Recursos de colección

Universidad Nacional de La Plata (75.687 recursos)

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vol. 30, no. 09

Mostrando recursos 1 - 20 de 32

  1. Evaluation of the effect of drug solubility behaviour on the rate of release from the hydrophilic matrix system

    Eaga, Chandramohan; Nageswara Reddy, M.V.V.; Kumar Narla, Santosh
    To select the suitable concentration level of controlled release polymer for the formulation of predefined extended release formulation based on the solubility behaviour of active substance, we have formulated and evaluated the extended release matrix tablets of two different antihypertensive drugs having different solubility profile by direct compression process. The selected antihypertensive drugs are metoprolol succinate of freely soluble category and propranolol hydrochloride of soluble category (solubility in terms of water). The selected drugs were formulated with various concentrations of selected highest viscosity grades of controlled release polymers viz. HPMC K200M & Polyox WSR 303 and evaluated for drug release...

  2. Spectroscopic characterization of [Cu(L-Lysinato)2Cl2]·2H2O

    Torre, María H.; González Baró, Ana C.; Barán, Enrique José
    Copper compounds and, in particular, Cu(II) complexes show relevant pharmacological interest. Copper complexes of most of the simplest amino acids showed a particular relevance, appearing even useful for copper supplementation in human and veterinary medicine. In this contribution, the infrared and Raman spectra of the Cu(II) complex of L-lysine of composition [Cu(L-Lysinato)2Cl2]·2H2O were recorded and analyzed in relation to its structural peculiarities and by comparison with the spectra of L-lysine hydrochloride. The electronic spectrum of the complex is also briefly discussed.

  3. Terpinen-4-ol is overproduced in tissue cultures of Alpinia zerumbet (Pers.) Burtt et Smith by induction of methyl jasmonate

    Lge, Celso Luiz S.; Kuster, Ricardo M.; Cruz, Iacinete P. da; Victório, Cristiane P.
    Alpinia zerumbet (Zingiberaceae) presents a high medicinal value, in part by its production of volatile compounds. Organogenic in vitro cultures of A. zerumbet were treated with the elicitor methyl jasmonate (MeJA), a natural volatile signaling molecule in biotic and abiotic stress, and the effect was evaluated on the in vitro production of volatiles. Leaves of plantlets were subjected to simultaneous distillation-extraction (SDE), and sabinene, β-pinene, 1,8 cineole and terpinen-4-ol were the main volatiles detected. However, after exposure to a solution of of MeJA for 3 and 10 days, terpinen-4-ol showed a remarkable increase, corresponding to 18.01 and 14.75 %, respectively,...

  4. Reversible and time-dependent inhibition of CYP3A4-mediated nifedipine oxidation by noscapine

    Wang, Li-Ming; Yang, Ling; Li, Ming; Sun, De-Guang; Tang, Bo; Gao, Zhen-Ming; Liang, Rui; Qu, Yan-Qing; Fang, Zhong-Ze; Tang, Shu-Hong; Jin, Xue Li
    Substrate-dependent inhibition of CYP3A4 might influence the extrapolation of drug interactions from the in vitro to in vivo situation. The aim of the present study is to investigate reversible and time-dependent inhibition of CYP3A4-mediated nifedipine oxidation by noscapine. Furthermore, in vitroin vivo extrapolation (IVIVE) was performed using in vitro parameters. The results showed that CYP3A4- mediated nifedipine oxidation activity was strongly inhibited with an IC50 of 25.7 ± 5.4 μM. Kinetic analysis showed that inhibition of CYP3A4-mediated nifedipine oxidation by noscapine was best fit to a noncompetitive manner with Ki value of 10.9 μM. IC50 shift experiment showed that IC50...

  5. Determination of ketamine in rabbit plasma by gradient elution liquid chromatography/electrospray mass spectrometry

    Hu, Lufeng; Wang, Xianqin; Wang, Xuebao; Zeng, Ming; Ma, Jianshe; Li, Wei
    A sensitive and simple liquid chromatography/electrospray mass spectrometry (LC-ESI-MS) method for determination of ketamine in rabbit plasma using one-step protein precipitation was developed and validated. After addition of methadone as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation. Chromatographically separation was achieved on an SB-C18 (2.1 mm × 50 mm, 3.5 μm) column with methanol-0.1 % formic acid as the mobile phase with gradient elution. Electrospray ionization (ESI) source was applied and operated in positive ion mode; multiple reaction monitoring (MRM) mode was used to quantification using target fragment ions m/z 237.7 → 219.7 for ketamine...

