Five compounds were isolated from the methanolic extract of the roots of Vitex negundo linn and purified by crystalisation and preparative TLC. They were identified as 2 β, 3α-diacetoxyoleana-5,12-dien-28-oic acid, 2α, 3β-dihydroxyoleana-5,12-dien-28-oic acid, 2α, 3β-diacetoxy-18-hydroxyoleanaQ,12-dien-28-oic acid, vitexin and isovitexin by spectral data and chemical conversions.

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A simple and sensitive spectrophotometric method has been developed for the determination of nimodipine in bulk and pharmaceutical dosage forms. The method is based on diazotisation of reduced nimodipine with nitrous acid followed by its coupling with β-naphthol in alkaline medium to form an orange red colored chromogen with an absorption maximum of 555 nm. Good agreement with Beer's law was found in the range of reduced nimodipine concentration of 0-10 μg/ml. The optimum reaction conditions and other analytical parameters are evaluated-The proposed method has been successfully applied to the analysis of the bulk drugs and their dosage forms. No interference was observed from talc, starch, dextrose and magnesium stearate in the proposed method. Statistical comparison of the results with those of reported method showed good agreement and indicated no significant difference in precision. This method does not require any extraction or heating.

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Murashige and Skoog medium supplemented with 2,4-D (2 mg/1) and kinetin (1 mg/1) was found to be suitable for the establishment of callus cultures of Hypericum perforatum. The callus upon extraction and analysis by TLC/HPLC revealed the presence of hypericin. The content of hypericin in callus cultures of H. perforaturn was significantly less than the intact plant. There is no significant effect of media or hormones on bioproduction of hypericin.

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Two spectrophotometric methods (I and II) in the visible region have been developed for the estimation of satranldazole in bulk drug and pharmaceutical formulations. Methods I and II are based on the reaction of reduced satranidazole with p-dimethylaminobenzaldehyde (PDAB) and p-dimethylarninocinnamaldehyde (PDACA) in acidic conditions to form orange red and purple coloured chromogens with absorption maxima at 511 nm and 568 nm respectively. The reduction of satratiidazole was carried out with zinc granules and 4 N hydrochioric acid at room temperature in ethanol. Beer's law was obeyed in the concentration range of 10-50μg/ml for both the methods. The results of analysis have been validated statistically and by recovery studies. The methods were found to be simple, rapid, accurate, reproducible and economic. The results are comparable with those obtained using UV spectrophotometric methods in alcohol at 315 nm.

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A new simple, sensitive spectrophotometric method in ultraviolet region has been developed for the determination of trimetazidine dihydrochloride in bulk and in tablet dosage form. Trimetazidine dihydrochloride shows maximum absorbance at 270 nm. Beer's law was obeyed in the concentration range of 400-700 μg/ml. Results of the analysis were validated satistically and by recovery studies.

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The Comparative Molecular Field Analysis (CoMFA) approach permits analysis of a large number of quantitative descriptors and uses chemometric methods such as partial least squares (PLS) to correlate changes in biological activity with changes in chemical structure. It is one of the most robust modern tools for quantitative structure activity relationship studies. This review gives the introductory overview and general methodology used to carry out CoMFA.

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Crude ethanol extract of Pergularia extensa leaves was successively fractionated with petroleum ether, solvent ether, ethyl acetate, butanol and butanone. The ethanolic extract and various fractions were investigated for antiinflammatory activity in rats at a dose of 100 mg/kg intraperitoneally. Ethanol extract and its butanol fraction exhibited significant antiinflammatory activity when compared with respective controls and were comparable with that of standard drug aspirin.

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Complex formation of itraconazole (ITR) with β-cyclodextrin (βCD) and hydroxy propyl β-cyclodextrin (HPβCD) in aqueous solution and in solid state and the possibility of improving the solubility and dissolution rate of ITR via complexation with the above cyclodextrins were investigated. The phase solubility studies indicated the formation of a 1:1 M inclusion complex in solution with both βCD and HPβCD. The apparent stability constant (Kc) was 206.2 M-1 and 270.7 M-1 for βCD and HPβCD complexes, respectively. Differential Scanning Calorimetry (DSC) studies indicated the formation of solid inclusion complexes of ITR-βCD and ITR-HPβCD at 1:4 ratio only. Solid complexes of ITR-βCD and ITR-HPβCD (1:l and 1:2 M) prepared by kneading and coevaporation methods exhibited higher rates of dissolution and dissolution efficiency values than the corresponding physical mixtures and ITR itself. Higher dissolution rates were observed with kneaded complexes than with those prepared by coevaporation. Increases of 23.4 and 83.4-fold in the dissolution rate were observed respectively with ITR-βCD (1: 2 M) and ITR-HPβCD (1:2 M) kneaded complexes.

