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| REVIEW ARTICLES |
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A decision tree for rapid quality assurance and control of rifampicin-containing oral dosage forms for global distribution for tuberculosis treatment |
p. 1 |
Y Ashokraj, Shrutidevi Agrawal, R Panchagnula DOI:10.4103/0250-474X.40323 PMID:20390072For centuries tuberculosis remained as a complex socioeconomic problem impeding human development. Directly observed treatment short-course and fixed dose combinations were implemented in tuberculosis therapy for maximum success of treatment. However, drug shortages primarily hindered the expansion of directly observed treatment short-course, which lead to development of the global tuberculosis drug facility. Since large geographical area is covered by the global tuberculosis drug facility for global drug supply for tuberculosis eradication programs, a rapid quality control and assurance has become necessary to ensure the quality and performance of supplied antituberculosis drugs. In this manuscript a decision tree is proposed for facilitating rapid quality control ( in vitro and in vivo ) of antituberculosis formulations procured by the global tuberculosis drug facility. This decision tree also predicted to be applicable at every stages of anti tuberculosis drug product development, especially in identification of poor quality products and monitoring batch-to-batch variability. Further, it provides opportunity for effective quality control in resource poor settings and the gained knowledge is anticipated to be applicable for development and evaluation of antimalarial and antiAIDS fixed dose combinations. |
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Transdermal delivery by iontophoresis |
p. 5 |
Swati Rawat, Sudha Vengurlekar, B Rakesh, S Jain, G Srikarti DOI:10.4103/0250-474X.40324 PMID:20390073Recently there has been an increased interest in using iontophoretic technique for the transdermal delivery of medications, both ionic and nonionic. This article is an overview of the history of iontophoresis and factors affecting iontophoretic drug transfer for the systemic effects and laws for development of Transdermal delivery system are discussed. |
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| RESEARCH PAPERS |
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In vivo evaluation of single dose tetanus toxoid vaccine formulation with chitosan microspheres |
p. 11 |
R Manivannan, SA Dhanaraj, Y Udaya Bhaskara Rao, A Balasubramaniam, NL Gowrishankar, N Jawahar, S Jubie DOI:10.4103/0250-474X.40325 PMID:20390074Chitosan adsorbed microspheres containing tetanus toxoid were prepared in the size range of 10 µm to 75 µm, by emulsion-cross linking technique at different speeds of agitation. The amount of tetanus toxoid incorporated into chitosan microspheres were estimated by limes flocculation test and in vivo evaluation of tetanus toxoid adsorbed chitosan microspheres were determined by toxin neutralization method using albino mice. The results of in vivo release for the batches of 10 µm and 25 µm correlates with the results of in vitro in which both the batches passes the limit of IP standard (4 Lf) where as, for the batches of 50 µm and 75 µm, the in vitro release of tetanus toxoid was 2 Lf. But our in vivo studies for the batches of 50 µm and 75 µm fail to pass the limit stated in IP. The release of tetanus toxoid from the chitosan microspheres was found to be sustained for the period of 6 months. |
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Ionic cross-linked chitosan beads for extended release of ciprofloxacin: In vitro characterization |
p. 16 |
A Srinatha, JK Pandit, S Singh DOI:10.4103/0250-474X.40326 PMID:20390075Chitosan beads loaded with ciprofloxacin hydrochloride were fabricated by ionic cross-linking with sodium tripolyphosphate. The beads showed an excellent water retention property. The degradation of fabricated beads was influenced by the pH of test medium. High drug load was achieved within the bead with a short curing time. Drug release was high in acidic medium (pH 1.2) vis-à-vis intestinal medium (pH 7.4). Ciprofloxacin hydrochloride release increased with an increasing concentration of ciprofloxacin and decreasing proportion of chitosan. Drug release followed both first-order and Higuchi's root time kinetics showing non-Fickian release mechanism. |
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Design and optimization of diclofenac sodium controlled release solid dispersions by response surface methodology |
