Nicorandil, N-[2-nitroxyethyl]-pyridine-3-carboxamide was synthesized by condensing nicotinoyl chloride with 2-nitroxyethylamine in presence of pyridine. 2-Nitroxyethylamine was prepared from 2- aminoethanol by a three step process. This process was less hazardous and comparatively economical than the literature reported methods.

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A new precise, selective and accurate reverse phase high performance liquid chromatographic method for simultaneous estimation of tinidazole and ciprofioxacin hydrochloride from their tablets has been developed. This chromatographic method utilises a 12.5 cm Nucleosil 100-5C18 bonded phase column with a mobile phase consisting of acetonitrile:methanol:0.002 M phosphoric acid (20:30:50) at a flow rate of 1.2 ml/min. Caffeine was used as the internal standard. Results of analysis gave standard deviation values below 1.5 and recovery study values between 98 to 103 per cent. Thus the method is suitable for routine analysis of multicomponent formulations of these two drugs.

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Compressed suppositories in indomethacin were formulated employing PEG 4000 as base with a view to minimize the gastric irritation of the drug upon oral administration. Preliminary pharmacodynamic experiments displayed comparable antiinflammatory activity and reduced ulcerogenic potential of the drug upon rectal administration. The influence of disintegrants (primogel and potato starch) on the in vitro release of drug was studied employing USPXX basket and dialysis methods. Based on the in vitro drug release studies from dialysis method, fast release suppositories containing 5% primogel and 10% potato starch were further evaluated for pharmacokinetic performance in healthy human volunteers. The study indicated that disintegrants did not influence either the rate or the extent of absorption of indomethacin compared to plain suppositories. It was concluded that in vitro drug release by dialysis method could not simulate the in vivo conditions.

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Terbutaline sulphate on oxidation with sodium periodate in alkaline medium followed by treatment with acetylacetone produces yellow coloured chromogen with maximum absorbance and 412 nm. The Beer’s Lambert range observed is 20-160 μcg/ml of the reaction mixture. The calculated % RSD is ± 1.61. The proposed method is applicable to the drug powder from and to pharmaceutical dosage forms.

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Spectrophotometric determination of hydroxy citric acid (HCA) present in Garcinia cambogia fruit is proposed here. This method is based upon, the colour complex formation (λmax: 467 nm) between hydroxy citric acid and sodium meta vanadate.

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Accurate and economical spectrophotometric method requiring no prior separation has been developed. The method employs multiwavelength ultraviolet spectrophotometry for the simultaneous estimation of tinidazole, diloxanide furoate and furazolidone from tablet formulation using N,N-dimethylformamide (15% v/v) as solvent. The three wavelengths selected for analysis are 367 nm, 317 nm and 262 nm. All the three drugs obey Beer's law in the concentration ranges employed for the analysis. The results of analysis have been validated by application of statistical principles to the data obtained and the method was found to give satisfactory results.

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The chemical examination of Barleria longiflora Linn. F. is described for the first time. Extraction of stems and roots with solvents and column chromatography led to the isolation of four anthraquinones of which two are new. The known anthraquinones were identified as tectoquinone and 1,3,5-trihydroxy-4- methoxy-2-methylanthraquinone and the new anthraquinones characterised as 3,8-dihydroxy-4- methoxy-2 methylanthraquinone and 1,3,4-trihydroxy-5 (or 8)-methoxy-2-methylanthraquinone by chemical and spectral studies. Arnidiol, a pentacyclic triterpene, was isolated without admixture with its isomer faradiol which usually is the case with many plants. A sterol mixture was also isolated, the minor components of which were Identified as campesterol, stigmasterol and b-sitosterol by GCMS of the acetate mixture.

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Different doses of 95% alcoholic extract of whole plant of Rivea hypocrateriformis (Convolvulaceae) was tested for antiimplantation activity in female albino rats. The alcoholic extract at a dose of 200 mg/kg body weight has showed 66.66% antiimplantation activity. Whereas, at 400 mg/kg body weight, significantly prevented pregnancy by 100%. The antiimplantation activity was reversible on withdrawal of the treatment of the extract.

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Lectins are carbohydrate-binding oligomeric proteins or glycoproteins of non-immune origin. Their occurrence is not restricted to plant sources but is ubiquitous and are found in animal cells also. These molecules bind reversibly with specific sugars and precipitate polysaccharides, glycoproteins and glycolipids bearing specific sugars, thus acting as cell recognizers. Their presence on tumor cells is being widely exploited for recognizing the specificity of tumor cells towards a possible means of targeting them. In addition, the presence of specific lectins on microorganisms and host tissues is being investigated for targeting drugs towards them. This review discusses the role of lectins in their-site-specific recognition of tissues and for targeted drug delivery.

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A method has been developed for the determination of sulphamethoxazole (SMX) and trimethoprim (TMP) in pharmaceuticals by fourier transform infrared (FTIR) spectrometry. The method is based on the fractional dissolving of SMX and TMP in acetone and chloroform respectively. SMX is then determined by absorbance measurements at 1165 cm-1 and TMP by using the absorbance values at 1126 cm-1, separately. The method provides precise and accurate results for the analysis of real samples of the binary dosage form of SMX and TMP, co-trimoxazole.

