A very important part of drug design is prediction of small molecule binding to a target macromolecule. A reasonable qualitative prediction of binding can be made by specifying the spatial arrangement of a small number of atoms or functional groups. Such arrangement is called pharmacophore. The pharmacophore search finds molecules with different overall chemistries, but which have the functional groups in the correct geometry. A common use of pharmacophores is to search 3D databases for molecules that contain the pharmacophore.

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Patients often due to lack of proper information on medication usage, fail to adhere to their medication. This leads to failure of achieving therapeutic goals and decreased quality of life. In developed countries, pharmacists take the responsibility of patient counselling. In India, pharmacists are silent in taking up the counselling responsibility. The prescribers due to heavy patient load are not in a position to spend enough time in educating the patient about their medication. Now the question remains, who actually should take the responsibility of patient counselling? Many professional organisations like International Pharmaceutical Federation, Pharmaceutical Society of Australia, and Royal Pharmaceutical society of Great Britain stress that patient counselling is pharmacist's responsibility. The present study was conducted to assess the pharmacists' opinion about the responsibility of patient counselling. The work was carried out in Karnataka and Kerala states. The respondents from Karnataka state opined that, patient counselling is shared responsibility of both doctor and pharmacist, 'where as respondents from Kerala mentioned that, patient counselling is pharmacist's responsibility. Age, professional education (Education Regulation-81 and 91 and B. Pharm.) and experience have shown influence on the responses. Young pharmacists responded that patient counselling is their responsibility. Major barriers to counselling were identified as doctor dispensing, lack of knowledge, and non legalisation of patient counselling.

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Zidovudine is a potent antiviral agent acting on acquired immunodeficiency virus. Orally administered zidovudine, however has strong side effects. Therefore an adequate zero order delivery of zidovudine is desired to maintain expected anti-AIDS effect. In the present study we encapsulated the zidovudine, in recently developed novel vesicular carrier ethosomes, for its enhanced transdermal delivery and results were compared with liposomes. Ethosomes of zidovudine were prepared and characterized in vitro and in vivo. The effect of different formulation variables on skin permeation of zidovudine was studied using locally fabricated Keshry-Chien type of diffusion cell. To understand the mechanism of better skin permeation of ethosomes, vesicle skin interaction study was carried out. To confirm the better skin permeability of ethosomes, fluorescence microscopy using rhodamine 123 as fluorescence probe was performed. Results were compared with those obtained after administration of liposomes and hydroethanolic and ethanolic solution of drug. The optimized ethosomal formulation showed transdermal flux 78.5±2.5 μg/cm2/h across the rat skin as compared to 5.2±0.5μg/cm2/h for control hydroethanolic solution of drug, and 7.2±0.6 μg/cm2/h for ethanolic drug solution. Vesicle skin interaction study showed that ethosomes affected the ultrastructure of the stratum corneum, distinct regions with lamellar stacks derived from the vesicle were observed in intercellular spaces of the stratum corneum. These lamellar stacks disrupted the organization of the skin bilayers leading to increased skin permeability. This was further confirmed by fluorescence microscopy. Finally, it can be concluded from the study that complex lipid molecule, ethosomes can increase the transdermal flux, prolong the release and present an attractive route for the sustained delivery of zidovudine. Our results indicate that the ethosomal system may be a promising candidate for transdermal delivery of number of problematic drug molecules.

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Piroxicam, a non-steroidal antiinflammatory agent is widely used as a first line drug in the symptomatic relief of rheumatoid arthritis and osteoarthritis. Major problem with this drug is its very low solubility in biological fluids, which results into poor bioavailability after oral administration. Therefore, tablet formulation of piroxicam with polyvinyl pyrolidone K-30 and sodium lauryl sulphate was prepared with a view to increase its water solubility. The dissolution profile of promising batch T1 was compared with marketed preparation (MP-dispersible tablet). Batch T1 gave far better dissolution than the marketed product, which released only 55% drug in 30 min while batch T1 released 86% drug in 30 min. Comparison of in vitro dissolution profile of batch T1 with that of cycladol (solid dispersion with b cyclodextrin) showed no significant difference in % dissolution efficiency except time for 50% dissolution (t50) for cycladol was 4.41 min while for batch T1 it was 9.29 min. Batch T1 was considered better than cycladol as far as the cost of raw materials used in the product is concerned. Selected formulation (batch T1) was subjected to stability studies. The formulation was found to be stable for 4 w at 45o with insignificant change in the hardness, disintegration time and in vitro drug release pattern.