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The present investigation was aimed at the production of medicinally important glycyrrhetinic acid from callus and cell suspension culture of Glycyrrhiza glabra using various phytohormones. Supplementation of MS medium with various combinations and concentrations of phytohormones enhanced biomass production as well as glycyrrhetinic acid level in stem, leaf and root derived calli and cell suspension culture of G. glabra.

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In this study microcapsules prepared from gum karaya (GK) and chitosan (CH) using the principle of complex coacervation for the first time with a continuous oil-phase were evaluated for their in vivo performance. Diclofenac sodium (DFS) was used as the drug of choice. The dissolution profiles of DFS from prepared microcapsules as well as commercial product followed non-Fickian diffusion. The formulation displayed a sustained in vivo blood level pattern that is comparable to that of a commercial controlled release formulation.

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A new simple, specific and precise high performance thin layer chromatographic method has been developed for estimation of lovastatin in its tablet formulations. In this method, standard solutions and sample solution of lovastatln were applied on precoated silica gel G60 F254, TLC plate and developed using toluene: methanol (75:25 v/v) as mobile phase. The plate was scanned and quantified at 239 nm for lovastatin. The method was validated for precision, accuracy and reproducibility.

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The new methods for making polymeric systems for the controlled release of rifampicin drug is described. This method is very simple, it consists of mixing drug and polymer powder (ethylene-vinyl acetate copolymer) and compressed at room temperature. The compressed fluffy matrices were kept at 60°, 70° and 80° for 1½, 3 and 4½ h for sintering. The sintering tablets were charcterised for their physical parameters and conducted in vitro dissolution tests. The sintering time markedly affected the drug release properties of EVA (ethylene vinyl acetate copolymer) matrices. It is notable that the release rate of rifampicin from EVA matrices was inversely related to the time of sintering. This may be due to the increase in the extent and firmness of sintering which compacts the mass further so that the drug release is affected. The cumulative percent of rifampicin release decreased as the sintering temperature was increased, for all formulations. The drug release follows diffusive mechanism with first-order release kinetics.

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A high performance thin layer chromatographic method was developed and described for the quantitative estimation of epigallocatechin gallate in green tea extract.

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The antiulcer activity of ZD 7114, aβ3, - adrenoceptor agonist was studied in aspirin plus pylorus ligation induced gastric ulcer in rats and its effect on continuous acid secretion was also studied against in vivo as well as in vitro models. For comparison, the effect of isoprenaline and salbutamol was studied simultaneously in all experimental models. In gastric ulcer model, β-adrenoceptor agonists at all doses were found to be highly effective in affording gastroprotection. ZD 7114 treatment caused significant reduction in acid secretion in vivo model whereas no significant change was observed in vitro model of continuous acid secretion. In contrary to this no significant change in acid secretion was observed by treatment with isoprenaline and salbutamol in vivo model and a significant rise in acid secretion in vitro model.

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Liver, the metabolic machinery of the body, is under constant threat of oxidants. Lipid peroxidation being a toxicity mediating process, drug induced lipid peroxidation may be a probable mechanism of drug induced toxicity. In the present study, drug induced lipid peroxidation has been studied taking hydrocortisone as representative drug and liver homogenate as the experimental model. The antioxidant effects of ascorbic acid, probucol and α-tocopherol on hydrocortisone induced lipid peroxidation were also studied in an attempt to explore the possible potential of these agents in reducing drug-induced toxicity. It was observed that hydrocortisone could cause time-dependent induction in lipid peroxidation which may be related to the toxic potential of the drug. Further, ascorbic acid, probucol and a-tocopherol could suppress hydrocortisone-induced lipid peroxidation to significant extent. The present findings are interesting and provide a scope for further extensive studies on the antioxidants with an aim to reduce toxic potential of the drug.

