Two simple, accurate and economical spectrophotometric methods in ultraviolet and visible region were developed for the determination of pioglitazone hydrochloride in bulk drag and in pharmaceutical formulation. In method A pioglitazone hydrochloride showed λmax at 269 nm in 0.2 N sulphuric acid solution, showing linearity in the concentration range of 10-60 μg/ml whereas in method B pioglitazone hydrochloride was reacted with diazotized sulphanilic acid in an alkaline medium. Yellowish orange coloured chromogen showed λmax at 420 nm, showing linearity in the concentration range of 10-50 μg/ml. The results of analysis have been validated statistically and recovery studies confirmed the accuracy of the proposed method.

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An ophthalmic gel of diclofenac sodium, a potent non-steroidal antiinflammatory drug was formulated using polymers of hydroxypropyl methylcellulose, sodium carboxymethylcellulose and methylcellulose. The gels were sterlized and assessed for various parameters like clarity, pH, physical appearance, physical stability, viscosity and uniformity of drug content. Almost 96% of drug was released from the hydroxypropylmethylcellulose formulation within a period of 9 h. Drug release obeys zero order kinetics. In vitro release for different gel formulation after 9 h is expressed in the decreasing order as follows hydroxypropylmethylcellulose gel>methylcellulose gel>sodium carboxymethylcellulose gel. Ocular irritation on score basis study in rabbits reveals that none of the gel formulation showed any redness, inflammation (or) increased tear production when compared with placebo. Diclofenac formulation was found t o b e more stable in hydroxypropylmethylcellulose gel compared to methylcellulose gel and sodium carboxymethylcellulose gel at ambient, refrigerator and incubator temperature. The stability of the gel was evidenced by the degradation rate constant. Formulated ophthalmic gel with hydroxypropylmethylcellulose proves to be a viable alternative to conventional eye drops as it offers longer precorneal residence time and excellent ocular tolerance.

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The available ocular drug delivery systems are fairly primitive and inefficient, but the stage is set for the rational design of newer and significantly improved systems. This review will discuss the progress of various types of ocular drug delivery systems and their characteristic advantages and limitations of each system, thus improvements can be made to overcome the constraints imposed by the eye. Two main approaches, i.e. improvement in bioavailability and controlled drug delivery systems are discussed. Combination of drug delivery systems could open a new directive for improving the therapeutic response of a non-efficacious system.

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The present study aimed at enhancing solubility and dissolution of nimesulide by applying solid dispersion technique followed by formulating it as suspension. Solid dispersions of nimesulide were prepared using propylene glycol, polyvinyl pyrrolidine-K30 and polyethylene glycol-6000 and formulated as respective suspensions. The suspensions were characterized by studying the particle size and sedimentation volume (Hu/Ho). In vitro evaluation was carried out in USP XXI dissolution apparatus. The in vivo evaluation of nimesulide suspensions were carried out in carrageenan induced rat paw edema method. Long term stability studies were carried out at different temperatures. Nimesulide suspensions with solid dispersion exhibited good suspendability and gave higher dissolution rates than those with plain nimesulide suspension. They also demonstrated enhanced anti-inflammatory activity when compared with plain drug suspension. The percentage edema inhibition obtained for different suspensions of nimesulide solid dispersion F2, F3 and F4 after 1 h were 76%, 79% and 82%, respectively. On the other hand edema inhibition of plain nimesulide suspension was only 40%. It can be concluded from the study that the suspension of nimesulide solid dispersion exhibited improved dissolution profiles, stability and in vivo efficacy.

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An attempt was made to formulate Boswellia serrata extract as a conventional tablet using various excipients in different proportions. Herbal raw materials and finished herbal medicinal products specifications were set according to committee for proprietary medicinal products. Eleven such formulations were prepared and evaluated for physical parameters such as thickness, hardness, friability, weight variation, drug content, disintegration time and drug release pattern. The formulations prepared with different proportions of disodium hydrogen phosphate in 10, 15 and 20% as solubilising agent showed maximum drug release. The formulated tablets had better appearance and drug release properties.