p. 22 |
HN Shivakumar, BG Desai, G Deshmukh DOI:10.4103/0250-474X.40327 PMID:20390076A 3 2 factorial design was employed to produce controlled release solid dispersions of diclofenac sodium in Eudragit RS and RL by coevaporation of their ethanol solution in a flash evaporator. The effect of critical formulation variables namely total polymer pay loads and levels of Eudragit RL on percent drug incorporation (% DI), drug release at the end of 12 hours (Rel 12 ) and drug release at the end of 3 hours (Rel 3 ) were analyzed using response surface methodology. The parameters were evaluated using the F test and mathematical models containing only the significant terms were generated for each parameter using multiple linear regression analysis and analysis of variance. Both the formulation variables studied exerted a significant influence ( p < 0.05) on the drug release whereas the total polymer levels emerged as a lone factor significantly influencing the percent drug incorporation. Numerical optimization technique employing desirability approach was used to develop a new formulation by setting constraints on the dependent and independent variables. The experimental values of % DI, Rel 12 and Rel 3 for the optimized batch were found to be 95.22 ± 1.13%, 74.52 ± 3.16% and 29.37 ± 1.26% respectively which were in close agreement with those predicted by the mathematical models. The Fourier transform infrared spectroscopy, Differential scanning calorimetry and Powder x-ray diffractometry confirmed that the drug was reduced to molecular or microcrystalline form in the hydrophobic polymeric matrices, which could be responsible for the controlled drug release from the solid dispersions. The drug release from the solid dispersions followed first order rate kinetics and was characterized by Higuchian diffusion model. |
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Evaluation of free radical scavenging activity of an ayurvedic formulation, Panchvalkala |
p. 31 |
Sheetal Anandjiwala, MS Bagul, M Parabia, M Rajani DOI:10.4103/0250-474X.40328 PMID:20390077We report the free radical scavenging activity of an Ayurvedic preparation Panchvalkala and its individual components (stem bark of Ficus benghalensis , F. glomerata , F. religiosa , F. virens and Thespesia populnea ). Being stem barks, these samples contain phenolics (ranging from 3.5% to 10.8% w/w) and tannins (1.6% to 7.0% w/w). This prompted us to study the free radical scavenging activity of Panchvalkala and its components which was evaluated in three in vitro models viz . 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity, superoxide radical scavenging activity and reducing power assay. Panchvalkala and its individual components showed significant antiradical activity by bleaching 1,1-diphenyl-2-picrylhydrazyl radical (EC 50 ranging from 7.27 to 12.08 µg) which was comparable to pyrogallol (EC 50 4.85 µg). Thin layer chromatography of the methanol extracts when sprayed with 0.2% 1,1-diphenyl-2-picrylhydrazyl in methanol revealed several bands with antiradical activity as seen by bleaching of 1,1-diphenyl-2-picrylhydrazyl. All the samples showed good superoxide scavenging potential (EC 50 ranging from 41.55 to 73.56 µg) comparable to ascorbic acid (EC 50 45.39 µg) in a dose-dependent manner. The reduction ability, Fe 3+ to Fe 2+ transformation was found to increase with increasing concentrations of all the sample extracts. |
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Validation of different methods of preparation of Adhatoda vasica leaf juice by quantification of total alkaloids and vasicine |
p. 36 |
S Soni, Sheetal Anandjiwala, G Patel, M Rajani DOI:10.4103/0250-474X.40329 PMID:20390078Leaf of Adhatoda vasica ( Vasaka ) is an important drug of Ayurveda, prescribed as an expectorant. Quinazoline alkaloids present in the leaves are established as active principles. In Ayurveda, its leaf juice ( Vasa swarasa ) is incorporated in many formulations. Classical method for extracting the juice ( swarasa ) from the leaf is an elaborate process, which involves subjecting a bolus of crushed fresh leaf to heat followed by squeezing out the juice. Commercially, to prepare the juice of Vasaka , manufacturers have been adopting different methods other than the traditional method. In an effort to evaluate these modified processes phytochemically to identify the process which gives juice of the quality that is obtained by traditional method, in terms of its alkaloid content, we prepared the