A simple, precise, accurate and rapid high performance thin layer chromatographic method has been developed and validated for the estimation of telmisartan and hydrochlorothiazide simultaneously in combined dosage forms. The stationary phase used was precoated silica gel 60F₂₅₄. The mobile phase used was a mixture of chloroform: methanol: toluene (2:5:5 v/v/v). The detection of spots was carried out at 272 nm. The method was validated in terms of linearity, accuracy, precision and specificity. The calibration curve was found to be linear between 250 to 500 ng/spot for telmisartan and 200 to 700 ng/spot for hydrochlorothiazide. The limit of detection and the limit of quantification for the telmisartan were found to be 75 and 190 ng/spot, respectively, and for hydrochlorothiazide 55 and 150 ng/spot, respectively. The proposed method can be successfully used to determine the drug content of marketed formulation.

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Zidovudine-ethylcellulose microspheres were prepared by water-in-oil-in-oil double emulsion solvent diffusion method. Spherical free flowing microspheres having an entrapment efficiency of 32-54% were obtained. The effect of polymer-drug ratio, surfactant concentration for secondary emulsification process, volume of processing medium and stirring speed of secondary emulsification process was evaluated with respect to entrapment efficiency and in vitro drug release behaviors. Infrared spectroscopy and differential scanning calorimetric analysis confirmed the absence of any drug polymer interaction. The in vitro release profile could be altered significantly by changing various processing and formulation parameters to give a controlled release of drug from the microspheres. The in vitro release profiles from microspheres of different polymer-drug ratios were applied on various kinetic models. The best fit with the highest correlation coefficient was observed in higuchi model, indicating diffusion-controlled principle. The n value varies between 0.23-0.54 obtained from korsemeyer-peppas model confirmed that the mechanism of drug release was diffusion controlled.

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The present work describes a validated reverse phase high performance liquid chromatographic method for simultaneous estimation of telmisartan and hydrochlorothiazide in tablet formulation. Chromatography was performed on a ODS Hypersil C18 (25 cm×4.6 mm I.D) column from thermo in isocratic mode with mobile phase containing acetonitrile:0.05 M KH₂PO₄ pH 3.0 (60:40). The flow rate was 1.0 ml/min and the eluent was monitored at 271 nm. The selected chromatographic conditions were found to effectively separate telmisartan (RT- 5.19 min) and hydrochlorothiazide (RT- 2.97 min). Linearity for telmisartan and hydrochlorothiazide were found in the range of 4.1-20.48 µg/ml and 1.28-6.4 µg/ml, respectively. The proposed method was found to be accurate, precise, reproducible and specific and can be used for simultaneous analysis of these drugs in tablet formulation.

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Three simple, accurate and economic methods; multicomponent, two wavelength and simultaneous equations using area under curve have been described for the simultaneous estimation of aceclofenac and paracetamol in tablet dosage form. Absorption maxima of aceclofenac and paracetamol in methanol diluted with glass double distilled water was found to be 274.5 nm and 244 nm, respectively. Beer's law was obeyed in the concentration range 2-20 mg/ml for aceclofenac and 5-40 mg/ml for paracetamol. The methods allow rapid analysis of binary pharmaceutical formulation with accuracy. Results of three methods were validated statistically and by recovery studies and were found to be satisfactory.

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Oxcarbazepine, a new anticonvulsant drug, has been used as an add-on or first line treatment in adults and children. As precision of dosing and patient's compliance become important prerequisite for a long term antiepileptic treatment, there is a need to develop a formulation for this drug which overcomes problems such as difficulty in swallowing, inconvenience in administration while travelling and patient's acceptability. Hence, the present investigation was undertaken with a view to develop a fast dissolving tablet of oxcarbazepine which offers a new range of product having desired characteristics and intended benefits. Fast dissolve tablets of oxcarbazepine were prepared containing Avicel PH 102 as a diluent and Ac-Di-sol as a superdisintegrant by wet granulation process. All the formulations were evaluated for characteristics such as hardness, friability, weight variation, wetting ability, disintegration time and dissolution rate. A modified disintegration method was used for studying disintegration. Since the drug is poorly water soluble, drug release was tested in various media and the effect of surfactant on drug release was studied. An effective, pleasant tasting and stable formulation containing 12% Ac-Di-sol, 25% Avicel PH 102 and 8.5% starch as a binder was found to have a good hardness of 4-4.5 kg/cm², disintegration time of 28±5 s and drug release of not less than 90% within 30 min. The drug release was found to be comparable to the marketed dispersible tablet.

