Olibanum and its resin and carbohydrate fractions were evaluated as rate controlling matrix materials in tablets for controlled release of diclofenac. Diclofenac matrix tablets were formulated employing olibanum and its resin and carbohydrate fractions in different concentrations and the tablets were evaluated for various tablet characters including drug release kinetics and mechanism. Olibanum and its resin component exhibited excellent retarding effect on drug release from the matrix tablets even at very low concentrations, 1 and 2% w/w in the formula. Diclofenac matrix tablets formulated employing olibanum and its resin component provided slow and controlled release of diclofenac over more than 24 h. Drug release from the matrix tablets was by Fickian diffusion and followed first order kinetics. Diclofenac release from some of the formulated tablets was comparable to that of Voveran SR tablets.

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The title compounds 1-substituted-4-phenyl-1,2,4-triazolo[4,3-a]quinazolin-5(4 H )-ones were synthesized by the cyclization of 2-hydrazino-3-phenylquinazolin-4(3 H )-one with various one carbon donors. The starting material 2-hydrazino-3-phenylquinazolin-4(3 H )-one was synthesized from aniline. Investigation of antimicrobial activity of the test compounds was made by agar cup-plate method against 8 pathogenic bacteria including Mycobacterium tuberculosis , 3 pathogenic fungi and antiHIV activity against replication of HIV-1(IIIB) and HIV-2(ROD) in MT-4 cells. The compound 7e inhibited 21% growth of M. tuberculosis at 6.25 µg/ml concentration, while the compounds 7c and 7d showed good antifungal activity against Candida albicans ; and the compounds 7c exhibited good antifungal activity against Aspergillus niger .

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The aim of the present work is to prepare and evaluate the oral mucoadhesive sustained release nanoparticles of clarithromycin in order to improve patient compliance by simplifing its administration, improving its therapeutic effect and reducing its dose related side effect. Clarithromycin containing gliadin nanoparticles were prepared by desolvation method using pluronic F-68® as a stabilizing agent. The results showed that this method is reproducible, very easy and led to the efficient entrapment of drug as well as formation of spherical particles ranging from 250-500 nm. Some process variables like effect of gliadin concentration and effect of surfactant were also evaluated with respect to their % drug entrapment and % yields. The maximum % drug entrapment and % yield were about 73 and 88%, respectively. The sustained release behavior of gliadin nanoparticles were evaluated both in phosphate buffer saline (pH 7.4) and simulated gastric fluid (pH 1.2), respectively, at 37±1°. Their mucoadhesive properties were determined by in vitro and in vivo methods. The shelf life of prepared nanoparticles was determined by storage at various temperatures while assessed in simulated gastric fluid (pH 1.2) with and without enzyme.

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Two simple, accurate and precise methods for simultaneous estimation of atorvastatin calcium and amlodipine besylate in combined dosage form have been described. First method employs formation and solving of simultaneous equations using 245 nm and 363 nm as two analytical wavelengths. Second is dual wavelength method, which uses the difference of absorbance value at 259.9 nm and 354 nm for estimation of atorvastatin calcium and absorbance at 363 nm for amlodipine besylate. Fifty percent methanol was used as solvent, in which atorvastatin calcium and amlodipine besylate shows linearity in the range of 0-40 µg/ml and 0-20 µg/ml, respectively. Standard deviation was <1.5 in the assay of tablets. Methods were validated as per ICH norms and accuracy, precision, repeatability and robustness was found to be with in the acceptable limit.

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Starting from 3-3-(4-methyl-benzoyl)propionic acid and using appropriate reagents, some new 2-arylidene-4-(4-methylphenyl)but-3-en-4-olides (IIIa-g) and their corresponding pyrrolone derivatives (IVa-d) have been synthesized. These compounds were evaluated for their antibacterial activity against Staphylococcus aureus and Escherichia coli as well as antifungal activity against Candida albicans . The compounds have considerable antifungal activity and moderate antibacterial activity.