leaf juice by traditional Ayurvedic method, its modification by steaming of leaf to simulate the traditional method and other methods adopted by some manufacturers. These juice samples were evaluated for the total alkaloid content by spectrophotometric method and vasicine content by thin layer chromatography densitometric method using high performance thin layer chromatography. The high performance thin layer chromatography method was validated for precision, repeatability and accuracy. The total alkaloid content varied from 0.3 mg/ml to 5.93 mg/ml and that of vasicine content varied from 0.2 mg/ml to 5.64 mg/ml in the juice samples prepared by different methods. The present study revealed that steaming of fresh leaves under 15 lb pressure yielded same quantity of juice as the traditional bolus method (25 ml/100 g leaf) and its total alkaloid content and vasicine content (4.05±0.12 and 3.46±0.06 mg/ml, respectively) were very high when compared to the other methods, though the traditional method was found to give the best quality juice with highest amount of total alkaloids (5.93±0.55 mg/ml) and vasicine (5.64±0.10 mg/ml) content . |
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Formulation and characterization of mucoadhesive buccal films of glipizide |
p. 43 |
Mona Semalty, A Semalty, G Kumar DOI:10.4103/0250-474X.40330 PMID:20390079Mucoadhesive buccal films of glipizide were prepared by solvent casting technique using hydroxypropylmethylcellulose, sodium carboxymethylcellulose, carbopol-934P and Eudragit RL-100. Prepared films were evaluated for weight, thickness, surface pH, swelling index, in vitro residence time, folding endurance, in vitro release, permeation studies and drug content uniformity. The films exhibited controlled release over more than 6 h. From the study it was concluded that the films containing 5 mg glipizide in 4.9% w/v hydroxypropylmethylcellulose and 1.5% w/v sodium carboxymethylcellulose exhibited satisfactory swelling, an optimum residence time and promising drug release. The formulation was found to be suitable candidate for the development of buccal films for therapeutic use. |
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Synthesis, antimicrobial and antiinflammatory activity of 2,5-disubstituted-1,3,4-oxadiazoles |
p. 49 |
G Nagalakshmi DOI:10.4103/0250-474X.40331 PMID:20390080In the present study, 2,5-disubstituted-1,3,4-oxadiazoles (3a-o) have been synthesized by the condensation of 4-methoxybenzohydrazide (1) with different aromatic acids (2a-o) in presence of phosphoryl chloride. The structural assignment of this compound (3a-o) has been made on the basis of elemental analysis, UV, IR, 1 H NMR and mass spectral data. The synthesized compounds were screened for their in vitro growth inhibiting activity against different strains of bacteria and fungi viz., Staphylococcus aureus , Bacillus subtilis , Bacillus megaterium , Escherichia coli , Pseudomonas aeruginosa , Shigella dysenteriae , Candida albicans , Aspergillus niger and Aspergillus flavus were compared with the standard antibiotics such as chloramphenicol (50 µg/ml) and griseofulvin (50 µg/ml) using well agar diffusion technique. Compounds 3e, 3g, 3h and 3m exhibits highest antibacterial activity and compounds 3d, 3g and 3h showed better antifungal activity. The synthesized compounds (3a-o) were screened for their in vitro antiinflammatory activity against carrageenan-induced rat paw oedema. Compounds 3f and 3i were found to be most active compound of this series, which shows 46.42% and 50% inflammation inhibitory activity, whereas standard drug phenylbutazone exhibit 53.57% antiinflammatory activity at a dose of 50 mg/kg po. |
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Ascorbic acid inhibits development of tolerance and dependence to opiates in mice: Possible glutamatergic or dopaminergic modulation |
p. 56 |