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To minimize the unwanted toxic effects of anti maniac drug lithium carbonate by kinetic control of drug release, it was entrapped into gastro resistant, biodegradable, waxes and fat such as beeswax, cetostearyl alcohol, spermaceti and cetylalcohol microspheres using meltable emulsified dispersion cooling induced solidification technique utilizing a wetting agent. Solid, discrete, reproducible free flowing microspheres were obtained. The yield of the microspheres was up to 90.0%. More than 98.0% of the isolated microspheres were of particle size range 115 to 855 mm. The microspheres had smooth surfaces, with free flowing and good packing properties. Scanning electron microscope confirmed their spherical structures within a size range of 339-355 mm. The drug loaded in waxes and fat microspheres was stable and compatible, as confirmed by DSC and FTIR studies. The release of drug was controlled for more than 8 hours. Intestinal drug release from waxes/ fat microspheres was studied and compared with the releases behavior of commercially available formulation Intalith CR®-450. The release kinetics followed different transport mechanisms. The drug release performance was greatly affected by the materials used in microsphere preparations, which allows absorption in the intestinal tract.

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The simple spectrophotometric methods for the determination of mefenamic acid and ethamsylate in pharmaceutical formulations have been developed. The methods are based on the additivity of absorbances and the determination of graphical absorbance ratio at two selected wavelengths, one being the isoabsorptive point for the two drugs (301 nm) and the other being the absorption maximum of mefenamic acid (336 nm) and ethamsylate (305 nm). The Beer Lambert's law is obeyed for mefenamic acid in the concentration range 4-28 µg/ml and for ethamsylate is 10-60 µg/ml. Both the methods were found to be simple, rapid, and accurate and can be adopted in routine analysis of drugs in formulations. The accuracy and reproducibility of the proposed method was statistically validated by recovery studies.

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A simple, specific, accurate and precise reverse phase high pressure liquid chromatographic method has been developed for the simultaneous determination of nimesulide and tizanidine from tablets. The sample was analyzed using methanol: water in the ratio of 65:35, pH adjusted to 4.15 with orthophosphoric acid on an octadecylsilane C₁₈ column. The effluent was monitored at 1.4 ml/min flow rate using 307 nm as detecting wavelength. The linear dynamic ranges for nimesulide and tizanidine were 0.2-1.0 mg/ml and 10-50 mg/ml, respectively. Coefficients of correlation obtained for nimesulide and tizanidine were 0.998 and 0.996 - respectively.

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Solubility enhancement of poorly aqueous soluble drug is an important aspect of formulation development. Although there is plethora of reports of solubility improvement using different techniques, a comparative study of different solubilization approaches are few. Valdecoxib chemically designated as 4-(5-methyl-3-phenyl-4-isoxazolyl) benzenesulfonamide is a novel potent COX-2 inhibitor having poor aqueous solubility (10 mg/ml). Since it is poorly water-soluble, various techniques could be applied to increase its aqueous solubility. Objective of present study was to provide a comparison of effect of various solubilization techniques, namely micellar solubilization, cyclodextrin complexation and cosolvency, on solubility of valdecoxib. Solubility of valdecoxib was determined in various ionic and nonionic surfactants using phase solubility analysis. Similar type of study was performed using different water:cosolvent mixture. In addition, solubility improvement by use of 2 novel hydrophilic β -cyclodextrin derivatives, hydroxypropyl β -cyclodextrin and sulfobutyl ether-7-β -cyclodextrin was examined. Results showed that highest solubility (70 fold) was achieved with use of Cremophor EL followed by Tween 80 and sulfobutyl ether-7-β -cyclodextrin. It was found that surfactants with higher HLB values were better solubilizers. Solubilization capacity was found to increase with increase in hydrocarbon chain of surfactant, suggesting hydrocarbon core of micelles as locus of solubilization. Similarly, less polar solvents were found to increase solubility by greater extent, thus accentuating hydrophobic interaction mechanism. Among cyclodextrin, higher binding constant and solubility enhancement was obtained by use of sulfobutyl ether-7-β -cyclodextrin. Thus, the study generated an important dataset so as to compare effect of various solubilizers on solubility of valdecoxib.

