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de Marco Bianca A,Maggio Rubén M.,Nunes Salgado Hérida R. 한국약제학회 2020 Journal of Pharmaceutical Investigation Vol.50 No.4
Purpose The presence of different polymorphic or pseudo-polymorphic forms in active pharmaceutical ingredients may affect the performance of the formulated products. Pseudo-polymorphs, especially hydrates, present a differential dissolution rate. In such a scenario, pseudo-polymorphism should be strictly controlled due to its impact on the bio-availability of formulates products. Methods In order to determine solid forms of cefadroxil present in commercial capsules, anhydrous and monohydrate pure the solid forms were prepared and fully characterized by optical microscopy, vibrational spectroscopy (middle and near infrared), calorimetric techniques (differential scanning calorimetry and thermogravimetry). Nuclear magnetic resonance was used to corroborate structural integrity. Two sets of synthetic samples for calibration (N = 12) and validation (N = 12) were prepared following a binary-mixtures design of monohydrate/anhydrous cefadroxil in the presence of the excipient matrix. NIR spectra were acquired and used as input of partial least squares (PLS) model. Results Three PLS-factors, mean scattering correction and MIN–MAX normalization demonstrated to be the optimal parameters on full range spectra (750–2500 nm). The method was validated for linearity/range, accuracy and precision by evaluation of validation set recovery. Once method validated, a commercial lot of capsules was analyzed and acceptable recovery results and low deviations were obtained. Conclusion Near infrared spectroscopy (NIR) emerged as the technique of choice to determine pseudopolymorphic-purity. Cefadroxil monohydrate was determined in a fast and accurate way in presentence of cefadroxil anhydrous and excipients by NIR–PLS methodology. The developed analytical methodology, arise as a general strategy for hydrates determination, making a direct determination of pseudopolymorphic form.
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Antidiarrheal Activity of Campomanesia xanthocarpa Fruit
Tatiana M. Souza-Moreira,Luiz Estêvão Salvagnini,Emerson Santos,Viviana Y.A. Silva,Raquel R.D. Moreira,Hérida R.N. Salgado,Rosemeire C.L.R. Pietro 한국식품영양과학회 2011 Journal of medicinal food Vol.14 No.5
The growing list of drug-resistant microorganisms and the persistence of deaths due to diarrhea are compelling reasons to study plants in search of new therapeutic agents. The chemical constitution and popular use of the edible fruits of Campomanesia xanthocarpa O. Berg motivated this study to assess the antimicrobial and antidiarrheal properties of the fruits. An extract in 70% ethanol was prepared, and its antimicrobial activity was tested against several strains of bacteria by the agar diffusion and microdilution methods. Antidiarrheal activity was analyzed by testing intestinal motility in an animal model. Preliminary phytochemical study indicated the presence of flavonoids, saponins, and tannins in the hydroalcoholic extract. Antimicrobial activity was significant, but the minimum inhibitory concentration proved to be higher than the maximum extract concentration tested. The extract did not show significant activity for intestinal motility. Although this fruit extract did not show great results as an antimicrobial or antidiarrheal agent, the study contributes to the search for new plant agents and could be referred to as a research protocol by investigators in this area.
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