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In the present study, we examined antiproliferative activity of quercetin in vitro and in vivo . Antiproliferative activity was demonstrated against MCF7 cell line in a dose and time dependent manner with IC50 value found to be 10 µg/ml. Further quercetin arrested MCF7 cells in G2/M phase of cell cycle in a dose and time dependent way. MCF-7 cells exposed to quercetin beta cyclodextrin complex showed reduced cell survival. Quercetin has found to act as an antiangiogenic molecule with concentrations up to 10 µg but had damaging effect on chick embryo chorioallantoic membrane at 25 µg. In animal studies quercetin inhibited tumor growth by more than 58% in mice grafted with mammary carcinoma and prolonged survival period of sarcoma 180 bearing mice by 2.3 times, respectively. We also evaluated whether quercetin enhances the therapeutic effect of mitomycin C, especially on mammary tumor growth. These studies indicated that quercetin markedly enhances the ability of mitomycin C to inhibit tumorigenicity in mammary adenocarcinoma. These effects are mediated in part by the often poorly vasalarized and hypoxic regions of tumors.

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In the present study four minoxidil gels were prepared using carbopol, hydroxypropyl cellulose, hydroxypropyl methylcellulose and combination of hydroxypropyl cellulose, hydroxypropyl methylcellulose for the treatment of alopecia. The gels were evaluated for drug content, viscosity determination, in vitro permeation (across dialysis membrane and mouse skin), skin irritation and stability at 4, 25 and 37° tests. The drug content of the gels was found to range from 96.40±0.57 to 98.10±0.32%. The viscosity of the gels ranged between 13,780±100 and 24,950±150 cps. The drug permeation across dialysis membrane from all the formulations at the end of 24 h was almost same and ranged between 92.05±1.52 and 93.52±1.95%. Although the difference is insignificant, the percentage release of drug was found to increase in the following order of the polymer composition: HPC>Carbopol>HPMC>HPMC+HPC. All the gel formulations released almost similar amounts of drug (90.05±1.92 to 91.56±1.65%) across the mouse skin; but the cumulative amount of drug permeated across dialysis membrane was more than that of the mouse skin. The marketed topical solution was found to diffuse almost 100% of drug across dialysis membrane and mouse skin at the end of 12 h. As supported by Higuchi's equation, the drug release mechanism from all the gels was found to be diffusion dominated. The prepared gels did not produce any dermatological reactions and were well tolerated by the mice. The gels were found to be stable with respect to viscosity, drug content and physical appearance at all temperature conditions for 3 months.

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Phenolics such as ferulic, caffeic, gallic acids and curcumin were tested for their potential anti proliferative and cytotoxic properties in human breast cancer cell line (MCF-7) as well as on a spontaneous mammary adenocarcinoma tumor. As a single agent, caffeic acid showed substantial growth inhibitory activity. In combination with cisplatin it was also found to be effective. For the current study we used a chick embryo model to assess antiangiogenic activity. Curcumin and its beta cyclodextrin complex were observed to interfere with capillary formation. The selected phenolics were structurally related which allowed us to gather additional information regarding the structure - activity relationship underlying the biological activity of these bioactive compounds. It was verified that the hydroxylated acid derivatives yielded better results than the merely hydroxylated ones in these tumor systems.

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A simple high-performance liquid chromatographic method for the determination of etoricoxib in human plasma has been developed. An aliquot quantity of 1 ml plasma sample was taken and 10 ml internal standard was added and mixed. Saturated borate solution of 0.3 ml was added to it and mixed for 1 minute followed by liquid-liquid extraction with ethyl acetate. Organic layer was separated and evaporated to dryness under nitrogen atmosphere at low temperature (below 50°). Residue was reconstituted with 150 µl of mobile phase. During the whole procedure the samples were protected from light. The assay was performed on Hypersil BDS, C18 (150×4.6 mm, 5 m particle size) column, using 10 milimol ammonium acetate buffer:acetonitrile = 65:35 v/v as mobile phase with ultra violet detection at 235 nm. Lower limit of detection was 10 ng/ml and lower limit of quantitation was 20 ng/ml. Maximum between-run precision was 7.94%. Mean extraction recovery was found to be 79.53 to 85.70%. Stability study showed that after three freeze-thaw cycles the loss of three quality control samples were less than 10%. Samples were stable at room temperature for 12 h and at -20° for 3 months. Before injecting onto HPLC system, the processed samples were stable for at least 8 h. The method was used to perform bioequivalence study in human.