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Crude aqueous extract of Cleome rutidosperma was investigated for diuretic and antibacterial activity. The diuretic activity was tested in rats at 400 and 600 mg/kg, orally and compared with furosemide (20 mg/kg, intraperitoneally) as the standard. The antibacterial activity was assessed by disc diffusion method against Bacillus subtilis , Bacillus laterosporus , Staphylococcus aureus , Micrococcous luteus, Pseudomonas aeruginosa , Vibrio cholerae , Escherichia coli and Salmonella typhi at concentrations of 100, 200 and 400 µg/disc respectively. Ciprofloxacin (5 µg/disc) was used as reference control for the antibacterial study. The extract was found to possess significant dose dependent diuretic activity and also effective against both gram-positive and gram-negative bacteria in a concentration dependent manner.

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A series of novel thiolactosides like S -hepta- O -acetyllactosyl-1-arylisothiocarbamides (1a-g) and hepta- O -acetyl lactosyl arydithiocarbamates (2a-g) were prepared by the interaction of hepta- O -acetyl lactosyl bromide with arylthiocarbamides and ammonium aryldithiocarbamates respectively. Similarly (hepta- O -acetyl lactosyl)-1,5-disubstituted-2-isothiobiurets (3a-g) 1,5-disubstituted-2,4-isodithiobiurets (4a-g) and-1,2,4-thiadiazolines (5a-g) were synthesized by the interaction of (1a-g) with phenyl isocyanate, phenyl isothiocyonate and S -chloro- N -phenyl isothiocarbamoyl chloride respectively. The compounds 3-Aryl-2,6-diphenylimino 4-S-hepta- O -acetyl lactosyl-2,3dihydro-1,3,5-thiadiazines hydrochlorides (6a-g) were prepared by the interaction of (4a-g) with phenyl isocyanodichloride. In the present investigation activities of these thiolactosides against pathogenic bacteria and fungi such as E. coli, S. aureus, P. vulgaris, Salmonella typhi, Candida guilliermondii and A. niger are discussed.

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A natural gum, damar was investigated as a novel microencapsulating material for sustained drug delivery. Microparticles were prepared by oil-in-oil emulsion solvent evaporation method. Ibuprofen and diltiazem hydrochloride were used as model drugs. Microparticles were evaluated for particle size, encapsulation efficiency and in vitro drug release kinetics. Images of the microparticles were obtained by bright field microscopy. The effect of different gum:drug ratios and solubility of drug on microparticle properties was principally investigated. Gum damar could produce discrete and spherical microparticles with both drugs. With a freely water soluble drug (diltiazem hydrochloride), gum damar produced bigger (45-50 µm) and fast drug releasing microparticles with low encapsulation efficiencies (44-57%). Contrary, with a slightly water soluble drug (ibuprofen), gum damar produced small (24-33 µm) microparticles with better drug encapsulation (85-91%) and sustained drug delivery. The increase in gum:drug ratio showed an increase in particle size, encapsulation efficiency and decrease in drug release rate in all cases. Drug release profiles of all microparticles followed zero order kinetics. In conclusion, gum damar can be used successfully to produce discrete and spherical microparticles of ibuprofen and diltiazem hydrochloride.

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A simple, precise, accurate and rapid high performance thin layer chromatographic method has been developed and validated for the determination of cefpodoxime proxetil in dosage form. The stationary phase used was precoated silica gel 60F₂₅₄. The mobile phase used was a mixture of chloroform: methanol: toluene (4:2:4 v/v/v). The detection of spot was carried out at 289.0 nm. The method was validated in terms of linearity, accuracy, precision and specificity. The calibration curve was found to be linear between 100 to 700 ng/spot for cefpodoxime proxetil. The limit of detection and the limit of quantification for the cefpodoxime proxetil were found to be 30 ng/spot and 90 ng/spot, respectively. The proposed method can be successfully used to determine the drug content in marketed formulation.

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A simple, efficient and reproducible method for the simultaneous determination of gatifloxacin and ornidazole from tablets has been developed using reversed phase high performance liquid chromatography. The separation was done using a mobile phase consisting of acetonitrile: methanol: water (50:37.5:12.5). Column used was Hypersil C₁₈ (250×4 mm i.d.) 5 m with a flow rate of 1 ml/min with detection at 280 nm. The external standard calibration method was employed for quantification. An elution order of gatifloxacin was 2.58 min and ornidazole was 5.54 min. The linear dynamic range was 20-100 mg/ml and 50-250 mg/ml for gatifloxacin and ornidazole, respectively. Analytical parameters were calculated and a full statistical evaluation included.

