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Fixed Dose Combinations In The Treatment Of Tuberculosis |
p. 1 |
| R Panchagnula, Shruti Agrawal, C.L Kaul Tuberculosis is a complex socio-economic problem that impedes human development. Tuberculosis exerts a toll of eight million new sufferers and two million deaths every year. Around one third of world population harbors Mycobacterium tuberculosis that is sensitive to rifampicin, isoniazid, pyrazinamide and ethambutol. As tuberculosis is contagious, it infects many others there by necessitating early diagnosis and treatment. A standard 6 months treatment regimen formulated by World Health Organization (WHO), in its operational point of view is a complex procedure leading to treatment failure and resurgence of drug resistant strains. To increase the patient compliance, in its recently revised Tuberculosis Treatment Guidelines for National Tuberculosis Programs, WHO encourages the use of Fixed Dose Combination (FDC) tablets, which assures ingestion of all the components of tuberculosis treatment regimen. However, the major quality issue associated with FDCs Is assuring the bioavailability of rifampicin. If not carefully manufactured, bioavailability of rifampicin is negatively affected which could directly lead to poor treatment outcome and may lead to drug resistance. In the light of above scenario, this review mainly focuses the potential advantages of FDC formulations with special emphasis on quality of FDC preparation to be used for tuberculosis control. |
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Formulation And Evaluation Of Depot Parenteral Preparations For A Combination Of Norfloxacin And Tinidazole |
p. 10 |
| K Virender, S. B Tiwari, N Udupa Norfloxacin and tinidazole in combination are used as antibacterial and antidiarrhoeal agents, respectively. In the treatment of bacterial infections, factors of paramount Importance are to maintain the therapeutically optimum drug concentration in the plasma and eliminate the need for frequent dose administration. In the present Investigation, an attempt was made to design micro spheres loaded with norfloxacin and tinidazole Intended for parenteral administration. Biodegradable, non-toxic polymers viz., bovine serum albumin (BSA) and chitosan were used to form micro spheres. Micro spheres were prepared using the chemical cross-linking method. Glutaraldehyde-saturated toluene (GST) was employed as the cross linking agent. Various process parameters, like drug: polymer ratio, did not effect the mean particle size or particle size distribution to a significant extent and relatively a narrow particle size distribution was obtained. Entrapment efficiency of the albumin micro spheres for both the drugs was more than the corresponding chitosan micro spheres. Results of in vitro release studies indicate a biphasic release pattern characterized by a initial burst-effect followed by a slow release over a period of 12 to 24 h. |
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Preparation And Evaluation Of Sustained Release Nimesulide Microspheres Prepared From Sodium Alginate |
p. 15 |
| V. B Patil, B Pokharkar Nimesulide-loaded calcium alginate beads were prepared. In this Investigation, a 23 full factorial design was used to study the joint influence of three variables, the polymer concentration (X1), the drug concentration (X2) and the cross-linker (calcium chloride) concentration (X3), on various dependent variables like per cent entrapment, sphericity, particle size and amount of drug released during the initial (t=60 min). and final stages (t=360 min) of release. A statistical model with a significant Interaction term is obtained to predict the results. The drug release mechanisms from micro spheres were studied using the Peppas equation. |
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Antibacterial Natural Products From Leaves Of Lantana Camara L. With Activity Comparable To Some Therapeutically Used Antibiotics |
p. 20 |
| S Sukul, S Chaudhuri Four fractions of petroleum ether extract of the leaves of Lantana camara in different solvents showed significant antibacterial activity against some human pathogens under in vitro conditions. The MIC of the methanol fraction, containing triterpenoids, active against these pathogens was found to be comparable with those of some therapeutically used antibiotics. |
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Formulation Of Controlled Release Matrix Tablets Of Isosorbide Dinitrate |
p. 24 |