SK Kulkarni, C Deshpande, A Dhir DOI:10.4103/0250-474X.40332 PMID:20390081In a recent study, it has been demonstrated that ascorbic acid possessed antidopaminergic activity and modulate the glutamatergic neurotransmission in mice. With this background, the present study was undertaken to study the effect of ascorbic acid on the development of tolerance and dependence to opiate and its mechanism of action. Male Swiss mice weighing 20-25 g were used in the present study. Mice were made physically dependent on opioid by the chronic administration of morphine (10 mg/kg, twice a day, for 9 days) intraperitoneally. Ascorbic acid, haloperidol (dopamine antagonist) or MK 801 (NMDA receptor antagonist) was administered daily for 9 d before challenging the animals with morphine. The development of tolerance was assessed by noting the tail-flick latency on day 1, 3, 9 and 10. On the 10 th day after the measurement of tail-flick latency, animals were challenged with naloxone (2 mg/kg., i.p.) and incidence of escape jumps were recorded by placing the animals in 45 cm high plexiglass container. Ascorbic acid (400-1600 mg/kg) dose dependently inhibited development of tolerance and dependence to morphine as noted from tail-flick latency. When given along with MK 801 (0.01 mg/kg., i.p) or haloperidol (0.1 mg/kg i.p.), ascorbic acid (800 mg/kg., i.p.) potentiated the response of MK 801 or haloperidol. In conclusion, it is hypothesized that inhibition of development of tolerance and dependence to morphine by ascorbic acid appears to have two components, namely dopaminergic and glutamatergic. |
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Design and in vitro characterization of buccoadhesive drug delivery system of insulin |
p. 61 |
J Sahni, S Raj, FJ Ahmad, RK Khar DOI:10.4103/0250-474X.40333 PMID:20390082A buccoadhesive drug delivery system of Insulin was prepared by solvent casting technique and characterized in vitro by surface pH, bioadhesive strength, drug release and skin permeation studies. Sodium carboxymethylcellulose-DVP was chosen as the controlled release matrix polymer. The optimized formulation J 4 contained Sodium carboxy methyl cellulose-DVP 2% (w/v), insulin (50 IU/film), propylene glycol (0.25 ml) and Isopropyl alcohol: water (1:4) as solvent system. Bioadhesive strength of the prepared patches was measured on a modified physical balance using bovine cheek pouch as the model membrane. In vitro release studies were carried out at 37 ± 2° using phosphate buffer pH 6.6, in a modified dissolution apparatus fabricated for the purpose. Cumulative amount of drug released from the optimized formulation J 4 was 91.64% in 6 hours. In vitro permeation studies were carried out on J 4 at 37 ± 2° using Franz diffusion cell. Cumulative amount of drug permeated from J 4 was 6.63% in 6 hours. In order to enhance the permeation of protein drug, different permeation enhancers were evaluated. The results suggested that sodium deoxycholate 5% (w/v) was the best permeation enhancer among those evaluated. It enhanced the permeation of insulin from 6.63% to 10.38% over a period of 6 hours. The optimized patches were also satisfactory in terms of surface pH and bioadhesive strength. It can also be easily concluded that the system is a success as compared to the conventional formulations with respect to invasiveness, requirement of trained persons for administration and most importantly, the first pass metabolism. |
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Development and evaluation of a chloramphenicol hypertonic ophthalmic solution |
p. 66 |
AV Jithan, C Krishna Mohan, M Vimaladevi DOI:10.4103/0250-474X.40334 PMID:20390083Hypertonic ophthalmic solutions are used to treat ocular diseases associated with edema. In this study, we developed a chloramphenicol hypertonic ophthalmic solution. These drops were developed based on the cosolvency and additional dielectric constant concepts. Two different solvents: PEG 300 and glycerol were used as cosolvents. Solubility curves were plotted. Based on the solubility curves, two different solutions were selected. These solutions were evaluated for physical parameters and accelerated stability. The results indicated that chloramphenicol was stable in these formulations. The selected blend of solutions was hypertonic. Thus, the solubility and stability of chloramphenicol was enhanced using a cosolvency technique so as to develop a chloramphenicol hypertonic ophthalmic solution. |
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Optimization of fast dissolving etoricoxib tablets prepared by sublimation technique |
p. 71 |