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The decoction of the leaves of Nyctanthes arbor-tristis Linn. of Oleaceae widely used in Ayurvedic system of medicine for the treatment of sciatica, arthritis, fevers, various painful conditions and diuretics, liver disorders and as laxative. The aim of the present study was to evaluate the alcoholic and aqueous extracts of the leaves of Nyctanthes arbor-tristis for hepatoprotective effect against carbontetrachloride-induced liver damage in rats.Administration of alcoholic and aqueous extracts of the leaves of Nyctanthes arbor-tristis protect the liver from toxic effects of carbontetrachloride by reducing the elevated levels of Serum glutamate pyruvate transaminase, Serum glutamate oxaloacetate transaminase and serum bilirubin (total and direct). Results revealed that both the alcoholic and aqueous extracts showed significant hepatoprotective activity by reducing the elevated levels of biochemical parameters at a dose of 500 mg/kg body weight. The results were supported by histopathological studies of liver samples which showed regeneration of hepatocytes by the extracts.

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The fruits of Terminalia chebula, Terminalia bellerica and Emblica officinalis are important herbal raw materials containing polyphenols. They form the major constituents of widely used Ayurvedic formulations like Triphala churna . The extracts of these materials were standardized with respect to their total polyphenol contents as determined by Prussian blue method using gum acacia and phosphoric acid as stabilizers. The antioxidant activities were determined by DPPH (1,1-diphenyl-2-picryl-hydrazyl) method and inhibition of lipid peroxide formation induced by Fe2+-ascorbate system. They were found to strongly correlate with total polyphenol contents. The EC50 value (µg/ml) for free radical scavenging activity by DPPH method and IC50 value (µg/ml) for lipid peroxidation inhibitory activity along with the total polyphenol contents can be used as quality control parameters for standardization of herbal raw materials containing polyphenols as major phytoconstituents.

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Olibanum resin was evaluated as microencapsulating agent and to prepare resin-coated microcapsules. Resin-coated microcapsules of nifedipine were prepared by an industrially feasible emulsification-solvent evaporation method and the microcapsules were investigated. The resin-coated microcapsules are spherical, discrete, free-flowing and multinucleate monolithic type. Microencapsulation efficiency was in the range 98-105%. Nifedipine release from the resin-coated microcapsules was slow over 24 h and depended on core: coat ratio, wall thickness and size of the microcapsules. Drug release was by non-fickian diffusion mechanism. Good linear relationships were observed between wall thickness of the microcapsules and release rate and T50 values. Resin-coated microcapsules of nifedipine exhibited good controlled release characteristics and were found suitable for once a day oral controlled release products.

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Suspension cultures of Withania somnifera cells were established and shown to produce withaferin A. The identification of withaferin A was done by TLC, UV absorption, HPLC and electron spray mass spectroscopy. These cultures could be strongly elicited by exposure to salacin. Addition of salacin at the concentration of 750 µM to the cultures in production medium enhanced production levels of withaferin A to 25±2.9 mg/l compared to 0.47±0.03 mg/l in unelicited controls. This report is the first to demonstrate withaferin A production in plant suspension cultures and provides prerequisites for commercial scale, controlled production of withaferin A.

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A new simple, colorimetric method was developed on the basis of a chemical reaction of amine group in ambroxol hydrochloride with carbon disulphide to form dithiocarbamic acid, which on further reaction with cupric chloride forms a colored copper chelate. The yellowish-orange chromophore has absorption maxima of 448 nm and obeys Beer's law in the concentration range of 10-100 µg/ml. Results of the analysis were statistically validated by recovery studies. The method was found to be suitable for routine determination of ambroxol hydrochloride in tablet formulation.