| I Haririan, A Ghaffari, M Mohammad-Pour Different retardant polymers Including Carbopol 934P, HydroxyPropyl Methyl Cellulose (HPMC) (Methocel K4M) and Eudragit NE30D, RL30D and RS30D as release controlling materials were evaluated. The drug release medium consisted of hydrochloric acid buffer, pH-1.2, for the first two hours and phosphate buffer, pH-6.8, for the remaining period of time during the experiments. The influence of variables including polymer type, drug: polymer ratio, tablet filler type and tablet hardness on isosorbide dinitrate (ISDN) release profile was discussed. From the retardant polymers investigated, Eudragit NE30D exhibited proper release characteristics. The pattern of drug release from formulation prepared from Eudragit NE30D was shown to correspond to the Higuchi equation. According to the equation, Mt/Mu=k.tn, lSDN release mechanism from Eudragit NE30D matrix tablets (40 mg) was based on non-Fickian-Diffusion process. It was also realized that, matrix preparation was a suitable method for the formulation of ISDN-CR tablets. |
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Studies On Hypoglycemic And Cardiotonic Effects Of Roots Of Cocculus Hirsutus |
p. 30 |
| K Satyanarayana, V Mangathayaru, J Sreekanth, V Venkateswarlu, C. K KoKate Methanol extract of roots of Cocculus hirsutus was tested for its hypoglycemic and cardiotonic effects on diabetic rats and isolated perfused frog heart respectively. The methanol extract exhibited significant hypoglycemic activity on diabetic rats and cardiotonic activity on normal and hypodynamic frog heart preparation. Activity-guided fractionation of methanol extract was carried out. Butanol fraction of methanol extract of roots of C. hirsutus was found to have significant cardiotonic activity comparable to that of ouabain. Total alkaloid fraction prepared from methanol extract showed considerable hypoglycemic activity on alloxan-induced diabetic rats. The TLC profile of total alkaloid fraction showed the presence of four alkaloids, whereas the TLC profile of butanol fraction showed the presence of steroids and/or triterpenoids. |
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Improvement Of Dissolution Rate And Bioavailability Of Piroxicam With Pregelatinized Starch |
p. 36 |
| N Rama Rao, K. P. R Chowdary Piroxicam (PPX) dispersions in pregelatinized starch (PGS) were prepared in different drug and carrier ratios and were characterized by X-ray diffractograms (XRD), differential scanning calorimetry (DSC), differential thermal analysis (DTA) and dissolution studies. Bioavailability studies were conducted on PRX-PGS dispersions and PRX pure drug in healthy human subjects as per cross over randomized block design (RBD). From Time Vs blood concentration data Cmax, Tmax, Ka, AUC and T1/2, were calculated. Higher dissolution rates were noted with dispersions when compared to piroxicam as such. PRX-PGS dispersions also gave fast absorption and higher blood levels of piroxicam when compared to pure drug. All the absorption parameters namely Cmax, percent absorbed In 1 and 2 h, Ka, AUC were higher indicating faster absorption of PRX from dispersions. |
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Wound Healing Activity Of Aegle Marmelos |
p. 41 |
| A Jaswanth, V Loganathan, S Manimaran Effects of topical and intraperitoneal administration of methanolic extract of Aegle marmelos ointment and injection was studied respectively on two types of wound models in rats, (i) the excision and (ii) the incision wound model. Both the injection and the ointment of the methanol extract of Aegle marmelos produced a significant response in both of the wound types tested. In the excision model the extract treated wounds were found to epithelialise faster and the rate of wound contraction was higher, as compared to control wounds. The extract facilitated the healing process as evidenced by increase in the tensile strength in the incision model. The results were also comparable to those of a standard drug nitrofurazone. |
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Preliminary Studies On The Development Of A New Non-Bitter Chloroquine Formulation Using Tannic Acid |
p. 45 |
| S. V Fulzele, S. B Jaiswal, S. B Joshi Chloroquine phosphate is a bitter antimalarial drug belonging to the 4-amino quinoline class of compounds. It was treated with tannic acid and precipitated to form a poorly soluble complex. The complex was analysed and evaluated for taste and in vitro release. It was then formulated in a syrup base. When orally administered to healthy human subjects, chloroquine level comparable to marketed preparation was obtained. On the basis of the preliminary results obtained in the present study the method may be further evaluated as a technique for taste masking of bitter amine drugs. |