DM Patel, MM Patel DOI:10.4103/0250-474X.40335 PMID:20390084The purpose of this investigation was to develop fast dissolving tablets of etoricoxib. Granules containing etoricoxib, menthol, crospovidone, aspartame and mannitol were prepared by wet granulation technique. Menthol was sublimed from the granules by exposing the granules to vacuum. The porous granules were then compressed in to tablets. Alternatively, tablets were first prepared and later exposed to vacuum. The tablets were evaluated for percentage friability and disintegration time. A 3 2 full factorial design was applied to investigate the combined effect of 2 formulation variables: amount of menthol and crospovidone. The results of multiple regression analysis indicated that for obtaining fast dissolving tablets; optimum amount of menthol and higher percentage of crospovidone should be used. A surface response plots are also presented to graphically represent the effect of the independent variables on the percentage friability and disintegration time. The validity of a generated mathematical model was tested by preparing a checkpoint batch. Sublimation of menthol from tablets resulted in rapid disintegration as compared with the tablets prepared from granules that were exposed to vacuum. The optimized tablet formulation was compared with conventional marketed tablets for percentage drug dissolved in 30 min (Q 30 ) and dissolution efficiency after 30 min (DE 30 ). From the results, it was concluded that fast dissolving tablets with improved etoricoxib dissolution could be prepared by sublimation of tablets containing suitable subliming agent. |
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Furosemide-loaded alginate microspheres prepared by ionic cross-linking technique: Morphology and release characteristics |
p. 77 |
MK Das, PC Senapati DOI:10.4103/0250-474X.40336 PMID:20390085Furosemide-loaded alginate microspheres were prepared by the ionic cross-linking technique using CaCl 2 , Al 2 (SO 4 ) 3 and BaCl 2 . The process induced the formation of microspheres with the incorporation efficiency of 65% to 93%. The effect of sodium alginate concentration, cross-linking agents and drying conditions was evaluated with respect to entrapment efficiency, particle size, surface characteristics and in vitro release behaviors. Infrared spectroscopic study confirmed the absence of any drug-polymer interaction. Differential scanning calorimetric analysis revealed that the drug was molecularly dispersed in the alginate microspheres matrices showing rough surface, which was confirmed by scanning electron microscopy study. The mean particle size and entrapment efficiency were found to be varied by changing various formulation parameters. The in vitro release profile could be altered significantly by changing various formulation parameters to give a sustained release of drug from the microspheres. The kinetic modeling of the release data indicate that furosemide release from the alginate microspheres follow anomalous transport mechanism after an initial lag period when the drug release mechanism was found to be fickian diffusion controlled. |
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| SHORT COMMUNICATIONS |
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Isolation of liver aldehyde oxidase containing fractions from different animals and determination of kinetic parameters for benzaldehyde |
p. 85 |
RS Kadam, KR Iyer DOI:10.4103/0250-474X.40337 PMID:20390086Aldehyde oxidase activity containing fractions from rabbit, guinea pig, rat and mouse livers were obtained by heat treatment and ammonium sulfate precipitation. Aldehyde oxidase activity was observed in rabbit and guinea pig livers, while aldehyde oxidase activity was absent in rat and mouse liver fractions. Enzyme kinetic parameters, K m and V max , were determined for the oxidation of benzaldehyde to benzoic acid by rabbit and guinea pig liver fractions, by spectrophotometric method, with potassium ferricyanide as the electron acceptor. The K m values obtained for both animal liver fractions were in the range of 10.3-19.1 µM. |
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Microwave-induced synthesis of schiff bases of aminothiazolyl bromocoumarins as antibacterials |
p. 88 |
KN Venugopala, BS Jayashree DOI:10.4103/0250-474X.40338 PMID:20390087A fast and highly efficient method for the synthesis of some of the schiff bases of aminothiazolylbromocoumarin (4a-m) has been performed by microwave irradiation of 2'-amino-4'-(6-bromo-3-coumarinyl) thiazole (3) and substituted aromatic aldehydes (a-m). Microwave assisted reactions have resulted in better yields of the desired products than when prepared under conventional conditions. The resulting products were evaluated for their qualitative and quantitative antibacterial activity. |
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In vitro antiviral activity of some novel isatin derivatives against HCV and SARS-CoV viruses |
p. 91 |
