The colon targeted drug delivery has a number of important implications in the field of pharmacotherapy. Oral colon targeted drug delivery systems have recently gained importance for delivering a variety of therapeutic agents for both local and systemic administration. Targeting of drugs to the colon via oral administration protect the drug from degradation or release in the stomach and small intestine. It also ensures abrupt or controlled release of the drug in the proximal colon. Various drug delivery systems have been designed that deliver the drug quantitatively to the colon and then trigger the release of drug. This review will cover different types of polymers which can be used in formulation of colon targeted drug delivery systems.

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Nucleic acid-based therapeutics have gained a lot of interest for the treatment of diverse ophthalmic pathologies. The first to enter in clinic has been an oligonucleotide, Vitravene^® for the treatment of cytomegalovirus infection. More recently, research on aptamers for the treatment of age related macular degeneration has led to the development of Macugen^® . Despite intense potential, effective ocular delivery of nucleic acids is a major challenge since therapeutic targets for nucleic acid-based drugs are mainly located in the posterior eye segment, requiring repeated invasive administration. Of late, nanotechnology-based nano-vectors have been developed in order to overcome the drawbacks of viral and other non-viral vectors. The diversity of nano-vectors allows for ease of use, flexibility in application, low-cost of production, higher transfection efficiency and enhanced genomic safety. Using nano-vector strategies, nucleic acids can be delivered either encapsulated or complexed with cationic lipids, polymers or peptides forming sustained release systems, which can be tailored according to the ocular tissue being targeted. The present review focuses on developments and advances in various nano-vectors for the ocular delivery of nucleic acid-based therapeutics, the barriers that such delivery systems face and methods to overcome them.

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Trimetazidine dihydrochloride, a cellular antiischemic agent indicated in the management and prophylaxis of angina pectoris is given as 20 mg thrice daily in the conventional dosage regimen. The purpose of the present study was to formulate and evaluate twice a day extended release tablets containing 30 mg trimetazidine dihydrochloride. The method developed to formulate these extended release tablets was melt congealing followed by wet granulation which exhibited uniform sustained release action and overcame the drawbacks of multidosing. The formulation was developed with Methocel^® K100M and stearic acid as release retardant.

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A multiple unit oral floating drug delivery system of famotidine was developed to prolong gastric residence time, target stomach mucosa and increase drug bioavailability. Drug and polymer compatibility was studied by subjecting physical mixtures of drug and polymers to differential scanning calorimetry. Cod liver oil entrapped calcium alginate beads containing famotidine, capable of floating in the gastric condition were formulated and evaluated. The gel beads were prepared by emulsion gelation method by employing sodium alginate alone and mixture of sodium alginate and hydrophilic copolymers such as carbopol 934P and hydroxypropylmethylcellulose K15M grade in three different ratios. The effect of selected factors, such as percentage of oil and amount of copolymers on floating properties was investigated. The beads were evaluated for percent drug loading, drug entrapment efficiency, buoyancy and in vitro drug release. The in vitro drug release study of the beads was carried out in simulated gastric media employing a modified Rosette-Rice test apparatus. Wherein, the apparatus was further modified by incorporating a water jacket to the apparatus to circulate hot water to maintain 37±2° for throughout the release study. All the oil entrapped calcium alginate beads floated if a sufficient amount of oil was used. Beads formulated employing sodium alginate alone could not sustain the drug release up to 8 h, whereas beads formulated with mixture of sodium alginate and copolymers demonstrated sustained release of famotidine up to 8 h. The results suggested that cod liver oil entrapped calcium alginate beads were promising as a carrier for intragastric floating drug delivery of famotidine.

