin-2-ones (3a-x). Similarly, cyclization of Schiff's base with thioglycolic acid furnished 3-(7-chloro-6-fluoro-benzothiazol-2-yl)-2-substituted-arylthiazolidin-4-ones (4a-h). The structures of the newly synthesized compounds have been established on the basis of their spectral data and elemental analysis. Some selected compounds were evaluated for antiinflammatory, analgesic, CNS depressant and skeletal muscle relaxant activity.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,403
626
8
SHORT COMMUNICATIONS
Formulation and evaluation of tramadol hydrochloride rectal suppositories
MA Saleem, M Taher, S Sanaullah, M Najmuddin, Javed Ali, S Humaira, S Roshan
September-October 2008, 70(5):640-644
DOI
:10.4103/0250-474X.45405
PMID
:21394263
Rectal suppositories of tramadol hydrochloride were prepared using different bases and polymers like PEG, cocoa butter, agar and the effect of different additives on
in vitro
release of tramadol hydrochloride was studied. The agar-based suppositories were non-disintegrating/non-dissolving, whereas PEGs were disintegrating/dissolving and cocoa butter were melting suppositories. All the prepared suppositories were evaluated for various physical parameters like weight variation, drug content and hardness. The PEG and cocoa butter suppositories were evaluated for macromelting range, disintegration and liquefaction time.
In vitro
release study was performed by USP type I apparatus. The prepared suppositories were within the permissible range of all physical parameters.
In vitro
drug release was in the order of PEG>Agar>cocoa butter. Addition of PVP, HPMC in agar suppositories retards the release. The mechanism of drug release was diffusion controlled and follows first order kinetics. The results suggested that blends of PEG of low molecular weight (1000) with high molecular weight (4000 and 6000) in different percentage and agar in 10% w/w as base used to formulate rapid release suppositories. The sustained release suppositories can be prepared by addition of PVP, HPMC in agar-based suppositories and by use of cocoa butter as base.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
2,561
462
-
RESEARCH PAPERS
Stability indicating RP-HPLC estimation of nebivolol hydrochloride in pharmaceutical formulations
DA Shah, KK Bhatt, RS Mehta, SL Baldania, TR Gandhi
September-October 2008, 70(5):591-595
DOI
:10.4103/0250-474X.45396
PMID
:21394254
A simple, specific, accurate and stability indicating reversed phase liquid chromatographic method was developed for the determination of nebivolol hydrochloride in tablet dosage forms. A phenomenex Gemini C-18, 5 mm column having 250×4.6 mm i.d., with mobile phase containing methanol: acetonitrile: 0.02 M potassium dihydrogen phosphate (60:30:10, v/v/v; pH 4.0) was used. The retention time of nebivolol hydrochloride was 2.6 min. The linearity for nebivolol hydrochloride was in the range of 0.2-10 mg/ml. The recovery was found to be in the range of 98.68-100.86%. The detection limit and quantification limit were found to be 0.06 mg/ml and 0.2 mg/ml, respectively. Nebivolol stock solutions were subjected to acid, alkali and neutral 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 nebivolol hydrochloride in tablet formulations.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,458
393
3
QSAR study on thiazolidine-2,4-dione derivatives for antihyperglycemic activity
BR Prashantha Kumar, MJ Nanjan
September-October 2008, 70(5):565-571
DOI
:10.4103/0250-474X.45392
PMID
:21394250
A set of seventy four molecules belonging to the class of thioglitazones were subjected to the QSAR analysis for their antihyperglycemic activity. All the molecules were subjected to energy minimization to get 3D structures, followed by conformational analysis to get the conformation of the molecule associated with the least energy and highest stability. Various physico-chemical parameters were then calculated using ALCHEMY 2000 software, namely, thermodynamic parameters, structure-dependant parameters, topological parameters and charge-dependant parameters. Multiple linear regression analysis was carried out on all the molecules. The final equation was developed by choosing optimal combination of descriptors after removing the outliers. Cross validation was performed by leave one out method to arrive at the final QSAR model for the chosen set of molecules to exhibit antihyperglycemic activity.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,198
453
5
SHORT COMMUNICATIONS
Synthesis and biological screening of 5-{[(4,6-disubstituted pyrimidine-2-yl)thio]methyl}-N-phenyl-1,3,4-thiadiazol-2-amines
