Recursos de colección

Universidad Nacional de La Plata (74.538 recursos)

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vol. 31, no. 01

Mostrando recursos 1 - 20 de 28

  1. Comparative pharmacokinetic study of ascaridole after oral administration of ascaridole and Jinghuaweikang capsule to rats

    Zhang, Boli; Zhou, Shuiping; Ma, Xiaohui; Wang, Xiangyang; Li, Wei; Chu, Yang; Zhu, Yonghong
    The objective of this study was to compare the pharmacokinetic characteristics of ascaridole following oral administration of pure ascaridole and Jinghuaweikang (JHWK) capsule. Besides, additional rats were given pure ascaridole via intravenous administration for the bioavailability study. The concentration of ascaridole in rat plasma was determined by a GC/MS method. Following oral administration of pure ascaridole and JHWK capsule, the maximum mean concentration in rat plasma (Cmax, 2701.4 ± 1282.6 ng/mL and 3008.0 ± 273.5 ng/mL) were achieved at 0.25 ± 0.09 h and 0.47 ± 0.22 h (Tmax), and the absolute bioavailabilities were approximately 20.8 and 26.9 %, respectively....

  2. Determination of esomeprazole in rabbit plasma by liquid chromatography-mass spectrometry and its application to a pharmacokinetic study

    Zhang, Meiling; Wang, Xuebao; Wang, Zhiyi; Deng, Mingjie; Xu, Zhisheng; Zheng, Yuancai; Zhang, Yuan; Huang, Xueli
    A sensitive and selective liquid chromatography-mass spectrometry (LC–MS) method for determination of esomeprazole in rabbit plasma was developed and validated. After addition of midazolam as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation, and chromatography involved Agilent SB-C18 column (2.1 x 150 mm, 5.0 μm) using 0.1 % formic acid in water and acetonitrile as a mobile phase with gradient elution. Detection involved positive ion mode electrospray ionization (ESI), and selective ion monitoring (SIM) mode was used for quantification of target fragment ions m/z 198 for esomeprazole and m/z 326 for midazolam (internal standard, IS). The...

  3. Quantification of torsemide in rabbit plasma by liquid chromatography/electrospray mass spectrometry and its application

    Hu, Lufeng; Chen, Xiaole; Chen, Chan; Wang, Jinjin; Wang, Zhibin; Wang, Zhiyi
    A sensitive and simple liquid chromatography/electrospray mass spectrometry (LC-ESI-MS) method for determination of torsemide in rabbit plasma using one-step protein precipitation was developed and validated. After addition of midazolam as internal standard (IS), protein precipitation by acetonitrile was used in sample preparation. Chromatographically separation was achieved on an SB-C18 (2.1 mm×150 mm, 5 μm) column with acetonitrile-0.1 % formic acid as the mobile phase with gradient elution. Electrospray ionization (ESI) source was applied and operated in positive ion mode; selected ion monitoring (SIM) mode was used to quantification using target fragment ions m/z 349 for torsemide and m/z 326 for...

  4. Enteroparasitological profile of patients assisted in the Lauro Wanderley University Hospital (HULW)

    Oliveira, Thompson L.; Lianza, Maria C. S.; Fernandes, Héllisson B.; Oliveira Filho, Abrahão Alves de; Fernandes, Heloísa M. B.
    Infections with intestinal parasites represent a worsening public health, given the large number of individuals affected and various organic changes that can be caused. The objective was to conduct a survey of individuals affected by these parasites assisted by the Clinical Laboratory of the HULW from January 2010 to January 2011, as well as characterizing data intrinsic to individuals. Data were obtained through a statistical analysis of 7844 reports of fecal examinations. Among the results was shown that 32.5 % of samples were parasitized, Ascaris lumbricoides being the most frequent in these reports, accounting for 36 %. Female patients were...

  5. In vitro effects of ivermectin upon trichomonas vaginalis trophozoites

    Vargas Villarreal, Javier; Cortes Gutiérrez, Elva I.; Garza González, Jesús N.; Rivera Silva, Gerardo; Mata Cárdenas, Benito D.; González Salazar, Francisco
    Trichomoniasis is the most common, curable sexually transmitted disease in the world. The first line treatment of trichomoniasis is metronidazole. Recently, the resistance of T. vaginalis to metronidazole and imidazoles has been shown to increase. Ivermectin is a synthetic machrolid drug with activity versus endo and ectoparasitic organisms. In this assay, was tested the effects of ivermectin on T. vaginalis trophozoites. Ivermectin have anti-parasitic activity upon trichomonas trophozoites. However, the IC50 of ivermectin against T. vaginalis was high compared with metronidazole.

