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2007| May-June | Volume 69 | Issue 3
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SHORT COMMUNICATION
Preparation and evaluation of mouth dissolving tablets of salbutamol sulphate
Sarasija Suresh, V Pandit, HP Joshi
May-June 2007, 69(3):467-469
DOI
:10.4103/0250-474X.34568
Asthma is an inflammatory disorder that results in the obstruction of air pathways and causes difficulty in breathing. Amongst the currently available means of treatment, oral dosage forms are associated with lag time and delayed onset of action. However, aerosols and parenterals have rapid onset of action but strongly affect patient compliance. Thus, an attempt was made to improve the onset of action of bronchodilator used commonly in the treatment of asthma. Fast dissolving tablets of salbutamol sulphate were prepared using sublimable ingredients. Selection of the filler also had an important role in deciding the disintegration time. Evaluation of the tablets showed that all the tablets were found to be within official limits and the disintegration time for the formulations ranged from 5 s to 40 s. Amongst all, the formulation containing microcrystalline cellulose and ammonium bicarbonate showed the least disintegration time of 5 s.
[ABSTRACT]
[FULL TEXT]
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[CITATIONS]
14
16,495
1,735
REVIEW ARTICLE
Biological importance of organoselenium compounds
C Narajji, MD Karvekar, AK Das
May-June 2007, 69(3):344-351
DOI
:10.4103/0250-474X.34541
Selenium, a nonmetallic element, has structural and enzymatic roles. Selenium influences a number of endocrine processes; selenium supplementation has recently shown some of the important pharmacological intervention, especially in cancer chemoprevention. During the last few years, a tremendous effort has been directed toward the synthesis of stable organoselenium compounds. The biochemistry and pharmacology of selenium-based compounds are subjects of intense current interest, especially from the point of view of public heath. The purpose of this review is to discuss the recent pharmacological applications of organoselenium compounds as therapeutic agents in the treatment of several diseases.
[ABSTRACT]
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13
7,700
551
RESEARCH PAPER
Mucoadhesive microspheres of propranolol hydrochloride for nasal delivery
PM Dandagi, VS Mastiholimath, AP Gadad, SR Iliger
May-June 2007, 69(3):402-407
DOI
:10.4103/0250-474X.34550
Gelatin A microspheres of propranolol hydrochloride for intranasal systemic delivery were developed with the aim to avoid first pass metabolism, to improve the patient compliance, to use an alternative therapy to conventional dosage form, to achieve controlled blood level profiles, and to improve the therapeutic efficacy of propranolol hydrochloride in the treatment of various cardiovascular disorders and as a prophylactic for migraine. Gelatin A microspheres were prepared by emulsion crosslinking method using glutaradehyde as a crosslinking agent. Gelatin and chitosan were used as polymer and co polymer respectively. All the prepared microspheres were evaluated for physical characteristics, such as particle size, incorporation efficiency, swelling index,
in vitro
bioadhesion using rat jejunum and
in vitro
drug release in pH 6.6 phosphate buffer. Average particle size of microspheres was found to be in the size range 1-50 mm. Increase in drug and polymer concentration in the formulation increased incorporation efficiency. All the microsphers showed good bioadhesive properties and swelling indices and good sustained release of drug. The data indicates that propranolol hydrochloride release followed Higuchi's matrix and Peppa's model. Stability studies showed stability of formulation at all the conditions to which they were subjected.
[ABSTRACT]
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[CITATIONS]
12
7,053
1,068
In vitro
and
in vivo
advantage of celecoxib surface solid dispersion and dosage form development
RP Dixit, MS Nagarsenker
May-June 2007, 69(3):370-377
DOI
:10.4103/0250-474X.34545
Celecoxib surface solid dispersions were prepared by various techniques using different ratios of drug and carriers. Infra-red spectroscopy and differential scanning calorimetry showed no significant change in solid state of celecoxib in the surface solid dispersions and physical mixtures of celecoxib and carriers. Surface solid dispersions exhibited superior dissolution profiles and improved antiinflammatory activity in rat paw oedema model. The increase in the dissolution rate and consequent enhancement of antiinflammatory effect in rats of celecoxib were attributed to reduced particle size of celecoxib deposited on the surface of carrier and enhanced wettability of the drug particles brought about by the carrier. Improved dissolution characteristics were retained when compressed into tablets.