MA Azam, B.R.P Kumar, S Shalini, B Suresh, TK Reddy, CD Reddy
September-October 2008, 70(5):672-677
DOI
:10.4103/0250-474X.45416
PMID
:21394274
A number of substituted-a,β -unsaturated carbonyl compounds (1a-i) were prepared by Claisen-Schmidt condensation of substituted acetophenone with selected araldehydes, which on cycloaddition with thiourea furnished 4,6-disubstituted pyrimidine-2-thiols (2a-i). Reaction of (2a-i) with ethyl chloroacetate followed by condensation with hydrazine hydrate yielded 2-[(4,6-disubstituted pyrimidine-2-yl) thio] acetohydrazides (4a-c). Condensation of compounds (4a-c) with phenyl isothiocyanate gave 2-{[(4,6-disubstituted pyrimidine-2-yl) thio] acetyl}-N-phenylhydrazinecarbothioamides (5a-c) which on treatment with concentrated sulphuric acid afforded titled compounds 5-{(4,6-disubstituted pyrimidine-2-yl) thio] methyl}-N-phenyl-1,3,4-thiadiazole-2-amines (6a-c). These compounds have been characterized on the basis of elemental analysis, IR,
1
H NMR and MS. Compounds have been evaluated for their anticancer and antioxidant activities. Compounds 2b, 2c and 6b exhibited significant antitumor activity against human breast cancer MCF 7 cell line. However, moderate antioxidant activity was observed with compounds 2c, 2d, 2g and 6b.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,004
469
3
Potency determination of antidandruff shampoos in nystatin international unit equivalents
D.B.G Anusha Hewage, W Pathirana, Amara Pinnawela
September-October 2008, 70(5):664-667
DOI
:10.4103/0250-474X.45413
PMID
:21394271
A convenient standard microbiological potency determination test for the antidandruff shampoos was developed by adopting the pharmacopoeial microbiological assay procedure of the drug nystatin. A standard curve was drawn consisting of the inhibition zone diameters vs. logarithm of nystatin concentrations in international units using the fungus
Saccharomyces cerevisiae
(yeast)
strain National Collection of Type Culture (NCTC) 1071606 as the test organism. From the standard curve the yeast inhibitory potencies of the shampoos in nystatin international unit equivalents were determined from the respective inhibition zones of the test samples of the shampoos. Under test conditions four shampoo samples showed remarkable fungal inhibitory potencies of 10227, 10731, 12396 and 18211 nystatin international unit equivalents/ml while two shampoo samples had extremely feeble inhibitory potencies 4.07 and 4.37 nystatin international unit equivalents/ml although the latter two products claimed antifungal activity. The potency determination method could be applied to any antidandruff shampoo with any one or a combination of active ingredients.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
2,158
277
-
Stability indicating HPTLC determination of meloxicam
Namita Desai, Purnima Amin
September-October 2008, 70(5):644-647
DOI
:10.4103/0250-474X.45406
PMID
:21394264
A simple, selective, precise and stability-indicating high-performance thin layer chromatographic method of analysis of meloxicam both as a bulk drug and in formulation has been developed. The mobile phase selected was ethyl acetate:cyclohexane:glacial acetic acid (6.5:3.5:0.02% v/v/v). The calibration curve of the drug was linear in the range of 100-500 ng. The spectrodensitometric analysis was carried out in the absorbance mode at 353 nm. The mean (±RSD) values of slope, correlation coefficient and intercept were 3183.8±0.358, 0.9996±0.0321 and 13012±7.1 respectively. The system precision and the method precision studies were carried out with RSD of 0.83 and 1.89 respectively. The limit of detection and quantitation were 30 ng and 99 ng respectively. The mean percent recovery was found to be 100.3%. The method was used to analyze meloxicam from marketed tablet formulation in the presence of commonly used excipients.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
2,019
342
4
Antiinflammatory, diuretic and antimicrobial activities of
Rungia pectinata
linn. and
Rungia repens
nees
SR Swain, BN Sinha, PN Murthy
September-October 2008, 70(5):679-683
DOI
:10.4103/0250-474X.45418
PMID
:21394276
The hydroalcoholic extracts prepared from leaves of
Rungia pectinata
and
Rungia repens
were investigated for antiinflammatory and diuretic activity in wistar rats. The results obtained were compared with that of standard drug aspirin and frusemide for their antiinflammatory and diuretic activity respectively. The acute toxicity study was also carried out using adult swiss albino mice of either sex which indicates the safety of the extracts even at a dose of 4000 mg/kg.