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The controversies surrounding the use of short acting calcium channel blockers in hypertension are discussed. Much of the controversy has been generated by the study conducted by Psaty et al. The study concluded that the use of calcium channel blockers was associated with a 58% to 70% increased risk of suffering from myocardial infarction than with diuretics. In another trial named Appropriate Blood Pressure Control in Diabetes (ABCD), which compared nisoldipine and enalapril, was stopped early because of an excess of myocardial infarction (MI) amongst the patients taking calcium channel blockers (CCB). However amlodipine, a long acting CCB has shown to be beneficial in hypertension and has been widely prescribed. Based on the implications and limitations of the data available for the treatment of hypertension, suggestions were given for the selection of a suitable regimen.

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Spinal Cord Injury (SCI) is damage to the spinal cord that results in a loss of function such as mobility or feeling. Frequent causes of damage are trauma (car accident, gunshot, falls, etc.) or disease (polio, spina bifida, Friedreich's ataxia, etc.). The spinal cord does not have to be severed in order for a loss of functioning to occur. In fact, in most people with SCI, the spinal cord is intact, but the damage to it results in loss of functioning. The horseback riding injury of 'Superman' actor Christopher Reeve in 1995 generated considerable publicity and focused attention on the tragedy of SCI. Research on spinal injuries at this time was gathering momentum and scientists all around the world were making progress on what had been considered an untreatable injury. This review article summarizes the background on SCI and discusses the cellular and molecular changes that occur in the spinal cord following injury. The article further provides a glimpse into the ongoing cutting edge research that is aimed at developing pharmacological treatments for SCI. Products and compounds undergoing clinical trials are also discussed.

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Based on the results obtained from geometry optimization, using molecular mechanics and ZlNDO/1 force fields, of some known antitumor ruthenium compounds we designed five ruthenium chelates and synthesized them. Effects of these compounds on the growth of a transplantable murine tumor and the life span of the hosts are studied. Remarkable decrease in tumor volume and viable ascitic cell count is observed (p<0.0.5). Treatment with the ruthenium compounds prolonged the lifespan of Ehrlich Ascites Carcinoma (EAC) tumor bearing mice. Tumor inhibition by the ruthenium chelates was followed by improvements in hemoglobin, RBC and WBC values. Thus the results suggest that these ruthenium chelates have significant antitumor property against experimental murine tumors and it does not adversely affect the hematological profile of the host.

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The purpose of this investigation is to evaluate the capability of some water soluble polymers to adhere to the ocular surface and the effect of solution viscosity on precorneal residence. Captive bubble technique was used to study the desorption kinetics of those polymers from freshly enucleated, rabbit eyes under physiological conditions. It was shown that the contact angle on mucin-coated corneal surface was 38.2±1.6° measured by sessile bubble method, and sodium hyaluronate (HA) had the most appropriate corneal wettability although not decreasing the surface tension. At a similar solution viscosity, the retentive capability of the five viscolyers was in the order Carbopol (residence time 15 to 25 min)>HA (15 to 22 min)>polyvinyl alcohol≡hydroxy-propylmethylcellulose (10 to 15 min)>sodium carboxymethylcellulose (10 min), which demonstrated that the viscosity had different effects on the residence time of various viscolyers.

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HIV-1 protease inhibitors are an important part of the arsenal for the treatment of AIDS. Currently available protease inhibitors are known to interact with CYP3A4. Consequently, they are highly prone to drug-drug interactions with other coadministered drugs that are substrates or inhibitors of CYP3A4. Thus, development of newer HIV-1 protease inhibitors with a lower tendency for drug-drug interactions would be advantageous. We have compared the CYP450 inhibitory profiles of several discovery phase HIV-1 protease inhibitor candidates with saquinavir, indinavir, nelfinavir, and a structurally related compound, PNU 140690.The data indicate that discovery phase compounds have a different inhibitory profile than the other test compounds and show a lower potential for CYP3A4 and CYP2D6 based drug-drug interactions. However, they have a higher potential for CYPlA2 and CYP2C9 based drug-drug interactions. None of the compounds tested inhibited CYP2El or CYP2A6 to any significant extent.

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Three isomeric biflavonoids, calodenins A and B and trans-α2, β2- dihydroderivative of calodenin B were isolated from the stem bark of Ochna afzelii. All of these are being reported for the first time from this plant.

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