  6. Chemical composition of essential oils and anticholinesterasic activity of Eugenia sulcata Spring ex Mart.

    Rocha, Leandro; Silva Filho, Moacélio V.; Santos, Marcelo G.; Botas, Gisele da S.; Cruz, Rodrigo A.S.; Fernandes, Caio P.; Tietbohl, Luis A. C.; Lima, Barbara G.
    The chemical composition of the essential oils from leaves and stems of Eugenia sulcata Spring ex Mart., obtained by hydrodistillation, was analyzed by GC-MS and quantified by CG-FID. In all, 37 components were identified and sesquiterpenes represented the largest fraction of both oils, in the leaves (58.2 %) and stems (85.3 %). The major constituent found in the essential oil from leaves and stems of E. sulcata was β-caryophyllene, corresponding to 24.6 % and 18.8 %, respectively. The substances α- cubebene (1.1 %), β-copaene (0.5 %), cis-muurola-3,5-diene (0.6 %), cis-muurola-4(14),5-diene (1.3 %), γ- himachalene (2.0 %), epizonarene (0.8 %), trans-calamenene...

  7. Cytochalasin E, a potential agent for anti-glioma therapy, efficiently induces U87 human glioblastoma cell death

    Xing, Biao; Zhang, Guofeng; Li, Meng; Hu, Weixing; Gu, Peiyuan; Wei, Dong; Xu, Jing; Ma, Banyou; Gu, Bing; Chen, Gong; Li, Junyang
    Glioblastoma is one of the most malignant brain tumors. Current treatments for glioblastoma usually make poor responses, and novel treatment strategies are extremely imperative. Cytochalasin E was reported to inhibit angiogenesis and tumor growth in some studies, but its effects on gliomas are still unknown. In this study, we found cytochalasin E inhibits U87 human glioblastoma cell growth in a very low concentration range of 10-8 to 10-6 M in a time and concentration dependent manner, and the IC50 were 1.17 ± 0.32 × 10-7 M for 48 h treatment, 6.65 ± 1.12 × 10-8 M for 72 h and...

  8. Preparation and characterization of floating gellan-chitosan polyelectrolyte complex beads

    Pandit, Jayant K.; Sharma, Suresh D.; Nagarwal, Ramesh C.; Verma, Anurag
    The objective of the present investigation was to evaluate the potential of gellan gum- low molecular weight chitosan (GG-LMCH) polyelectrolyte complex (PEC) in the form of beads as prolonged release stomach specific floating drug delivery system. PEC beads were prepared in one step, without using any chemical crosslinker, by dropwise addition of GG to a solution of LMCH in acetic acid. Buoyancy to the beads was attributed to the use of CaCO3 . The % buoyancy, encapsulation efficiency and drug release from PEC beads were compared with Ca++ crosslinked GG floating beads prepared under same conditions using rifabutin as model...

  9. Anti HSV-1 activity of five strawberry cultivars

    Simões, Cláudia Maria Oliveira; Reginatto, Flávio Henrique; Calvete, Eunice; Blum Silva, Carlos H.; Carvalho, Annelise
    Five strawberry (Fragaria x ananassa) cultivars harvested in Passo Fundo (State of Rio Grande do Sul, Brazil) were quantified for their total flavonoids (TF) and total anthocyanins contents (TA) and the extracts were evaluated for their in vitro antiherpes (anti-HSV-1, KOS strain) activity. The cultivars Camarosa and Aromas presented the highest TF (149.1 and 129.4 mg RE/100g FF), respectively; and TA (92.8 and 84.4 mg CGE/100 g FF), respectively. On the other hand, Camino Real cultivar showed the lowest TF (69.9 mg RE/100 g FF) and TA (46.2 mg CGE/100 g FF). With regard to the antiherpes activity, Camarosa and...

  10. A UPLC-DAD-MS method for the quality analysis of "JiangYaBiFeng" tablet

    Wang, Yuefei; Liu, Haitao; Qi, Aidi; Chai, Xin; Olaleye, Olajide; Peng, Siwei; Zhu, Lin
    "JiangYaBiFeng" (JYBF) tablet for treatment of hypertension in China is a composite prescription of Chinese and western medicines. By using ultra high performance liquid chromatography coupled with mass spectrometry (UPLC-MS), twenty-five compounds were simultaneously identified or tentatively characterized based on their retention times and MS spectra. Nine target compounds, hydrochlorothiazide (HC), rutin, genistin, sophoricoside, baicalin, wogonoside, genistein, baicalein and wogonin, were further quantified by ultra high performance liquid chromatography with diode-array detector (UPLC-DAD). Chromatographic separation was successfully performed on a C18 column with gradient elution of 0.1 % formic acid aqueous solution and acetonitrile at the flow rate of 0.4...