[ABSTRACT]
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[CITATIONS]
10
4,988
946
Seed mucilage from
Ocimum americanum
linn. as disintegrant in tablets: Separation and evaluation
DM Patel, DG Prajapati, NM Patel
May-June 2007, 69(3):431-435
DOI
:10.4103/0250-474X.34556
Plant products serve as an alternative to synthetic products because of local accessibility, eco-friendly nature and lower prices compared to imported synthetic products. Natural gums and mucilage have been widely explored as pharmaceutical excipients. The present study was undertaken to separate mucilage from the seeds of
Ocimum americanum
Linn
.
and explore its use as a tablet disintegrant. Methods for extraction of mucilage from the seeds were developed and the yield by the method C was found to be 14%. The mucilage was evaluated for various parameters as per Indian Pharmacopoeia. The loss on drying, ash value and microbial load were well within the official limits. The disintegrating efficiency of separated mucilage was compared with that of the starch in tablets prepared using lactose, propranolol hydrochloride and polyvinyl pyrrolidone as model diluent, drug and binder, respectively. The disintegration time for tablet formulations prepared using mucilage (10% w/w) was less (154 s) than that of the tablet formulations prepared using starch as a disintegrant (269 s). The mucilage not interfered with the release of a drug from tablet formulations. Formulated tablets were found stable at 45
o
C for 4 weeks without significant change in hardness, disintegration time and
in vitro
drug release.
[ABSTRACT]
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9
6,418
599
REVIEW ARTICLE
Pyrimidine as antiinflammatory agent: A review
M Amir, SA Javed, Harish Kumar
May-June 2007, 69(3):337-343
DOI
:10.4103/0250-474X.34540
Pyrimidine nucleus exhibited remarkable pharmacological activities. Literature indicates that compounds having pyrimidine nucleus have wide range of therapeutic uses that include antiinflammatory, antibacterial, anticancer, antiviral, antiHIV, antimalarial, antihypertensive, sedatives and hypnotics, anticonvulsant and antihistaminic. The present review provides a broad view of the antiinflammatory activity possessed by compounds having a pyrimidine nucleus.
[ABSTRACT]
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8
7,414
1,308
RESEARCH PAPER
Design and evaluation of diclofenac sodium controlled drug delivery systems
KM Manjunatha, MV Ramana, D Satyanarayana
May-June 2007, 69(3):384-389
DOI
:10.4103/0250-474X.34547
Sustained release dosage form of diclofenac sodium containing immediate and controlled release components was designed. Solid dispersion of immediate release component was prepared using polyvinyl pyrrolidone and mannitol carriers by common solvent method. Controlled release component was prepared in form of spherical beads by ionotropic gelation technique. The beads were prepared based on dispersing drug in solutions of ionic polysaccharides such as chitosan and sodium alginate. These dispersions were dropped into solutions of counter ions such as tetrasodium pyrophosphate and calcium chloride, respectively. The beads were also prepared using agar by dropping agar-drug hot solution into a mixture of chilled liquid paraffin and water. Then, diclofenac sodium controlled release drug delivery systems were prepared by combining the immediate release and controlled release components in different ratios. The formulations were found to be effective in providing controlled release of drug for a longer period of time. The beads were characterized by scanning electron microscopy and X-ray diffraction studies.
[ABSTRACT]
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11,896
1,640
SHORT COMMUNICATION
Synthesis and biological evaluation of some novel pyrazolines
V Harinadha Babu, CH Sridevi, A Joseph, KK Srinivasan
May-June 2007, 69(3):470-473
DOI
:10.4103/0250-474X.34569
Chalcones (2a and 2b) were prepared from 2-acetyl benzofuran (1) and condensed with different aromatic acid hydrazides (3a-o) to get the corresponding pyrazolines (4a-o and 5a-o). The structures of all these compounds have been established on the basis of analytical and spectral data. Compounds have been screened for antiinflammatory, antioxidant and antibacterial studies. Among the 7 compounds that were screened for antiinflammatory activity, compounds 4g and 5m showed 83.4% and 80.5% inhibition of oedema volume, while the standard drug (ibuprofen) showed inhibition of 91.9%. Compounds 4k and 5h showed moderate activity of 72.8% and 59.6% respectively. All the 30 compounds were tested for antioxidant activity at 1000, 500, 250, 100, 50, 25 and 10 mg/ml concentrations against standard drug ascorbic acid. Compounds 4g, 4h, 4k, 4m, 5g, 5h, 5k and 5m showed excellent antioxidant activity as compared with ascorbic acid. Among the 30 compounds that were screened against two Gram +ve (
Staphylococcus aureus
and
Bacillus subtilis
) and two gram -ve (
Escherichia coli
and
Pseudomonas aeruginosa
) organisms, compounds possessing p-chloro, p-fluoro, 2-amino-5-bromo, 2-hydroxy-5-nitro and 3,5-dichloro substitutions on the phenyl ring showed good activity against
Escherichia coli
and
Bacillus subtilis
. The activity is comparable with that of the standard drug ciprofloxacin.
