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Aguiar F.A.,University of Sao Paulo | Do Carmo Malvar D.,University of Sao Paulo | Kanashiro A.,University of Sao Paulo | Seoane M.F.,Subsecretaria CEPROCOR | And 3 more authors.
Journal of Liquid Chromatography and Related Technologies | Year: 2012

Diclofenac sodium (DS) is a non-steroidal anti-inflammatory drug that is widely prescribed for the treatment of rheumatoid arthritis and post-surgery analgesia. The active pharmaceutical ingredient is the anhydrous form; however, it can also exist in hydrate form. In this context, knowing the properties of the solid state is important and relevant in the pharmaceutical area because they have a significant impact on the solubility, bioavailability, and chemical stability of the drugs. In the present study, data from XRPD, FTIR spectroscopy, and thermal analysis were used for the identification and characterization of DS forms (anhydrous and hydrate). An HPLC method was optimized to evaluate the plasma concentration of DS in rabbits. The optimized method exhibited good linearity over the range 0.1-60μg/mL with correlation coefficients of >0.9991. The mean recovery was 100%. Precision and accuracy were determined within acceptable limits. Finally, to compare the pharmacological properties of anhydrous and hydrate DS forms, we investigated their effects in the febrile response induced by lipopolysaccharide from E. coli in rabbits. The results show that the antipyretic effect of anhydrous and hydrate DS forms are similar. © 2012 Copyright Taylor and Francis Group, LLC.


Bordon D.L.,National University of Cordoba | Villalba L.D.,Subsecretaria CEPROCOR | Aimar M.L.,National University of Cordoba | Cantero J.J.,National University of Rio Cuarto | And 4 more authors.
Biocatalysis and Agricultural Biotechnology | Year: 2015

This paper describes the search for novel vegetal biocatalysts for the stereoselective reduction of prochiral phenylketones. In this study, twenty native weeds were tested and Eryngium horridum Malme (Apiaceae) was proven to be an effective biocatalyst for the stereoselective reduction of acetophenone to (S)-1-phenylethanol (96% conversion, >99.9 e.e.%). Using this biocatalyst, fourteen chiral (S)-phenylethanols with excellent enantiomeric excesses (>98%) and variable conversions (30-100%) were obtained. © 2015 Elsevier Ltd.


Salvano M.S.,Subsecretaria CEPROCOR | Cantero J.J.,National University of Rio Cuarto | Vazquez A.M.,Catholic University of Cordoba | Formica S.M.,National University of Cordoba | Aimar M.L.,National University of Cordoba
Journal of Molecular Catalysis B: Enzymatic | Year: 2011

A screening for the capacity of wild plants growing in the Province of Córdoba to bioreduce benzaldehyde was carried out. From this study, thirteen species showed quantitative reduction yields to benzyl alcohol, with Conium maculatum showing the best reduction efficiency. This plant was also tested against different substituted benzaldehydes, and quantitative yields of substituted benzylic alcohols were obtained, except for vanillin, where only 27% of vanillic alcohol was formed (main product: 2-methoxyphenol at a 73% yield). A scaling study of the reaction using C. maculatum and benzaldehyde was carried out, and it was observed that high substrate-catalyst relationships reduced the efficiency of the reaction due to side reactions of oxidation. The bioreduction method presented here permits substituted benzylic alcohols to be obtained using an environmentally friendly methodology, with excellent yields produced on a laboratory scale. © 2011 Elsevier B.V. All rights reserved.


Rodriguez P.E.A.,Subsecretaria CEPROCOR | Sanchez M.S.,Subsecretaria CEPROCOR | Sanchez M.S.,CONICET
Journal of Toxicology and Environmental Health - Part A: Current Issues | Year: 2010

Although the effects of triclosan have been examined in male reproductive functions, it is unknown whether this potent antibacterial agent affects pregnancy and female pubertal development. Effects of maternal exposure to triclosan on thyroid homeostasis (TH) and reproductive-tract development in female Wistar rats were thus studied. Dams were exposed daily to triclosan (0, 1, 10, or 50 mg/kg/d) from 8 d before mating to lactation day 21. Offspring were also exposed after weaning. In vivo triclosan estrogenic activity was screened by uterotrophic assay and vaginal opening (VO), with first estrus and uterus and ovarian weight determined in offspring. Dam blood samples were taken during pregnancy and lactation to examine the effect of triclosan on TH. No apparent external signs of toxicity or differences in mean numbers of implantation sites were observed in treated rats. Triclosan treatment decreased total serum T 4 and T3 in pregnant rats and also lowered sex ratio, lowered pup body weights on postnatal day (PND) 20, and delayed VO in offspring. In addition, the highest dose of triclosan significantly reduced the live birth index (percentage) and 6-d survival index. Data indicate that triclosan impairs thyroid homeostasis and reproductive toxicity in adult rats and produces fetal toxicity in offspring exposed in utero, during lactation, and after weaning. Copyright © Taylor & Francis Group, LLC.


Limandri S.,National University of Cordoba | Visnovezky C.,National University of Cordoba | Perez S.C.,National University of Cordoba | Schurrer C.A.,National University of Cordoba | And 6 more authors.
Analytical Chemistry | Year: 2011

Pharmaceuticals can exist in many solid forms, which can have different physical and chemical properties. These solid forms include polymorphs, solvates, amorphous, and hydrates. Particularly, hydration process can be quite common since pharmaceutical solids can be in contact with water during manufacturing process and can also be exposed to water during storage. In the present work, it is proved that NQR technique is capable of detecting different hydrated forms not only in the pure raw material but also in the final product (tablets), being in this way a useful technique for quality control. This technique was also used to study the dehydration process from pentahydrate to trihydrate. © 2011 American Chemical Society.

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