P Selvam, N Murgesh, M Chandramohan, E De Clercq, E Keyaerts, L Vijgen, P Maes, J Neyts, MV Ranst DOI:10.4103/0250-474X.40339 PMID:203900884-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)amino]-N(4,6-dimethyl-2-pyrimidiny)benzene sulphonamide and its derivatives were evaluated for antiviral activity against Pathogenic viruses such as Hepatitis C Virus and SARS-CoV in Vero and Huh 5-2 cells, respectively. The 5-fluoro derivative inhibited the HCV RNA synthesis at 6 µg/ml, without toxicity at a concentration up to 42 µg/ml in Huh 5-2 cells. Among the compounds tested SPIII-5F exhibits the 45% maximum protection against replication of SARS-CoV in Vero cells. |
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Physicochemical and pharmacokinetic parameters in drug selection and loading for transdermal drug delivery |
p. 94 |
NS Chandrashekar, RH Shobha Rani DOI:10.4103/0250-474X.40340 PMID:20390089Skin of an average adult body covers a surface of approximately 2 m2 and receives about one-third of the blood circulating through the body. The transdermal route of administration cannot be employed for a large number of drugs. The rationality of drug selection based on pharmacokinetic parameters and physicochemical properties of the drug are the important factors to be considered for deciding its suitability of drug for delivery by transdermal route. |
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HPLC estimation of berberine in Tinospora cordifolia and Tinospora sinensis |
p. 96 |
GV Srinivasan, KP Unnikrishnan, AB Rema Shree, Indira Balachandran DOI:10.4103/0250-474X.40341 PMID:20390090A high-performance liquid chromatographic method for the estimation of berberine in the stem of Tinospora cordifolia (Willd.) Miers. ex Hook.f. and Thoms. and Tinospora sinensis (Lour.) Merrill is described. The dried stems of T. cordifolia and T. sinensis were defatted with petroleum ether (60-80°). The marc was dried and further extracted with methanol. The concentration of berberine in methanol extract was determined using a C-18 reverse phase column with a mobile phase of acetonitrile:water (10:90 v/v) at a flow rate of 0.6 ml/min and with UV detection at 266 nm. TLC and HPLC comparison of both the species revealed significant variation in the chemical constitution of the two species. This observation becomes important in the context of the use of T. sinensis in place of the genuine drug T. cordifolia . |
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Parenteral formulation of zopiclone |
p. 99 |
PV Swamy, P Sushma, G Chirag, K Prasad, M Younus Ali, SA Raju DOI:10.4103/0250-474X.40342 PMID:20390091The present study was undertaken with an intention to develop a stable and effective parenteral formulation, containing the drug zopiclone. Since zopiclone is a water insoluble drug, various methods such as co-solvency, pH control and hydrotrophy have been tried in order to enhance its solubility. When all these methods could not give adequate solubility enhancement of the drug, a hydrochloride salt was prepared, and it was found to be thermostable. Various batches of zopiclone hydrochloride injection formulation were prepared in order to assess the influence of light, atmospheric oxygen and antioxidant on the stability of the drug and the formulations were also subjected to accelerated stability testing in order to predict approximate shelf-life of the product. |
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Simultaneous spectrophotometric determination of lansoprazole and domperidone in capsule dosage form |
p. 102 |
AP Sherje, AV Kasture, KN Gujar, PG Yeole DOI:10.4103/0250-474X.40343 PMID:20390092Two simple, accurate and precise spectrophotometric methods have been developed for simultaneous determination of lansoprazole and domperidone in pharmaceutical dosage form. Method A involves formation of Q-absorbance equation at 256.0 nm (isoabsorptive point) and at 294.2 nm while method B is two wavelength method where 277.6 nm, 302.1 nm were selected as 'λ1 and 'λ2 for determination of lansoprazole and 231.3 nm, 292.0 nm were selected as 'λ1 and 'λ2 for determination of domperidone. Both the methods were validated statistically and recovery studies were carried out. The Beer's law limits for each drug individually and in mixture was within the concentration range of 5-50 µg/ml. Linearity of lansoprazole and domperidone were in the range of 24-36 µg/ml and 8-12 µg/ml, respectively. The proposed methods have been applied successfully to the analysis of the cited drugs either in pure form or in pharmaceutical formulations with good accuracy and precision. The method herein described can be employed for quality control and routine analysis of drugs in pharmaceutical formulations. |
