A rapid assay procedure based on RP-HPLC has been developed for the simultaneous determination of metformin and glimepiride in dosage form. The HPLC determination was carried out on a μBondapak C18 (300x3.9m m) 10μm with use of a flow rate of 1.0 ml/min. The programming regime was, 0-5.8 min at 265 nm, 5.8-9.0 min at 230 nm and 9.0-11 min again at 265 nm. The calibration graphs were linear in the range of 400-600 and 1.6-2.4 μg/ml for metformin and glimepiride respectively with correlation coefficient of 0.9999 for both.

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Bark extracts of Saraca asoca (Roxb.) de Willde were investigated for in vitro antibacterial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Proteus vulgaris, Bacillus aureus and Klebsiella pneumoniae at 4 mg/ml using agar well diffusion method. The ethanol and distilled water extracts showed significant broad spectrum antibacterial activity.

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Matrix tablets of glipizide were formulated using two mucoadhesive polymers namely sodium carboxymethylcellulose and hydroxypropylmethylcellulose and with and without ethylcellulose and the tablets were evaluated. Tablets formulated employing sodium carboxymethylcellulose or hydroxypropylmethylcellulose and with ethylcellulose provided slow release of glipizide over a period of 12 h and were found suitable for maintenance portion of oral controlled release tablets. Glipizlde release from these tablets was diffusion controlled and followed zero order kinetics after a lag time of 1 h and up t o 90 per cent release. The matrix tablets exhibited good mucoadhesion in the small intestine for 10 h as evaluated by X-ray studies. Two layered tablet formulations, designed with an immediately releasing layer consisting of glipizide and a super disintegrant (Ac-Di-Sol) and a slow releasing matrix consisting of glipizide in sodium carboxymethylcellulose or hydroxypropylmethylcellulose and ethylcellulose as second layer, gave release close to the theoretical sustained release needed for glipizide based on its pharmacokinetic parameters.

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Mebendazole and β-cyclodextrin molecular inclusion complexes and mebendazole solid dispersions with polyethylene glycol 6000 were prepared by solvent method in different mixing ratios to increase the rate and extent of dissolution and absorption of mebendazole for an effective chemotherapy of human echinococcosis. The enhancement of dissolution of mebendazole was dependent on the carriers used and the nature of presentation of mebendazole in the carriers (physical mixturelsolid dispersion/molecular inclusion). The differential scanning calorimetry indicated the solid inclusion complex formation of mebendazole and β-cyclodextrin at 1:2 molar ratio and mebendazole-polyethylene glycol solid dispersion at 1:4 weight ratio. Stability study reported a significant decline in the potency of mebendazole in all mebendazole-polyethylene glycol solid dispersions. Dissolution rate and dissolution efficiency of mebendazole were improved by both molecular inclusion complexes and solid dispersions of all mixing ratios than the corresponding physical mixtures and pure drug, 1:2 mebendazole-βcyclodextrin showing the highest dissolution among all the preparations. As mebendazole has been reported to undergo extensive first pass metabolism, also a single dose plasma level bioavailability study in rabbits was conducted to confirm the bioavailability performance of mebendazole from the 1:2 mebendazole-βcyclodextrin complex. In the study, not only a statistically significant (p<0.05), but also a great improvement in bioavailability of mebendazole was achieved with 1:2 mebendazole-βcyclodextrin complex as compared to its physical mixture. Bioequivalency study was also performed for 1:0.5 mebendazole- bcyclodextrin complex and 1:4 mebendazole-polyethylene glycol solid dispersion (which were equivalent to each other in dissolution behavior) and this study showed a result opposite to what was expected on the basis of their in vitro drug release profiles. The reported risks in the use of cyclodextrins and the observed stability problem associated with mebendazole-polyethylene glycol solid dispersions were considered in deciding a choice for the treatment of human echinococcosis.

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The effect of alcoholic extract of dried fruits of Carica papaya were investigated in rats to evaluate the antiulcer activity by using pyloric ligation and aspirin-induced gastric ulcer. The parameters taken to assess antiulcer activity were volume of gastric secretion, free acidity, total acidity and ulcer index. The results indicate that the alcoholic extract significantly (P<0.001) decreases thevolume of gastric acid secretion, free acidity, total acidity and ulcer index with respect to control.

