De novo drug design is an iterative process in which the three-dimensional structure of the receptor is used to design newer molecules. It involves structure determination of the lead target complexes and the design of lead modifications using molecular modeling tools. It can also be used to design new chemical classes of compounds that present similar substituents to the target using a template or scaffold, which is chemically distinct from previously characterized leads.

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Two simple economical procedures for simultaneous estimation of ibuprofen and methocarbamol in two-component tablet formulation have been developed. The method employs Q-analysis and two-wavelength method. Ibuprofen has absorbance at 222 nm and-methocarbamol has absorbance maxima at 224 nm and 272 nm. The isoabsorptive point of ibuprofen and methocarbamol was found to be 231.4 nm. Both drugs obeyed the Beer's law in the concentration ranges employed for these methods. The results have been validated statistically and by recovery studies.

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The present paper describes three simple, accurate, rapid and precise visible spectrophotometric methods for the estimation of levofloxacin in tablet formulations. Methods A and B were based on the formation of lon- association complex of the drug with Eriochrome black T and bromocresol green. The absorbance of chloroform extracted complexes was measured at 490 and 420 nm, respectively. Method C was based on the formation of blue coloured chromogen with Folin-Ciocalteau reagent which showed maximum absorbance at 720 nm. The optical characteristics and the statistical analysis for all the methods were satisfactory. Interference studies were carried out using common excipients and the percentage recovery of levofloxacin using method A, B and C was found to be 99.9, 101.6, 100.5 %, respectively.

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Two spectrophotometer methods have been developed for the determination of nateglinide in pure and its pharmaceutical dosage from. In UV spectrophotometric method, nateglinide showed absorption maxima at 210 nm in ethanol (95 %), where as in visible spectrophotometric method it imparted a purple color with Ninhydrin reagent showing absorption maxima at 570 nm. The methods obeyed beer's law in the concentration range of 20-100 μg/ml and 200-1000 μg/ml, respectively. The methods are statistically evaluated for accuracy and precision.

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Propranolol hydrochloride matrix tablets were prepared with hydroxypropyl methylcellulose polymer to control the release of drug with a view to develop twice daily sustained release dosage form. The resulting matrix tablets prepared with hydroxypropyl methylcellulose K4M fulfilled all the official requirements of tablet dosage forms. The in vitro drug release was measured in aqueous solutions for a total period of 12 h using 1.2 pH buffer for first 1 h and pH 7.5 buffer for the rest of period. The drug release was within the limits of predetermined set vis-à-vis USP requirements. The results provide a method of achieving sustained drug action through uniform drug release.

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Two, simple, accurate, rapid and sensitive methods have been developed for the estimation of tranexamic acid in pharmaceutical dosage forms. Method A is based on the oxidation of tranexamic acid with potassium permanganate in an alkaline medium giving green coloured chromogen, which shows maximum absorption at 620 nm while method B is based on condensation of the drug with p-dimethylaminobenzaldehyde in sulphuric acid to form yellow coloured species which shows maximum absorption at 410 nm against reagent blank. In both the methods, Beer's law was obeyed in the concentration range of 10-80 μg/ml.

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Ayurveda, the ancient system of herbal medicine is growing popular world wide, but a number of factors such as standardization and stability studies are still at an infant stage for an ayurvedic product. This research paper deals with the study of interaction in some ayurvedic preparations containing vidang with loha bhasma under different storage conditions. The formulations selected were Vidangadi Lauha, Candanadi Lauha and Navayasa Churna. The ratio of vidang and loha bhasma in these preparations were 1:9 and 1:12, hence test samples containing this ratio and pure vidang were subjected to different storage conditions such as, at room temperature, in a dessicator at room temperature and at cold temperature for a period of 6 months. The samples were also evaluated for antimicrobial activity. It was observed that the test samples (except pure vidang) showed a decrease in embelin content with time. The embelin content in pure vidang remained constant.

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This review addresses the issue of amorphization of poorly water soluble drugs in the solid state. Amorphous phase formation of the drugs is desirable for enhancement of dissolution rate, which can lead to a significant improvement of bioavailability. Grinding, a regularly used process in the pharmaceutical industry can bring about changes in molecular mobility and consequently induce amorphous phase formation. Sorbed water into the amorphous regions increases molecular mobility and subsequently affects physical and chemical stability. Adsorption and entrapment of drug molecules or amorphous molecular dispersion of drug into microporous carrier granules lead to an enhancement of physicochemical stability of the drug. Enthalpy relaxation experiments could be used to indicate relative molecular mobility and relative likelihood of reversion from amorphous to lower energy crystalline state.