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Formulation And Evaluation Of Niosome Entrapped Pentoxifylline Using In Vivo Bronchodilatory Activity In Guinea Pigs |
p. 49 |
| Aarti Jagtap, Deepali Inamdar The objective of this study is to formulate niosomes of pentoxifylline, characterize niosomes In terms of entrapment efficiency, particle size distribution, in vitro release and stability and investigate the bronchodilatory activity of plain and niosomal pentoxifylline in vivo in guinea pigs. Pentoxifylline was entrapped in niosomes by lipid layer hydration method using Span 60, cholesterol and dicetyl phosphate. The entrapment efficiency of niosomes of pentoxifylline was determined by separating the entrapped drug from the free drug by centrifugation. The in vitro release profile of the drug frorn niosomes was carried out in phosphate buffer saline (pH 7.4). The stability of niosomes was assessed by storage at 4±1°, 25±1°, 37±1° and 45±1° for one month. The plain (20,40 and 80 mg/kg) and niosomal pentoxifylline (5, 10, 20 and 40 mg/kg) was injected intraperitoneally to guinea pigs for evaluating bronchodilatory activity. The entrapment efficiency of niosomes of pentoxifylline was found to be 9.26±1.93% giving a sustained release of drug over a period of 24 h and better stability over the period of storage. The plain and niosomal pentoxifylline produced significant bronchodilatory effect in guinea pigs on histamine-induced bronchoconstriction. The study indicates that pentoxifylline may be an effective bronchodilator. |
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Simultaneous Determination Of Mefenmic Acid And Paracetamol From Combined Dosage Forms By Spectrophotometry |
p. 55 |
| A. S Dhake, D. B Sonaje, Veena S Kasture, P. T Nikam, R. S Talekar A new simple and sensitive spectrophotometric method in the UV region has been developed for the simultaneous determination of mefenamic acid and paracetamol in bulk and in dosage forms. Mefenamic acid shows three absorbance maxima at 219,284 and 336 nm and paracetamol shows a single absorbance maximum at 257 nm in 0.1N sodium hydroxide. Absorbance corrected for interference was used for estimation. Both these drugs obey Beer's law In the concentration ranges used in this method. The method has been validated statistically and by recovery studies. |
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Antifungal Activity Of Trimethyltinbenzoate-4-Picoline |
p. 58 |
| M. K Choudhury, S. A Ado, A Triny, A. S Shettima Trimethyltlnbenzoate-4-picolinwe as screened for its antifungal activities against six fungi consisting of four moulds, Aspergillus flavus, Aspergillus fumigatus, Aspergillus niger, Aspergillus versicolor and two yeasts, Brettanomyces anomala, Saccharomyces cerevisiae isolated from diseased grape plants (Vitis vinifera). A. niger and A. versicolor were inhibited by the compound at a concentration of 0.5 mg/ml, while A. flavus and S. cerevisiae required 1 mg/ml concentration. A, fumigatus and B. anomala required a higher concentration of 2.5 mg/ml for Inhibition. The Minimum Inhibitory Concentration (MIC) for A. versicolor, A. niger, A. flavus, S, cerevisiae, A. fumigatus and B. anomala were found to be 0.4,0.45, 0.8,0.9,2.5 and 2.5 mg/ml, respectively. |
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Spectrophotometric Determination Of Some Phenothiazine Drugs With Lodic Acid |
p. 61 |
| A. G Sajjan, J Seetharamappa, M. B Melwanki A sensitive and accurate spectrophotometric method for the quantitative determination of four phenothiazine drugs in either pure form or in pharmaceutical formulation is proposed. The method is based on the development of a red or bluish-green coloured product with iodic acid in phosphoric acid medium. The reaction proceeds via oxidation of the phenothiazine nucleus into a semiquinonoid radical. The optimum reaction conditions and other analytical parameters are evaluated. The influence of substrates commonly employed as excipients with phenothiazine drugs has been studied. Results of analysis of pure drugs and their dosage forms by the proposed method are in good agreement with those of the official method. |
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Salubrious Effect Of Tridax Procumbens On Paracetamol Hepatotoxicity |
p. 64 |
| S Senthil Kumar, D Asokan, P Sampath Kumar, S Kalavathy, N Manoharan Tridax procumbens is a hepatoprotective agent. Over dosage of paracetamol induces hepatotoxicity. This paper reports the salubrious effect of Trldax procumbens on the paracetamol-induced hepatotoxicity in Wister rats. |