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The present investigation was designed to prepare chitosan microspheres and evaluate the in vitro release pattern of the drug isoniazid. The microspheres were formulated by glutaraldehyde cross-linking method using various concentrations of chitosan. The prepared microspheres were evaluated for drug content, particle size distribution, stability studies and compared with marketed tablets. The percentage of entrapment obtained was 60 %. In vitro release studies were carried out in 0.1 N HCI and 88.1, 83.8, 79.3 and 73.0 % of drug was released from 0.5, 1.0, 1.5 and 2.0 % of chitosan microspheres respectively after 8 h. Stability studies were carried out at different temperatures and found that all the formulations were more stable at 4o and room temperature.

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Transdermal drug delivery of ethinylestradiol and levonorgestrel for contraception and hormone replacement therapy was attempted from the proniosomal gel formulations prepared by coacervation phase separation technique. The proniosomes were hydrated with saline solution to form niosomes. Proniosomal gels were prepared from nonionlc surfactants e.g. Span 20, 40, 60 and 80 with egg lecithin, Brij 58, dicetyl phosphate, soya lecithin and cho1esterol.These gels were characterized and evaluated for particle size distribution, spontaneity, entrapment efficiency and stability. In vitro drug diffusion was studied through cellophane membrane and rat skin. The estrogenic activity in immature albino rats was also studied. The formulations prepared using Span 20 and Span 40 (3:1) have shown better in vitro and in vivo performance. This study indicates that proniosomal gel preparation of contraceptive hormones may be used as an effective means for population control programme.

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A new simple, sensitive spectrophtometric method in ultraviolet region has been developed for the determination of sibutramine hydrochloride in bulk and in capsule dosage form. Sibutramine hydrochloride shows maximum absorbance at 220 nm. Beer's law was obeyed in the concentration range 10-50 μg/ml. Results of the analysis were validated statistically and by recovery studies.

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An HPTLC method has been developed for the simultaneous estimation of gliclazide and rosiglitazone from its combined dosage form. The method involves separation of components by TLC on a precoated silica gel 60 F 254 plate using a mixture of toluene:ethylacetate:methanol (85:5:10) as the mobile phase. Detection of the spot was carried out at 225 nm in absorbance mode. The retardation factors of gliclazide and rosiglitazone were found to be 0.36 and 0.47, respectively. The linearity range was found to be 1-3 μg/10 μI for gliclazide and 0.05-0.1 5 μg/10 μ1 for rosiglitazone.

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Spherical crystallization was carried out by ammonia diffusion method to achieve agglomerates of primary crystals of the drug. Both agglomerated and primary crystals were subjected to measurement of micromeritic properties, compressibility, powder compaction properties and effect of crystal shape on tablet strength. Dispersible tablets of agglomerated ampicillin trihydrate were prepared using suitable excipients in formula and were evaluated for various physical parameters.The tablets gave comparable drug release with that obtained from a market product.

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Ultraviolet absorption spectrophotometric method for the estimation of celecoxib, rofecoxib, meloxicam and nimesulide in pure form and in pharmaceutical formulations has been developed. The solvents employed were 10% (v/v) aqueous dimethylsulfoxide for rofecoxib, 10% (v/v) aqueous dimethylformamide for meloxicam, 20% (v/v) aqueous acetonitrile for celecoxib and nimesulide. 0.1 N sodium hydroxide was also used as solvent for all the drugs except rofecoxib. All the solvents were found to give accurate, sensitive and reproducible results for the estimation of drugs in pure form. These solvent systems could also be used for the estimation of drugs from solid formulations. For the estimation of drugs in pure form, method involving the use of 0.1 N sodium hydroxide was found to be relatively more precise, economical and safer than the one involving the use of organic solvents. For the estimation of celecoxib, rofecoxib and meloxicam from the formulations, on the other hand, the use of organic solvents gave better results and should be preferred. For the estimation of nimesulide from formulations, however, again 0.1 N sodium hydroxidewas found to be a better solvent.

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A simple extractive spectrophotometric method has been developed for the estimation of clarithromycin in both pure and pharmaceutical dosage forms. The method is based on the formation of an ion-pair complex of the drug with bromocresol green, which is extracted into chloroform. The absorbance of the chloroform layer is measured at 415 nm against a reagent blank. The method has been statistically evaluated.

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Crude ethanol extract of Celosia argentea leaves was successively fractionated with petroleum ether, solvent ether, ethyl acetate, butanol and butanone. The ethanolic extract and various fractions were investigated for antiinflammatory activity in rats at a dose of 100 mg/kg i.p. The ethanolic extract exhibited antiinflammatory activity when compared to control and was comparable to that of standard drug aspirin.