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The in vitro antifungal activity of Eclipta alba (whole plant) extracts has been investigated against Candida tropicalis, Rhodotorula glutinis and Candida albicans. The extracts of Eclipta alba showed high degree of activity against all test fungi. The inhibitory effects of extracts are very similar to those of standard antibiotics used.

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A simple sensitive HPTLC method developed for the analysis of bacoside A in the plant Bacopa monnieri and in its commercial monoherbal capsule formulation. The stationary phase was precoated silica gel G60F254 (20x11cm, aluminum sheet). The mobile phase used was chioroform:methanol:water (18:9:0.6). The plate was scanned and quantified at 540nm for bacoside A. The method was validated in terms of linearity, accuracy and specificity. The proposed HPTLC method provides a faster and cost effective qualitative control for routine analysis of bacoside A in formulations containing Bacope monnieri saponins.

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The present work was carried out to evaluate the effects of angiotensin converting enzyme inhibitor as well as angiotensin receptor antagonist on cognitive functions impaired by scopolamine in rats. In Wistar rats of either sex amnesia was induced by administering scopolamine butyl bromide (2 mg/kg). Ramipril and losartan (1 and 2 mg/kg) were evaluated for their nootropic activity In terms of spatial memory and working memory using Morris water maze task. Ramlpril (1 and 2 mg/kg) and losartan (1 and 2 mg/kg) have shown significant improvement in basal as well as scopolamine-impaired performance with respect to acquisition (P<0.05) and retention of memory (P<0.05) in both spatial and working memory. The observed results suggest that ramipril and losartan improve cognitive function with respect to spatial and working memory processes.

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Effect of cholesterol content on entrapment efficiency and influence of surfactant HLB on the vesicle size has been studied on sorbitan esters vesicles also known as nicsomes prepared using a mechanical shaking technique without sonication. Primaquine phosphate was used as a model drug. Entrapment efficiency increased with Increasing cholesterol content. Mean size of unsonicated niosomes showed a regular increase with increasing HLB from Span 85 (HLB 1.8) to Span 20 (HLB 8.6).

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Sodium alginate was selected as film-forming polymer because of its water solubility and low cost. Metronidazole tablets were coated to mask their bitter taste. The present work was carried out by initially developing aqueous film coating formulae with various concentrations of sodium alginate (4, 6 and 8% w/v). Secondly, the properties of the cast films were evaluated. When compared with dilute solutions, concentrated solutions gave thick films, as the density was more. UV light transmission, water vapour transmission and gas permeability of the films decreased with the increase in the thickness of the films. They were freely soluble in distilled water and simulated intestinal fluids but precipitated in simulated gastric fluid. Thirdly, 2 kg of tablets were coated using solutions of the above concentrations. Some tablets were withdrawn after application of 400, 600 and 800 ml of coating solutions, respectively. Coated and uncoated tablets were evaluated for weight variation, hardness and friability, which were all within the acceptable limits. Coating increased hardness and decreased friability. All the coated and uncoated tablets disintegrated within 10 min in water and complied with the USP and BP limits for the assay. The rate of drug release decreased as the concentration of sodium alginate increased. Only 400, 600 and 800 ml coats of 4% w/v solution and 400 ml coats of 6% and 8% w/v solutions In buffer pH 1.2 met USP dissolution requirements. Based on the results of above work along with statistical analysis and accelerated stability studies, 400 ml coat of 6% w/v solution was chosen as the best.

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Deionised water is used in the production of active pharmaceutical ingredients and pharmaceutical applications such as cleaning of equipments. It must meet the prescribed chemical and microbiological requirements. Total aerobic bacterial count is estimated to evaluate the microbiological quality of deionised water. Deionised water samples were tested for total aerobic bacterial count on three different media, plate count agar, soyabean casein digest agar and R2A agar using pour plate method. The results obtained were compared and it was observed that R2A agar gave slightly higher results as compared to plate count agar media while the count on soyabean casein digest agar were significantly low. Therefore, on the basis of the comparative validation of media, it can be decided whether low nutrient media like R2A agar is to be included or excluded in the routine testing, thus saving resources.