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A large number of Chinese and Japanese medicinal plants have been widely studied and data generated to provide scientific basis to the traditional claims. In majority of herbal formulations, preformulations and post formulation studies are lacking. Hence, an attempt is made to develop senna formulations using crude powder, standardized extract and calcium sennosides. Senna powder tablets were prepared by wet granulation method. Different binders and diluents affected the % compressibility and hardness of the formulations. Polyvinyl pyrrolidone and cocrystallized lactose-microcrystalline cellulose showed improved tablet characteristics. Senna powder contains mucilage, which slows the disintegration of the tablet. Cross-linked polyvinyl pyrrolidone improved disintegration time of senna power tablets. To improve the bioavailability, incorporate more amounts of actives and to reduce the dosage size, tablets of senna extract and calcium sennosides were prepared. Sennosides content was analyzed using HPLC method. Formulation parameters and dissolution study results of senna powder tablet were compared with tablet containing senna extract calcium sennosides. Calcium sennosides and senna extract tablet showed better dissolution than senna powder tablet.

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In the present study, the roots of Sariva (Decalepis hamiltonii, Cryptolepis buchananii, Ichnocarpus frutescens and Hemidesmus indicus) were investigated for antiinflammatory activity in carrageenan- induced rat paw oedema. The ethanol extracts of roots of various species of Sariva exhibited significant antiinflammatory activity at a dose of 350 mg/kg (p.o.) when compared to control group. The activity is compared with standard phenylbutazone. Cryptolepis buchananiiwas found to exhibit significantly more antiinflammatory activity when compared to the other three, Decalepis hamiltonii, lchnocarpus frutescens and Hemidesmus indicus.

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Earlier we have reported the antidiabetic activity of fresh juice of rhizomes of Zingiber officinale and its correlation with 5-HT receptor antagonism. Since 6-gingerol the marker compound of Z. officinale is reported to posses 5-HT antgonistic activity, the present investigation was undertaken to find out the concentration of 6-gingerol present in methanolic extract and ethyl acetate extract of Z. officinale. We also evaluated these extracts for antidiabetic activity in streptozotocin-induced type 2 diabetic rats. Streptozotocin-induced type 2 diabetic rats showed a significant increase in fasting glucose levels that was associated with increase in insulin levels. Treatment with methanolic extract and ethyl acetate extract of Z. officinale produced a significant decrease in fasting glucose and insulin levels in type 2 diabetic rats. In oral glucose tolerance test, treatment with methanolic extract and ethyl acetate extract of Z. officinale was found to significantly decrease AUCglucose and AUClnsulin, values in type 2 diabetic rats. Treatment with methanolic extract produced greater reduction in elevated levels of glucose and AUCglucose compared to ethyl acetate extract. Treatment with methanolic extract and ethyl acetate extract of Z. officinale also produced decrease in serum cholesterol, triglyceride, LDL-cholesterol and VLDL-cholesterol levels in type 2 diabetc rats. The concentration of &ginger01 was found to be greater in methaolic extract (3.08%) and lower in ethyl acetate extract (1.64%). In conclusion our data suggest methanolic extract of Z. officinale to have better antidiabetic activity in type 2 diabetic rats as compared to ethyl acetate extract of Z. officinale. The extent of activity appears to be dependent on the concentration of 6-ginger01 present in the extracts.

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An isocratic reverse phase high performance liquid chromatographic method with UV absorbance detection was developed for quantification of clozapine in rat serum. This method involves a single solvent extraction step with ethylacetate. Celecoxib served as the internal standard. The analytes were separated by HPLC using C18 Wakosil II RS (SGE) analytical column (5 μm particle size; 250'4.6 mm ID). Mobile phase comprised of methanol-water-triethylamine (75:25:0.5, v/v/v). The eluent was monitored at 254 nm by UV absorbance detection. Retention times of clozapine and celecoxib were 10.5 and 7.9 min, respectively. The mean absolute recovery value was about 75.8 to 79.9%,while the intra day and inter day coefficient of variation values were in the range of 2.1 to 5.7%.The calibration was linear over a concentration range of 100-4000 ng/ml. Accuracy ranged from 96.8 to 99.7%.The method was used to study the pharmacokinetics of clozapine after an intravenous bolus (10 mg/kg) and oral (20 mg/kg) administration of clozapine solution to rats.

