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    Preparation and Characterization of Controlled-Release Floating Bilayer Tablets of Esomeprazole and Clarithromycin

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    Controlled-release effervescent floating bilayer tablets reduce dosage frequency and improve patient compliance with enhanced therapeutic outcomes. Generally, two different tablets of clarithromycin and esomeprazole, respectively, are given for the treatment of Helicobacter pylori infection and it might be worth incorporating both in a single tablet. In the current study, controlled-release floating bilayer tablets of clarithromycin and esomeprazole (F1–F4) were developed with different rates of polymeric materials by a direct compression method. During the formulation, Fourier-transform infrared spectroscopy (FTIR) analysis was performed for possible interactions between drugs and excipients. No interactions between drugs and excipients were noted. Moreover, the bilayer tablets’ thickness, diameter, friability, hardness, weight variation, dissolution, and percent purity were found within the acceptable limits. The floating lag time and total floating time of all formulations were found to be < 25 s and 24 h, respectively. The release of both the clarithromycin and esomeprazole started at the same time from the controlled-release floating bilayer tablets by anomalous non-Fickian diffusion, and the polymeric materials extended the drug release rate up to 24 h. In the case of F1, the results approached ideal zero-order kinetics. The dissolution profiles of the tested and reference tablet formulations were compared, but no significant differences were observed. It can be concluded that such controlled-release effervescent floating bilayer tablets can be efficiently used in clinical practice to reduce dosage frequency and increase patient compliance with continuous drug release for 24 h, which ultimately might enhance therapeutic efficacy

    Interaction of <i>Semecarpus anacardium </i>L. with propranolol against isoproterenol induced myocardial damage in rats

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    200-206With a view to evaluate the cardioprotective effect of ethanolic extract of S. anacardium nut and the possible interaction with propranolol against isoproterenol induced myocardial damage in rats, female Sprague-Dawley rats were pre-treated with propranolol (10 mg/kg for 7 days), low and high doses of S. anacardium (100 and 500 mg/kg for 21 days) and their combination orally and subsequently subjected to isoproterenol administration (150 mg/kg, sc) for two consecutive days. The influence of prophylactic treatment was analysed by quantification of biomarkers and antioxidants, electocardiographic parameters and histopathological observations. The activities of lactate dehydrogenase and creatinine phosphokinase-MB were reduced in serum and raised in heart tissue with concurrent elevation in superoxide dismutase and catalase activities as well as reduction in thiobarbituric acid reactive species levels significantly in all treated groups compared to isoproterenol group. Similarly, electrocardiographic changes were restored to normalcy in all treated groups. To conclude, combination of high dose of S. anacardium with propranolol was found to be most effective in alleviating the abnormal conditions induced by isoproterenol

    Influence of betel quid on effect of calcium channel blockers on isoprenaline induced myocardial necrosis in mice

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    730-736It is known that chewing Betel quid with tobacco (BQT) or without tobacco (BQ) is a major etiological factor for cardiovascular complications and calcium channel blockers (CCBs) are the major class of drugs prescribed widely for myocardial disturbances. The possible pharmacodynamic interaction between CCBs (verapamil, amlodipine and diltiazem) and BQ/BQT was studied on isoproterenol (ISO)-induced myocardial necrosis in mice. Influence of (CCBs) therapy on pretreated animals at times of myocardial stress were determined by estimating diagnostic marker enzymes such as lactate dehydrogenase (LDH) and creatine phosphokinase isoenzyme (CK-MB) in serum and heart tissue homogenate (HTH). Administration of CCBs to mice pretreated with BQ produced a significant decrease and increase in biomarker enzyme levels in serum and HTH respectively. Further, incorporation of diltiazem and amlodipine in BQT pretreated mice significantly elevated enzyme levels in HTH, whereas, amlodipine administration during BQT treatment showed significant fall in enzyme levels in serum. The results indicated that BQT is cardiotoxic and its effect cannot be reversed using CCBs while BQ is cardioprotective, whose activity was further augmented by amlodipine. Histopathological studies confirmed the biochemical findings

    Effect of conventional antihypertensive drugs on hypolipidemic action of garlic in rats

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    176-181The present study was undertaken to determine the possible alteration in hypolipidemic actions of garlic homogenate (GH) in presence of conventional antihypertensive drugs, propranolol (PRO), hydrochlorothiazide (HYD) and captopril (CAP). Albino rats fed with normal fat diet (NFD) or high fat diet (HFD) were treated with GH at three different doses (125, 250 and 500 mg/kg) orally for 30 days or in combination with PRO (10 mg/kg, po), HYD (10 mg/kg, po) and CAP (30 mg/kg, po) during last 7 days of GH treatment. After the treatment, total cholesterol (TC), LDL-cholesterol, triglyceride (TG) and HDL-cholesterol were measured in serum and antiatherogenic index was calculated. The result showed that moderate and high doses of GH possessed potential antiatherosclerotic property that was significantly attenuated by PRO and HYD. However, GH antihyperlipidemic activity was augmented by CAP. It was concluded that administration of PRO and HYD decrease the hypolipidemic effect of GH and administration of GH along with CAP augmented the hypolipidemic effect of GH in rats