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A simple, rapid, precise, accurate and highly specific spectrophotometric method has been developed for the determination of venlafaxine in its pharmaceutical dosage form. The method is based on the formation of blue colored chromogen due to the reaction of venlafaxine with Folin Ciocalteu reagent in presence of alkali, which exhibits λmax at 730 nm. Beer's law obeyed in the concentration range of 2.5-25 μg/ml. The blue color obtained was stable for more than 24 hours. The method was successfully applied for the quantitative determination of venlafaxine and its pharmaceutical dosage form. The accuracy and reproducibility of the proposed method was statistically validated by recovery studies.

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The permeation of ampicillin sodium patch from ethanol/pH4.7 buffer solution containing antinucleant polymers across mouse skin, was investigated. The in vitro release of ampicillin sodium was determined under open condition at 25o and 65% relative humidity. Therefore the influence of evaporation of vehicle components on the permeation of ampicillin sodium was examined. Evaporation of the vehicle led to drastic compositional changes leading to supersaturation. However, supersaturation solutions started to crystallize reducing the thermodynamic activity of ampicillin sodium. Antinucleant polymers where used in the preparation of volatile vehicles in order to maintain the Increased activity state of the drug. Carboxymethylcellulose and hydroxypropylmethylcellulose were efficient antinucleant polymers to increase the permeation of ampicillin sodium.

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The present investigation is a preformulation study on stabilization of vitamin C with disodium edetate and some antioxidants. The concentration of disodium edetate for the stabilization of vitamin C in aqueous solution at pH 4.0 was found to be critical: less than 0.05% w/v was insufficient and more than 0.05% w/v was detrimental. The first order kinetics was the prevailing mechanism in this case and kinetic rate constants were calculated by regression analysis. Differential scanning calorimetric study suggested the effect of disodium edetate concentration on the thermal behavior of vitamin C and results are reciprocative of kinetic study. The study was further extended to understand the effect of some antioxidants such as cysteine, thiourea and nicotinic acid on the stabilization of vitamin C. In all the cases the effect of stabilization increased with increased concentration. Cysteine was found to be more protective to the aqueous stability of vitamin C. In total both disodium edetate and antioxidants were found to improve the stability of vitamin C. However, required stability was not achieved with permissible concentration of both the stabilizers suggesting the need of further investigation.

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Diethyl ether and methanol extracts of dried powdered, aerial parts of Artemesia sleverslana (Asteraceae), Origanum majoram (Lamiaceae), fruit peel of Musa paradisiaca var sapienturn (Musaceae) and stem bark of Moringa pterygosperma (Moringaceae) were evaluated for antimicrobial activity against Bacillus subtilis, Staphylococcus aureus, Escherichia coll, Pseudomonas aeruginosa, Candida albicans and Cryptococcus neoformans by cup-plate method. Both the extracts of Moringapterygosperma and methanol extract of Musaparadisiaca have shown significant activity in comparison with the standards benzyl penicillin and streptomycin. All others except ether extract of Musa paradisiaca are inhibitory to the tested human pathogenic fungl.

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Captopril was quantitatively determined using chloranilic acid through charge-transfer complexation. Favourable conditions like time and temperature for the complex formation were determined. The wavelength for maximum absorption of light by the complex was 520 nm. The complex formation was maximum 30 min after mixing the reactants and room temperature was favourable for the complex formation. Captopril and chloranilic acid formed 1:1 complex in a mixture of dioxan:chloroform activated with dimethylsulphoxide. The association constant, molar absorptivity and free energy change for the complex were 0.6971 I/mol, 2.2462x102 l/mol.cm and 8.828 kcal/mol, respectively. Beer-Lambert's law was obeyed in the concentration range of 0.4- 1.4 mg% (w/v) of captopril. This method was employed in the analysis of captopril in dosage forms and the mean percentage recovery was 96.7%.

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A simple method for synthesis of oleanolic acid hemiphthalate disodium salt has been successfully, developed. The structures of the newly synthesized compounds were elucidated on the basis of analytical and spectral data. The antiinflammatory activity of oleanolic acid hemiphthalate disodium salt was performed on dimethyl benzene-induced acute ear oedema model. In the acute inflammatory model, oleanolic acid hemiphthalate disodium salt exhibited significant antiinflammatory activity with single and multiple doses with no matter oral, or subcutaneous or intraperitoneal administration. Furthermore antiinflammatory activity of oleanolic acid hemiphthalate disodium salt was better than oleanolic acid with single dose with various administration methods and with multiple doses with oral administration method.