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A simple and sensitive spectrophotometric method for the determination of ciprofloxacin hydrochloride in tablets is proposed. The solution of drug has been found to give a light reddish orange chromogen with β-naphthol in acidic medium, which absorbs at λmax 365 nm. This light reddish color was sufficiently stable to be used for quantitative purposes. The Beer-Lambert's law was found to be obeyed in the concentration range of 10-80 μg/ml.

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A rapid, selective and precise HPLC method for quantification of ofloxacin in tablets has been developed. The chromatographic resolution of ofloxacin was achieved using acetonitrile:0.1%v/v triethylamine (20:80, pH-4.0) as the mobile phase, in an isocratic run on a chromatographic system (Waters) equipped with Waters 600 pump controller, 2487 dual λ absorbance detector, Waters32 millennium chromatography manager software and C8 kromasil 5μ (4.6x150 mm) column. The flow rate was 1 ml/min and ofloxacin was monitored spectrophotometrically at 280 nm. Ornidazole was used as an internal standard.

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A simple, rapid, precise, highly specific and economical spectrophotometric method has been developed for the determination of tranexamic acid in its pharmaceutical dosage forms. The method is based on the reaction of the drug with sodium 1,2-napthoquinone-4-sulphonate forming reddish orange coloured chromogen with absorption maximum at 474 nm. The chromogen obeyed linearity in the concentration range of 10-70 μg/ml.

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Matrix tablets of cisapride and atenolol were prepared with varying proportions of hydroxypropylmethylcellulose of different viscosity grades viz; E15, E4M, K4M and K15M (15,4000, 4000 and 15 000 cps at 2% aqueous solution, respectively), alone and in combinations by wet granulation technique. The prepared tablets were evaluated for uniformities of weight, thickness, drug content and diameter, hardness and tensile strength, friability and disintegration time. The in vitro release kinetics of the matrix tablets were studied using USP XXI apparatus with distilled water as the dissolution medium. The tablet properties complied with the official limits. The efficiency of viscosity grades of hydroxypropylmethylcellulose in sustaining the release was observed to be in the following order E15>E4M>K4M>K15M. As the solubility of drug increases from cisapride to atenolol, an increase in the release rate was observed. The release of cisapride and atenolol from their respective tablets followed predominantly diffusion controlled mechanism, based on Higuchi's model. The study also indicated that the amount of drug released decreased with an increase in the polymer concentration (from 10, 20 to 30%).The combination of the different viscosity grades did not provide any additional advantage.

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2-Aryl-3-isonicotinamido-4-oxo-1,3-thiazolidine-5-yl ethanoic acid (2a-h) have been synthesized via cycloaddition of 4-arylidenehydrazido pyridine (1a-h) with mercaptosuccinic acid in THF containing a pinch of ZnCI2, which on treatment with thionyl chloride give corresponding ethanoyl chloride derivatives (3a-h).These on treatment with N-hydroxyphthalimide afford titled compounds (4a-h). IR, 1H NMR, Mass and 13C NMR determined their structures. All the synthesized compounds were screened for antibacterial (Bacillus subtilis, Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Pseudomonas aeruginosa and Salmonella typhi) and antifungal (Candida albicans and Aspergillus fumigatus) activities. All the compounds exhibited significant activity against the bacteria and fungl tested.

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Two simple, rapid, precise, highly specific and economical spectrophotometric methods have been developed for the determination of clopidogrel bisulphate in its pharmaceutical dosage forms. Method A is based on the reduction of ferric ions to ferrous ions which produce blue colour with potassium ferricyanide with absorption maximum at 760 nm. The chromogen obeyed linearity over 18-32 μg/ml. Method B is based on the hydrolysis of ester linkage of drug into acid form by heating with sulphuric acid. This acid form of drug has absorption maximum at 217 nm. Beer's law is obeyed in the concentration range of 4-18 μg/ml.