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The ethyl acetate and n-butanol fractions of ethanol extract of Bacopa monnieri Linn. aerial parts were screened for antibacterial and antifungal activities by both zone of inhibition study and determination of minimum inhibitory concentration (MIC). The ethyl acetate fraction was found to be more potent than the n-butanol fraction, though both of them were endowed with antimicrobial activity. The present study reveals the potential usefulness of B. monnieri aerial parts in the treatment of various pathogenic diseases as mentioned in the Ayurvedic literature.

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Dissolution is the rate-limiting step in the absorption of drugs from solid dosage forms. This is to be focused especially when the drug is poorly soluble. Etoposide is a poorly soluble drug and its absorption is dissolution rate limited. The present study is aimed at improving the dissolution of etoposide. Solid dispersions of drug with surfactants were prepared by using kneading technique. Kneading technique is more applicable to industry. Surfactants such as cetrimide, sodium lauryl sulphate, Tween 80 and Cremophor RH40 were used in different proportions. Etoposide gave faster dissolution rates when Cremophor RH40 was used. The DSC thermograms and IR spectra revealed no interaction of etoposide with these surfactants and no degradation in etoposide molecule was observed.

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The primary aim of the study was to assess the medication knowledge of hemodialysis patients and to evaluate the impact of education on their medication knowledge. This was a prospective randomised study, conducted in two phases. Study population consisted of 90 hemodialysis patients, randomised into two groups. Baseline medication knowledge of these patients was assessed using medication knowledge assessment questionnaire developed for the study. During the first phase of the study, group I patients received the education provided by a trained clinical pharmacist regarding their medications for eight-weeks and group II patients were deprived of clinical pharmacist provided education but received services only by usual healthcare group. At the end of week eight, medication knowledge assessment questionnaire was applied to both the groups of patients. In the second phase, group I patients were deprived of clinical pharmacist education and group II patients were rendered with clinical pharmacist provided education for eight-weeks and medication knowledge assessment questionnaire was once again administered to both the groups at the end of week 16. At the end of week eight, there was a statistically significant ( P< 0.05) improvement in the medication knowledge assessment questionnaire scores observed in group I, compared to baseline medication knowledge assessment questionnaire scores and week eight scores of group II patients. There was no significant ( P >0.05) improvement observed in scores of group II compared to baseline. At the end of week 16 of the study period, there was a statistically significant ( P< 0.05) improvement in the medication knowledge assessment questionnaire scores of the group II patients compared to their baseline and week eight scores. At the end of week 16 there was a significant ( P< 0.05) drop in the medication knowledge assessment questionnaire scores of group I patients compared to their week nine scores. The study confirms that medication knowledge of the hemodialysis patients was extremely poor regarding the name, indication and dosage regimen of their medications. Study emphasizes the need for the continued education to the hemodialysis patients for better understanding of the medications they use. A trained clinical pharmacist could play a vital role in educating hemodialysis patients, which has obvious benefits on therapeutic outcome.

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The title compounds 2-methyl-3-(substituted methylamino)-(3 H )-quinazolin-4-ones were synthesized by condensing the active hydrogen atom of the amino group of 3-amino-2-methyl-(3 H )-quinazolin-4-one with formaldehyde and appropriate amines. Their structures were confirmed by spectral data (IR, ¹H-NMR and Mass) and the purity was ascertained by elemental analysis. Investigation of antimicrobial activity of the test compounds was performed by agar dilution method against 7 pathogenic bacteria, 3 pathogenic fungi and antiHIV activity against replication of HIV-1(IIIB) and HIV-2 (ROD) in MT-4 cells. The compounds exhibited significant antibacterial and antifungal activities.

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A simple new spectrophotometric method has been developed for determination of rabeprazole in pharmaceutical bulk dosage form. The method was based on the formation of ion-pair complexes of the drug with four dyes, viz. bromo thymol blue, bromocresol green, bromophenol blue and bromocresol purple in acidic buffer solutions followed by their extraction in chloroform. The absorbance of the organic layer was measured at its respective wavelength of maximum absorbance against the corresponding reagent blank. The method has been statistically evaluated and was found to be precise and accurate. Phosphate buffer of pH 2 and bromocresol green dye gave maximum absorbance of rabeprazole at 454 nm.

