In the present study, a novel series of 2-methyl-qninazolin-4(3H)-ones were synthesized and characterized by IR, 1H-NhlR, 13C-NMR and mass spectral analysis. The synthesized compounds were screened for analgesic (100, 200 and 400 mg/kg), antiinflammatory (200 and 400 mg/kg), antibacterial (Bacillus subtilis, Bacillus cereus, Staphylococcus epidermidis, Micrococcus Iufeus and Escherichia coli) and antifungal (Candida albicans and Aspergillus niger) activities. The minimum inhibitory concentrations of the compounds were also ascertained by agar dilution method. Graded dose response was observed with the compounds. 6,8-dibromo-2-methyl-3-(4'-morpholino-phenyl)- 4(3H)-one (2) exhibited the highest analgesic and antiinflammatory activity. 6-Bromo-2-methyl- 3-(4'-morpholino-phenyl)-quinazolin-4-(3H)-one (1) was found to exhibit the highest antimicrobial activity. All the compounds exhibited significant activity against the bacteria and fungi tested.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

Transdermal films of ketotifen fumarate were formulated using combination of eudragit L 100:hydroxypropylmethylcellulose and ethyl cellulose:hydroxypropylmethylcellulose polymeric combinations plasticized with polyethylene glycol 400. Effect of permeation enhancers like dimethyl sulfoxide and propylene glycol at different concentrations were studied on skin permeation kinetics by Keshary-Chein diffusion cell. The films were also evaluated for various physicochemical properties. From in vitro diffusion studies it was found that there was increase in permeation rate with increase in permeation enhancer concentration. Both water vapour transmission rate and skin permeation rate followed zero order kinetics. It was concluded that films of eudragit L 100: hydroxy propyl methylcellulose and ethyl cellu1ose:hydroxypropyl methylcellulose polymeric combinations may be feasible for formulating rate controlled transdermal therapeutic system of ketotifen fumarate for effective control and prophylaxis of allergic asthma.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

Mannich reaction involves condensation of a carbonyl compound with formaldehyde and a secondary amine. It is a mild procedure for obtaining unsaturated ketones (usually -CO-C=CH2). Mannich bases derived from chalcones and 2-dimethyl amino ethyl benzo suberone methiodide have shown promise as anticancer agents, I-Ethyl-6-fluoro-l,4-dihydro-4-oxo-7-[(N4-(5'-chloro-3'- thiosemicarbazono-isatin-I-yl) methyl)-N-piperazinyll-3-quinolinec arboxylic acid had been foundto be more active than norfloxacin.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

Glipizide microcapsules wlth a coat consisting of alginate and a mucoadhesive polymer such as sodium carboxymethylcellulose, methylceilulose, carbopol and hydroxypropylmethylcellulose were prepared by an orifice-ionic gelation process and were investigated with a view to develop mucoadhesive microcapsules. The resulting microcapsules were discrete, large, spherical and free flowing. Microencapsulation efficiency was 60-84%. The microcapsules exhibited good mucoadhesive property in the in vitro wash-off test. Glipizide release from these mucoadhesive microcapsules was slow and extended over longer periods of time and depended on the composition of coat of the microcapsules. Drug release was diffuslon controlled and followed zero order kinetics after a lag period of 1 h. In the in vivo evaluation, alglnate-carbopol microcapsules could sustain the hypoglycemic effect of glipizide over a period of 14 h. These mucoadhesive microcapsules are, thus, suitable for oral controlled release of glipizlde.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

A reverse phase high performance liquid chromatography method for the simultaneous estimation of tizanidine hydrochloride and nimesulide in tablets is presented. Cynopropyl column is used to retain tizanidine hydrochloride (k`=1.52) and also have reasonable retention for nimesulide (k`=2.37) with a good resolution and peak symmetry. Effect of change of chromatographic conditions such as pH, %organic modifier (acetonitrile) in mobile phase on retention of drugs were studied and optimized. Both the drugs showed linear response in the concentration range employed (tizanidine hydrochloride, 1.2-2.8 μg/ml and nimesulide, 60-140 μg/ml) and was validated by least squares method at 95% confidence level. The results of analysis have been validated statistically and by recovery studies. The mean recoveries obtained for tizanidine hydrochloride and nimesulide were 99.6% and 100.1%, respectively.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

AntiHlV and antibacterial activities of 2-substituted-(1,3,4)-thiadiazolo (2,3-b) quinazolin-5(4H)- ones, were determined. Among the compounds tested for antiHlV activity, the compound VA5 gave maximum protection against HIV-2 (ROD).The compound VA2 (at 100μg/rnl) exhibited equivalent antibacterial activity with the standard ciprofloxacin (at 10 μg/ml) against Klebsiella pneumoniae, Bacillus subtilis, Staphylococcus epidermitis, Shigella flexnari and Citrobacter ferundi.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