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Novel 2-pyrazoline derivatives as potential antibacterial and antifungal agents |
p. 105 |
Suvarna Kini, AM Gandhi DOI:10.4103/0250-474X.40344 PMID:20390093The 1,3,5-trisubstituted-2-pyrazolines were synthesized by refluxing isoniazid with various substituted diarylchalcones in N,N-dimethylformamide at 120-140°. The physical and spectral data such as M.P., R f , elemental analysis, IR, NMR and Mass was obtained for the synthesized compounds and the structures were confirmed. The screening of the synthesized compounds for antimicrobial activity was performed against Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coli and Aspergillus niger . |
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Spectrophotometric estimation of ethamsylate and mefenamic acid from a binary mixture by dual wavelength and simultaneous equation methods |
p. 108 |
Anju Goyal, I Singhvi DOI:10.4103/0250-474X.40345 PMID:20390094Two simple, accurate, economical and reproducible spectrophotometric methods for simultaneous estimation of two-component drug mixture of ethamsylate and mefenamic acid in combined tablet dosage form have been developed. The first developed method involves formation and solving of simultaneous equation using 287.6 nm and 313.2 nm as two wavelengths. Second developed method is based on two wavelength calculation. Two wavelengths selected for estimation of ethamsylate were 274.4 nm and 301.2 nm while that for mefenamic acid were 304.8 nm and 320.4 nm. Both the developed methods obey Beer's law in the concentration ranges employed for the respective methods. The results of analysis were validated statistically and by recovery studies. |
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Novel colon targeted drug delivery system using natural polymers |
p. 111 |
V Ravi, TM Pramod Kumar, Siddaramaiah DOI:10.4103/0250-474X.40346 PMID:20390095A novel colon targeted tablet formulation was developed using pectin as carrier and diltiazem HCl and indomethacin as model drugs. The tablets were coated with inulin followed by shellac and were evaluated for average weight, hardness and coat thickness. In vitro release studies for prepared tablets were carried out for 2 h in pH 1.2 HCl buffer, 3 h in pH 7.4 phosphate buffer and 6 h in simulated colonic fluid. The drug release from the coated systems was monitored using UV/Vis spectroscopy. In vitro studies revealed that the tablets coated with inulin and shellac have limited the drug release in stomach and small intestinal environment and released maximum amount of drug in the colonic environment. The study revealed that polysaccharides as carriers and inulin and shellac as a coating material can be used effectively for colon targeting of both water soluble and insoluble drugs. |
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Effect of some clinically used proteolytic enzymes on inflammation in rats |
p. 114 |
A.H.M Viswanatha Swamy, PA Patil DOI:10.4103/0250-474X.40347 PMID:20390096The study was designed to investigate the role of three proteolytic enzymes viz ., chymotrypsin, trypsin and serratiopeptidase on hind paw edema and cotton pellet induced granuloma and their possible interactions with aspirin in albino rats. Animals were treated with proteolytic enzymes alone in three different doses or aspirin or in combination with subantiinflammatory dose of aspirin or saline, 30 min before injection of 0.1ml 1% carrageenan. Paw volume was measured before and 3 h after the injection of carrageenan. Chymotrypsin, (5, 18 and 36 mg/kg), trypsin (1.44, 2.88 and 5.76 mg/kg) and serratiopeptidase (0.45, 0.9 and 2.70 mg/kg) were showed dose dependent antiinflammatory activity in acute model of inflammation. Serratiopeptidase showed better antiinflammatory activity on carrageenan induced inflammation than other two proteolytic enzymes and aspirin. However, chymotrypsin and serratiopeptidase were found to be more effective than aspirin in subacute model of inflammation. Chymotrypsin, trypsin and serratiopeptidase possess antiinflammatory activity and exhibit synergistic effect with aspirin in both acute and subacute models of inflammation in rats. |
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Synthesis and pharmacological evaluation of (6-substituted 4-Oxo-4 H -chromene-3 yl) methyl N-substituted aminoacetates |
p. 118 |