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Fruits and vegetables have been used as medicinal agents because of their health promoting properties attributed by different compounds, which primarily includes flavonoids. Flavonoids, the secondary polyphenols have been suggested to prevent atherosclerosis by its antioxidant property. Oxidation of low density lipoprotein may play a significant role in atherosclerosis. Various flavoniods in different fruits such as catechin, myricetin and quercetin (grapes); tannins and anthocyanins (pomegranate); quercetin, catechin and phyloridizin (apple); hesperedin and naringenin (citrus fruits); myricetin and kampferol (berries) are considered as potent antioxidants of low density lipoprotein. The status of antioxidants in such fruits is reviewed in detail.

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Two new spectrophotometric methods (absorbance ratio method and multiwavelength spectroscopy) for the simultaneous estimation of nimesulide and tizanidine hydrochloride in their combined dosage form have been developed and validated for linearity, accuracy, precision, limit of detection, limit of quantitation and robustness. In the first method, the wavelength selected to develop equations were 297.8 nm and 318.8 nm in methanol for nimesulide and tizanidine respectively and the isoabsorptive point is 302.6 nm. The wavelengths 297.8 nm and 318 nm were selected for the multiwavelength spectroscopy method. Both drugs obeyed Beer-Lambert's law in the concentration range of up to 60 μg/ml for nimesulide and up to 30 μg/ml for tizanidine. The results of both methods have been statistically validated and were found to be satisfactory. These methods were found to be simple, rapid, accurate, precise and reproducible.

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Calamus rotang is a shrub, which is not much explored scientifically. Studies on the ethanolic (95%) extract of rhizome exhibited antiinflammatory activity in carrageenan-induced paw oedema and cotton pellet granuloma pouch models and the results were comparable with that of standard drug Phenylbutazone.

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A simple rapid, precise, accurate and highly specific spectrophotometric method has been developed for the determination of β-arteether in its pharmaceutical dosage forms. Arteether is a newer antimalarial derivative of artemisinin. Arteether has no UV absorption above 220 nm because of the absence of any chromophore group in its molecule. Therefore, it has to be degraded with 5M HCI, which produces chromophore groups that can absorb at 254 nm. Beer-Lambert law is followed in the concentration range of 5-50 μg/ml. The accuracy and reproducibility of the proposed method was statistically validated by variation studies.

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A series of novel 2,3-disubstituted/6,8-dibromo-2,3-disubstituted quinazolin-4(3H)-ones have been synthesized by condensing the primary amino group of lamotrigine with benzoxazin-4-one.The structure of the synthesised compounds was elucidated by spectral analysis (IR, NMR and Mass). The compounds synthesized were screened for antibacterial and antiHlV activities against replication of HIV-1 and HIV-2 in acutely infected LIT-4 cells. The compounds SPC-I, SPC-I Brand SPCIII Br (100 μg/ml) exhibited equivalent antibacterial activity with the standard ciprofloxacin (10 μg/ ml) against salmonella typhi. All the compounds exhibited cytotoxic properties in the MT-4 lymphocyte cell line,.

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A series of N-(4,6-dimethyl-2-pyridlnyl)benzamldeas s non-acidic antiinflammatory drugs was subjected to a 3D-quantitative structure activity relationship using Comparative Molecular Field Analysis. The series was studied with an attempt to derive a co-relationship between biological activity as dependent variable and descriptors as independent variables. The statistical method used was partial least square analysis to ascertain a co-relationship.

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The microwave-assisted syntheses of N-hydroxy-N1-aminoguanidines (S1-S8) starting from thiosemicarbazide are reported herein. These derivatives were evaluated against infection by the human immunodeficiency virus type-1 using human T4 lymphocyte cell line and yellow fever virus strain 17D activity in Vero cells. Compound 1-(4'-chlorobenzylidene) amino-3-hydroxy guanidine (S3) showed maximum percentage protection of 43.68% against HIV-1 induced cytopathogenicity. Compound S3 was also found to be the most active compound against YFV with EC50 of 2.5 μM, and CC50 of more than 100 μM when compared to ribavirin.