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Two simple, accurate, precise and economical procedures for simultaneous estimation of famotidine and domperidone in two component tablet dosage form have been developed utilizing concept of standard addition. Both the methods utilize DMF/0.1N HCl (1:3) as solvent. Famotidine and domperidone at their respective lmax 267 nm and 285 nm shows linearity in the concentration range of 10-60 mg/ml. Wavelengths selected for estimation of famotidine and domperidone in simultaneous equation methods were 267 nm and 285 nm, respectively and for dual wavelength method were 275 nm, 291.1 nm and 275 nm, 257.9 nm, respectively. The result of analysis have been validated statistically, standard deviation lies in the range from 0.600-1.187, recovery studies range from 98.4-101.4% confirmed the accuracy of the proposed methods.

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The nonsteroidal antiinflammatory drugs are among the most widely prescribed and used drugs in the community for rheumatologic as well as nonrheumatologic conditions, which include acute and chronic pain; biliary, ureteric colic; dysmenorrhoea; fever; and other applications that derive from the suppression of prostaglandin synthesis. Almost all nonsteroidal antiinflammatory drugs irritate gastric mucosa and enhance ulceration by blocking protective action of the prostaglandins on gastric mucosa, causing ulcer formation not only in stomach but also in lower part of oesophagus and in duodenum too. This review focuses on the adverse effects of nonsteroidal antiinflammatory drugs, severity of these adverse effects and attempts made to reduce the side effects through the concomitant use of other drugs.

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Montelukast is a potent orally active cysteinyl leukotriene receptor antagonist that significantly improves parameters of asthmatics. A new liquid-liquid extraction based reverse phase liquid chromatography method has been developed and subsequently validated for the determination of montelukast in human plasma. The separation was achieved with C8 column (150×4.6 mm, 5 micron) and a mobile phase comprising of a mixture of 10 mM ammonium acetate buffer (pH 3.0) and acetonitrile in a ratio of 35:65 v/v. Montelukast was extracted from human plasma using a liquid-liquid extraction technique with ter-butylmethylether. The limit of detection and lowest limit of quantification were 5 and 10 ng/ml respectively. This method was found to be linear over the range of 10 to 1000 ng/ml with a recovery of 53 to 62%. Intraday and interday precision (% CV) was <15% and accuracy ranged from 96.23 to 108.39%. Stability studies showed that montelukast in human plasma is stable during the short-term period of sample preparation and analysis. This method can be used with small volume sample during pharmacokinetic studies.

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Aristolochia bracteate Retz, family, Aristolochiaceae is a common annual herb widely distributed in India and widely used in indigenous system of medicine. The objective of the present study was to investigate the antibacterial activity of crude extracts of Aristolochia bracteate Retz leaves by disc diffusion method. The leaves of Aristolochia breacteate Retz were extracted with petroleum ether, chloroform and alcohol. The concentrated crude leaf extracts of Aristolochia bracteate Retz were tested against Bacillus subtilus, Lactobacillus plantarum, Escherichia coli, Staphylococcus aureus, Streptococcus faecalis and Pseudomonas aeruginosa . Alcoholic extract showed significant antibacterial activity as compared to that of other extracts.

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Tablets of mutual prodrugs of ibuprofen, i.e, 'ibuprofen with paracetamol' and 'ibuprofen with salicylamide,' were prepared by direct compression method. The preformulation studies such as flow property, solid state stability at elevated temperatures, solid state stability under different humidity conditions, photolytic stability and compatibility studies of prodrugs with excipients were also performed to design and develop tablet formulations of prodrugs. Quality control tests and in vivo studies of prepared tablets of prodrugs were performed. The result of preformulation studies revealed that prodrugs have good flow property, good solid state stability at elevated temperatures and unstable under different humidity conditions. The photolytic stability study showed that prodrugs are quite stable to light; hence prodrugs are nonphotolytic. The compatibility study indicated that there was no incompatibility or interaction between prodrugs and excipients, which were tried. The prepared tablets of prodrugs were found to satisfy all quality control requirements of tablets mentioned in the Indian Pharmacopoeia. In vivo study of tablet formulations of prodrugs confirmed that they possessed the ability of parent drug, i.e., ibuprofen. In vivo study also showed better extent of bioavailability (indicated by AUC0-24) of tablet of prodrugs as compared to tablets of ibuprofen.