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Polystyrene nanoparticles containing cefotaxime were prepared by emulsion polymerization in continuous aqueous phase. Scanning electron microphotograph showed that the morphological structures of the nanoparticles are discrete, spherical and uniform in size. The drug content in the polystyrene nanoparticles were considerably increased proportionately with increasing polymer concentration. The infrared spectroscopic analysis revealed that there was no significant chemical interaction between the polymer and the drug. The in vitro release studies carried out across the artificial membrane indicated that the release of the drug from the nanoparticles followed zero order kinetics.

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The detection of adverse drug reactions has become increasingly important. This study aimed to determine adverse drug reactions of currently-used antihypertensive drugs in a rural hospital, and to assess the effect of pharmacist's intervention on the process of antihypertensive therapy management. Patients were identified to have adverse reactions by interview, using laboratory investigation data and in consultation with physicians and other health care professionals. Patients randomized to pharmacist's intervention received counselling during course of study. Of the 138 patients enrolled, 42% were women, and the average age was approximately 51 y. The study identified adverse drug reactions in 56.5% of the patients. Significant changes in patient satisfaction were observed as result of counselling (P< 0.001).

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Chyavanprash is a well known Ayurvedic formulation claimed to be an immunomodulator and is useful in the treatment of chronic conditions such as pulmonary tuberculosis, asthma and cough. It is also widely used as a food supplement for strength and energy. It maintains youthfulness by renewing tissues and counterattacking degeneration. It has been reported to contain proteins which play an important role in fundamental processes of tissue formation, regeneration and function. Since no studies have so far been undertaken to analyze the amino acids which are the building blocks of proteins in Chyavanprash, a quantitative HPLC analysis of the different amino acids present was carried out. Six different samples of Chyavanprash were analyzed by HPLC using a pre column derivatization technique. Analysis results showed that although the concentration varied, only 3 amino acids, alanine, valine and leucine were present in all 6 samples where as proline was present only in 3, lysine was present only in 2 while one was found to be lacking in both proline and lysine. Also, the results were found to be nearly consistent for the two batches prepared in the lab where as there was marked variation in those procured from the market.

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A simple and sensitive spectrophotometric method has been developed for the determination of acidipine in bulk and tablets. The method is based on the reaction of lacidipine with ferric chloride, potassium ferricyanide and hydrochloric acid to form a bluish green colored chromogen with an absorption maximum of 740 nm. Beer's law was obeyed in the range of 0-10 μg/ml. The proposed method has been successfully applied to the analysis of the bulk drug and its dosage forms. Statistical comparison of the result with that obtained with reported method showed good agreement and indicated no significant difference in precision. This method does not require any extraction or heating.

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Mutual prodrugs of ibuprofen and diclofenac with glucosamine were synthesized by reacting their acid chlorides with glucosamine with an aim to reduce gastrointestinal side effects possessed by these drugs. In vitro hydrolysis of these prodrugs in HCI buffer (pH 1.2) indicated that they were quite stable in gastric acid whereas in phosphate buffer (pH 7.4) undergo hydrolysis following first order kinetics, releasing free drug and glucosamine. These compounds were characterized by analytical and spectral data. The amides were evaluated for analgesic and antiinflammatory activity, Fruend's adjuvant-induced arthritis assay and ulcerogenic potential. They showed better to comparable analgesic and antiinflammatory activity with excellent antiarthritic activity and negligible ulcerogenicity.

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In the present study dopamine was conjugated with amino acids, glycine, alanine, phenylalanine, and valine, with a view to enhance bioavailability by increasing permeability to brain, lower the rate of clearance by reducing metabolism and eliminate undesirable effects. These conjugates were synthesized and characterized by infrared spectroscopy. The partition coefficient of dopamine and dopamine conjugates was determined in n-octanol and phosphate buffer saline pH 7.4 and the conjugates showed 7 to 10 fold increase in their partition coefficients. Moreover, these conjugates exhibited less protein binding as compared to dopamine and in vitro hydrolysis study revealed that the conjugates have long duration of action because of slow hydrolysis. The reduction in the degree of chlorpromazine-induced catatonia was significantly increased as compared with plain dopamine and combination of levodopa and carbidopa.

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A new series of N-Mannich bases (la-lh) of 3-semicarbazino isatin (I) was synthesized by reacting (I) with formaldehyde and various aromatic primary amines. The chemical structures were confirmed by means of IR, 1H NMR and elemental analysis. The compound; synthesized were screened for antimicrobial activity against Staphylococcus aureus, Escherichia coli and Candida albicans by cup plate method. All the compounds showed remarkable antimicrobial activity except compound If that showed moderate activity against S. aureus.