[ABSTRACT]
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[CITATIONS]
6
5,331
706
Spectrophotometric estimation of famciclovir in bulk and tablet dosage form
S Nizamuddin, BM Gurupadayya, MC Ravi, YN Manohara, S Appala Raju
May-June 2007, 69(3):451-453
DOI
:10.4103/0250-474X.34562
Two, simple, accurate, rapid and sensitive methods have been developed for the estimation of famciclovir in tablet dosage forms. Method A is based on the nucleophillic substitution product with Folin's reagent to form colored chromogen exhibiting absorption maximum at 454 nm with apparent molar absorptivity of 3.99×10
4
l/mol.cm and obeyed Beer's law in the concentration range of 2-10 µg/ml. Method B is based on diazotisation and coupling reaction with resorcinol to form colored chromogen exhibiting absorbance maximum at 386 nm with apparent molar absorptivity of 3.15×10
4
l/mol.cm and obeyed Beer's law in the concentration range of 7-21 µg/ml.
[ABSTRACT]
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6
2,936
265
Antimicrobial screening of some newly synthesised transition metal complexes of a dithiocarbazate derived from isoniazid
Shashi B Kalia, V Sharma, Kamakshi Lumba, Geetanjli Kaushal, Anuradha Sharma
May-June 2007, 69(3):438-441
DOI
:10.4103/0250-474X.34558
Some new metal (II) isonicotinoyldithiocarbazates of the general formula [M(IN-DtczH)
2
]Cl
2
(M = Mn, Co, Ni, Zn; IN-DtczH = isonicotinoyldithiocarbazic acid) and Mn(IN-Dtcz)
2
, having sulphur-nitrogen linkage were synthesized. All the compounds were screened for their antimicrobial activity against the pathogenic bacteria
Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus
and
Enterococcus
sp
.
and the pathogenic fungus
Candida albicans
by agar dilution method. All the compounds showed good antimicrobial activity.
[ABSTRACT]
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[CITATIONS]
6
5,793
257
Spectrophotometric determination of andrographolides in
Andrographis paniculata
nees and its formulation
Karishma Shah, Priti Trivedi, Shivprakash , K Pundarikakshudu
May-June 2007, 69(3):457-458
DOI
:10.4103/0250-474X.34564
A simple, sensitive and reproducible spectrophotometric method was developed for the estimation of andrographolides in
Andrographis paniculata
(
Kalmegh
) and its formulation. The method is based on the condensation of g-unsaturated lactone ring of andrographolides and picric acid in alkaline medium which results in the formation of colored complex, that which could be measured at 494 nm. Linearity of the proposed method was found between 5-50 µg/ml. The powdered samples of
A. paniculata
procured from different sources were found to contain 0.9-1.5% w/w of andrographolides. Formulation containing
A. paniculata
showed 0.3% w/w of the andrographolides. Our studies clearly indicated that Baljet reagent can also be employed for estimation of andrographolides. The method was found to be reliable and precise and could be used for analyzing formulations containing andrographolides for regular quality control purposes.
[ABSTRACT]
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5
4,492
493
REVIEW ARTICLE
Organic volatile impurities in pharmaceuticals
SB Puranik, PNS Pai, GK Rao
May-June 2007, 69(3):352-359
DOI
:10.4103/0250-474X.34542
Organic volatile impurities are residual solvents that are used in and are produced during the synthesis of drug substances, or in excipients used in the production of drug formulations. Many of these residual solvents generally cannot be completely removed by standard manufacturing processes or techniques and are left behind, preferably at low levels.