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In the present study, the effect of Withania somnifera extracts prepared by two different methods on behavioral parameters assessed using open field exploratory behavior, behavioral despair and passive avoidance tests were compared in young and old stressed Wistar rats. Stress was induced on the animals by giving 30 intermittent shocks for 3 s consecutively for 7 d. W. Somnifera extracts prepared with 50% methanol and solvent containing water, ghee and honey were administered orally as fine suspension during the shock period. The results revealed that stress produced depression anxiety and retention deficit in young and old rats. Administration of W. Somnifera methanolic extract 250 mg/kg during shock period in young and old rats attenuated the stress-induced depression and enhanced memory. W. Somnifera traditional extract 250 mg/kg produced memory enhancement in both control and stressed young and old rats. Both the W. Somnifera extracts failed to reverse the stress-induced anxiety. It can be concluded that in comparison to methanolic extract, traditional extract was found to be more active in memory enhancement than anxiolytic and antidepressant activity.

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Some novel heterocyclic compounds have been evaluated for antifertility activity in Wistar rats. Compounds 3 and 4 showed 66.3% and 83.4% antiimplantation potency when compared with control. Compounds 1, 2 and 5-10 did not exhibit any antiimplantation activity. Uterine weight was increased significantly with compounds 3 and 4 when compared to control. Histological studies indicated the increase in the diameter, thickness of endometrium and height of the endometrial epithelium of the uterus revealing estrogenic activity of compounds 3 and 4. The estrogenic activity was significant when compared to control. Compounds have been evaluated for antiinflammatory activity using carrageenan-induced rat paw oedema model. Phenylbutazone (100 mg/kg), was used as the standard. Compounds 1, 2 and 3 exhibited significant antiinflammatory activity at the dose of 15 mg/kg, whereas compounds 5,6 and 7 showed significant antiinflammatory activity at the dose of 30 mg/kg. Compounds 1, 2 and 4-7 exhibited 58.9%, 58.1%, 66.2%, 64.5%, 63.0% and 63.0% inhibition respectively in carrageenan-induced rat paw oedema, while the standard showed an inhibition of 63.8%. Compound 4 exhibited maximum antiinflammatory activity. Analgesic activity of the compounds 1 to 4 was evaluated using acetic acid-induced writhing model at 15 mg/kg. Acetyl salicylic acid (150 mg/kg) was used as a standard. Compounds 2 and 4 showed significant analgesic activity of 67.2% and 66.1% maximum possible effect respectively, when compared to standard acetylsalicylic acid which exhibited 74.9% maximum possible effect.

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Leucaena gum derived from seeds of Leucaena leucocephala has been evaluated as a suspending agent. Suspensions of sulphadimidine powder were prepared with different concentrations of leucaena seed gum, and tragacanth gum, and compared. Studies indicate that this gum may be used as a pharmaceutical adjuvant and as a suspending agent depending on its suspending abilityand the stability of the resulting suspension.

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Peroral multi-drug administration is often associated with severe drug-drug interactions. These interactions can occur either in the gut lumen, at absorptive site or after absorption. Present work was undertaken to study the interaction between atenolol and furosemide at the absorption site. Alteration in the intestinal permeability was studied using rat single-pass intestinal perfusion technique, to assess the changes on administration of single and combination drugs. Permeability coefficient (Peff) of atenolol reduced to a statistically significant level (P<0.05) when co-perused with furosemide, with Peff, values (X10-4 cm/sec) of 0.0686±0.0433 and 0.01 54±0.0326 for drug perfused individually and in combination, respectively, indicating the possibility of drug-drug interaction occurring at the absorption site.

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Prescription monitoring study was conducted to rationalize the prescription writing habits of the physicians and to assess the pharmacy practice at the dispensing section by the pharmacists at the Panjab University Health Centre. Five hundred prescriptions were monitored by random chance method and data were filled as per WHO guideline based prescription monitoring performa. Study reported name, age, sex and disease diagnosed as 100, 38.4, 42, 12.8%, respectively of the total prescriptions. Analgesic antiinflammatory drugs (23.0%) were highly prescribed followed by antibiotics (20.7%), antihistamines (16.7%), gastrointestinal drugs (10.4%), vitamins (6.6%), cardiovascular drugs (5.8%), antiinfectives (5.2%), minerals (3.9%), steroids (3.0%), antiasthmatics (2.2%), antifungal agents (1.5%), vaccineisera (1.0%). Doses were mentioned for 19.3% of the antibiotics prescribed. Diagnosis was written only in 12.8% of the prescription monitored. No written instruction on the container was noticed in any of the dispensed drug by the pharmacist. 85.3% of the prescribed drugs were available from Panjab University Health Centre pharmacy, of which 43.6% were dispensed in loose envelopes (without labeling). Only 17.2% of the patients knew about the nature of medication prescribed to them and 68.3% were aware of the medication. The study highlighted certain lacunae in the area of prescribing, instructions to patients and labeling of drugs. However, a need to monitor the prescriptions was felt by proper involvement of physicians, pharmacists and other staff in order to improve the prescribing practice of the physicians as well as dispensing attitudes of pharmacists.