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The absorbance maxima of pseudoephedrine and chlorpheniramine maleate in methanolic hydrochloric acid are 257 and 265 nm, respectively whereas; bromhexine hydrochloride shows two absorbance maxima at 245 and 311 nm. This paper presents two methods based on first derivative spectrophotometry for simultaneous estimations of these three drugs in combination in pharmaceutical formulations. The first derivative amplitudes at 264, 278.2 and 327 nm were utilized for simultaneous estimations. Proper selection of wavelengths with utilization of correlative regression equation and simultaneous equation to avoid complex interference raised in estimation of one drug by others in derivative spectra lead to successful development of methods for simultaneous estimations. Linearity was validated by Least Squares Method. The results of analysis were validated statistically and by recovery studies. Both methods are simple, economical, accurate, reproducible and rapid.

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The major obstacle in the development of centrally active therapeutics is the lipoidal blood-brain barrier. While a variety of systems to transport compounds into the central nervous system have been designed. The current challenge is to develop drug delivery strategies that will allow the passage of drug molecules through the blood-brain barrier in a safe and effective manner. The invasive approach involves the blood-brain barrier disruption either by osmotically or by using biologically active agents. The above strategies are primarily aimed at short-term application in the treatment regimens of malignant brain tumours while chronic degenerative disorders will require long term application of the therapeutic agent. Owing to this fact non-invasive approach for drug delivery to brain via the systemic route have been developed. Physiological strategy has been to conjugate the therapeutic drug with a protein or a vector or a monoclonal antibody that gains access to the brain by receptor mediated transcytosis. The uses of the drug delivery devices such as liposomes and nanoparticles enhance the penetration of several drugs across the brain. This review will provide an insight into some of the strategies developed to enhance drug delivery across the blood-brain barrier.

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Fifty cultures of inulinase producing fungi were isolated from 5 different soil samples using a synthetic medium with inulin as the sole carbon source. Among these, an isolate AUP19 exhibited maximum inulinase activity and was identified as Aspergillus niger. Studies were carried out on concentration of inulin, different carbon and nitrogen sources, process parameters like optimum temperature, pH, fermentation time, and inoculum level using this strain. The optimized process parameters for inulinase production are incubation temperature, 28°; fermentation time, 72 h; pH, 6.5 and inoculum level, 10% (v/v). Maximum inulinase production (176 u/ml) in indented flasks was achieved under optimized conditions with medium containing inulin, 5%; galactose, 1%; corn steep liquor, 1% and (NH4) H2PO4, 1%.

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The levels of blood glucose and malondialdehyde in type 2 diabetic patients have been studied after the administration of amalakic capsules containing 250 mg fruit powder of Emblica officinalis twice a day for 60 d. It was observed that the drug treatment decreases blood glucose levels from 203±82 mg/dl (initial) to 189±255.2 mg/dl (after 60 d of treatment). However, the decrease was statistically insignificant (p>0.05). On the other hand, administration of amalaki for the same period of time resulted in a significant decrease in malondialdehyde levels from 7.55±2.3 nM (initial) to 5.36±0.8 nM (after 60 d of treatment). The decrease in the levels of the malondialdehyde was statistically significant (p<0.05). In the present study, no direct relationship was observed between blood glucose levels and malondialdehyde levels (lipid peroxide levels) of type 2 diabetic patients.

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Two simple photometric titration methods for the determination of thiopentone sodium in injections at milligram and sub-milligram levels have been developed. That the drug compound hydrolyses in aqueous tert-butanol to form sodium hydroxide which is instantaneously transformed into bright yellow sodium benzyl trithiocarbonate (λmax, 430 nm) through reaction with carbon disulphide and benzyl mercaptan has been made the basis of first method. For sub-milligram amounts, the method is based on the formation of yellowish green colour (λmax, 360nm) on mixing the drug with cobalt (II) acetate in dimethylformamide.

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Due to varied pharmacokinetic behavior and inter individual variation of phenytoin, serum level monitoring is necessary to optimize the drug therapy. The present study was designed to study the relationship between serum levels of phenytoin and different patient related factors like the dose administered, effects of age, sex, control of seizures and the influence of co-medication on the phenytoin concentration. Blood samples were collected from the selected patient group (126 patients) and analyzed using a sensitive HPLC method. Of the 111 patients receiving phenytoin as mono therapy, complete seizure control could be achieved in 80 patients. Seventy four percent of these patients had seizures completely controlled with serum phenytoin level below therapeutic range. The following are the conclusions: In the epileptic patients on monotherapy, the seizure control with phenytoin was observed in the concentration range of 3.9 to 29 μg/ml with a mean (±SD) of 11.56±13 μg/ml. Patients showing therapeutic benefit ranged with serum drug level from sub therapeutic level to toxic level indicating the reference therapeutic range (10 to 20 μg/ml) has to redefined for Indian epileptic patient population.