[ABSTRACT]
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[CITATIONS]
5
10,488
638
RESEARCH PAPER
Design, development and
in vitro
evaluation of sennosides tablets containing pectin HPMC for colonic drug delivery
Munira Momin, K Pundarikakshudu
May-June 2007, 69(3):394-401
DOI
:10.4103/0250-474X.34549
The purpose of the present investigation was to achieve colon specific delivery of sennosides using the polysaccharide pectin as a compression-coating agent. In this study, pectin along with hydroxypropylmethylcellulose was used for compression coating of the core tablets of calcium sennoside. Drug dissolution and erosion studies were carried out in pH 1.2 and phosphate buffer pH 7.4 using a pectinolytic enzyme. The system was designed based on the gastrointestinal transit time concept, assuming colon arrival time to be 6 h. It was found that pectin alone was not sufficient to protect the core tablets during entire gastrointestinal transit time. Addition of hydroxypropylmethylcellulose was required to control the erosion of tablets. In this investigation a 3
2
factorial design was constructed to investigate the influence of two variables; the amount of hydroxypropylmethylcellulose (X1) and coat weight of the tablets (X2) on the time taken for 50% erosion of tablet in presence of pectinase enzyme (TE
50
) and average percent weight difference between tablets with and without enzyme at the 10
th
hour (% WD). The results revealed that for protecting the calcium sennosides core tablets in upper gastrointestinal tract, the core tablets should be coated with lower amount of hydroxypropylmethylcellulose and higher amount of coat weight. The main effects were found to be statistically significant in nature. The amount of hydroxypropylmethylcellulose exhibited predominant action as compared to coat weight.
In vivo
performance was assessed by X-ray roentegenography study. The pectin-hydroxypropylmethylcellulose coating was found to be a promising colon delivery system for those drugs like sennosides.
[ABSTRACT]
[FULL TEXT]
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[CITATIONS]
4
4,708
717
Preparation and
in vitro
evaluation of sustained release drug delivery system for verapamil HCL
MR Bhalekar, J Avari, RA Umalkar
May-June 2007, 69(3):418-422
DOI
:10.4103/0250-474X.34553
Verapamil HCl is a calcium channel blocker administered on thrice a day dosage regimen. In the present study resinates of verapamil HCl were formulated using Indion resins. Drug loading process was optimized with respect to drug:resin ratio, pH of loading solution, and particle size of resin. Resinates were characterized using XRPD.
In vitro
drug release rates from resinate was not adequately sustained. Hence resinates were incorporated in pellets using extrusion spheronization to achieve desired release pattern. Optimum drug loading was seen at pH of 3.5 in drug resin ratio of 1:1 and was seen to increase with temperature. XRPD studies revealed verapamil to be present in amorphous form in resinates. Drug release from resinates was complete in four hours. Resinates were pelletized using hydroxypropylmethylcellulose. Resinate of Indion 254 with 5% hydroxypropylmethylcellulose fulfilled USP criteria for extended release verapamil preparation.
[ABSTRACT]
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[CITATIONS]
4
5,131
825
The effect of particle properties on the semisolid spreadability of pharmaceutical pastes
Soheila Honary, M Chaigani, A Majidian
May-June 2007, 69(3):423-426
DOI
:10.4103/0250-474X.34554
The effect of different shapes and size solids and varying solid content added to semisolid base containing Eucerin
®
and liquid paraffin on the spreadability of obtained pastes were evaluated. Zinc oxide, salicylic acid, acetyl salicylic acid, and sodium chloride) were used as model solids for different shape and size. The samples were tested by extensometer, and the mean values of spread surface for at least three samples were plotted against the exerted weights on the extensometer's upper plate. The results show that, the semisolid spreadability decreased significantly (
P
<0.05) as the powder level in the paste increased and decreased by decreasing the particle size of the solids. The results also illustrate that the particle shapes significantly (
P
<0.05) affect semisolid spreadability.
[ABSTRACT]
[FULL TEXT]
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[CITATIONS]
4
4,693
253
SHORT COMMUNICATION
HPTLC analysis of hepatoprotective diterpenoid andrographolide from
Andrographis paniculata
nees (
kalmegh
)
Archana P Raina, A Kumar, SK Pareek
May-June 2007, 69(3):473-475
DOI
:10.4103/0250-474X.34570
A rapid, accurate and simple high performance thin layer chromatography method for quantitative estimation of andrographolide in
Andrographis paniculata
is described here. The assay combines separation of andrographolide on silica gel 60 F
254
HPTLC plates followed by scanning of the spots at 232 nm using a Camag Scanner 3. Thirty germplasm collections of
Andrographis paniculata
were evaluated for andrographolide content by this method. Andrographolide content ranged from 1.14% to 2.60%.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
4
5,786
673
Synthesis and biological evaluation of some novel quinazolones
EM Jessy, A Thirugnana Sambanthan, J Alex, CH Sridevi, KK Srinivasan
May-June 2007, 69(3):476-478
DOI
:10.4103/0250-474X.34571
In view of the potent antimicrobial and antiinflammatory activities exhibited by quinazolin-4-(3H)-ones, a series of novel 2, 3-disubstituted-3,1-quinazolin-4-(3H) ones have been synthesized. The synthesized compounds were screened for antibacterial and antiinflammatory activities. Compounds 3a and 3l showed significant antiinflammatory activity comparable to ibuprofen, while the compound 3J showed antibacterial activity comparable to ciprofloxacin.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
3
2,945
358
A HPTLC method for quantitative estimation of swetiamarin in marketed polyherbal antidiabetic formulations
PM Patel, KN Patel, NM Patel, RK Goyal
May-June 2007, 69(3):446-448
DOI
:10.4103/0250-474X.34560
Swetiamarin is one of the phytoconstituents present in
Enicostemma littorale
Linn.