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The aim of the present investigation was to develop oral films of valdecoxib using Eudragit EPO and hydroxypropylmethylcellulose. Films of Eudragit EPO, hydroxypropylmethylcellulose and Eudragit EPO combined with hydroxypropylmethylcellulose were prepared by film casting method. Glycerol, menthol and aspartame were incorporated in the drug containing films as plasticizer, cooling agent and sweetener, respectively. The drug loading was 10 mg valdecoxib per 4 cm² of the film. The films were evaluated for hydration study, folding endurance and in vitro drug dissolution in the distilled water. The films containing both Eudragit EPO and hydroxypropylmethylcellulose films showed neutral surface pH when prepared using 0.1 N HCl as a solvent. Glycerol played a critical role in imparting flexibility to the film and improving the drug release from film. The bitter taste of the drug was masked by using aspartame and menthol accompanied by the synergistic effect of Eudragit and glycerol. Water uptake by films was found to be dependant both on the amount of Eudragit EPO and glycerol. The films containing the higher proportion of glycerol showed higher water uptake and faster drug release at all the sampling time in the in vitro dissolution test. Optimum plasticity was obtained using the required concentration of hydroxypropylmethylcellulose and glycerol. The study revealed that taste masked valdecoxib films can be developed by the selection of appropriate film former and by the use of auxiliary excipients.

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Influence of processing variables on the solid-state of a model drug, piroxicam in cyclodextrin-based system and its effect on dissolution behavior of the drug was investigated in the present study. Binary systems containing piroxicam and hydroxypropyl-β -cyclodextrin prepared by various processes, were characterized by FTIR, thermal stability, photo stability and dissolution studies. Hydroxypropyl-β -cyclodextrin enhanced the solubility of piroxicam and increased dissolution rates from the binary systems. The complex prepared by co-evaporation method was found to yield better dissolution rate and stability as characterized in present study over those of the complex prepared by other methods.

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Two simple and sensitive spectrophotometric methods (A and B) for the determination of racecadotril in bulk drugs and pharmaceutical formulations are described. In method A, methanol was used as solvent and shows absorption maximum at 231 nm. In method B, the solvent used was acetonitrile:water in the ratio of 1:3 and shows absorption maximum at 232 nm. The Beer's law range for method A is 25-100 mg/ml and 20-80 mg/ml for method B. When capsules dosage forms were analyzed, the results obtained by the proposed methods are in good agreement with the labeled amounts and the results were validated statistically.

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A sensitive and rapid extractive spectrophotometer method has been developed for the assay of carvedilol in pharmaceutical formulations. The method is based on the formation of a chloroform soluble ion-pair complex between carvedilol and bromocresol green in an acidic medium. The complex shows absorption maximum at 415 nm and the system obeys Beer's law in the concentration range of 5-25 µg/ml. The results obtained by the proposed method were validated statistically and by recovery studies.

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Wound healing activity of aqueous and ethanol leaf extracts of L. serratum was studied by excision, incision and dead space wound models on rats. As compared to aqueous and control group of animals, ethanol extract showed significant wound healing activity which was evidenced by significant decrease in the period of epithelialisation (17.84±0.06) and increase in wound contraction rate, skin breaking strength (581.45±4.98), granulation tissue breaking strength (512.80±5.08), dry weight of granulation tissue (47.23±0.10) and elevated concentration of hydroxyproline (2322.83±8.49). Histopathalogy of the granulation tissue of the ethanol extract treated animals showed few macrophages with increase in collagenation indicating the potency of the ethanol extract in promoting the process of wound healing. The present finding provides a scientific base to the ethno medicinal use of L. serratum.

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A simple, precise, accurate and rapid high performance thin layer chromatographic method has been developed and validated for the simultaneous estimation of irbesartan and hydrochlorothiazide in combined dosage forms. The stationary phase used was precoated silica gel 60F[254]. The mobile phase used was a mixture of acetonitrile: chloroform: glacial acetic acid (7:3:0.1 v/v/v). The detection of spots was carried out at 260 nm. The method was validated in terms of linearity, accuracy, precision and specificity. The calibration curve was found to be linear between 100 to 700 ng/spot for irbesartan and 100 to 350 ng/spot for hydrochlorothiazide. The limit of detection and the limit of quantification for the irbesartan were found to be 30 and 100 ng/spot respectively and for hydrochlorothiazide 25 and 100 ng/spot respectively. The proposed method can be successfully used to determine the drug content of marketed formulation.