  6. Essential oil composition and antioxidant and antimicrobial properties of Campomanesia pubescens O. Berg, Native of Brazilian Cerrado

    Martins, Carlos H. G.; Cunha, Wilson; Rocha, Edmilson de O.; Cunha, Luís C.S.; Nascimento, Evandro A. do; Morais, Sérgio A.L. de; Chang, Roberto; Aquino, Francisco J. T. de; Souza, Maria G. M.
    In this study, the essential oil composition, total contents of phenolics and proanthocyanidins, antioxidant and antimicrobial activities from different plant parts (root, stem, leaf and fruit) of Campomanesia pubescens (DC) O. Berg from Brazilian Cerrado are reported. The root essential oil is distinguished from others by having only one representative of monoterpenes (alpha-terpenylacetate). The aerial parts of C. pubescens are rich in volatile terpenes, as expected, especially in fruits whose essential oil contained approximately 80 % of monoterpenes. The essential oils showed antimicrobial activity against oral pathogens. The root essential oil showed the strongest inhibition against Fusobacterium nucleatum (ATCC 25586)....

  7. A new transdermal drug delivery system containing hydroquinone

    Caetano, Maria N. P.; Costa, Roseane M.R.; Alves, Taís V.G.; Deus, Dayse M.V. de; Bezerra, Simone S.; Santos Magalhães, Nereide S.
    Hydroquinone (HQ) is a drug reported to possess manifold biological activities. HQ is highly unstable into various topical vehicles, presenting low topical bioavailability and a relevant level of toxicity. The Pluronic® Lecithin Organogel (PLOme) is a phospholipidic microemulsion designed for transdermal purposes. The aim of this work was therefore to incorporate HQ into PLOme. We evaluated the stability, the kinetic profile and the antimicrobial activity of HQ- incorporated PLOme. No relevant pH variation was observed. Long-term stability test showed an HQ degradation which led to a short shelf life. HQ permeation rate obtained was lower from PLOme than from a...

  8. Formulation and evaluation of chitosan/chondriotin sulphate complex microcapsules for controlled delivery of water soluble drug

    Shivakumar, Hosakote G.; Singh, Mangla N.; Yadav, Hemant K.S.; Ram, Yaduvanshi M.
    Oral route of drug administration is the most preferred route of drug administration but this route has its own limitations like pH of gastric media and controlling release rate of water soluble drug. To overcome these limitations, formulations containing controlled release matrix need to be developed. Controlled release of drug can be achieved by incorporating the drug into a release rate controlling carriers. Chitosan (CH)/Chondroitin Sulphate (CS) complex microcapsules were prepared to encapsulate the cardio vascular drug Propranolol hydrochloride (PHCl) by emulsion-chemical crosslinking method using sodium tripolyphosphate (STPP) as cross-linking agent. The FT-IR and DSC spectra’s revealed that there is...

  9. Development and characterization of biodegradable chitosan nanoparticles loaded with lovastatin using factorial design

    More, Harinath N.; Shinde, Anilkumar J.
    The objective of the present work was to formulate chitosan nanoparticles as carriers for the lovastatin, since this drug undergoes extensive first pass extraction in the liver, and bioavailibity is low (< 5 %). Nanoparticles were prepared by modified ionotropic gelation method using 32 full factorial design. From the preliminary trials, the constraints for independent variables X1 (concentration of chitosan) and X2 (concentration of sodium tripolyphosphate) have been fixed and examined to investigate effect on particle size, encapsulation efficiency, zeta potential, % release, SEM, FTIR, XRD and DSC analysis of lovastatin. The diameter of prepared nanoparticles was controlled in the...

  10. Preparation and characterisation of controlled release ciprofloxacin HCl microspheres

    Bhat, Sudeendra R.; Roopa, G.
    The aim of the study was to formulate and evaluate controlled release microspheres. Ciprofloxacin HCl, belonging to the class of fluroquinolones, was chosen as the model drug. The drugloaded microspheres were prepared with different ratios of polymers like sodium alginate and sodium carboxy methyl cellulose (CMC) by w/o emulsification solvent evaporation method. The prepared microspheres were characterized by FT-IR spectroscopy, differential scanning colorimetry for drug polymer compatibility studies and scanning electron microscopy for surface morphology. The resulting microspheres were found to be small, discrete, spherical and free flowing. They were further evaluated for their micromeritic properties, particle size analysis, drug...

