Inclusion complexes of ß-cyclodextrin and polymorphs of mebendazole: Physicochemical characterization.

Mebendazole (MBZ), designated as a WHO essential drug, can exist in diverse solid forms and presents low absorption at the gastrointestinal level. Considering the potential of cyclodextrins to enhance the solubility and permeability of drugs, inclusion complexes of polymorphs A and C of MBZ with ß­cyclodextrin were obtained. The characterization of the complexes in solid state was performed by using a combination of experimental techniques including Fourier transform infrared spectroscopy, powder X-ray diffractometry and solid state nuclear magnetic resonance. Moreover, the effect of the binary complexes on their physical stability was evaluated. In addition, for a complete characterization of polymorphs A and C, one dimensional spectra and correlation nuclear magnetic resonance experiments were employed. Our physical studies showed that the inclusion complexes were new crystalline forms that induced shifts and broadening in the infrared and nuclear spectra. A molecular modelling analysis performed on the inclusion modes, demonstrated that the most favourable structure for the complex was the head down orientation. Moreover, the intermolecular interactions calculated for the complex with the atoms in molecules theory are in good agreement with the spectroscopic results. The inclusion complexes exhibited an increment of solubility in simulated physiological media. Furthermore, it was demonstrated that the complex formation did not affect the physical stability of the polymorphs.

Caracterización por HPLC y FTIR de los extractos acuosos de tres especies diuréticas del centro-oeste argentino / Characterization by HPLC and FTIR of the aqueous extracts of three diuretic species from the Argentine center-west

Euphorbia serpens Kunth var. microphylla Müll. Arg. (Euphorbiaceae), Amaranthus muricatus (Moq.) Hieron. (Amaranthaceae) y Lithraea molleoides (Vell.) Engl. (Anacardiaceae) son plantas usadas tradicionalmente en el Cono Sur de América como diuréticas. Las dos primeras son hierbas denominadas vulgarmente "yerbas meonas", mientras que la última, un árbol perennifolio, es conocido como "molle de beber" o "molle dulce". El objeto de este trabajo es caracterizar los extractos acuosos de estas drogas vegetales, identificando y cuantificando manitol por HPLC, debido a que este alcohol sería el principal responsable de la actividad diurética que han mostrado las tres plantas. Se realizó además, la caracterización fisicoquímica de las especies vegetales por comparación de los espectros de FT-IR. Los cromatogramas obtenidos por HPLC muestran picos con tiempos de retención a 35,44 min (estándar) característicos para manitol, y el área por debajo de las respectivas curvas permitió establecer concentraciones respecto a materia seca entre 23,056 g Kg-1 en E. serpens var. microphylla; 4,638 g Kg-1 en L. molleoides; y 2,080 g Kg-1 en A. muricatus. Estas cifras explican las diferencias en la potencia diurética descripta en la bibliografía para las especies en estudio. Los espectros IR presentan una relación de áreas de las bandas CO/CH que resultó distintiva para las dos especies (8,42 para E. serpens var. microphylla; 9,28 para A. muricatus; y 11,18 para L. molleoides). El valor mayor correspondiente a L. molleoides indica mayor cantidad de compuestos oxigenados. Los datos espectrales obtenidos permiten contribuir a la caracterización de los extractos acuosos de estas especies y aportan datos para un control de calidad efectivo de las drogas vegetales y los medicamentos herbarios que los contengan en su formulación. (AU)

Green method based on a flow-batch analyzer system for the simultaneous determination of ciprofloxacin and dexamethasone in pharmaceuticals using a chemometric approach.

A green FBA method with UV detection was developed for simultaneous determination of ciprofloxacin (CIP) and dexamethasone (DEX) in ophthalmic and otic preparations. A lab-made mixing detection chamber (MDC) was designed and coupled to the spectrophotometer in order to perform the mixing of solutions and the detection in the same receptacle. Only water was used as solvent and no previous separation of the components was required. Both analytes have a strong absorption between 190 and 370 nm in aqueous medium, at pH 7. However, the spectrum of DEX is embedded in the CIP spectrum. Thus, while CIP was analyzed using univariate calibration, DEX analysis was carried out comparing partial least squares (PLS-1) and multiple linear regression (MLR). The latest required a previous variable selection step, which was performed using the genetic algorithm (GA) and the successive projections algorithm (SPA). The FBA system made it possible to automatically prepare the calibration and validation sets. The statistical parameters, in terms of relative errors of calibration and prediction, were acceptable for the determination of both CIP and DEX. Also, a comparative study of chemometric models was carried out. Commercial samples were analyzed and the obtained results are in close agreement with HPLC pharmacopeia methods. The joint interval test for the slope and the intercept was used to test for the presence of bias. There were no statistical differences between the proposed method and the reference method (α=0.05). The sample throughput was 10h(-1). The combination of automation and chemometric tools allows us to develop an environmental friendly method for the quality control of CIP and DEX in pharmaceuticals.

Larrea divaricata Cav (Jarilla): production of superoxide anion, hydrogen peroxide and expression of zymosan receptors.

Larrea divaricata is a plant widely used in folk medicine in Argentina. This work aimed to study the mechanisms of decoction activity on the release of oxygen reactive species. Decoction increased the binding of zymosan-FITC and superoxide production. Cadmium decreased the superoxide production as well as malonate and barbital. Decoction decreased the release of hydrogen peroxide. Decoction increased the reduction of MTT but not when malonate and barbital were included. Together, decoction increased the expression of dectin-1 leading to increased superoxide production. It is possible that decoction increases the activity of peroxidase, and decreases the Cu, Zn-superoxide dismutase.