Enicostemma littorale
is known for its hypoglycemic activity from ancient times. In the present study an attempt has been made to develop a HPTLC method for quantitative estimation of swetiamarin in plants and different marketed antidiabetic polyherbal formulations. This HPTLC method was found to be reproducible, accurate and precise and could detect swetiamarin concentration at nanogram level. The developed HPTLC method would be an important tool in the way of acceptability of quality control method of polyherbal formulations.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
3
3,893
525
RESEARCH PAPER
Studies to enhance dissolution properties of carbamazepine
ST Prajapati, MC Gohel, LD Patel
May-June 2007, 69(3):427-430
DOI
:10.4103/0250-474X.34555
Carbamazepine a dibenzapine derivative with structural resembling to the tricyclic antidepressant, it is used to control some types of seizures in the treatment of epilepsy. It is also used to relieve pain due to trigeminal neuralgia. One of the major problems with this drug is its very low solubility in biological fluids, which results into poor bioavailability after oral administration. Hence present study was carried out to enhance dissolution properties of carbamazepine. Physical mixtures and solid dispersions of carbamazepine were prepared to enhance its water solubility. Physical mixtures and solid dispersions of carbamazepine were prepared by using polyvinyl pyrrolidone K-30, polyethylene glycol 4000 and polyethylene glycol 6000 as water-soluble carrier at various proportion (1:0.1, 1:0.2, 1:0.4, 1:0.6, 1:0.8, by weight) by employing solvent evaporation method. The drug release profile was studied according to USP XXIII monograph in 1% sodium lauryl sulphate solution. It was found that the dissolution rate and the dissolution parameters of the drug from the physical mixture as well as solid dispersion were higher than those of the intact drug. The degree of the dissolution rate enhancement depended on the nature and the amount of the carrier, i.e., the higher amount of the carrier used, the higher dissolution rate was obtained except for polyvinyl pyrrolidone K-30 and PEG 4000 solid dispersions. Among carrier studied solid dispersion of Carbamazepine: PVP K-30 at 1:0.2 (drug:carrier ratio) gave highest dissolution. The increase in dissolution rate of the drug may be due to increase wettability, hydrophilic nature of the carrier and also possibility due to reduction in drug crystalinity.
[ABSTRACT]
[FULL TEXT]
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[CITATIONS]
3
5,454
877
Evaluation of protective effects of water extract of
Spirulina platensis
(blue green algae) on cisplatin-induced lipid peroxidation
S Ray, K Roy, Chandana Sengupta
May-June 2007, 69(3):378-383
DOI
:10.4103/0250-474X.34546
Attempt has been made to evaluate free radical scavenging activity of water extract of
Spirulina platensis
on cisplatin-induced lipid peroxidation using some common laboratory markers. In this present study goat liver has been used as lipid source. This
in vitro
evaluation was done by measuring the malondialdehyde, 4-hydroxy-2-nonenal, reduced glutathione and nitric oxide content of tissue homogenates. The results suggest that cisplatin could induce lipid peroxidation to a significant extent and it was also found that water extract of the algae has the ability to suppress the cisplatin-induced toxicity.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
3
8,965
406
An approach to minimize
Pseudomembranous
colitis
caused by clindamycin through liposomal formulation
MV Ramana, AD Chaudhari, M Himaja, D Satyanarayana, Kamal Dua
May-June 2007, 69(3):390-393
DOI
:10.4103/0250-474X.34548
Liposomal encapsulation is known to significantly improve the therapeutic index of a drug. In the present investigation liposomal formulations were chosen to transport clindamycin, which is considered as the most effective topical antibiotic for acne, into the skin layers. Liposomes with clindamycin phosphate were prepared using lipid film hydration method and the optimum ratio of the components was determined. The liposomes were characterized for their vesicle size, shape, encapsulation efficiency, % drug content and for
in vitro
skin permeation study. The results suggest that the average size of vesicles was found to be in range of 4.91-6.75 µm. Highest encapsulation efficiency (45.4%) and
in vitro
skin permeation (62%) was achieved with a formulation containing drug: lipid: cholesterol in the ratio of 1:1:1. Liposomal formulation of clindamycin phosphate with good skin permeation properties was incorporated into gel base and comparison of