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Simultaneous Spectrophotometric Estimation Of Losartan Potassium And Hydrochlorothiazide From Combined Dosage Form |
p. 66 |
| N. R Lande, B. M Shetkar, S. S Kadam, S. R Dhaneshwar Two simple, accurate and economical procedures for simultaneous estimation of losartan potassium and hydrochiorothiazide In two component tablet formulations have been developed. The methods employ program in the multicomponent mode of analysis of the instrument used and simultaneous equations using area under curve. In all glass double distilled water losartan potassium has an absorbance maxima at 205 nm, hydrochiorothiazide has three absorbance maxima at 225,272 and 315 nm. Both the drugs obey the Beer's Law In the concentration ranges employed for these methods. The results of analysis have been validated statistically and by recovery studies. |
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Visible Spectrophotometric And HPLC Methods For Estimation Of Rimapril From Capsule Formulation |
p. 69 |
| I Singhvi, S. C Chaturvedi Two visible spectrophotometric and one HPLC method have been developed for estimation of rimapril from its capsule formulation. The developed visible spectrophotometric methods were based on formation of chloroform extractable coloured complexes of drug with nitrosonaphthol and with bromophenol blue. The formed coloured complex with nitrosonaphthol showed absorbance maximum at 445.5 nm and Beer's law was obeyed In the concentration range of 50-300 μg/ml of drug while the formed coloured complex with bromophenol blue showed absorbance maximum at 414 nm and Beer's law was obeyed in the concentration range of 20-100 μg/ml of rimapril. Developed HPLC method was a reverse phase chromatographic method using inertsil C13 column and methanol: acetate buffer:: 80:20 as mobile phase with detection at 230 nm. Loratidine was used as internal standard for the HPLC method. Linearity was observed in concentration range of 10-300 μg/ml of rimapril. Results of analysis for all the methods were validated statistically and by recovery studies. |
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Chemical Examination Of The Flowers Of Couroupita Guianensis Aubl |
p. 72 |
| Jayashree B Rane, Severina J Vahanwala, Suprabha G Golatkar, R.Y Ambaye, B.G Khadse From the flowers of Couroupita gulanensis Aubl, an aliphatic hydrocarbon and stigmasterol have been isolated. The structure of stigmasterol has been established on the basis of spectral data and by chemical means. |
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Rheological Study Of Guar Gum |
p. 74 |
| J. S Tantry, Nagarsenker S Mangal A rheological study of guar gum indicated a non-Newtonian, pseudoplastic behaviour of its solutions. When the data was treated mathematically by the modified Newton's law, FN= η’G, the exponential constant N was found to Increase with Increasing concentration of gum. The viscosity of the solutions remained fairly constant in the pH range from 1.5 to 10.5. |
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Spectrophotometric Estimation Of Total Alkaloids From Cinchona Officinalis Stem Bark And Marketed Formulations Containing Cinchona |
p. 76 |
| M. N Ravishankara, Neeta Shrivastava, N Mahendru, Harish Padh, M Rajani The alkaloids of stem bark of Cinchona officinal is and the marketed formulations containing the stem bark of Cinchona were estimated by spectrophotometric method using tropaeolin 'OO' for the formation of colour complex. In Cinchona stem bark, the alkaloids are bound to tannins. The method adopted for the extraction of alkaloids from the samples has the advantage of extraction of mainly the alkaloids and not the other Interfering substances like tannins. The method of analysis was found to be sensitive, precise and accurate and it can be adopted for routine quality control purposes. |
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Antibacterial Activity Of Trimethyltinbenzoate-4-Picoline |
p. 79 |
| M. K Choudhury, S. A Ado, J. B Ameh, D. A Machido, A Triny, A. S Shettima The antibacterial activity of trimethyltinbenzoate-4-picoline (an organotin compound) was determined against five bacteria Isolated from diseased grape Plants (Vitis vinifera, family: Vitaceae).The zones of inhibition were observed, the minimum Inhibitory Concentrations (MIC) against bacteria that belonged to Pseudomonas, Corynebacterium, Bacillus, Klebsiella and Xanthomonas species were found to be 0.5, 0.8, 2.5, 2.5 and 2.5 mg/ml respectively. |
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