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Alzheimer's disease is a progressive neurodegenerative disorder and is the most common cause of dementia in elderly people. There are four different genetic loci associated with inherited susceptibility to Alzheimer's disease. The four genes to be identified in association with inherited susceptibility to Alzheimer's disease are amyloid precursor protein, apolipoprotein E epsilon 4, presenilin 1 and presenilin 2. The mutations or polymorphisms in these genes cause excessive cerebral accumulation of the amyloid beta-protein and subsequent neuronal and glial pathology in brain parts which are important for memory and cognition. Other miscellaneous genes involved in Alzheimer's disease are interleukin-1 alpha, interleukin-6, interleukin-10, tumor necrosis factoralpha, cystatin C, neprilysin, angiotensin converting enzyme, BACE 1, cathepsin D and brainderived neurotrophic factor.

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The authors tested 27 formulations, picked up randomly from local market under WHO and ICH prescribed accelerated stability test conditions of 40°/75% RH for 3 months in the presence and the absence of light. In several formulations, the physical changes were stronger in light than in dark, though examples existed where results were similar in the two conditions. Under light, both primary and secondary packaging was affected, and fading of container color and the print fading were the common problems. Even formulations within the packs were affected in some cases, and the changes were in the form of gain of moisture and loss of integrity in case of effervescent tablets, color fading of capsules in blisters, sticking of capsules in a glass bottle and spread of powder within strip pockets. There were other changes, that include softening of suppositories; change in viscosity of a gel, jelly, cream and ointment; melting of lozenges and phase separation of emulsions, but these were among those expected to occur normally under accelerated storage conditions.

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Resorcinol on reaction with ethylacetoacetate in the presence of concentrated sulphuric acid afforded 7-hydroxy-4-methyl chromen-2-one (1), which when refluxed with 1-bromo-3-chloropropane in acetonitrile and in the presence of anhydrous potassium carbonate yielded 7-(3-chloropropoxyl)- 4-methyl chromen-2-one (2). Substitution of chlorine from (2) with secondary amines in toluene and in the presence of triethylamine resulted in the title compounds (3a-e) in 50-60 % yield. Their chemical structures have been assigned by elemental analysis , IR ,and 1HNMR analyses. The compounds were screened for 5-HT2A antagonist activity and spontaneous motor activity. All title compounds have been found to show significant 5-HT2A antagonist activity and caused reduction in spontaneous motor activity.

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Lipophilicity profile of mosapride citrate dihydrate over a broad pH range has been determined by potentiometry. The lipophilicity of mosapride citrate dihydrate increases with the increase in pH but after pH 5.5, any change in pH does not affect the lipophilic behaviour of mosapride citrate dihydrate.

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A reversed-phase high-performance liquid chromatographic method for the estimation of carthamin in Carthamus tinctorius is described. The aim of this work is to provide a simple and accurate method of standardization of C. tinctorius flower petals, extracts and formulations made from them for carthamin.

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In the present investigation ibuprofen prodrugs of α-, β- and γ-cyclodextrins were synthesized. The primary hydroxy group of α-, β- and γ-cyclodextrins was 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 faecal 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 ibuprofen and equivalent doses of the esters.

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A reverse phase high performance liquid chromatography method for the simultaneous estimation of rofecoxib and tizanidine hydrochloride in tablets is developed. The determination was carried out on a Wakosil C18 (250x4.6mm, 5 μm) column using a mobile phase of acetonitrile and phosphate buffer pH 5.0 (50:50%v/v). The flow rate was 0.5 ml/min with detection at 240 nm. The retention time for tizanidine hydrochloride was 4.9 min and rofecoxib 12.2 min. Rofecoxib showed a linear response in the concentration range of 50-200 μg/ml and tizanidine hydrochloride 10-80 μg/ml. The results of analysis have been validated statistically and by recovery studies. The recoveries obtained for standard rofecoxib and tizanidine hydrochloride from the formulation ranged from were 98.20 to 101.6%.

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Several 1,3-thaizolidin-4-ones bearing variously substituted diaryl ring at C-2 and N-3 positions have been synthesized utilizing microwave irradiation and evaluated for their antiHlV and antiYFV activities. The results of the in vitro antiHlV evaluation showed that compound DS13 proved to be an effective inhibitor of HIV-1 replication with EC50 of 10 μM, CC50 of 120 μM and percentage protection of 104%.

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