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The ability of β-cyclodextrin, hydroxypropyl-β-cyclodextrin, polyvinyl pyrrolidone and urea to influence the percutaneous absorption of meloxicam through isolated rat skin was evaluated. Carrier complex were prepared by kneading method in 1:1 and 1:2 in molar ratios for β-cyclodextrin and hydroxypropyl-β-cyclodextrin and in 1:1, 1:3 and 1:5 in weight ratios for polyvinyl pyrrolidone and urea. The complexes were characterized by IR, DSC and evaluated for solubility, dissolution and skin permeability. The solubility, dissolution and permeability of meloxicam were enhanced by using the carriers. The influence of cyclodextrins, polyvinyl pyrrolidone and urea on in vitro permeation of meloxicam through rat skin was investigated by incorporation of prepared carrier complex in 1% carbopol gel. The prepared gel was evaluated for drug content, pH and viscosity and in vitro permeation. All the percutaneous parameters like flux (Jss), amount permeated (Q ₆ ), diffusivity (D), permeability coefficient (K _p ), partition coefficient (K) and release rate constant (k) were calculated statistically. In vitro permeation study showed the trend that the penetration flux and enhancement factor increases with increasing concentration of β-cyclodextrin and hydroxypropyl-β-cyclodextrin and then decrease dramatically in case of hydroxypropyl-β-cyclodextrin gel formulation with the increase to 1:2 ratio. Similar changes in pattern of permeation were also observed with polyvinyl pyrrolidone and urea carrier complex. These findings concluded that the carriers cyclodextrins, polyvinyl pyrrolidone and urea could be used as transdermal permeation enhancer in topical preparation of meloxicam.

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Many plants are claimed to possess antidiabetic and antioxidant activity. In practice, it is being increasingly recognized to be an alternative approach to modern medicine. This study assess the antioxidant capacity of Tinospora cordifolia stem methanol extract in daily oral administration of 500 mg/kg of body weight for 40 days in alloxan induced diabetic rats. The erythrocytes membrane lipid peroxide and catalase activity was increased where as the activities of superoxide dismutase, glutathione peroxidase were found to be decreased significantly (P<0.01) in alloxan-induced diabetic rats. The levels of lipid peroxide in liver of diabetic rats increased significantly (P<0.01) and catalase, superoxide dismutase, glutathione peroxidase in liver was significantly decreased in alloxan-induced diabetic rats, when compared to normal rats. After treatment of methanol Tinospora cordifolia stem extract brings back to normal (P<0.01) in the erythrocytes membrane and liver cell enzymes activities.

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Modification of polymers by covalent attachment of thiol bearing pendant groups is reported to impart many beneficial properties to them. Hence in the present study, sodium alginate-cysteine conjugate was synthesized by carbodiimide mediated coupling under varying reaction conditions and the derivatives characterized for thiol content. The thiolated alginate species synthesized had bound thiol content ranging from 247.8±11.03-324.54±10.107 ΅mol/g of polymer depending on the reaction conditions. Matrix tablets based on sodium alginate-cysteine conjugate and native sodium alginate containing tramadol hydrochloride as a model drug were prepared and mucoadhesive strength and in vitro drug release from the tablets were compared. Tablets containing 75 mg sodium alginate-cysteine conjugate could sustain release of 10 mg of model drug for 3 h, whereas 90% of the drug was released within 1 h from corresponding tablets prepared using native sodium alginate. An approximately 2-fold increase in the minimal detachment force of the tablets from an artificial mucin film was observed for sodium alginate-cysteine conjugate as compared to native sodium alginate. In vitro cytotoxicity studies in L-929 mouse fibroblast cells studied using an MTT assay revealed that at low concentrations of polymer, sodium alginate-cysteine conjugate was less toxic to L-929 mouse fibroblast cell line when compared to native sodium alginate. Hence, thiolation is found to be a simple route to improving polymer performance. The combination of improved controlled drug release and mucoadhesive properties coupled with the low toxicity of these new excipients builds up immense scope for the use of thiolated polymers in mucoadhesive drug delivery systems.

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Diclofenac sodium and alginate was intercalated into montmorillonite to form uniform sized beads by gelation method. The structure and surface morphology of the synthesized composite beads were characterized by powdered X-ray diffraction, Fourier transform infrared spectroscopy, thermo gravimetric analysis and scanning electron microscopy. Diclofenac release kinetics of the composite in simulated intestinal fluid medium (pH 7.4) and effect of montmorillonite content on the in vitro release of diclofenac from diclofenac-montmorillonite-alginate composites bead was investigated by UV/Vis spectrophotometer. Diclofenac encapsulation efficiency in the montmorillonite-alginate composites bead increases with an increase in the montmorillonite content. The control release of diclofenac from diclofenac-montmorillonite-alginate composites beads was observed to be better as compared to diclofenac-alginate beads.