    Hepatoprotective studies of &lt;i&gt;Coccinia indica&lt;/i&gt; Linn. in carbon tetrachloride induced hepatic injury

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    Cocciana indica Linn (Cucurbitaceae) is widely distributed throughout India. It was employed in ancient system of medicine as anti-inflammatory, anthelmintic, digestant, liver tonic, and expectorant. Though it is traditionally used in jaundice and other hepatic manifestations, there are no reports on their validation and standardization for hepatoprotective activity. This study was undertaken to evaluate hepatoprotective effects of hydroalcoholic extract of the leaves and fruits of the plant against carbon tetrachloride (CCl4) induced hepatotoxicity in rats and mice. The extract of the plant material significantly increased the bromosulphthaline clearance and significantly reduced the pentobarbitone induced sleeping time. Furthermore, serum examination of treated animals revealed that the plant extract reduced the levels of alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase and bilirubin. Morphological studies demonstrated the hepatoprotective activity of the extract by showing a decrease in liver weight. Free radical scavenging studies indicated an increase in glutathione concentration and reduced liver lipid peroxidase after treatment with the plant extract. Keywords: Cocciana indica, cucurbitaceae, hepatoprotective, carbon tetrachloride, free radical scavenging Ethiopian Pharmaceutical Journal Vol. 23 2005: 39-4

    Going Beyond Counting First Authors in Author Co-citation Analysis

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    The present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed

    Communication: Effect of diperoxovandate on isolated rat heart

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    Diperoxovanadate (DPV), a product of vanadate is gaining importance as a biologically active vanadium compound. The aim of the present study was to evaluate the chronotropic and inotropic activity of DPV using isolated rat heart and to determine the concentration at which it is toxic to the heart. The study was carried out using modified Langendorff\'s setup. DPV was injected at varying concentrations (from 10-9 to 10-4) either as bolus (0.1 ml) or the heart was perfused continuously with varying concentrations of DPV for 10 min. Low concentration of DPV did not produce any significant effect on chronotropy and on developed tension. However, as the dose of DPV was increased, tension developed and heart rate was enhanced to significant extent (P < 0.05) and both were found to be maximum at a dose of 10-7M. Further increase in DPV dose did not show either an increase in force or rate of contraction of heart but instead produced a relative decrease in both of these parameters when compared with the 10-7 M dose. When heart was perfused with a dose of 10-7 M DPV continuously for 10 min there was a significant increase in heart rate and developed tension (P < 0.01). It was also found that at a dose of 10-5M, DPV showed not only further increase in developed tension but also produced marked disturbances in the rhythm indicating cardiac toxicity. This was further confirmed by lactate dehydrogenase (LDH) activity determination. Keywords: diperoxovanadate, reperfusion, isolated rat heart, hydrogen peroxide, lactate dehydrogenase Ethiopian Pharmaceutical Journal, vol. 22 (2004): 47-5

    Immunomodulatory activity of methanolic fruit extract of Aegle marmelos in experimental animals

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    AbstractAimThe aim of the present study was to investigate the immunomodulatory action of methanolic extract of Aegle marmelos fruit (FEAM) in experimental model of immunity.MethodsCellular immunity was carried out by neutrophil adhesion test and carbon clearance assay, whereas, humoral immunity was analyzed by mice lethality test and indirect haemagglutination assay. FEAM dose was selected by Stair case method (up and down) and administered at 100 and 500mg/kg orally. The Ocimum sanctum (OSE, 100mg/kg, p.o) was used as standard.ResultsFEAM at 100 and 500mg/kg produced significant increases in adhesion of neutrophils and an increase in phagocytic index in carbon clearance assay. Both high and low doses of FEAM significantly prevented the mortality induced by bovine Pasteurella multocida in mice. Treatment of animals with FEAM and OSE significantly increased the circulating antibody titre in indirect haemagglunation test. Among the different doses, low one was more effective in cellular immunity models than the high. However, all the doses exhibited similar protection in humoral immunity procedures.ConclusionFrom the above findings, it is concluded that FEAM possesses potential for augmenting immune activity by cellular and humoral mediated mechanisms more at low dose (100mg/kg) than high dose (500mg/kg)

    Variations on the Author

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    “Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship
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