Metoprolol tartrate was formulated as biodegradable microspheres using chitosan by the phase separation emulsification technique. Microspheres of 1:0.5, 1:1 and 1:2 drugs to carrier ratios were prepared and thermally cross-linked. Drug to carrier ratio 1:1 showed maximum percentage yield and highest drug entrapment. The size range of the microspheres varies from 3.5 to 31.5 pm. UV and DSC studies were carried out to confirm the presence and stability of the drug in the microspheres. Short-term stability studies were carried out at different temperatures. In vitro release studies were carried out at different pH for a period of 10 h and compared with the pure drug. The release of rnetoprolol tartrate from the chitosan microspheres was found to be sustained.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

A novel approach, using artificial neural networks, has been made to analyse multicomponent sample by UV spectrophotometry. Artificial neural network, based on back propagation paradigm, was custom developed to process the ultraviolet spectral data. A typical drug combination, diclofenac sodium and paracetamol, was chosen as model drug mix to evaluate the suitability of neural approach to quantify the components in a mixture. The ability of the artificial neural network to predict the concentrations was tested with several spectra of known ratios of the drugs under several neural network parameters. Our study indicated that artificial neural networks could produce accurate and precise results and could be used for routine analysis of multicomponent samples.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

A simple and reproducible spectrophotometric method has been developed for the estimation of cefpodoxime proxetil. This method is based on the reaction of the drug with ferric chloride and potassium ferricyanide, which forms a green chromogen exhibiting maximum absorption at 780 nm.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

Piroxicam, a nonsteroidal antiinflammatory agent, is widely used as a first line drug in the symptomatic relief of rheumatoid arthritis and osteoarthritis. One of the major problems with this drug is its very low solubility in biological fluids, which results into poor bioavailability after oral administration. Therefore, solid dispersions of piroxicam with polyethylene glycol 400 and polyvinyl pyrolidone K-30 were prepared to increase its water solubility. Solid dispersions of piroxicarn were prepared using polyethylene glycol 400 as a water soluble carrier (1:4, 1:8, 1:12, 1:16, 1:20 by weight) employing solvent evaporation method. The drug release profile was studied according to USP XXlll monograph in simulated gastric fluid. Piroxicam was released at a much higher rate from solid dispersions containing polyethylene glycol 400 and physical mixture as compared to that of pure drug powder. Faster dissolution rate was observed in 1:12 drug:carrier ratio. Physical mixture of piroxicam and polyethylene glycol 400 in a same ratio released the drug at a slower rate as compared to that of solid dispersions. Solid dispersions of piroxicam were also prepared using PVP K-30 as a water-soluble carrier (1:1, 1:2, 1:3, 1:4 and 1:5 by weight) employing solvent evaporation method. Piroxicam was released at a much higher rate from solid dispersion and physical mixture as compared to that of pure drug powder. Faster dissolution was exhibited by solid dispersion containing 1:4 ratio of drug: PVP compared to physical mixture and pure drug. The increase in dissolution rate of the drug may be due to increase of wettability, hydrophilic nature of carrier and also possibly due to reduction in drug crystalinity.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

Some new Schiff bases (1a-g), 4-thiazolidinones (2a-g) have been synthesized and tested for their antibacterial activity. The structures of these compounds have been established on the basis ofelemental analysis and spectral data (IR and 1H NMR).

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

Over the last two decades attempts have been made repeatedly and sometimes successfully to carry agents into the body through the intact skin by using lipid suspension. Use of composite lipidic agent carrier (liposomes, niosomes) was not successful to date due to the inability of such vesicles to pass through the narrow (<30 nm) intercellular passage in the outer skin layers. A solution to this problem is the use of orders of magnitude more deformable supramolecular aggregates, transfersomes. Such innovative drug carriers are driven across the skin by the naturally occurring transdermal gradients and promote transfer of various agents very efficiently and reproducibly. Transfersomes were successfully used animal and humans also for the transcutaneous and protein delivery. In this review we discuss the theoretical prospect, basic principle behind the development, mechanism of penetration and applications of transfersomes.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

The dissolution characteristics of ketoprofen enantiomers from matrices containing chiral excipients sodium alginate, β-cyclodextrin and hydroxypropylmethylcellulose under three different pH values (pH 1.5,4.6 and 7.4) in aqueous environment were determined. An achiral excipient, Eudragit RL 100, was used to generate a control dissolution profile. This study demonstrates that release of ketoprofen enantiomers from formulation containing hydroxypropylmethylcellulose matrix at pH 7.4 is stereoselective and statistically significant. It is observed that the release of S-ketoprofen (eutomer) was faster than the R-ketoprofen (distomer). Further, it indicates that the differential release is pH-dependent. The research implication is that by choosing the appropriate chiral excipient and other formulation conditions one can deliberately manipulate the release of a specific enantiomer from a racemic therapeutic. This intended stereospecific retardation/acceleration in the release of enantiomers could be exploited for the design of stereoselective drug delivery systems.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