  11. Evaluation of drug interactions in prescriptions of a hospital specialized in cardiology

    Leal, Adriana A. F.; Simões, Mônica O. da S.; Ramos, Alessandra T.; Portela, Alyne da S.; Werner, Rossana P.B.; Queiroz, Hamon E.O.
    Simultaneous multiple prescription drugs increases the possibility of drug interactions, situation particularly critical in a hospital. The objective of the present work was to identify interactions by evaluating the originals of prescriptions archived from ward clinical of a hospital specializing in cardiology in the city of Campina Grande/PB, Brazil. The study had transversal, retrospective, and observational character with quantitative approach, and was held in the period from June to July 2010. A total of 196 prescriptions were analyzed and of these, 89.6 % had some type of interaction, and 28.0 % of prescriptions had at least one interaction. The most...

  12. A high performance liquid chromatography method for determination of hydroxyzine hydrochloride in syrup

    Ferreira, Anderson O.; Grossi, Lívia N.; Raposo, Nádia N. B.; Vaz, Urias P.; Montesano, Gabriela; Fonseca, Roberta G.; Polonini, Hudson C.; Nascimento, Luiz G.B.; Brandão, Marcos A. F.
    A simple isocratic method for quantification of hydroxyzine dihydrochloride by HPLC with UV detection at 232 nm in syrup has been developed and validated. Separation was achieved on a C18 column (250 x 4.6 mm, 5 μm) maintained at 90 ºC with 0.5 mol/L potassium dihydrogen phosphate buffer : acetonitrile (1:1, v/v) as mobile phase at a flow rate of 2.0 mL/min. The method was proven to be linear over the range of 80–120 μg/mL, accurate (recovery = 97.8 %), precise (coefficient of variation = 1.52 % for sample) and robust.

  13. Potential use of cellulose acetate butyrate and pluronic F68® blends in the modulation of the diclofenac sodium release from microspheres

    Medeiros, Daniela C. de; Soldi, Valdir; Poli, Anicleto; Lemos Senna, Elenara
    Microspheres were prepared using the emulsion/solvent evaporation method with the aim of obtaining diclofenac sodium (DFS) prolonged release dosage forms. The effects of the drug:polymer ratio and addition of Pluronic F68® to the formulations on drug content, particle size and DFS release rate were evaluated using a 22 factorial design. The DFS encapsulation efficiency (%) and the drug content varied from 40 to 70 % and from 4.5 to 13 mg/100 mg, respectively. The mean particle diameter varied from 720 to 850 μm. The addition of Pluronic F68® to the formulations led to an increase in the roughness of the...

  14. Taste masked orodispersible tablet of atomoxetine hydrochloride

    Huda, Inderjeet S.G.; Toshniwal, Sanjay S.
    In the present work, orodispersible tablets of atomoxetine HCl were designed by preparing tasteless complexes of atomoxetine HCl with weak cation ion exchange resins (Kyron T 134). The ion exchange complex were prepared by the batch process using activated Kyron T 134 with a drug: resin ratios 1:1, 1:2, 1:3 and 1:4 (% w/w). IR analysis, assay content and decomplexation studies confirmed complex formation. It was found that maximum complexation of drug with resin was noted between pH range 5-7, while activation of ion exchange resin affects the percent drug loading. Drug release from drug: resin complex in salivary pH...

  15. Hepato- and nephro-protective as well as hypoglycemic effects of sea buckthorn berries (Hippophae rhamnoides L.) in rabbits and humans

    Chaman, Saadia; Syed, Nawazish-i-Husain; Danish, Zeeshan; Ahmad, Mobasher; Khan, Farrakh Zia
    The hepato- and nephro-protective effects of sea buckthorn berries (Hippophae rhamnoides L) were investigated in paracetamol-induced toxicity in animals and hypoglycemic effects in type II diabetic patients. Crude drug preparation and its methanol extract have shown a profound decrease in paracetamol-induced elevated serum levels of liver and kidney functions under investigation, which suggests a possible therapeutic role of its constituents in hepatic injury and altered kidney functions. Similarly, in human patients with raised glucose levels, sea buckthorn shows hypoglycemic effect which could likely make it a potential therapeutic agent to mange type II diabetes mellitus. However, further investigations are required...