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Pharmacogenetics has revolutionized the way in which drug metabolism was looked upon in the pre-genomic era. Today with the advent of genomics it is possible to genotype an individual. The genetic differences, which determine the disposition of a given drug in an individual, ultimately give differences in drug response. Genotyping and phenotyping tests to predict dose requirement are now increasingly introduced during preclinical and clinical studies of new drugs. However, the hypothesis for the genotype and the phenotype correlation has to be established. Once this correlation will be established and technology to genotype advances enough to give predictive values over 90%, pharmacogenetics will enter the clinics. Pharmacogenetics will help to tailor the drug type and its dosage according to the individual's genotype. It will help to minimize adverse drug reactions as well as cases of non-responders to the drug therapy. In addition, this will provide better understanding of pharmacogenetic variations both within as well as among major populations/groups of the world.

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The aim of the study is to evaluate free radical scavenging activity of water extract of Spirulina platensis on cyclophosphamide-induced lipid peroxidation using some common laboratory markers. In this study goat liver has been used as liver source. This in vitro evaluation was done by measuring the malondialdehyde, 4-hydroxy-2-nonenal, reduced glutathione and nitric oxide content of tissue homogenates. The results suggest that cyclophosphamide could induce lipid peroxidation to a significant extent and it was also found that water extract of the algae has the ability to suppress the drug-induced lipid peroxidation.

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The distribution coefficient (log D) values of rifampicin, an essential first-line antitubercular drug, at gastrointestinal pH conditions are not reported in literature. Hence determinations were made using n-octanol and buffers ranging between pH 1-7. Also, log D values were predicted using Prolog D. Both the determinations showed opposite behaviour. The atypical experimental log D profile of rifampicin could be attributed to its surface-active properties, which also explained the reported permeability behaviour of the drug in various gastrointestinal tract segments.

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Pharmacogenomics is an emerging arena which aims to improve the therapeutic efficacy of a drug based on the genetic profile of a patient. This technology tries to detect the link between the genetic blueprint of a person and the heterogenous response to a drug so as to use this information to maximize the efficacy of the drug. This article explores the genesis of this field along with its benefits and the various techniques used for the same.

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Untreated HIV infection is characterized by a gradual deterioration of immune function. Most notably, crucial immune cells known as CD4 positive T lymphocytes are disabled and killed during the typical course of infection. These T lymphocyte cells play central role in the immune response. The study of HIV structure, genome and its life cycle has revealed many exciting target sites for acquired immunodeficiency syndrome treatment. Many conventional treatments for acquired immunodeficiency syndrome are merely capable of prolonging the patient's life but are unable to completely eradicate the virus as the virus mutates rapidly and develops resistance. So there are many recent novel approaches under consideration like integrase inhibitor, fusion inhibitors and ribozymes for the treatment of acquired immunodeficiency syndrome.

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Waxes have been used in many cosmetic preparations and pharmaceuticals as formulation aids. Rice bran wax is a byproduct of rice bran oil industry. Present study aims to investigate possible use of rice bran wax as occlusive moisturizer. The rice bran wax obtained was purified and its physicochemical characteristics were determined. In vitro studies were carried out to determine trans epidermal water loss through stratum corneum and water holding capacity of stratum corneum of human cadaver skin treated with pure rice bran wax and formulation of rice bran wax. The results show that rice bran wax can be used as a promising occlusive moisturizer.

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Various hydrophilic polymers from synthetic origin such as methylcellulose, PEGs, HPMC as well as those from natural world such as guar gum, tragacanth, xanthan gum have been used to formulate oral sustained release formulations. Psyllium husk has the ability to swell 10-14 times of its original volume and form a hydrogel. It is biocompatible, inexpensive, inert, non-absorbable, environment friendly and easily available. However, its use as a release retardant has not been fully explored. Owing to large dose, high sensitivity to light, moisture and heat and also very short half-life of 1-2 h; formulation of sustained release dosage form of amoxicillin trihydrate is a challenge. Hence the present study has been undertaken to develop sustained release granules as well as matrix tablets of amoxicillin trihydrate using psyllium husk as a primary release retardant. The drug release of these formulations was compared with those containing HPMC K4M.The results showed insignificant difference in t_80% value for drug release as assessed by student's t-test at 5% level of significance. Selected formulations were kept at controlled conditions of 40o/75% RH and 30o/65% RH for a period of 3 mo. Microbiological assay was used as a stability indicating method of assay. Sustained release granules and tablet formulations containing HPMC alone were found to be more stable than the similar formulations containing husk with percent drug content at the end of 3 mo at 40o/ 75% RH being 92.66%, 93.81%, 86.74%, 88.31% and the rate of degradation being 8.46×10^-4 d^-1, 7.1×10^-4 d^-1, 1.58×10^-3 d^-1 and 1.38×10^-3 d^-1, respectively. Thus it was concluded that psyllium husk can be effectively used as a hydrogel polymer in sustained release formulations. However, there is a need to keep moisture level under control during and after formulation.