Asmita Gajbhiye, V Mallareddy, G Achaiah DOI:10.4103/0250-474X.40348 PMID:20390097A series of the title compounds were synthesized and characterized by spectral data. All the compounds were evaluated for in vitro antihistaminic activity by inhibition of isotonic contractions induced by histamine on isolated guinea pig ileum and the compound 6-k showed significant activity. A few compounds have also been screened for in vivo bronchodilatory activity. These compounds exhibited significant protection against histamine-induced convulsions in guinea pig at the dose of 50 µmol. |
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Development and In vitro evaluation of buccoadhesive tablets of metoprolol tartrate |
p. 121 |
PD Nakhat, AA Kondawar, LG Rathi, PG Yeole DOI:10.4103/0250-474X.40349 PMID:20390098Buccoadhesive tablet of metoprolol tartrate was developed to prolong its release and improve bioavailability by avoidance of hepatic first pass metabolism during the treatment of chronic hypertension. The formulations were tested for weight, hardness, friability, content uniformity, swelling index, bioadhesive force and drug release rate. Carbopol 934 P was used as bioadhesive polymer and methocel K4M was added as a matrix former. Backing layer of ethyl cellulose was given to the tablets. Optimised formulation containing carbopol 934 P and methocel K4M in the ratio of 1:1 showed surface pH values in the range of 6 to 7 and 91.50% cumulative release of drug in 10 h. Stability study revealed that the optimized formulation was stable for atleast 3 mo. |
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RP-HPLC estimation of venlafaxine hydrochloride in tablet dosage forms |
p. 124 |
SL Baldania, KK Bhatt, RS Mehta, DA Shah, Tejal R Gandhi DOI:10.4103/0250-474X.40350 PMID:20390099A simple, specific, accurate, and precise reverse phase high performance liquid chromatographic method was developed and validated for the estimation of venlafaxine hydrochloride in tablet dosage forms. A Phenomenex Gemini C-18, 5 µm column having 250 x 4.6 mm i.d. in isocratic mode, with mobile phase containing methanol: 0.05 M potassium dihydrogen orthophosphate (70:30, v/v; pH 6.2) was used. The flow rate was 1.0 ml/min and effluents were monitored at 226 nm. Carbamazepine was used as an internal standard. The retention time of venlafaxine hydrochloride and carbamazepine were 3.7 min and 5.3 min, respectively. The method was validated for specificity, linearity, accuracy, precision, limit of quantification, limit of detection, robustness and solution stability. Limit of detection and limit of quantification for estimation of venlafaxine hydrochloride were found to be 100 ng/ml and 300 ng/ml, respectively. Recoveries of venlafaxine hydrochloride in tablet formulations were found to be in the range of 99.02-101.68%. Proposed method was successfully applied for the quantitative determination of venlafaxine hydrochloride in tablet dosage forms. |
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Simultaneous estimation of esomeprazole and domperidone by UV spectrophotometric method |
p. 128 |
S Lakshmana Prabu, A Shirwaikar, Annie Shirwaikar, C Dinesh Kumar, A Joseph, R Kumar DOI:10.4103/0250-474X.40351 PMID:20390100A novel, simple, sensitive and rapid spectrophotometric method has been developed for simultaneous estimation of esomeprazole and domperidone. The method involved solving simultaneous equations based on measurement of absorbance at two wavelengths, 301 nm and 284 nm, 'λ max of esomeprazole and domperidone respectively. Beer's law was obeyed in the concentration range of 5-20 µg/ml and 8-30 µg/ml for esomeprazole and domperidone respectively. The method was found to be precise, accurate, and specific. The proposed method was successfully applied to estimation of esomeprazole and domperidone in combined solid dosage form. |
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In vitro anthelmintic activity of Baliospermum montanum muell. arg roots |
p. 131 |
RG Mali, RR Wadekar DOI:10.4103/0250-474X.40352 PMID:20390101Alcohol and aqueous extracts from the roots of Baliospermum montanum Muell. Arg were investigated for their anthelmintic activity against Pheretima posthuma and Ascardia galli . Various concentrations (10-100 mg/ml) of each extract were tested in the bioassay, which involved determination of time of paralysis and time of death of the worms. Both the extracts exhibited significant anthelmintic activity at highest concentration of 100 mg/ml. Piperazine citrate (10 mg/ml) was included as standard reference and distilled water as control. |
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