  16. Determination of sulpiride in rabbit plasma by LC-ESI-MS and its application to a pharmacokinetic study

    Lin, Guanyang; Wu, Haiya; Wang, Zhibin; Zhang, Haiyang; Chien, Lianguo; Wang, Xianqin; Hu Lufeng; Ma, Jianshe
    A sensitive and selective liquid chromatography-mass spectrometry (LC-MS) method for determination of sulpiride in rabbit plasma was developed and validated. The analyte and internal standard (IS) were extracted from plasma by liquid-liquid extraction using ethyl acetate, and chromatography involved Agilent Extend-C18 column (2.1 mm x 50 mm, 3.5 μm) using 0.2 % formic acid in water and acetonitrile (60: 40, v/v) as a mobile phase. Detection involved positive ion mode electrospray ionization (ESI), and selective ion monitoring (SIM) mode was used for quantification of target fragmentions m/z 342.0 for sulpiride and m/z 294.8 for estazolam (internal standard, IS). The assay...

  17. Physical characterization and in vitro evaluation of some generic medications available in pharma market of United Arab Emirates (UAE)

    Abdul Rasool, Bazigha K.; Khan, Saeed A.; Shamsueldin, Eiman; Sadik, Raghad
    This study is the first attempt in UAE to prove the trustworthiness of the in vitro evaluation to assess the reliability of the generic medications comparing to the brand name. Five generic medicines, two Local (codes: L1, L2), three Arabic (codes: A1, A2 and A3) and the International brand (code: I1) of diclofenac sodium (DS) sustained release tablets, as a model product, was collected randomly from the UAE pharma market. The products were characterized by physical parameters including weight variation, thickness, friability, hardness and moisture content. The in vitro release study was conducted in simulated gastric medium (0.1 N HCl,...

  18. Formulation and evaluation of gliclazide loaded controlled release microspheres

    Dey, Sanjay; Mohanta, Bibhash C.; Das Gupta, Sandipan; Mazumder, Bhaskar
    The aim of this study was to formulate gliclazide loaded controlled release microspheres. Microspheres were prepared by quasi emulsion solvent diffusion technique using eudragit RLPO, eudragit RSPO and with their various combinations. The effect of different formulation variables (drug-polymer ratio and polymer-polymer ratio) on percent yield, mean particle size, encapsulation efficiency and in vitro release of drug were evaluated. In vivo test of the optimized formulation was performed on streptozotocin induced type-2 diabetic rat model. The formulated microspheres showed higher encapsulation efficiencies within the range of 72-84 %. Mean particle size, encapsulation efficiency and in vitro release were found to...

  19. Obtaining microcapsules with albumin with programmed properties

    Dolinska, Barbara; Galczynska-Pawlik, Anna; Ostrózka-Cieslik, Aneta; Pluta, Janusz; Rosak, Beata; Ryszka, Florian
    The aim of this study was: a) the determination of the relation between composition of mixture for microencapsulation (gelatin concentration 5, 10, and 15 %; sodium alginate 2, 4, and 6 %; acetic acid 15, 20, and 30 %) and the efficiency of the obtained microcapsules, b) the degree of human serum albumin (HSA) incorporation, and c) the release time of HSA from microcapsules. Existing relations was described by multiple regression equations on the basis of which it can be obtained HSA gelatin-alginate micocapsules with specified release time and with specified efficiency and degree of protein incorporation. The aim was...

  20. Evaluation of the pharmacotherapeutic profile of HIV/AIDS bearers

    Bessa Filho, Valter; Bezerra, Everton R.; Ferreira, Aluísio M.; Janebro, Daniele I.; Queiroz, Maria do S.R.; Monteiro, Matheus M. de O.; Santana, Jorge E.G.; Vicente, Carlos H.T.B.
    In this work was evaluated the pharmacotherapeutic profile of HIV/AIDS bearers registered in the Service of Specialized Attendance located in Campina Grande–PB, Brazil. The research was of the type traverse, documental, descriptive and analytical and was realized in the period of August to October 2010. Were appraised the patient records of 188 people being 66 % males and 34% females. The most part (36 %) just studied the education fundamental level and presented age group between 40-49 years old. Antiretrovirals more prescribed were nucleoside reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse-transcriptase inhibitors (NNRTIs). Schemes no recommended by the Ministry of...

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