  11. Validation of an UV spectrophotometric method for determining diffractaic acid from Usnea sp. in inclusion complexes with hydroxypropyl-β-cyclodextrin

    Silva, Camilla V.N.S.; Santos, Noemia P. S.; Santos Magalhães, Nereide S.; Lira, Mariane C. B.; Honda, Neli Kika; Ferraz, Milena S.
    Diffractaic acid (DA) presents several biological activities. The goal of this study was to develop and validate a UV spectrophotometric method for determining diffractaic acid in inclusion complexes with hydroxypropyl-β-cyclodextrin. Validation parameters were determined according to international guidelines for standardization. The linearity range of analytical curve was from 1 to 5 μg/mL and the regression equation: CDA = (Area - 0.0053)/0.1541 (r2 = 0.99998; n = 3). The intermediate precision indicated that the difference between the means was statistically insignificant (p < 0.05). Accuracy revealed a mean recovery percentage of diffractaic acid in inclusion complexes of 100.1 %. The method...

  12. Simultaneous quantification of 6,7-di-hydroxyligustilide and gastrodin in rat plasma by LC-MS: application to pharmacokinetic study of tianshu capsule

    Bi, Kaishun; Yan, Baoqing; Huo, Yanshuang; Chen, Xaohui; Sun, Linxin; Zhang, Huifen
    A LC-MS method was developed and validated for simultaneous determination of 6, 7-di-hydroxyligustilide and gastrodin in rat plasma, and which was subsequently applied in the pharmacokinetic analysis of an administration of a Chinese herbal extract containing Chuanxiong Rhizoma and Gastrodia Elata Rhizome, i.e. TianShu capsule against migraine. The analytes were separated on a Kromasil C18 column with a gradient elution program and detected without interference in the selected ion monitoring mode with positive electrospray ionization. The linear range was 0.010-10.0 μg/mL for 6,7-di-hydroxyligustilide and 0.025-25.0 μg/mL for gastrodin with the limit of quantitation of 0.01 and 0.025 μg/mL, respectively. The...

  13. Processing of Apeiba tibourbou Aubl. extract via spray drying

    Conceição, Edmilson C. da; Paula, José R. de; Bara, María Teresa. F.; Freitas, Osvaldo de; Martins, Frederico S.; Oliveira, Ezequiane M. S.; Couto, Renê O.
    The effects of drying air inlet temperature (IT) and concentration of Aerosil® 200 (CA) on several properties of spray-dried Apeiba tibourbou extracts were investigated following a 32 full factorial design. Powder recovery varied from 9.83 to 46.95% and dried products showed moisture contents below 7%. Although the spray-dried products lost some of their polyphenols, they still present excellent antioxidant activity, opening perspectives for its use to medicinal purpose. CA exerted a key role on the properties of spray-dried extracts, while IT did not present a significative influence. Aerosil® 200 proved to be an interesting alternative as an excipient for the...

  14. Validation of a UV spectrophotometric method for determining trans-dehydrocrotonin in inclusion complexes with hydroxypropyl-β-cyclodextrin

    Santos Magalhães, Nereide S.; Maciel, Maria A. M.; Lira, Mariane C. B.; Morais, Waldenice A.; Lapenda, Taciana L.S.
    Trans-dehydrocrotonin (t-DCTN) is a 19-nor-clerodan diterpen with several important pharmacological properties, including hypoglycemic and antitumor activity. However the low water solubility and hepatotoxicity of t-DCTN limit its use in therapeutic applications. Drug inclusion complexes with cyclodextrins (CDs) can modify physicochemical properties of parent drugs, such as improving their aqueous solubility and reducing their toxicity. A UV method was therefore validated for determining t-DCTN in HP-β-CD inclusion complexes with a view to future applications in research and therapy. The regression equation of the analytical curve (1–20 μg/mL) was [t-DCTN] = absorbance + 0.00147/0.04214. The precision of the method was satisfactory, producing...

  15. Comparison of impurity profiles of Lipiblock® vs. Orlistat using HPLC and LC-MS/MS

    Wagner, Vilegas; Severi, Juliana A.; Wessjohann, Ludger A.; Schneider, Alex
    Comparative HPLC-UV and LC-MS/MS studies of impurity profiles of a reference sample (Xenical®, F. Hoffmann-La Roche Ltd., Switzerland) vs. generic (Lipiblock®, EMS-Sigma Pharma, a generic drug) were carried out with ethanol extracts of commercial samples. The generic formulation contained higher levels of common impurities as well as a considerable number of impurities not found in the reference product. The detected impurity profile of Lipiblock® revealed that it most likely is based on fermentation. Since the effect of the impurities is unknown, at this point fully synthetic Xenical® appears to offer a better safety margin than Lipiblock® which, however, compares quite...