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Since solubility is the main constraint for oral bioavailability of silymarin, an attempt has been made to design tablet formulations of silymarin-HP-β -CD solid dispersion in order to improve oral bioavailability. Tablet formulations were prepared by direct compression technique using superdisintegrants such as crosscarmellose sodium, sodium starch glycolate and polyplasdone XL in different concentrations. Developed formulations were evaluated for various pharmaceutical characteristics viz. hardness, % friability, weight variation, drug content, disintegration time and in vitro dissolution profiles. Amongst different batches, formulations containing crosscarmellose sodium showed superior disintegration and dissolution profiles compared to other formulations. However all the formulations showed improved dissolution over marketed formulation reflecting vital role of HP-β -CD dispersion in promotion of silymarin oral bioavailability. Moreover, optimized formulation showed stability at varying temperature and relative humidity.

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A high performance thin layer chromatographic method for the determination of gatifloxacin in human plasma using paracetamol as internal standard is proposed. Gatifloxacin in plasma was extracted with dichloromethane at pH 4.5 (phosphate buffer). The dichloromethane layer was evaporated and residue was reconstituted with ethanol and quantified using the mobile phase consisting of chloroform:methanol:ethanol:ammonia (4:2:2:2% v/v/v/v). The limit of quantitation was 50 ng/spot. The % RSD of the intra-day and inter-day was less than 15. The method was found to be simple, sensitive, rapid and could be used in the pharmacokinetic study involving human volunteers.

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The present investigation describes the influence of content of polyethylene oxide and ratio of lactose to starch 1500 on dipyridamole release from self correcting floating matrix tablets using 3² full factorial design. Tablets were evaluated for in vitro floating ability and drug release study using USP 24 type II apparatus using 0.1 N HCI at 100 rpm and temperature of 37±0.5⁰. Multiple regression analysis and two way analysis of variance followed by Tukey test were performed for dependent variables. All formulations floated within 2 min regardless of factors studied and had total floating time of more than 12 h. It was observed that both the factors had significant influence on all dependent variable studied ( P< 0.05) except the ratio of lactose to starch 1500 did not significantly contribute for Q₁ ( P > 0.05). As content of polymer increased the release rate declined with increase in value of diffusion exponent giving anomalous drug release to zero order drug release ( P < 0.05). It was observed that above a certain threshold level of polymer content further increase did not contribute significantly for percentage drug release. Lactose gave higher drug release with release mechanism towards zero order compared to starch 1500 which gave slower release with release mechanism towards diffusion based. Although both the factors significantly contribute for percentage drug release at different time point, the content of polymer dominated. It was observed that polymer content was a dominant controlling factor for drug release kinetics and it could be controlled by employing various blends of fillers.

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An extractive spectrophotometric method was developed for the estimation of tegaserod maleate. This method is based on the formation of a yellow colored ion-pair complex with bromo cresol green in phthalate buffer (pH 2.5). The complex was extracted into chloroform and absorbance measured at 415 nm. The calibration curve was found to be linear in the range of 1 to 30 μg/ml. The molar absorptivity and Sandell sensitivity values were found to be 2.9775 × 10⁴l mol^-1cm^-1 and 0.2264 ×10^-2 μg/cm²/0.001, respectively. The limit of detection and limit of quantification were found to be 0.0524 μg/ml and 0.1749 μg/ml, respectively. The method was successfully applied for assay in tablet formulation and the recovery was found to be in good agreement with label claim. The method was found to be precise, accurate and sensitive.

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Three novel fluoroquinolones with general structure 1-t-butyl-7-[4-substituted (piperazin-1-yl/piperidin-1-yl)]-6-fluoro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acids were synthesized and evaluated for antitubercular activity in vitro against M. tuberculosis H37Rv in Middlebrook 7H9 broth using sparfloxacin, ciprofloxacin and isoniazid as standards. Test compounds were found to be less potent than sparfloxacin; however, one of the compounds was more potent than ciprofloxacin.