R. pectinata
showed better anti-inflammatory activity than
R. repens
. In the present study, it was demonstrated that hydroalcoholic extracts of both
R. repens
and
R. pectinata
produce diuretic effect by increasing the excretion of Na
+
, K
+
and Cl
-
. Results showed that
R. repens
is most effective in increasing urinary electrolyte concentration of Na
+
and K
+
ions. The antimicrobial potency of the aerial parts of
Rungia pectinata
and
Rungia repens
have been studied using the petroleum ether, benzene, chloroform, acetone and ethanol extract against a wide number of bacteria and fungi by disc diffusion method. The ethanol extract at a concentration of 30 to 60 µg/disc showed significant activity against the bacteria and fungus investigated. All the extracts of
R. pectinata
and
R. repens
have got moderate action but chloroform and acetone extracts of
R. repens
and ethanol extract of
R. pectinata
have got significant activity against
Trichophyton mentagrophytes
.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
1,802
284
-
Transcorneal permeation of ciprofloxacin and diclofenac from marketed eye drops
N Patidar, MS Rathore, DK Sharma, A Middha, VB Gupta
September-October 2008, 70(5):651-654
DOI
:10.4103/0250-474X.45409
PMID
:21394267
The purpose of this research was to evaluate the in vitro permeation characteristics of various marketed eye drops of ciprofloxacin (0.3% w/v aqueous solution) and diclofenac (0.1% w/v aqueous solution) through isolated goat cornea. Effect of these drugs on isolated goat eye lenses was also evaluated. Permeation studies were conducted by putting 1 ml of formulation on the cornea fixed between the donor and receptor compartments of an all glass modified Franz diffusion cell and monitoring ciprofloxacin and diclofenac concentration in the receptor (containing normal saline or bicarbonate ringer solution under continuous stirring at 37±2
0
) spectrophotometrically at their respective absorption maxima, after 120 min. Paired isolated goat lenses (i.e. of same animal) were used to evaluate the effect of these drugs at selected concentrations against oxidative stress (1 mM hydrogen peroxide solution). After 24 h of incubation at 37
0
, the lens treated with test solution (hydrogen peroxide+drug in bicarbonate ringer solution) was estimated for soluble protein content and compared with control (only hydrogen peroxide). Among marketed eye drops of ciprofloxacin, Joxin (Jawa Pharmaceuticals) showed maximum
in vitro
transcorneal permeation (0.558%) while I-Gesic (Centaur Pharmaceuticals) showed maximum %
in vitro
permeation or
in vitro
ocular availability among diclofenac eye drops after 120 min of permeation. The soluble protein content estimation studies revealed that these drugs at selected concentrations (permeated after 120 min.) had no deleterious effect on eye lenses rather possessed protective effect, since all formulation showed more soluble protein content when compared with control.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
1,815
218
-
Prescribing pattern of antidiabetic drugs in Indore city hospital
Sudha Vengurlekar, Prerna Shukla, P Patidar, R Bafna, S Jain
September-October 2008, 70(5):637-640
DOI
:10.4103/0250-474X.45404
PMID
:21394262
Diabetes mellitus is a metabolic disorder characterized by hyperglycemia, glycosuria, and sometimes ketonemia. The present study was carried out to assess prescribing practice and general trend of diabetes among patients at the Bombay Hospital, Indore. Prescriptions and complete records of diabetic patients were monitored and data was filed as per WHO prescription proforma. The study revealed that prescription of metformin (27%) and glimepiride (22.60%) were found to be maximum among various available antidiabetic drugs. Category wise the maximum prescribed drugs are glimepride (22.60%, sulfonylurea category), metformin (27%, biguanide category) and pioglitazones (13.90%, glitazone category). Insulin prescription was found to be very less (4.5%). Combination of metformin and glimepiride (20.86%) was prescribed most commonly. Most common disease associated with diabetes mellitus was found to be hypertension (35%). Highest prevalence of disease was found to be in the age group of 51 to 60 followed by age group of 41 to 50. Men patients (66.36%) were found to be predominated over women patients (33.64%).