in vitro
skin permeation was made with non liposomal marketed gel, both containing 1% clindamycin phosphate. Higher rate of drug release across the rat abdominal skin was found with liposomal gel (54%) than non-liposomal marketed gel (48.7%). Biological study revealed that by encapsulating clindamycin phosphate into liposomes the occurrence of
Pseudomembranous colitis
could be reduced significantly in comparison to plain clindamycin phosphate.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
2
3,810
266
SHORT COMMUNICATION
Determination of microsomal CYP2A6 activity by high performance liquid chromatography
SS Lavhekar, AK Bhopale, AA Lohade, EC Coutinho, KR Iyer
May-June 2007, 69(3):448-451
DOI
:10.4103/0250-474X.34561
Coumarin has been reported to be a reliable probe for the determination of human microsomal CYP2A6 activity. Coumarin is converted to 7-hydroxycoumarin by CYP2A6. A high pressure liquid chromatographic assay for the estimation of CYP2A6 activity in microsomes was evaluated. A RP C-18 Novapak Waters (15 cm x 3.9 mm, 5 µm) column was used for the assay. The mobile phase composition was methanol : 1% glacial acetic acid (35:65 v/v) (pH~3.1), with a flow rate of 0.6 ml/min, injection volume of 100 µl and detection at 320 nm. The retention times for coumarin and 7-hydroxycoumarin were 8.7 min and 5.3 min, respectively. The limit of detection (LOD) was 0.05 µM, and the limit of quantitation (LOQ) was 0.1 µM, for 7-hydroxycoumarin. The percent coefficient of variation associated with 7-hydroxycoumarin determination after duplicate estimation was found to be in the range 0.03 to 3.6% for buffer matrix and 0.1 to 6.5% for microsomal matrix. The mean rate of 7-hydroxycoumarin formation in guinea pig liver microsomes was 0.084 nmol/min/nmol P450. Coumarin 7-hydroxylase activity was absent in rat liver microsomes. No interference was observed from incubation mixture components.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
2
2,740
215
Improved dissolution rate of valdecoxib inclusion complexes with hydroxypropyl-β-cyclodextrin
SN Hiremath, N Bharti, PV Swamy, SA Raju
May-June 2007, 69(3):442-445
DOI
:10.4103/0250-474X.34559
Valdecoxib is a hydrophobic molecule that is practically insoluble in aqueous media and exhibits an exceedingly slow intrinsic dissolution rate. The present study was emphasized on improving the solubility and dissolution rate of drug by forming inclusion complex with hydroxypropyl-β -cyclodextrin. The inclusion complexes were prepared by physical mixture, kneading and common solvent methods. Phase solubility studies indicated the formation of a 1:1 M complex in solution. Drug excipient interactions were characterized using Fourier transformed infrared spectroscopy and differential scanning calorimetry studies. Differential scanning calorimetry studies indicated the formation of solid inclusion complex of valdecoxib hydroxypropyl-β -cyclodextrin at 1:2 M ratio in kneading and common solvent method. Solid inclusion complexes of valdecoxib hydroxypropyl-β -cyclodextrin (1:2 M) prepared by kneading and common solvent method exhibited higher rates of dissolution and dissolution efficiency values both in 0.1N HCl and 0.1N HCl with 0.25% sodiumlauryl sulphate.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
1
3,265
333
RESEARCH PAPER
Formulation strategy for low absorption window antihypertensive agent
MJ Qureshi, J Ali, Alka Ahuja, Sanjula Baboota
May-June 2007, 69(3):360-364
DOI
:10.4103/0250-474X.34543
In the present study a hydrodynamically balanced system of celiprolol hydrochloride was developed as single unit floating capsule. Various grades of low density polymers were used for formulation of this system. They were prepared by physical blending of celiprolol hydrochloride and the polymer in varying ratios. The formulation was optimized on the basis of
in vitro
buoyancy and
in vitro
release in citrate phosphate buffer at pH 3.0. Effect of various release modifiers was studied to ensure the delivery of drug from the hydrodynamically balanced system capsule over a period of 12 h. Capsule prepared with HPMC K4 M and liquid paraffin gave the best
in vitro
percentage release and was taken as optimized formulation. By fitting the data in zero order, first order and Higuchi model it could be concluded that the release followed zero order release, as the correlation coefficient was higher for zero order release. It could be concluded from R
2
value for Higuchi model and K-Peppas model that drug release followed fickian diffusion mechanism.