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Establishment of a new molecule as a therapeutic agent requires extensive inputs in terms of money, energy and time. Therefore the worldwide pharmaceutical R and D are focusing its attention on the development of new drug delivery systems. After designing a new delivery system, its optimization Involves the in vitro and in vivo studies. Pharmacopoeial dissolution testing is an important in vitro test to study the release of the drug from its formulation. In vivo studies can be carried out either by blood sampling method or urine analysis. Besides, being cumbersome and tedious these methods do not give any information regarding the biopharmaceutics. Pharmacoscintigraphy, a much-touted technology can answer all above-mentioned queries regarding a delivery system. g-Emitting radionuclide (preferably 99mTc) is tagged with the active constituent or the excipient of the formulation. The radioactive dosage form is administered via Intended route of administration and the subject (humans/animals) is scanned under a gamma camera. Radionuclides tagged with drugs/formulations/devices can provide vital information regarding the extent, rate, site, and mode of drug release and morphology of the drug delivery system during release in humans under the ethical norms. Pharmacodynamics and pharmacokinetics of new drug molecules studied by this technique gives qualitative as well as quantitative data. Present study proposes an effective approach for the development and evaluation of new drug molecules and drug formulations.

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Floating flaps containing albendazole and closantel were prepared by casting technique, employing Poly (dl-lactide-co-glycolide, 75:25), Eudragit RL100, and Eudragit RS100, along with polyethylene glycol 400 as plasticizer. These flaps were evaluated for tensile strength, thickness, percent moisture absorption, water vapor transmission, density, drug content, and in vitro buoyancy test. The release rate was determined in phosphate buffer saline (pH 6.4) and diluted natural ruminal fluid. The floating flaps showed a near zero order release profile for 60 d and were stable over the period. The in vivo anthelmintic activity of the flaps was evaluated using eggs per gram method in adult calves. The floating flap containing albendazole and closantel provided protection against all types of parasitic infections for about 3 mo.

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A simple, accurate and reproducible method for simultaneous estimation of amoxycillin and metronidazole in combined dosage form has been developed. The method involves analysis by multicomponent mode. Amoxycillin and metronidazole have absorption maxima at 272 nm and 320 nm, respectively, in alkaline borate buffer (pH 8.1). The results of analysis were validated statistically.

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In the present investigation methotrexate prodrugs of α-and γ-cyclodextrins were synthesized. The primary hydroxy group of α- and γ-cyclodextrins were used to block the acid group. The synthesis involved a series of protection and deprotection reaction. The esters were evaluated for stability in simulated gastric and intestinal fluid. The hydrolysis of cyclodextrin conjugates in colon is confirmed by the hydrolysis kinetics studies in rat fecal material. The esters were also evaluated for ulcerogenicity. Results of these studies established the primary aim of masking the ulcerogenic potential of free drug, by using 12-fold dose of the normal dose of methotrexate and equivalent doses of the esters.

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The bioconverted product of vinblastine (alkaloid from Vinca raosea), vinblastine monohydrazide was administered to cell line-induced solid tumour in mice and the changes in life span and tumour size were noted. It was found that the bioconverted product was an antitumour agent as it helps in the reduction of solid tumour and also in increasing the life span of tumour induced mice when compared to the crude alkaloid vinblastine.

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Trimetazidine is a cellular antiischemic agent with cytoprotective action and devoid of any hemodynamic activity. Extensive work has been carried out on this drug in cardiovascular therapeutics and in transplantation surgery. It was thus decided to investigate possible antiinflammatory activity it could exert by virtue of it being a calcium channel blocker. Trimetazidine being a cytoprotective agent could offer protection against experimentally induced ulcerations. Another objective was to extend the antiischemic activity of trimetazidine in the brain in the cryogenic cerebral ischemic injury model and finally to assess the free radical scavenging activity of the drug in the murine peritoneal macrophage model. Trimetazidine potentiated the antiinflammatory effect of ketoprofen and also significantly reduced the rate of edema formation. It was able to protect animals against the experimentally induced gastric ulcerations. Trimetazidine produced a significant antiischemic activity in the brain and also brought about a significant free radical scavenging effect.