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Emblica officinalis , commonly known as Indian gooseberry ( Amla ), is found to be effective for the reversal of dyslipidemia and intima-media thickening and plaque formation in the aorta in hypercholesterolaemic rabbits. In this study, cholesterol powder (100 mg/kg body weight) was administered orally to healthy NZ white rabbits for 4 mo to induce hypercholesterolaemia; and thereafter, amla extract was given in two doses (10 mg and 20 mg/kg/d orally) for 4 mo. Fasting lipid profile was done monthly and also at the end of treatment. After sacrificing the animals, tissue cholesterol (liver, heart and kidney) and 3-hydroxy-3-methylglutaryl-Coenzyme A reductase activity of liver were estimated and part of aorta and myocardium were processed for histological studies. Feeding of amla extract (10 mg and 20 mg/kg) for 4 mo reversed these changes and the lumen of the aorta became normal as in the normal control group. Reversal of dyslipidemia and atheromatous plaques achieved by amla extract seems to be brought about by a number of factors, such as its ability to prevent low-density lipoprotein oxidation, its antioxidant action, besides decreasing synthesis of cholesterol by inhibiting 3-hydroxy-3-methylglutaryl-Coenzyme A reductase activity and elevating high-density lipoprotein level to enhance reverse cholesterol transport.

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The ethanol extract of Tephrosia purpurea Linn. (Family: Leguminosae) was found to significantly inhibit the carbon tetrachloride-induced lipid peroxidation in vivo and superoxide generation in vivo . The ethyl acetate fraction of the same extract was studied for free radical scavenging and antilipid peroxidation activity. The IC50 values in both of these in vitro assays were found to be significantly reduced for ethyl acetate fraction compared with the ethanolic extract of the plant. The observation was further supported by comparing the in vivo antioxidant activity for both the ethanolic extract and its ethyl acetate fraction. The study concluded that the ethanolic extract of T. purpurea exhibits antioxidant activity in vivo and the ethyl acetate soluble fraction has improved antioxidant potential than the extract.

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A simple, rapid, selective and sensitive reversed phase HPLC method was developed and validated for the determination of rebamipide from plasma. The drug was extracted with a mixture of chloroform and isopropyl alcohol. Rebamipide was measured in plasma using a validated HPLC method with UV detection at 280 nm. Chromatographic peaks were separated on a 5 µm C-18 silica column using a mixture of acetonitrile, water, methanol and acetic acid as a mobile phase. The chromatograms showed good resolution and no interference from plasma.The retention time of rebamipide and internal standard were approximately 4.9±0.3 min and 7.6±0.3 min, respectively. The mean recovery from human plasma was found to be above 91%. The method was linear over the concentration range of 10 to 500 ng/ml with coefficient of correlation (r2) 0.991. Both intra-day and inter-day accuracy and precision data showed good reproducibility. This method can be successfully applied to pharmacokinetic studies.