[ABSTRACT]
[FULL TEXT]
[PDF]
[CITATIONS]
1
5,182
949
In vitro
and
in situ
absorption studies of vasicine in rats
HNA Ram, Annie Shirwaikar, A Shirwaikar
May-June 2007, 69(3):365-369
DOI
:10.4103/0250-474X.34544
Vasicine is a pyrralazoquinazoline monobasic alkaloid obtained from the plant
Adhatoda zeylanica.
In the current experiment, we have made an attempt to determine the sites of absorption for the bioactive component vasicine from the various segments of small intestine (duodenum, jejunum and ileum) and colon. Everted intestinal sac method was used to assess the
in vitro
absorption of vasicine. The absorption of standard vasicine, vasicine from methanol and ethanol extracts of
vasaka
from the small intestine of rats was studied using the Doluisio technique. Maximum absorption of 87.3±5.256% of vasicine was observed in the duodenal region, whilst the colon showed the minimum absorption of 42.6±7.314%. The jejunum and ileum showed 77.2±3.415% and 46.9±3.271% absorption of vasicine respectively. The luminal disappearance of vasicine by Doluisio technique was determined from the standard curve. Absorption of vasicine was found to be better from the ethanol extract than from the methanol extract. Standard vasicine has revealed steady absorption as evidenced by a typical sigmoidal curve. The absorption rate was found to be of the first order for the tested samples.
[ABSTRACT]
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4,151
344
SHORT COMMUNICATION
Validated TLC densitometric method for the quantification of paroxetine hydrochloride in solid dosage form
RN Sharma, MS Bagul, SC Chaturvedi, KK Vasu, M Rajani
May-June 2007, 69(3):436-438
DOI
:10.4103/0250-474X.34557
A simple, specific, accurate and precise high performance thin layer chromatography method has been developed for the estimation of paroxetine hydrochloride in tablet dosage forms. The quantification was carried out at 296 nm. Developed method was validated in terms of linearity, accuracy, precision, repeatability and specificity. Limit of detection and limit of quantification of paroxetine hydrochloride were found to be 60 ng/spot and 160 ng/spot, respectively. The linearity range for paroxetine hydrochloride was found to be 160-960 ng/spot with correlation coefficient of 0.995. Content of paroxetine hydrochloride in two tablet dosage forms was found to be 100.10 and 100.20%, respectively.
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3,060
200
RESEARCH PAPER
Stability studies on a cough syrup in plastic containers
Renuka Gupta, Kamalinder K Singh
May-June 2007, 69(3):408-413
DOI
:10.4103/0250-474X.34551
Packaging of pharmaceuticals is a critical process. Plastics are unanimously used for solid dosage packaging. Due to their numerous advantages over glass, they are now being considered as an alternative to packaging of liquid dosage forms also. Cough syrups are preparations containing antitussive drugs, and are most commonly packaged in glass bottles. The interactive nature of plastics makes it essential that a detailed study be carried out before their use for any pharmaceutical packaging. The present work reports the stability and suitability of packaging antitussive syrup in plastic containers.
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10,749
581
Effect of buspirone on blood sugar levels in humans
SK Ojha, M Nandave, C Sharma
May-June 2007, 69(3):414-417
DOI
:10.4103/0250-474X.34552
Psychiatric disorders such as depression, schizophrenia and anxiety disorders are seen more common in diabetic patients. The present study investigated the effect of an antianxiety drug, buspirone on blood glucose and plasma insulin level in healthy humans. Twelve healthy adult male volunteers were administered single oral doses of buspirone (10 mg) or placebo, in a randomized, crossover way, followed by oral glucose challenge (75 g in 200 ml) at reported T
max
of the respective administered drugs. The blood samples were collected as predose, postdose and post oral glucose load at 0.5, 1.0, 1.5, 2.0, 2.5 and 3.0 h. Blood glucose and plasma insulin concentrations were estimated by glucose hexokinase and enzyme linked immunosorbent assay methods respectively. The concentration of blood glucose was significantly (
p
<0.05) decreased after oral glucose challenge following administration of buspirone in comparison with placebo. However no significant change was observed in the fasting blood glucose and fasting and oral glucose challenge induced plasma insulin. These results suggest that buspirone may have important risks particularly for diabetics, glucose intolerant and nondiabetics who are on long therapy with buspirone.