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A simple, selective, rapid, precise and economical reverse phase HPLC method has been developed for the determination of rofecoxib in tablets. The analyte is resolved by using a mobile phase (methanol and water in the ratio 50:50) at a flow rate of 1 ml/min on an isocratic HPLC system (Shimadzu) consisting of LC 10AT liquid pump, SPD 10A UV-Visible detector, a ODS C-18 RP column (4.6 mm I.DX25 cm) at a wavelength of 230 nm. The linear dynamic range for rofecoxib was 2-40 μg/ml by this method. Paracetamol was used as an internal standard.

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A series of novel 2-substituted-3-(sulphonamido) quinazolin-4 (3H)-ones have been synthesized by condensing the primary amino group of sulphamoxole and sulphadimidine with 2-substituted benzoxazin-2-one. The compounds synthesized were screened for antibacterial activity (Escherichia coli and Staphylococcus aureus) antiviral activity (Herpes simplex virus type 1 and 2 in E6SM cells, HIV-1 and 2 in MT-4 cells), all the test compounds exhibited comparable antibacterial activity with that of standards sulphamoxole and sulphadimidine.

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Several N -arylamino-1,3-diazabuta-1,3-dienes were prepared by the reaction of N-arylbenzimidoyl isothiocyanates with primary aromatic amines followed by S-methytation of the resultant thioureas. All these compounds were characterised by analytical and spectral data. Antibacterial activity was determined using agar diffusion technique against Escherichia coli MTCC 42, Pseudomonas aeruginosa MTCC 1034, Bacillus subtilis MTCC 121, Bacillus cerus MTCC 1272 and Staphylococcus aureus MTCC 1430. Some of the compounds showed significant antibacterial activity.

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To predict permeability of drugs through the skin chitosan membranes have been formulated. The in vitro permeability of ionized and unionized diclofenac through chitosan membranes has been compared with that of dorsal skin of Wistar rats. The chitosan membranes were prepared by cast drying to achieve thickness of hairless-dorsal-skin of Wistar rats. The thickness of chitosan membrane varied with change in concentration of chitosan and sodium tripolyphosphate. The chitosan membrane has been observed to mimic the flux of ionized and unionized diclofenac through rat skin. Chitosan membranes are easy to prepare with controlled composition and reproducibility.

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Since 1986, the immunization programmes throughout the world have changed their focus to the control or elimination of major childhood diseases, and new vaccines have become available, while yet others are being developed. Challenges included the reduction of measles incidence and elimination of neonatal tetanus by 1995, global eradication of poliomyelitis by the year 2000, and the achievement of 90% immunization coverage for all vaccines by the year 2000. These challenges were reinforced in the declaration on the survival, protection, and development of children, which was endorsed at the world summit for children held at United Nations in September 1990 (World Summit Child 1990). Immunization programmes in different countries now present a broad spectrum of progress. Some countries, particularly the poorest and those affected by war or civil disturbance, continue to have low immunization coverage, while others are close to eliminating certain of the target diseases. This article provides a review of present immunization policies.

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Ayurvedic preparations contain various plant extracts. Plants take up number of mineral elements from various sources and when these plant extracts are used in the final preparation it is likely that some concentration of these elements may be present in the final ayurvedic preparation also. If the concentration of these elements exceeds the recommended value, it leads to toxic effects. Hence in the present study, a widely prescribed ayurvedic preparation used in infants and young children as digestive tonic was selected in order to find the concentration of various trace elements present in that preparation using inductively coupled plasma-mass spectrometer.

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A polymeric pro-drug of indomethacin was synthesised. The pro-drug was evaluated for drug content and in vitro drug release behavior at pH 1.2 and 7.2. The in vitro and studies show that the drug-release takes place predominantly at the higher pH and also in a sustained manner as hypothesized. The bioavialability investigations show complete drug absorption from the polymeric pro-drug, thus showing its potential for site-specific and sustained drug delivery.

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Synthesis and evaluation of some novel monocyclic beta-lactam compounds as anti-inflammatory and anti-hyperalgesic agents has been carried out in the present study. Such type of compounds has been reported in literature as human leukocyte elastase (HLE) inhibitors. The compounds were administered orally (15 mg/kg) to rats 30 min before injecting carageenan in the planter aponeurosis. The compounds showed a marked effect on paw edema and associated inflammatory pain. Compound 1 showed antiinflammatory effect even better than indomethacin (10 mg/kg) used as reference standard. These results suggest the need of carrying out further in vitro studies on the mechanism of action, which may be HLE inhibition.

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