  16. Formulation design and evaluation of bioadhesive vaginal films of metronidazole for vaginal candidiasis

    Younus Pasha, Mohammed; Bhat, Sudeendra R.; Hani, Umme
    The purpose of this work was to design and evaluate a novel vaginal delivery system for the local treatment of vaginal candidiasis. Bioadhesive vaginal films of metronidazole that could be retained in the vagina for prolonged period for more effective treatment against vaginal candidiasis were formulated by solvent casting technique using bioadhesive polymers such as chitosan, HPC and sodium CMC. Glycerine and propylene glycol were used as plasticizer. The films were characterized for various physical, mechanical, and aesthetic properties. Bioadhesive strength and in vitro release studies suggested that the prolonged release bioadhesive vaginal film formulation of metronidazole is useful and...

  17. Study of drug release retardant capability of hydroxypropylmethylcellulose and carbopol in matrix tablets

    Hussain, Izhar; Azhar, Saira; Murtaza, Ghulam; Ullah, Majeed
    The present study was undertaken to investigate the effect of nature of polymers like HPMC, carbopol-934P and their content levels on the release profiles of water soluble drug, diclofenac potassium. For this purpose, different tablets were prepared by wet granulation technique using HPMC-K15, carbopol-934P and blends of HPMC with carbopol-934P. Release kinetics was evaluated using USP apparatus II at 50 rpm in phosphate buffer pH 6.8 for 12 h. HPMC showed less release retardant effect compared to carbopol-934P at same concentration, while blends of these polymers gave an intermediate release profile, i.e. decreasing the quantity of carbopol-934P while increasing the...

  18. Polyethylene glycol-phosphatidylethanolamine conjugate as a pulmonary nanocarrier for poorly soluble drug

    Tan, Yvonne T.F.; Abdulameer, Shaymaa A.; Peh, Kok K.; Darwis, Yusrida; Sahib, Mohanad N.
    The aim of this study was to investigate the potential of a polyethylene glycol-phosphatidylethanolamine conjugate (PEG2000 -DSPE) to solubilize budesonide (BUD) for pulmonary delivery. The BUD-strictly stabilized phospholipid nanomicelles (SSMs) were prepared using the coprecipitation and reconstitution method and the physicochemical characteristics and pharmacodynamic duration of the BUD-SSMs were determined. The solubility of BUD was highly improved by at least 52 times its intrinsic solubility. The hydrodynamic particle size and zeta potential were 14.31 ± 1.40 nm and -46.61 ± 2.94 mV, respectively. The in vitro release of BUD from SSMs was completed within 6 days. Aerosolization of rehydrated BUD-SSMs...

  19. Phytochemical profile and anti-Inflammatory effect of the orchid Catasetum macroglossum

    Consolini, Alicia; Spegazzini, Etile Dolores; Debenedetti, Silvia Laura; Rosella, María Adelaida; Colareda, Germán A.; Ramos, Pablo
    The pseudobulbs of Catasetum macroglossum (Orchidaceae) are popularly used as topical anti-inflammatory and antirheumatic in the forests and medium lands of Ecuador, but they were never studied. We evaluated whether the decoction of C. macroglossum has antiinflammatory effect and which is its phytochemical profile. The effect of 30 and 90 mg lyophilized/kg via i.p. was studied on the carrageenaninduced edema in the paw rat, in comparison with saline and indomethacin. The paw edema was inhibited in about 60 to 80 % after 1 to 3 h of carrageenan injection. The phytochemical profile was done by chemical tests to evaluate the...

  20. In vitro trypanocidal activity of nitroimidazole derivatives

    Ramos Ligonio, Ángel; López Monteon, Aracely; Carrera Huerta, Francisco; García Gálvez, Ana M.; Márquez López , Elizabeth; Sánchez Pavón, Esmeralda
    Chagas' disease, caused by the protozoan parasite Trypanosoma cruzi, affects 9-12 million of people in Latin America and it is an important cause of heart disease. Although transmission has been reduced, an effective therapy for the infected population is lacking. New isomers nitroimidazole derivatives [4(5)-bromo-1-phenacyl-5(4)-nitroimidazoles] were developed and their antichagasic properties were studied. Five compounds (with different substituents in their aromatic ring) displayed remarkable in vitro activities against T. cruzi. The results demonstrated that 4(5)-bromo-1-(4-methoxiphenacyl)-2-methyl-5(4)- nitroimidazole, 4(5)-bromo-1-(4-chlorophenacyl)-2-methyl-5(4)-nitroimidazole, and 4(5)-bromo-1-(4- cianophenacyl)-2-methyl-5(4)-nitroimidazole have IC50 values of of 3.95, 2.3, and 1.15 μg/mL, respectively, and show acceptable values of cytotoxicity, at concentrations below...

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