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A selective and sensitive, stability-indicating reverse phase high performance liquid chromatography method has been first developed and validated for the estimation of miglitol in bulk and tablet dosages form. Samples were separated on a prepacked, Inertsil amino C ₁₈ column (150Χ4.6 mm i.d.) using a mobile phase comprised of acetonitrile and monobasic sodium phosphate pH 7.5 (80:20, v/v) delivered at 1.5 ml/min flow rate. Detection was performed on a SPD-20A prominence UV/Vis detector at 220 nm. The retention time for miglitol was 13.93±0.0367. The method was validated in terms of linearity, precision, accuracy, ruggedness, and specificity, limit of detection and limit of quantification. The linearity (r ² ) and percentage recoveries of miglitol were 0.9986 and 99.85%. This method is suitable for routine estimation of miglitol in bulk and tablet dosages form.

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In the present study petroleum ether and alcoholic extracts of Centratherum anthelminticum (L) Kuntze seed (100 mg and 200 mg/kg p.o.) were evaluated for antiinflammatory activity in acute and subacute models of inflammation. It was found that both petroleum ether and alcoholic extracts showed significant reduction in paw oedema in carrageenan-induced model. In subchronic inflammatory phase both extracts provoked a significant reduction of transudation phase and too little extent proliferative phase when tested in cotton pellet-induced granuloma model. Both the extracts also reduced alkaline phosphatase activity in serum. The histopathology of granuloma tissue showed significant inhibition of lymphocytes, neutrophils, exudates, necrosis and giant cell when compared with control without ulcerogenic effect. The results suggest that petroleum ether and alcoholic extracts may exert antiinflammatory activity through prostaglandin inhibition, reduced myeloperoxidase and antitransudation.

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In the present research work mouth dissolving tablets of domperidone were developed with superdisintegrants like crospovidone, croscarmellose sodium and sodium starch glycollate in various concentrations like 3%, 4% and 6% w/w by direct compression method. All formulations were evaluated for physical characteristics of compressed tablets such as weight variation, hardness, friability, content uniformity, in vitro disintegration time, wetting time and in vitro dissolution study. Among all, the formulation F3 (containing 6% w/w concentration of crospovidone) was considered to be the best formulation, having disintegration time of 9 s, wetting time of 15 s and in vitro drug release of 99.22% in 15 min.

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A simple, specific, accurate, and precise ultra performance liquid chromatographic method was developed and validated for the estimation of venlafaxine hydrochloride in tablet dosage forms. A acquity TM BEH column having C18, 100Χ2.1 mm i.d. in isocratic mode, with mobile phase containing dipotassium hydrogen phosphate: Acetonitrile (30:70 v/v; pH 7.00 with dilute o-phosphoric acid) was used. The flow rate was 0.75 ml/min and effluents were monitored at 227 nm. The retention time of venlafaxine hydrochloride was 0.548 min. The method was validated for specificity, linearity, accuracy, precision, limit of quantification, limit of detection, robustness and solution stability. Limit of detection and limit of quantification for estimation of venlafaxine hydrochloride were found to be 6.11 μg/ml and 20.33 μg/ml, respectively. Recoveries of venlafaxine hydrochloride in tablet formulations were found to be in the range of 99.3-99.5%. Proposed method was successfully applied for the quantitative determination of venlafaxine hydrochloride in tablet dosage forms.

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The aim of the present work was to investigate the in vivo hepatoprotective potential of coumarinolignoids (cleomiscosins A, B, and C) isolated from the seeds of C. viscosa. The study was performed against CCl ₄ -induced hepatotoxicity in albino rats. Rats were divided into four groups. The animals of group I served as normal and was given only vehicle. Group II served as toxin control and administered with CCl ₄ (50% solution liquid paraffin, 2 ml/kg intraperitoneally). The animals of group III received coumarinolignoids (50 mg/kg) for six days orally as well as CCl ₄ (2 ml/kg) on 4 ^th day i.p. Similarly animals of group IV received silymarin (50 mg/kg) for six days orally as well as CCl ₄ on 4 ^th day i.p. On 7 ^th day various parameters viz. serum glutamyl oxaloacetic transaminase, serum glutamyl pyruvate transaminase, serum alkaline phosphatase, serum bilirubin, liver glycogen were estimated and histopathology was performed. Additionally, acute oral toxicity of the said coumarinolignoids was carried out in swiss albino mice. The coumarinolignoids were found to be effective as hepatoprotective against CCl ₄ -induced hepatotoxicity as evidenced by in vivo and histopathological studies in small animals. Safety evaluation studies also exhibit that coumarinolignoids are well tolerated by small animals in acute oral toxicity study except minor changes in red blood cell count and hepatic protein content at 5000 mg/kg body weight as a single oral dose. Coumarinolignoids which is the mixture of three compounds (cleomiscosin A, B and C) is showing the significant protective effects against CCl ₄ -induced hepatotoxicity in small animals and also coumarinolignoids are well tolerated by small animals in acute oral study.