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The aims of this study were to determine the total cost of drug treatment in patients of rheumatoid arthritis, to estimate the costs of management of gastrointestinal side effects of non-steroidal antiinflammatory drugs and to estimate the cost of monitoring the side-effects of disease modifying antirheumatic drugs. The original prescription of the patients was used to calculate the direct cost of treatment. For calculating the indirect cost, the patients were interviewed. The cost of monitoring the side-effects was also calculated from the patient records. The study was carried in out patient department of a government teaching hospital. A total of 96 patients were recruited in this study between August-November 2003. The average total cost of drug treatment was found to be Rs.999±76 per month. The average monthly direct cost of rheumatoid arthritis was estimated to be Rs. 623±31. The average indirect cost was found to be Rs.368±62 per month. The average iatrogenic cost factor value was found to be 1.78. The average monthly cost of monitoring side-effects in patients prescribed with disease modifying antirheumatic drugs was Rs. 57 per patient. The study provides preliminary results for costs of drug treatment and monitoring in patients suffering from rheumatoid arthritis.

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The cyclooxygenase-2 enzyme inhibition activity of 5-aryl-2,2-dialkyl-4-phenyl-3(2 H )furanone derivatives is quantitatively analyzed through Fujita-Ban and Hansch type of approaches. The analyses have helped to ascertain the role of different substituents in explaining the observed inhibitory activity of these congeners. From both approaches it is revealed that more hydrophobic susbtituents at 4- R1, a non-hydrogen bond acceptor substitutent, preferably a -F substituent, at 3- R1 in 4-phenyl ring of 3(2 H )furanone scaffold improve inhibitory action of a compound. The substituents exhibiting collective molecular bulk smaller than spirocyclopentyl at X and Y positions are preferred as these geminal positions seems to be involved in steric interation. Similarly, 4-aminosulfonyl in 5-aryl ring of 3(2 H )furanone moiety emerged as a better choice than 4-methylsulfonyl substitution.

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The plasma concentration time profiles for nicotine were characterized after a single application of nicotine transdermal system to the upper fore arm of healthy smokers. A 12 cm² system was applied for 24 h. Blood samples were withdrawn at predetermined time intervals. Plasma nicotine concentrations rose rapidly and achieved a mean C_maxvalue of 14.5 ng/ml .The half life was estimated as 4.78 h and AUC_(0-24)181.0 ng.h/ ml. The nicotine transdermal system was well tolerated. The results indicate that the system has potential usefulness in smoking cessation. The pharmacokinetic profiles of marketed patch system was compared with the developed system. Significant difference was observed in the pharmacokinetic parameters.

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Certain 4'-(4''-substituted phenyl)-4-methylfurobenzopyrones were synthesized and evaluated for antibacterial activity. Six of the synthesized compounds were also screened for their antiinflammatory activity. Substituted resorcinols were condensed with ethyl acetoacetate to afford different coumarins (2a-c). Various substituted phenacyl bromides (4a-g) were prepared by the bromination of para-substituted acetophenones. The coumarins (2a-c) and phenacyl bromides (4a-g) were condensed to give oxoethers (5a-s). These were cyclised by using 1 M sodium hydroxide to afford the desired furobenzopyrone derivatives (FCa-s). All the compounds have been evaluated for their antibacterial activity against different strains of gram positive and gram negative bacteria. All the compounds have shown good activity against Pseudomonas aeruginosa . Compounds, 3-(4-chlorophenyl)-5-methylfuro-[3,2-g][1]benzopyran-7-one, 3-(4-chlorophenyl)-5,9-dimethylfuro[3,2-g][1]benzopyran-7-one and 4,5-dimethyl-3-phenylfuro[3,2-g][1]benzopyran-7-one (FCe, FCi, FCn) were active against E. coli . A few compounds showed moderate activity against Bacillus subtilis also. Antiinflammatory activity of six selected compounds was also tested using the carrageenan-induced rat paw oedema method. Among them, 5-methyl-3-p-tolylfuro[3,2-g][1]benzopyran-7-one (FCg) showed excellent activity. 5-Methyl-3-phenylfuro[3,2-g][1]benzopyran-7-one (FCa) and 4,5-dimethyl-3-(4-nitrophenyl)-furo[3,2-g][1]benzopyran-7-one (FCc) showed activity comparable to that of the standard drug ibuprofen.

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