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4,849
189
SHORT COMMUNICATION
Influence of
Calotropis procera
roots on biochemistry of reproductive organs of ovariectomized rats
D Ahirwar, Bharti Ahirwar, MD Kharya
May-June 2007, 69(3):459-461
DOI
:10.4103/0250-474X.34565
Biochemical alterations have been observed in the uterus, cervix and vagina of ovariectomized rats treated with alcoholic extract of
Calotropis procera
roots administered in the presence and absence of ethynilestradiol. Ovariectomy resulted in the decrease of glycogen and protein content as well as activity of acid and alkaline phosphatase in the uterus, cervix and vagina. Administration of the alcoholic extract of
Calotropis procera
increases glycogen and protein content and activity of acid and alkaline phosphatase in uterus and cervix with increasing weights, whereas, the glycogen contents decreased significantly in vagina. Combined treatments of the alcoholic extract with ethynilestradiol act synergistically confirm the estrogenic action of alcoholic extract of
Calotropis procera
roots in adult ovariectomized rats.
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3,981
258
Colorimetry method for estimation of glycine, alanine and isoleucine
SA Shah, IS Rathod, Dharitri Kanakia
May-June 2007, 69(3):462-464
DOI
:10.4103/0250-474X.34566
A simple and sensitive colorimetry method has been developed for estimation of amino acids glycine, alanine and isoleucine. Amino acids were derivatized with dichlone in presence of sodium bicarbonate. Amino acids showed maximum absorbance at 470 nm. The method was validated in terms of linearity (5-25 µg/ml for glycine, alanine and isoleucine), precision (intra-day variation 0.13-0.78, 0.22-1.29, 0.58-2.52% and inter-day variation 0.52-2.49, 0.43-3.12, 0.58- 4.48% for glycine, alanine and isoleucine respectively), accuracy (91.43-98.86, 96.26-105.99 and 95.73-104.82 for glycine, alanine and isoleucine respectively), limit of detection (0.6, 1 and 1 µg/ml for glycine, alanine and isoleucine respectively) and limit of quantification (5 µg/ml for glycine, alanine and isoleucine). The method was found to be simple and sensitive.
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6,510
400
Colorimetric estimation of sulphacetamide sodium in bulk and in formulations
Ajay Gaur, RK Gupta, B Shrivastava
May-June 2007, 69(3):464-467
DOI
:10.4103/0250-474X.34567
A new simple and sensitive colorimetric method has been developed for estimation of sulphacetamide sodium in bulk and in pharmaceutical formulations. The method is based on the formation of a yellow colored azo dye by diazotization of sulphacetamide sodium, followed by a diazo-coupling reaction between the resulting product and acetyl acetone. The azo dye exhibited maximum absorbance at 420 nm with apparent molar absorptivity 7.8983 x 10
3
l mol
-1
cm
-1
. Beer's law was found to be obeyed in the concentration range of 2-20 mg/ml. Results of the analysis were validated statistically and by recovery studies.
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3,678
238
Study of anti ulcer activity of sodium metavanadate on alcohol and pylorus ligation induced gastric ulcers in rats
PB Suthar, SM Jain, AA Mehta, DD Santani
May-June 2007, 69(3):454-456
DOI
:10.4103/0250-474X.34563
The present study was designed to evaluate the effects of sodium metavanadate against experimentally-induced gastric ulcers. In an attempt to establish the antiulcer effect and its mechanism of action, sodium metavanadate (3, 5 mg/kg, i.p.) was studied in ethanol and pylorus ligation-induced gastric ulcer models. Sodium metavanadate significantly reduced ulcer index in both the ulcer models. Besides it showed significant reduction in total acid out put along with significant rise in total carbohydrates and mucin activity in gastric juice in pylorus ligation model. Therefore, it is suggested that sodium metavanadate possesses significant antiulcer activity. The probable mechanisms for its antiulcer effect can be attributed to decrease in acid secretion and increase in mucoprotective substances.
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© 2006 - Indian Journal of Pharmaceutical Sciences | Published by
Medknow
Online since 20
th
April, 2006