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The α1a-antagonistic activity of dihydropyrimidinone C-5 amides is analyzed through the Fujita- Ban and Hansch approaches. The analyses have helped to ascertain the role of different substituents in explaining the observed antagonistic activity of these analogues. From both approaches, it is predicted that the more hydrophobic X-substituents and the phenyl or P-cyanophenyl substituents at the 4-position of the piperidine ring are beneficial in raising the α1a-receptor antagonist action of a compound. Likewise, the presence of Fat R4 (the para-position of either phenyl or 2-cyanophenyl ring) further helps in augmenting it. The positions R1 and R3, of the dihydropyrimidinone ring are in favour of Me and H respectively. In addition, a non hydrogenbond acceptor substituent at R3 is least preferred. Substituents at position R6 of this ring, however, by either H or CH2OMe leads to better potency compounds.

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The effect of sodium starch glycollate, a dispersant on the dissolution of ferrous fumarate capsules was studied. Ferrous fumarate was formulated into capsules with sodium starch glycollate and the capsules were evaluated (immediately after preparation and after storage at exaggerated conditions of temperature and relative humidity) for physical parameters, disintegration, drug content, and dissolution rate. Marked increase in the dissolution of ferrous fumarate was observed when sodium starch glycollate was included in the capsule formulation. This formulation gave fast and rapid dissolution of ferrous fumarate fulfilling the BP 1999 dissolution requirement.

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Spectrophotometric, spectrofluorimetric and high performance liquid chromatographic methods for the determination of hexamine in pure form and in hiprex tablet are described Both hexamine and hiprex form stable yellow colored 3,5-diacetyl-1,4-dihydrolutidinae t 100o when treated with acetylacetone in phosphate buffer (pH 6.0). The chromogen shows absorption maximum at 410 nm and a fluorescence emission maximum at 510 nm. In the case of hiprex, Beer's law linearity was observed in the concentration ranges of 10-150 μg/ml, 3-30.5 μg/ml and 0.02-0.35 μg/ml in spectrophotometric, fluorimetric and high performance liquid chromatographic determinations, respectively. The common additives usually present in the tablet did not interfere in the proposed methods.

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Bupropion, a monocyclic aminoketone is used primarily for the treatment of major depression. On oral administration, the drug undergoes extensive first pass metabolism. Delivery of bupropion via transdermal route would minimize some of the deficiencies associated with the oral delivery. In the present study, effect of various vehicles and penetration enhancers on diffusion kinetics of the salt and free drug through the human cadaver skin was studied using a modified diffusion cell. The diffused drug was quantified by UV spectrophotometry at 298 nm in phosphate buffer saline. A 100-fold increase In permeability rate was observed with free base compared to salt form. As a vehicle, alcohol was found to be superior compared to phosphate buffer saline and propylene glycol in permeation of free base. Permeation was enhanced by up to 30 %with linseed oil and myristic acid when propylene glycol was used as a vehicle. The study provides suitable clues for delivery of bupropion by the transdermal route..

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Several N1-(arylidine hydrazidomethyl)-indoles were prepared by condensing N1-indolyl acetyl hydrazine with different substituted benzaldehydes. 2-(substituted aryl)9-(N1-indolyl acetamidyl)- 4-oxo-thiazolidines were prepared by condensing N1-(arylidine hydrazidomethyl)-indoles with mercaptoacetic acid followed by the Knoevanagel condensation with benzaldehyde leading to the 5-benzylidine derivatives. The IR, 1HNMR and mass spectral studies confirmed the structures of these compounds. The synthesized compounds were tested in vitro against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Salmonella typhi, Pseudomonas aeruginosa, Proteus vulgaris, Candida albicans and Aspergillus niger. The zones of inhibition were compared with the standard drugs under the identical conditions.