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The term transcranial route means the brain targeted transfer of drug molecules across the cranium through the layers of the skin and skin appendages of the head, arteries and veins of the skin of the head, the cranial bones along with the diploe, the cranial bone sutures, the meninges and specifically through the emissary veins. The administration of drugs through the scalp in ayurvedic system for the diseases associated with the brain was evaluated with a view to develop a novel targeted route for central nervous system drugs. It is expected to circumvent the systemic side effects of oral route. Diazepam was dissolved in an oil medium and applied on scalp as practiced in the ayurvedic system. Thirty rats were tested on the rotating rotarod for muscle relaxant effect of diazepam. Five groups of rats tested were the control, diazepam i.v. injected (280 µg/0.1 ml) group, two groups treated with transcranial diazepam oil solution (1.5 mg/0.2 ml) and the transcranial blank vehicle treated groups. Holding time in triplicate for each rat on the rotating rotarod was measured. The holding times following each treatment was statistically compared (one-way ANOVA). The pooled average times for the control, diazepam i.v. injected, diazepam oil solution transcranial treated two groups and the blank vehicle treated groups were 35.45, 4.73, 16.5, 15.39 and 33.23 seconds respectively. The two groups subjected to the brain targeted transcranial route showed a statistically significant decrease (50% drop) in the holding time against the control group indicating the centrally acting muscle relaxant effect due to absorption of diazepam into the brain through the proposed route.

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The title compounds were synthesized by the condensation of nitro-substituted 2-hydroxy-5- (nitro-substituted phenylazo) benzaldehyde (3) with different aromatic amines in presence of ethanol in good yield. The chemical structures were confirmed by IR, 1H NMR and elemental analysis. All the synthesized compounds (4a-j) have been evaluated for their in vitro antimicrobial activity against S. aureus , P. aeruginosa , E. coli , A. fumigatus , A. niger and C. neoformans .

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A simple, reproducible and efficient reverse-phase high performance liquid chromatographic (HPLC) method was developed for simultaneous determination of tizanidine and valdecoxib from their pharmaceutical dosage forms. Separation was done by using mobile phase of composition ammonium acetate buffer (0.1 M): methanol: acetonitrile in the ratio of 50:30:20 v/v. Quantitation was achieved with UV detection at 232 nm based on peak area, with linear calibration curves at concentration ranges from 1-100 µg/ml for tizanidine and valdecoxib respectively. The method has successfully been applied to pharmaceutical dosage forms. No chromatographic interference from the tablet excipients was found. The method was validated using ICH guidelines and was found to be highly precise, accurate and robust.

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A simple, sensitive, rapid, accurate and precise spectrophotometric method has been developed for estimation of acyclovir in bulk and pharmaceutical dosage forms. Acyclovir shows maximum absorbance at 253 nm with molar absortivity of 1.3733 ×104 l/mol×cm Beer's law was obeyed in the concentration range of 2-20 µg/ml. Results of the analysis were validated statistically and by recovery studies.

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In the present paper attempt was made to produce an excipient, β-cyclodextrin from starch by the action of an enzyme cyclodextrin glucosyl transferase. The microbial strain utilized was Bacillus circulans because of its specificity for production of β-cyclodextrin. First the culture was grown under controlled conditions to obtain an enzyme cyclodextrin glucosyl transferase which was isolated and purified. The crude enzyme was employed for bioconversion of starch to β-cyclodextrin. Some parameters like incubation pH, incubation and fermentation time and effect of certain additives like polyethylene glycol and calcium chloride added during incubation were studied to optimize its yield. The maximum yield of cyclodextrin glucosyl transferase was after 36 h of fermentation. β-cyclodextrin yield was found to increase with the increase in incubation period, by the addition of polyethylene glycol 200, polyethylene glycol 400 and at pH 6. The activity and stability of enzyme was found to increase by addition of calcium chloride.