Flurbiprofen is an analgesic and antiinflammatory drug with poor water solubility and compressibility. Flurbiprofen conventional drug crystals were converted into spherical crystal agglomerates via the spherical crystallization technique using acetone-water-hexane solvent system. The various parameters optimized were type, amount and mode of addition of bridging liquid, temperature, and agitation speed to get maximum amount of spherical crystals. These were characterized for micromeritic properties (particle size and shape, flowability), packability (bulk density), wettability (contact angle) and compressibility. It was revealed from the study that spherical agglomerates exhibited improved flowability, wettability and compaction behaviour.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

Three dimensional quantitative structural activity relationship studies have been performed on a series of 17 compounds of 1,3,4 triaryl-3-pyrrolin-2-ones, for their cyclooxygenase-2 inhibitory activities by using the logico-structural based pharmacophore mapping approach employing APEX 3D software program. Among several biophoric models, two models were selected based on statistical consideration; chance ≤0.15, correlation coefficient >0.75 and match >0.65. Both models showed three common biophoric sites, one being oxygen atom, second being it's lone pair and third being center of phenyl ring at 1st position and center of phenyl ring at 4th position for model No. 1 and 2 respectively. In model No. 2, three secondary sites are indicated. At one site, the steric refractivity contributes positively, whereas at the remaining sites both steric refractivity and totalrefractivity contribute negatively. Among the two models, model No.1 has better acceptability having r2=0.91, Root mean square error of approximation =0.10, Root mean square error of prediction "leave one out"=0.11 and n=17. In this model there are four secondary sites, which are total refractivity, H-acceptor, hydrophobicity and steric refractivity and all these found to contribute negatively.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

Ibuprofen and rifampicin are high dose drugs and are known for having compression related problems. There drugs were modified to directly compressible forms by granulation and spherical crystallization technique. In granulation technique, drug was mixed with pre-gelatinized starch and sprayed with polyvinyl pyrrolidone 20% in isopropyl alcohol as binder and wet mix was passed through sieve no. 10, 16, 22 and 44 and dried. In spherical crystallization technique, a centrifuge tube containing supersaturated solution of drugs was rotated at 500-600 rpm and recrystallized by non-solvent addition along with suitable bridging liquid and formed spherical agglomerates were separated from solvent, non-solvent and bridging liquid by centrifugation and dried. The experimental parameters like effect of type of bridging liquid, concentration of bridging liquid, agitation speed, effect of temperature and mode of addition of bridging liquid on formation of spherical crystals were optimized. The resulted granules and crystals produced by respective technique were mixed with disintegrant and lubricants and compressed on running single stroke tablet compression machine by direct compression. The prepared tablets of both drugs were found to satisfy all quality control requirements of tablets mentioned in the Indian Pharmacopoeia.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

A simple reversed-phase liquid chromatography method was developed for the quantitative determination of cyclooxygenase-2 inhibitor celecoxib in small volume of rat plasma. The method is simple, sensitive, and highly selective and involves single step extraction of plasma with methanol, with as low as 0.1 ml of rat plasma. The retention time of celecoxib was 5.4 min. The method has been validated for linearity precision, accuracy and inter- intra day variation. Recoveries of celecoxib were around 78 % over the calibration curve range. The method was found to be suitable in studying the pharmacokinetic aspects of celecoxib during the preliminary studies in rats.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

Two visible spectrophotometric methods have been developed for estimation of loratadine from tablet formulation. These visible spectrophotometric methods are based on formation of chloroform extractable coloured complex of drug with cobalt thiocynate and bromophenol blue. The coloured complex formed with cobalt thiocynate showed absorbance maxima at 624.5 nm and linearity in the concentration range of 1.2-3.6 mg/ml of loratadine while the coloured complex formed with bromophenol blue showed absorbance maxima at 413 nm and linearity in the concentration range of 0-120 μg/ml of loratadine. Results of analysis for both the methods were validated statistically.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

The purpose of this investigation is to evaluate the bioavailability in rats after oral administration of puerarin or puerarin-phospholipid solid dispersion. A simple and sensitive HPLC method was developed for determination of puerarin in rat plasma. It was shown that its plasma concentration reached a peak of 0.35 μg/ml at 0.64 h after oral administration (50 mg/kg). However, after intake of puerarin-phospholipid solid dispersion, a peak of 0.78 μg/ml occurred at a later time, 1.06 h. There was a significant difference in the mean area under the concentration-time curves (AUC)between the free drug and the puerarin-phospholipid solid dispersion.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