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Cissus quadrangularis L. is a promising remedy prescribed in the ancient Ayurvedic literature for bone fracture healing properties. As this activity has been extensively investigated and well established, a range of formulations containing C. quadrangularis has been marketed. This work reports the development and validation of a reliable RP-HPLC method for the analysis of phytosterols in the various extracts of the plant. The proposed method utilizes a Cosmosil C ₈ column (250 ΄ 4.6 mm) with a compatible Phenomenex C ₈ guard column with isocratic elution of acetonitrile and water (95:5 v/v) at 25΀. An effluent flow rate of 2 ml/min and UV detection at 202 nm was used for the analysis of phytosterols. The described method was linear in the range of 1-500 μg/ml, with excellent correlation coefficients. The precision, robustness and ruggedness values were also within the prescribed limits (less than 2%). The recovery values were within the range, which indicates that the accuracy of the analysis was good and that the interference of the matrix with the recovery of phytosterols was low. The phytosterols were found to be stable in a stock solution for 48 h (% RSD was below 2%) and no interfering extra peaks were observed under controlled stress conditions. The proposed method is simple, specific, precise, accurate, and reproducible and thus can be used for routine analysis of C. quadrangularis phytosterols in quality control laboratories.

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The present study investigate the protective effect of aqueous root extract of Desmodium gangeticum in preserving mitochondrial and sarcoplasmic ATPase during ischemia reperfusion injury. The isolated rat hearts in both drug and control group were subjected to warm ischemia (37°), followed by reperfusion with the Langendorff perfusion system. The aqueous root extract of Desmodium gangeticum (L) at a dose of 50 mg/kg body weight was found to be effective in the rat heart for the management of ischemic reperfusion injury. Physiological parameters were significantly (P<0.05) improved in drug treated rat hearts. Creatine phosphokinase in coronary perfusate found to be declined. Moreover, sarcoplasmic ATPase and mitochondrial enzymes were significantly (P<0.05) improved in drug treated rat hearts. In fact, histological analysis of the myocardium also suggested an improved ultra structure in Desmodium gangeticum treated rat heart. These results suggest that Desmodium gangeticum aqueous root extract can preserve the mitochondrial and sarcoplasmic ATPase in the myocardium, resulting in the improvement of cardiac function after ischemia reperfusion injury.

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Shoot biomass production, alkaloid content and composition as influence by cadmium, manganese, nickel and lead at uniform dose of 5 mM were investigated in Catharanthus roseus plants grown in sand culture. Treatment with Mn, Ni, and Pb significantly enhanced total root alkaloid accumulation. Cd and Ni treatment resulted in two-fold where as Pb treatment resulted in three fold increase in serpentine content of roots. The non-significant affect on biomass suggests that plants can withstand metal stress at the level tested with positive affect on root alkaloid content.

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Chalcones and their synthetic analogues appear to have the same binding site of tubuline as phenstatin, combretastatin steganacin and podophylotoxin and are therefore capable to inhibit cancer cell proliferation. The phenyl rings with appropriate substitutions maintain a fixed distance between two centers of aryl rings. The two aromatic rings in these molecules are arranged like the two wings of a butterfly having certain dihedral angle between them, therefore a "butterfly model" is proposed an important structural feature responsible for their antitubulin activity. In this sequence a series of chalcones were synthesized and evaluated for in vitro cytotoxic activity against a panel of human cancer cell lines. In addition the synthetics reduced MIC of ciprofloxacin upto four fold this indicates their bioavailability enhancing potential.

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A simple, accurate, rapid, specific and reproducible UV spectrophotometric method was developed for estimation of content uniformity of atenolol and losartan potassium in its combined tablet dosage form. The method involves formation and solving the simultaneous equation using 226.4 and 254 nm as two wavelengths for atenolol and losartan, respectively. Developed method was employed to determine the atenolol and losartan content in ten individual tablet units of five market formulations. Methanol was used as solvent. The method was validated. From the results, it was concluded that all brands are within the content uniformity limit, 85-115%.

