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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.
Tatiana A. Pa´dua,Bianca S. S. C. de Abreu,Thadeu E. M. M. Costa,Marcos J. Nakamura,Lı´gia M. M,Antonio C. Siani,Elaine C. Rosas 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.11
Ursolic acid (UA), a pentacyclic triterpene acidfound in apple peels (Malus domestica, Borkh, Rosaceae),has a large spectrum of pharmacological effects. However,the vegetal matrix usually produces highly viscous andpoorly soluble extracts that hamper the isolation of thiscompound. To overcome this problem, the crude EtOH–AcOEt extract of commercial apple peels was exhaustivelytreated with diazomethane, after which methyl ursolate(MU) was purified by column chromatography and characterizedspectrometrically. The anti-inflammatory effectsof UA and MU (50 mg/kg) were analyzed by zymosaninducedpaw edema, pleurisy and in an experimentalarthritis model. After 4 h of treatment with UA and MU,paw edema was reduced by 46 and 44 %, respectively. Both UA and MU inhibited protein extravasation into thethoracic cavity; tibio-femoral edema by 40 and 48 %,respectively; and leukocyte influx into the synovial cavityafter 6 h by 52 and 73 %, respectively. Additionally, bothUA and MU decreased the levels of mediators related tosynovial inflammation, such as KC/CXCL-1 levels by 95and 90 %, TNF-a levels by 76 and 71 %, and IL-1b levelsby 57 and 53 %, respectively. Both the compounds wereequally effective when assayed in different inflammatorymodels, including experimental arthritis. Hence, MU maybe considered to be a useful anti-inflammatory derivative toovercome the inherent poor solubility of UA for formulatingpharmaceutical products.