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
1,595
398
2
Antibacterial activity of
Barringtonia acutangula
against selected urinary tract pathogens
S Sahoo, PK Panda, SR Mishra, RK Parida, P Ellaiah, SK Dash
September-October 2008, 70(5):677-569
DOI
:10.4103/0250-474X.45417
PMID
:21394275
Barringtonia acutangula
(L.) Gaertn belonging to family Barringtoniaceae was investigated to evaluate
In vitro
antibacterial activity of aqueous, ethanolic, petroleum ether and chloroform extracts against
Staphylococcus aureus
,
Pseudomonas aeruginosa, Klebsiella pneumoniae, Enterococcus faecalis
and
Escherichia coli
the major urinary tract infection causing pathogens were tested by disc diffusion assay method and the minimum inhibitory concentration was evaluated. Ethanol (95%) extract exhibited broader spectrum of inhibition followed by chloroform, petroleum ether and aqueous extracts against the urinary tract pathogens under test. An attempt has been made to compare the activity of extracts with standard antibiotics against selected urinary tract infection causing pathogens.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
1,688
272
-
RPLC determination of tinidazole and diloxanide furoate in tablets
P.N.S Pai, GK Rao, B Srinivas, S Puranik
September-October 2008, 70(5):670-672
DOI
:10.4103/0250-474X.45415
PMID
:21394273
A simple reverse phase liquid chromatographic method has been developed and subsequently validated for simultaneous determination of tinidazole and diloxanide furoate. The separation was carried out using a mobile phase consisting of acetonitrile, methanol and 0.2 M potassium dihydrogen phosphate (pH 5) in the ratio 2:3:2.The column used was SS Wakosil-II C-18 with a flow rate of 1 ml/min and UV detection at 282 nm. The described method was linear over a concentration range of 10-70 mg/ml and 10-90 mg/ml for the assay of diloxanide furoate and tinidazole, respectively. The mean recovery was found to be 100-101% for tinidazole and 97-103% for diloxanide furoate when determined at three different levels.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
1,759
188
3
Optimization of physical and nutritional parameters for hyaluronidase production by
Streptococcus mitis
S Sahoo, PK Panda, SR Mishra, A Nayak, SK Dash, P Ellaiah
September-October 2008, 70(5):661-664
DOI
:10.4103/0250-474X.45412
PMID
:21394270
The effect of some physical and nutritional parameters were studied for the optimum production of extracellular enzyme hyaluronidase employing
Streptococcus mitis
MTCC*2695 by submerged fermentation. The effects of initial pH, incubation temperature and time, inoculum level and age of inoculum were studied. The maximum enzymatic activity was obtained with an initial pH 5.8, incubation temperature 37º, incubation time for 48 h and inoculum level 6% with inoculum age 24 h. The effect of different carbon and nitrogen sources and antibiotics were studied. The results indicated that sucrose and ammonium chloride showed the highest enzymatic activity among various carbon and nitrogen sources. Antibiotic clarithromycin showed strong inhibitory effect on hyaluronidase production.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
1,713
200
-
Spectrophotometric determination of cefetamet pivoxil hydrochloride and pitavastatin calcium in tablet dosage form
NH Vadia, Vandana Patel, HN Bhalara
September-October 2008, 70(5):649-651
DOI
:10.4103/0250-474X.45408
PMID
:21394266
Two simple, rapid, specific and accurate analytical methods for the estimation of cefetamet pivoxil hydrochloride and pitavastatin calcium in bulk drug and in their tablet formulations are described. These methods are based on difference spectrophotometry, wherein the measurement is done at maximum 221 nm and minimum 275 nm for cefetamet whereas at maximum 240 nm and minimum 259 nm for pitavastatin. The Beer's law was obeyed in the concentration range of 1-35 µg/ml and 1-25 µg/ml and the molar absorptivities were 1.3×10
4
lit mol
-1
cm
-1
and 2.4×10
4
lit mol
-1
cm
-1
for cefetamet pivoxil hydrochloride and pitavastatin calcium, respectively. The proposed methods were validated and successfully applied to the estimation of drugs in tablet formulations.
[ABSTRACT]
[FULL TEXT]
[PDF]
[PubMed]
1,660
234
-
Spectrofluorimetric method for determination of citalopram in bulk and pharmaceutical dosage forms
SG Vasantharaju, S Lakshmana Prabu, A Jacob
September-October 2008, 70(5):647-648
DOI
:10.4103/0250-474X.45407
PMID
:21394265
A simple accurate, sensitive reproducible spectrofluorimetric method was developed for the analysis of citalopram in pure and pharmaceutical dosage form. Citalopram showed strong native fluorescence in 0.05 M sulphuric acid having excitation at 239 nm and emission at 300 nm. All parameters like the effect of different solvents, pH, dilutions, reaction time, temperature and effect of excipients were thoroughly investigated. The calibration graph was linear in the range from 0.100 to 0.900 mg/ml. The proposed method was statistically validated and successfully applied for analysis of tablet dosage forms. The percentage recovery was found to be between 99.08% to 99.28%.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
[PubMed]
1,200
169
1
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© 2006 - Indian Journal of Pharmaceutical Sciences | Published by
Medknow
Online since 20
th
April, 2006