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The present prospective study was conducted in order to establish the drug-prescription trend of non-steroidal antiinflammatory drugs in the management pattern of osteoarthritis at Panjab University Health Centre, Chandigarh, India. The study was carried out in between the months of November 2003 and March 2004. Data was collected from outpatients who visited Panjab University Health Centre. WHO based prescription-auditing performa was used for data collection. Demographic analysis of this prospective and observational study revealed that out of 84 patients most were females (63.1%) and maximum patients were in the age group of 40-60 (59.5%). Most of the patients at Panjab University Health Centre had primary generalized Osteoarthritis with the back (50%) being the site most commonly affected followed by knee (45.23%) and hips (14.3%). Pain and joint stiffness was the common feature of the clinical presentation. Non-Steroidal Antiinflammatory Drugs were mostly prescribed during the observation period predominantly for pain relief. The most commonly prescribed agents were nimesulide, paracetamol, diclofenac and ibuprofen. Mostly the drugs were administered in the tablet form (86.05%) with least use of gels/creams and capsules. The use of non-drug therapies including physiotherapy and exercise was least found. The present study represents the current prescribing trend of non-steroidal antiinflammatory drugs for osteoarthritis at Panjab University Health Centre and it also suggested that there is still considerable scope for improvement, particularly in prescribing non-drug therapies and improving dispensing habits.

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The study aims at preliminary phytochemical investigation and antifertility activity of dried flowers of Woodfordia fruticosa Kurz. The dried flowers were extracted successively with various solvents and individually with water and aqueous alcohol (50:50). The extracts were evaluated for phytochemical studies, including qualitative tests and high performance thin layer chromatography (HPTLC) analysis. Antifertility activity of successive alcoholic, individual aqueous and individual hydroalcoholic extracts was studied in female albino rats. The results revealed that the alcoholic extract showed significant abortifacient activity, whereas aqueous and hydroalcoholic extracts showed moderate activity as compared to the control. Thus, the successive alcoholic extract showed promising abortifacient activity at 100 mg/kg body weight.

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Transformed dedifferentiated cultures of Artemisia annua L. were established using four wild type strains of Agrobacterium tumefaciens . From the Ti-transformed in vitro gall calli so obtained cell suspension cultures were developed. Growth kinetics of Ti-transformed cell suspension cultures were studied and compared with untransformed (control) cultures. Ti transformed cell suspension cultures were found to exhibit faster growth rate than the control. Gall callus synthesized 0.2011 g/100 g DW of artemisinin while only 0.0178 g/100 g DW was detected in untransformed callus cultures Likewise. 38.6 µg/ml was found in spent medium of cell suspension culture at day 21, which shows a five fold increase in artemisinin over control (7.5 µg/ml).Cell suspension cultures are found to be practically more feasible than static cultures, hence an empirical approach is taken to scale up the Ti-transformed cell suspension culture in laboratory scale bioreactor (Batch process). The bioreactor cultivation yielded 45.56 µg/ml of artemisinin at day 21.The result suggests that the Erlenmeyer flasks results could be successfully scaled-up into the bioreactor and condition can be further optimized to have best artemisinin yield.

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Combinatorial chemistry is a novel synthetic strategy which leads to produce a large number of chemical libraries with predetermined structures. The advances in the research of combinatorial library synthesis and screening methods have enabled the medicinal chemists to identify highly active compounds rapidly. This method has revolutionized basic research and drug discovery. A number of combinatorial methods have been developed to boost the morale of medicinal chemists. Out of those, positional scanning synthesis plays a significant role to generate libraries from libraries. This approach is capable of producing infinite libraries. Our aim is to explore this method to understand the principle of synthesis and deconvolution screening methods to identify individual active compounds.

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Spliceosome-mediated RNA trans-splicing is a new technology for gene therapy that exploits the expressed genetic differences between normal and diseased cells. This technology may be applied to a wide range of diseases that involve the expression of unique or mutated genes. Spliceosome-mediated RNA trans-splicing technology can be employed to control the expression of any delivered gene by the presence of the chosen target pre-mRNA.