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A reversed-phase liquid chromatographic method for the determination of 1,7,7-trimethyl-bicyclo(2,2,1)heptan-2-one in a cream formulation is developed and validated. The separation was achieved using an isocratic mobile phase, on a Lichrosorb C8 column. The calibration curve is linear (r ² = 0.9999) from 25-175% of the analytical concentration of 1.0 mg/ml. The mean percent standard deviation values for intra-day and inter-day precision studies were <1%. The recovery ranges 99.80-100.06% from a cream formulation. The method can be used reliably in quality control for the analysis of bulk cream samples and final product release.

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A simple, accurate and precise spectrophotometric method has been developed for simultaneous estimation of clopidogrel bisulphate and aspirin by employing first order derivative zero crossing method. The first order derivative absorption at 232.5 nm (zero cross point of aspirin) was used for clopidogrel bisulphate and 211.3 nm (zero cross point of clopidogrel bisulphate) for aspirin.Both the drugs obeyed linearity in the concentration range of 5.0 μg/ml to 25.0 μg/ml (correlation coefficient r ² <1). No interference was found between both determined constituents and those of matrix. The method was validated statistically and recovery studies were carried out to confirm the accuracy of the method.

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A series of 1,4-dihydropyridine derivatives (1a-g) were prepared from three compounds condensation of Hantzsch synthesis. A new series of 2,2'-{[4-(aryl)-2,6-dimethyl-1,4-dihydropyridine-3,5-diyl]dicarbonyl}dihydrazinecarbothioamide (2a-g) were prepared from compounds diethyl 4-(aryl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate (1a-g) reacted with thiosemicarbazide to give the corresponding compounds (2a-g) by hydrazinolysis method. The synthesized compounds were confirmed by IR, ¹HNMR, ¹³CNMR, mass spectral and elemental analyses. The newly synthesized compounds (2a-g) were screened for anticonvulsant activity against in swiss albino rat. The test was evaluated by maximal electrode induced convulsion method. Synthesized compounds were used two (50 and 100 mg/kg) concentrations. Compounds (1a-g) were inactive while compounds (2a-g) have moderate anti-convulsant activity compared with standard phenytoin drug. The compound 2,2'-{[4-(furan-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-diyl]dicarbonyl} dihydrazinecarbothioamide (2a) has highly active compared with other compound (2b-2g).

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A rapid and sensitive reverse phase RP-HPLC method is proposed for the estimation of tamsulosin hydrochloride in tablets. Tamsulosin hydrochloride was chromatographed on a reverse phase C18 column with a mobile phase consisting of acetonitrile and water in the ratio of 50:50 v/v. The mobile phase was pumped at a flow rate of 1.5 ml/min. The eluents were monitored at 214 nm. The retention time of the drug was 1.7 min. With this method, linearity was observed between area under curve and concentration of tamsulosin hydrochloride in the injected solution, in the range of 5 to 100 μg/ml. The method was found to be applicable for analysis of the drug in tablets. The results were validated statistically.

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Plants are an important source of neutraceuticals that have proved to be effective against important microbial infections of humans. Lower plants are gaining importance in this regard. The present study is aimed at investigating the antimicrobial properties of three selected ferns, Psilotum nudum, Nephrolepis biserrata and Nephrolepis cordifolia. The aerial parts of the selected ferns, P. nudum, N. biserrata and N. cordifolia, were fractionated in different solvents. These fractions were concentrated to obtain a powder and were tested against nine bacterial and three fungal strains according to disc diffusion method. The water and ethanol fractions were active against most of the tested bacterial and fungal strains, some of these were more effective than the controls tested. Present study suggests that the pteridophytes, P. nudum, N. biserrata and N. cordifolia could be good source of antimicrobials. These natural compounds might be more effective as the microbes may have lesser chance of developing resistant mutants.