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A new simple, sensitive spectrometric method was developed on the basis of a colour reaction of formoterol with diazotised p-nitroaniline.The method is based on formation of yellow chromophore which has an absorption maxima at 398 nm and obeys Beer's law in the concentration range of 1- 40 μg/ml. Results of the analysis were statistically validated by recovery studies. The method was found to be suitable for routine determination of formoterol fumarate in rotacap formulation.

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The enzyme, cyclooxygenase is now well recognized to exist in two isoforms i.e. cyclooxygenase-1 and cyclooxygenase-2. Cyclooxygenase-1 is constitutively expressed serving the so-called 'house-keeping' role while, cyclooxygenase-2 was thought to be expressed in pathophysiological conditions such as inflammation. It is now known that cyclooxygenase-2 plays a key role in a wide range of physiological processes. In the current article the multifaceted profile of cyclooxygenase-2 enzyme in th'e body is described indicating its potential clinical and diagnostic applications. It is also discussed how the currently available selective cyclooxygenase-2 inhibitors can affect the normal physiological role of cyclooxygenase-2 enzyme.

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The n-hexane soluble fraction of the ethanolic extract of the roots of the plant Trewia polycarpa yielded a rare triterpenoid of taraxarane series, 3β-acetoxytaraxaren-14-en-28-oic acid (I) whose identity has been confirmed by spectroscopic studies. This is the second report on the isolation of I from nature and first from the genus Trewia. Compound I exhibited prolongation of prothrombin time and also showed mild antibacterial and antifungal activities.

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A rapid and sensitive spectrophotometric method has been developed for the determination of two antihistamines, mebrophenhydramine hydrochloride and hydroxyzine hydrochloride in pure form and in different dosage forms. The method is based on the formation of stable donor-acceptor complex between the studied antihistamines and chloranilic acid in acetonitrile. The resulting intensely coloured purple chloranilic acid radical anion possesses a characteristic maximum at ' 535 nm. Beer's law is obeyed over the concentration range 25-150 μg/ml in respect of both drugs. The stoichiometric ratio and stability constant of each charge-transfer complex are determined and the mechanism of the reaction is discussed. The molar absorptivity and Sandell sensitivity of the charge-transfer complexes formed are reported. Statistical treatment of the experimental results indicates that the method is precise and accurate. Excipients used as additives in pharmaceutical formulations did not interfere in the proposed procedure. The procedure described was successfully applied to the determination of the bulk drugs and their pharmaceutical formulations.

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Agents having selectivity to α1a, α1b, and α1d adrenoceptors could be useful in generation of effective molecules for treatment of variety of diseases. In order to gain an insight into the structural principles governing subtype selectivity, three dimensional quantitative structural activity relationship studies have been performed on a set of arylpiperazines for their α1a-adrenergic receptor antagonistic activity by using the logico-structural based approach for pharmacophore mapping. All compounds were superimposed on the identified biophores and three dimensional quantitative structurel activity relationship models were developed. The resulting models exhibited good r2(>0.80) values. Among several models, one model of comparable probability was selected on the basis of r2>0.80, chances≤0.10, sizes≤3 and match>0.30, which might show optimum desired effects.

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Inflammation is a biological response to a series of chemical reactions whose major function is protection from infection and the resolution of tissue damage caused by injury. There are several mediators released during the process of inflammation. Activation of phospholipase-A2 (PLA2) family is a key step in the production of precursors in biosynthesis of inflammatory lipid rnediators. Platelet activating factor, cyclooxygenase-2, leukotrienes, nerve growth factor, inducible nitric oxide synthase, bradykinins, adhesion molecules, nuclear factor-kB and cytokines are also important mediators for inflammation. There are several agents, which inhibit the endogenous mediators that can be used for the treatment of inflammation. Apoptosis is another important mechanism, where several agents that act by different mechanisms of action can treat the inflammation.

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A series of bis-(acridine-4-carboxamide) analogues possessing significant cytotoxicity against P388 leukemia cell cultures, which were designed as bis-DNA intercalating agents, was subjected to the quantitative structure activity relationship analysis. Quantitative structure activity relationship studies by Fujita-Ban model gave excellent correlations (correlation coefficient, r=0.997) for the 24 compounds included in the final regression analysis. It was observed that substitutions on position 5 favor the activity while any group on position 6 decreases the activity strongly. Theseresults will be useful in designing 'lead' compounds to be useful as bis-DNA intercalators for the therapy of leukemia.

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