Four simple and sensitive procedures (methods A, B, C and D) for the assay of lisinopril in pure form and formulations are described. Methods A and B are based on the condensation of lisinopril (acyclic imino acid) with ninhydrin (indane-1,2,3-trione hydrate) in the presence of ascorbic acid (method A, λmax 560 nm) or ascorbic acid (method B, λmax 520 nm). Method C is based on the initial , formation of water insoluble adduct involving lisinopril and phosphomolybdic acid, followed by release of phosphomolybdic acid from the adduct with acetone and color development with cobalt nitrate-ethylenediaminetetraacetic acid disodium salt complex (λmax 840 nm). Method D is based on the formation of colored radical anion on treating lisinopril with 2,3-dichloro,5,6-dicyanol, 4-benzoquinone (λmax 4 60 nm). The variable parameters in all these methods have been optimized. The results were statistically validated.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

Panchagavya is a term used in Ayurveda to describe the five important bovine products, milk, curd, ghee, urine and dung. Several formulations based on panchagavya are reported in Ayurvedic texts. One such formulation, Chandanadi Yamak was tested in the present study for its topical wound healing activity. Studies were conducted in male Wistar rats. Two wound models, incision wounds for tensile strength and excision wounds for wound contraction were employed along with histopathological evaluation. The application of the test formulation alone promoted wound contraction and reduced the time for wound closure showing healing potential comparable to marketed framycetin sulphate cream (1% w/w).The histological studies reveal complete healing with the test formulation showing good keratinization, epithelialization, fibrosis and angiogenesis. The present study demonstrates the wound healing potential of the test formulation.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

Effect of carbontetrachloride treatment on hepatic and brain antioxidant status in rats pretreated with aqueous extract of Phyllanthus amarus Linn. (Euphorbiaceae), nirocil (a tablet made up of aqueous extract of P. amarus), phyllanthin (a bioactive lignan from p amarus), and silymarin were studied. Plasma aspartate aminotransferase and alanine aminotransferase were estimated to monitor the extent of hepatocellur damage. Tissue lipid peroxide, ascorbic acid and total protein levels were used as the markers for functional and antioxidant efficiency of liver and brain cells. Phyllanthin reversed the elevated plasma aminotransferase levels but did not affect hepatic antioxidant status. In all the paradigms tested for hepatoprotection, nirocil, silymarin and aqueous extract (90 mg/kg) showed significant protection. There was a drastic impairment in the functional and antioxidant status of brain on treatment with carbontetrachloride. None of the drugs except silymarin showed good protection against carbontetrachloride-induced lipid peroxidation in the brain, but all these produced a significant increase in the protein levels. All the drugs administered, augmented the ascorbate levels in liver and brain, with the aqueous extract of p. amarus clearly outdoing the others.

[ABSTRACT]   Full text not available  [PDF] [CITATIONS]

For thousands of years human beings have made medicines from the plants, which surrounded them. In recent times, pharmaceutical companies have gathered or synthesized the active compounds from these plants, stabilized them, and intensified them for broad distribution and long (and profitable) shelf lives. Its well known that every substance when used in the right dose andway has medicinal value but it is wrong to believe that natural products are free of any side effects. To mention an example is honey, when its taken in excess can cause liver damage due to its high fructose content. The only reason why people suffer from the side effects of the medicine is because they are not used properly. Some of the medicinal plants that were taken for discussion are, milk thistle, black cohosh, bilberry, hawthorne, horse chestnut, honey, turmeric, White, red, purple, yellow and green vegetables and fruits, ephedra, grapefruit juice and drug interactions and saw palmetto.

[ABSTRACT]   Full text not available  [PDF]

The petroleum ether and chloroform extracts of the roots of Cyclea burmanni (Fam. Menispermaceae) have been found to possess significant antifertility effect in rats. Both these extracts exhibited partial and complete resorption of implants at 200 and 400 mg/kg body weight dose levels. In estrogenic activity study, both the extracts increased uterine weight and caused opening and cornification of vagina in immature rats. The present work justifies its effectiveness in preventing pregnancy in all rats when administered at 400 mg/kg p.o.

[ABSTRACT]   Full text not available  [PDF]

The effects of granule size and concentration of magnesium stearate as lubricant on the dissolution rate of paracetamol tablets were studied. The results obtained show that dissolution rate was increased as the granule size of the tablet was increased for tablets prepared with 1.5% magnesium stearate as lubricant. However, tablets prepared with different granule size, exhibited no pronounced effect on the dissolution characteristics when concentration of magnesium stearate was used as 0.75%.

[ABSTRACT]   Full text not available  [PDF]