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A promising new approach to drug discovery concerns with the synthesis and screening of combinatorial libraries in order to identify new compounds that express high affinity and specificity for a pharmacologically relevant, biomolecular target. Advances in molecular biology, automated chemical synthesis and robotics have facilitated the formulation of vast libraries of structurally related molecules. An essential aspect of screening large combinatorial libraries is the ability to identify the active components in these complex mixtures, which is usually based on the strength of binding to a selected target macromolecule.

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The N-acetylation of isoniazid was studied in three different groups of lranian and Afghani population (182 healthy volunteers, 78 infectious non-tuberculotic patients and 111 tuberculous patients, total of 371 subjects). The frequency of slow acetylator was determined using the percentage of acetylisoniazid excreted in urine which was about 59% in both populations. Also, the frequency distribution histogram of isoniazid phenotypes in studied population showed an apparent bimodal pattern. Statistical analysis of healthy volunteer's data versus all other patient's data indicated that there is no significant difference between slow and rapid acetylators. The finding of this study is very similar to that of the earlier results found among other cauccasian groups. However, The knowledge of the acetylator phenotype of a patient can help to determine the relative risk for some of the drug-related toxic and therapeutic responses.

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Parkinsonia aculeata stems have been shown to contain glycerol β-butanoate α, α’-dipentanoate, β-sitosterol, glycerol α-heptanoate ∞'octanoate, β-sitosteryl- β-D-glucoside and sucrose. Of these, the two glycerides are being reported for the first time.

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Metastasis is the major impediment to successful eradication of cancer. Therefore, development of antimetastatic agents is of prime importance. The present investigation is a modest step in that direction. Nicotinic acid is one of the products of nicotinamide hydrolysis by proteases and has been shown along with the parent compound (nicotinamide) to possess anticarcinogenic property. Therefore, it was interesting to find out whether it had any antimetastatic properties also. These studies have been done in a well standardised experimental metastasis model viz. B16F10 melanoma. Our results clearly demonstrates that at a dose level of 150 mg/kg on 1 through 9 schedule, there was a significant decrease in lung metastasis. Considering the fact that nicotinic acid is a dietary constituent related to vit. B3 (nicotinamide), these results suggest that nicotinic acid could be used as an antimetastatic agent along with cytotoxic anticancer drug treatment in the therapy of human cancers.

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A simple sensitive and accurate spectrophotometric method is developed for the determination of vicinal dihydroxybenzene derivatives [pyrocatechol (PCL), dopamine (DPH), levodopa (LDP) and methyldopa (MDP)] using pyridine-4-carboxylic hydrazid (isoniazid) in alkaline medium. Beer's law of the coloured species is obeyed in the range 1.2 to 12μg/ml at the maximum absorption of 480 nm. The molar absorptivity found to be 1.4312 x 104, 1.5015 x 104, 1.0924x104 and 7.2163x1031/mol/cm for DPH, PCL, LDP and MDP respectively. The proposed method is successfully applied for the determination of DPH, LDP and MDP in injections and tablets of pharmaceutical preparation. The reliability of these methods is established by parallel determination with the reported and official methods.

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3-Nitrolawsonemonoxime, 3-aminolawsonemonoxime and their chelates of Ca(II), Mg(II), Sn(II), Pb(II) and Zn(II) have been synthesized and their antibacterial activity studies were carried out. The results obtained were analysed to find the effect of change in concentration of test compounds, change in the substituents at C-3 position in the quinonoid ring of the ligand and the effect of change of central metal ion. The NO2 group at C-3 position in the quinonoid ring of the ligand showed greater activity than NH2 group. The activity of 3-nitrolawsonemonoxime was found to be decreased while that of 3- aminolawsonemonoxime, was observed to be increased due to chelation. In case of the chelates, activity was increased if their concentrations were increased sufficiently (doubled). But in case of Ca(II)-3- aminolawsonemonoximate, generally there has been no change in the activity with concentration. Elemental analysis and TG indicated ML22H2O molecular composition for the chelates.

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Considering the high lipophilicity (log P=7.41) of centchroman playing a critical role in the mediation of its biological activities (both therapeutic and toxic), effects of the drug on blood lipid constituents were studied using goat’s whole blood as the lipid source. The results reveal that the drug has significant affinity in binding with phospholipid which is further corroborated by changes in fatty acid composition. Lipid binding potential of the drug may have role in its therapeutic effect. Lipid peroxidation induction potential of centchroman has been quantitatively measured in the context of its toxicity. However, the drug does not cause significant extent of lipid peroxidation and this is in good agreement with its safety record.

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A series of 3,5-dialkyl-4-ethoxycarbonylamino-4H-1,2,4-triazoles and 3,5-dialkyl-4-tertbutoxycarbonylamino-4H-1,2,4-triazoles were tested for their in vitro antibacterial and antifungal activities in solid agar cultures against eight microorganisms. In tests, some of the compounds were shown to be very potent in vitro antifungal activity against the fungi used.

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