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Crude methanol, chloroform and petroleum ether (60-80°) extracts of Cleome rutidosperma were investigated for analgesic (narcotic and non narcotic) and locomotor activity in mice at a dose of 100 mg/kg administered orally. All these extracts showed significant analgesic and depressed locomotor activity when compared to control and standard drug treatment with morphine sulphate, aspirin and chlorpromazine, respectively.

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The natural insecticide azadirachtin is produced (930 mg/I) in cell cultures of Azadirachta indica grown on MS medium containing sucrose (3%), naphthalene acetic acid (1 mg/l) and kinetin (0.5 mg/l). Azadirachtin in culture extracts was identified by Co-TLC, UV and HPLC analysis. 90% of azadirachtin is retained in the cells. The addition of elicitors such as methyl jasmonate (1-500 mm/I), salacin (200-500mm/l), arachidonic acid (100-500mm/l) and cellulase (100 and 500 units/l) did not improve the production of azadirachtin.

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The development of multivariate calibration model with back-propagation neural network using calibration sets constructed from the spectral data of pure components is proposed for the simultaneous estimation of active components, losartan potassium and hydrochlorothiazide in tablet dosage. The calibration sets were designed such that the concentrations were orthogonal and span the possible mixture space fairly evenly. The back-propagation neural network model was optimized with respect to the spectral input, training parameters and topology including transfer functions for each layer so as to yield accurate and precise estimations on model validation. The optimized model showed sufficient robustness even when the calibration sets were constructed from different set of pure spectra of components thus enabling periodical validation of model rapidly and economically. Although the components showed significant spectral overlap, the model could accurately estimate the drugs, with satisfactory precision and accuracy, in tablet dosage with no interference from excipients as indicated by the recovery study results.

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Ethanol extract of the plant Aristalochia tagala Cham. (Fam: Aristalochiasae) was investigated for antifertility activity in female Wistar rats. Rats treated with the plant extract showed reduction in the number of corpora lutea and implantation sites. The extract exhibited significant activity (72%) on oral administration of 100 mg/kg and 100% activity at a dose of 200 mg/kg.

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Classical non-steroidal antiinflammatory drugs being non selective cyclooxygenase (cyclooxygenase-1 and 2) inhibitors are associated with serious adverse effects while selective cyclooxygenase-2 inhibitors are gastro safer non steroidal antiinflammatory drugs, as it is now well established that antiinflammatory activity of non steroidal antiinfiammatory drugs is due to the inhibition of cyclooxygenase-2 enzyme. In view of that we have identified essential biophoric (pharmacophoric) features on novel terphenyls (terphenyl methyl sulphonamides and sulphones) by the molecular modeling studies using APEX-3D expert system for selective inhibition of cyclooxygenase-2 and cyclooxygenase-1 enzyme. In addition to that multiparameter 3 dimensional quantitative structure activity relationship equations have also been generated, described relationships of biological activities with biophoric centers, global property and secondary sites and results can be used for structure optimization of novel terphenyls for selective inhibition of cyclooxygenase-2 enzyme and also for lead generation. As results of this study corroborates with the active sites of cyclooxygenase-2 and cyclooxygenase-1 enzymes, validate this study. Among several biophoric models generated, two models (1 and 2) for inhibition of cyclooxygenase-2 enzyme and other two models (3 and 4), for inhibition of cyclooxygenase-1 enzyme with good statistical values were selected. The purpose of study was to optimize selectivity of novel terphenyls towards inhibition of cyclooxygenase-2 enzyme, in order to that we have predicted the activity of prediction set compounds and described perfect prediction in 80% of the cases, validate the robustness of biophoric models for selective inhibition of cyclooxygenase-2. Different biophoric features and secondary sites for inhibition of cyclooxygenase-2 and cyclooxygenase-1 enzyme give an opportunity to design potent and highly selective cyclooxygenase-2 inhibitors.

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2-Substituted benzoic acid derivatives are known to possess wide variety of chemotherapeutic activity. Among these 2-hydroxy-benzoic acid derivatives are found to be very useful uricosuric agents and have powerful analgesic activity. In the present research work, two series of 2-substituted benzoic acid derivatives were synthesized and structure elucidation was done by spectral analysis using IR and pNMR spectroscopy. They were then tested for uricosuric and analgesic activities.

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Certain 5-(4'-pyridyl)-4-substituted benzylideneamino-3-mercapto (4H)-1,2,4-triazoles having different substitutions on the aromatic ring possessing azomethine linkage were synthesized and evaluated for their antimicrobial activities. The compounds with a 4-dimethylamina, 3,4-dimethoxy, 2-nitro and 4-chloro group on the aromatic ring showed good antimicrobial activity.

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