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In the present study, an attempt was made to develop a low-dose controlled-release delivery system for the treatment of periodontal infections. Nylon fibres were taken as core material. The coating solution contained polyvinyl acetate and amoxycillin trihydrate. The fibres were coated five times to maximize drug loading. The coating composition was optimized and fibres were subjected to in vitro release studies. For the study, a continuous-flow-through apparatus for in situ drug release, simulating the in vivo conditions of periodontal pocket, was designed in a manner that the drug released was well above the minimum inhibitory concentration of amoxycillin trihydrate. In situ samples were further subjected to microbiological evaluation against the microorganisms which are implicated in periodontal infections. Optimized fibre was further subjected to permeation rate study using modified Franz diffusion cell. The drug-coated fibres provided sustained effect up to a period of 11 d (264 h) and followed first-order release. The drug release followed Fickian diffusion mechanism. In situ samples revealed that the drug level at different time intervals remained above its minimum inhibitory concentration (1.5 µg/ml) for a period of 11 d. In situ release samples when subjected to microbiological evaluation against microorganisms inhibited the growth of S. aureus, S. mutans and B. cereus . Permeation rate studies through bovine cheek pouch membrane revealed that only a low level of drug permeated through the membrane and it followed zero-order permeation rate. The retentive fibres were shown to provide controlled delivery of amoxycillin trihydrate.

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Diclofenac sodium is one of the most widely used NSAIDS and its short half-life of 1-2 h necessitates preparation of a controlled release formulation. Spray drying, a one step process establishes intimate contact of the drug with the polymer and finds increasing applications in the area of controlled release formulations. Eudragit NE 30D is reported to be useful for preparation of controlled release formulations. An attempt has been made to prepare microparticles of diclofenac sodium with Eudragit NE 30D, using spray-drying technology in aqueous system. Aerosil was found to overcome the tackiness caused by Eudragit NE 30D and improved yield and flowability of the product, while talc did not overcome tackiness and did not prove to be suitable excipient. The microparticles were evaluated for percent yield, average particle size and flowability and were compressed into tablets. The tablets were studied for drug assay and dissolution profiles. The tablets containing drug polymer ratio of 1:1.212 were found to release the drug at the rate of 9.3 mg/h over the period of 10 h.

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The petroleum ether, chloroform, acetone and water extracts of mushroom Osmoporus odoratus were selected for examine the antibacterial activity against Staphylococcus aureus, Streptococcus pyogenes, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa by disc diffusion method using Muller Hinton agar media. And the extracts were compared with that of standard ampicillin (30 µg) and chloramphenicol (30 µg). The water extract alone showed antibacterial activity against the tested organisms and the results were comparable with that of ampicillin rather than chloramphenicol.

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A simple and sensitive spectrophotometric method has been developed for determination of roxithromycin in its pharmaceutical dosage forms. In the proposed method, roxithromycin is oxidized with potassium permanganate to liberate formaldehyde, which is determined in situ using acetyl acetone in the presence of ammonium acetate to give a yellow-coloured chromogen with absorption maxima at 412 nm. The method is found to be linear in the concentration range of 10-75 µg/ml with regression coefficient of 0.9987. No significant difference was found between the proposed method and the reported method when two-tailed t-tests are applied. Various reaction parameters, such as concentration of potassium permanganate and reagent, time required for oxidation and maximum colour intensity, were optimized. The method was validated and can be used successfully to assay roxithromycin in its pharmaceutical dosage form, viz, tablets.

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Chloroquine and hydroxychloroquine screened for antiviral activity against Hepatitis C virus in Huh-5-2 cells. Chloroquine and hydroxychloroquine reduces the HCV RNA and promote the cell growth with respect to untreated control at concentration of 10.75 µM and 6.6 µM respectively

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The purpose of this study was to examine the activity of ampicillin sodium developed as transdermal patch against Escherichia coli . In the present work, the efficiency of ampicillin sodium against E. coli was investigated in an in vitro infection model which simulates human pharmacokinetics. The E. coli stains were exposed to transdermal patch with different kinds of polymers such as sodium alginate, cellulose acetate phthalate, hydroxypropylmethylcellulose, chitosan and carboxymethylcellulose and the drug releasing capacity was studied through colony-forming units (CFU). The process was carried out for 24 h at 37°. It was found out that hydroxypropylmethylcellulose was the best polymer that gave less number of CFU, followed by carboxyl methyl cellulose, chitosan, cellulose acetate phthalate and sodium alginate.

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