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The primary aim of this study is to identify and analyze the importance of adverse drug reaction due to drug-drug interaction as a contributing factor towards drug safety. Patients more than 18 years of age admitted in multidisciplinary intensive care unit of a tertiary care hospital were included in this study. Patients who stayed less than 48 h and patients in whom all treatment modalities have been withdrawn and were on comfort measures only (no drugs were prescribed), were excluded. All the drugs that were given during intensive care unit stay were checked for presence of potential interactions which led to adverse drug reaction. Drug-drug interactions that were detected clinically or through investigations were recorded and also any therapeutic actions taken for drug-drug interactions were noted. From June 2006 to April 2007, 400 patients-prescriptions were analyzed. Adverse drug reactions due to drug-drug interactions were identified in 64% patients. Among those patients 38.67% had a single drug-drug interaction. Potential drug-drug interactions were 602. Clinically significant drug-drug interactions among the potential were 208 (34.55%). Clinically relevant drug-drug interactions were 103 (49.52% of 208 episodes). The adverse drug reactions due to drug-drug interactions in our sample were managed either by substituting another drug (50.48% of 103 episodes) or by adjusting the dose (1% of 103 episodes) or by omitting the drug (48.54% of 103 episodes). Among the 208 observed drug-drug interactions induced adverse drug reactions 21.63% was severe drug-drug interactions induced adverse drug reactions, 23.08% was moderate drug-drug interactions induced adverse drug reactions and 55.29% was minor drug-drug interactions induced adverse drug reactions. The interactions which were life threatening and/ or require medical intervention to minimize or prevent serious adverse effects were considered as severe drug-drug interactions and those interaction which resulted in an exacerbation of the patient's condition and/ or require an alteration in therapy were considered as moderate drug-drug interactions. The interactions which were limited clinical effects and manifestations may include an increase in the frequency or severity of side effects but generally would not require a major alteration in therapy were classified as minor drug-drug interactions. The correlation coefficient was 0.86 between the number of drugs given to the patient & number of average potential adverse drug reactions found among the patients. Increase in number of prescribed drug significantly (one way) increases number of potential adverse drug reaction due to drug-drug interaction (p<0.0001). Critically ill patients are more susceptible to drug-drug interactions due to the administration of multiple drugs and complex drug combinations. Several drug-drug interactions were clinically irrelevant.

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A new, simple high performance thin layer chromatographic method has been proposed for the determination of rizatriptan benzoate in a tablet dosage form. The drug was separated on aluminum plates precoated with silica gel 60 F­­ ₂₅₄ with dichloromethane-acetone-acetic acid 3:2:0.2(v/v/v) as mobilephase. Quantitative analysis was performed by densitometric scanning at 230 nm. The method was validated for linearity, accuracy, precision and robustness. The calibration plot was linear over the range 200-700 ng/band for rizatriptan benzoate. The method was successfully applied to the analysis of drug in bulk and marketed tablets.

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An analytical method based on high-performance liquid chromatography with ultraviolet detection (245 nm) was developed for the determination of actarit in human plasma. Coumarin was used as an internal standard. Chromatographic separation was achieved with a C8 column using a mobile phase of methanol: 1% acetic acid (50-50, v/v) with a flow rate of 1.0 ml/min. The calibration curve was linear over the range of 0.1-4.0 μg/ml (r ² > 0.99) and the lower limit of quantification was 0.1 μg/ml. The method was validated for sensitivity, accuracy, precision, recovery and stability. The method was used to determine the concentration-time profiles of actarit in the plasma following oral administration of 100 mg actarit tablets.

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A series of novel 2,3-disubstitutedquinazolin-4(3H)-ones have been synthesized by condensation of 2-substituted benzo[1,3]oxazine-4-ones and anthranilic acid. Synthesized compounds were evaluated for in vitro antiviral activity against HIV, HSV and vaccinia viruses. 5-Bromo-2-(6-bromo-4-oxo-2-phenyl-4H-quinazolin-3-yl)-benzoic acid (MBR2) exhibited distinct antiviral activity against Herpes simplex and vaccinia viruses.

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A pyrimidne nucleobase, 5-phenylthio-2,4-bisbenzyloxypyrimidine and its analogs were synthesized and scanned for in vitro antifungal activity using cup-plate and macrobroth dilution method against Candida albicans, Aspergillus niger, Aspergillus flavus and Aspergllus fumigatus. In the cup-plate method, 5-phenylthio-2,4-bisbenzyloxypyrimidine showed very good antifungal activity compared to clotrimazole at the concentrations of 100 and 1000 μg/ml and in the macrobroth dilution method, it showed comparable activity with respect to standard drugs fluconazole and itraconaole. In vivo antifungal activity of 5-phenylthio-2,4-bisbenzyloxypyrimidine at the dose levels of 10 and 30 mg/kg was carried by causing systemic infection of mice using the same fungi used in in vitro testing. The results from in vivo studies with 5-phenylthio-2,4-bisbenzyloxypyrimidine and fluconazole indicated that 5-phenylthio-2,4-bisbenzyloxypyrimidine had similar potency as fluconazole at both dose levels.

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