Efecto del raloxifeno (Modulador Selectivo del Receptor Estrogénico (SERM)) como coadyuvante del tratamiento antidepresivo. A propósito de un caso / Effect of raloxifene (a Selective Estrogen Receptor Modulator [SERM]) as coadjuvant to antidepressant treatment: A case report

Se presenta el caso de una paciente con un trastorno depresivo con respuesta parcial al tratamiento antidepresivo. A la paciente se le añadió raloxifeno, Modulador Selectivo del Receptor Estrogénico (SERM), y se consiguió una remisión completa del episodio depresivo que presentaba. El interés de nuestro caso radica en el hecho que ejemplifica la relación entre los trastornos depresivos y los cambios hormonales durante la menopausia. Además, el raloxifeno puede ser una nueva opción terapéutica en algunas mujeres en la postmenopausia que no responden o lo hacen de forma parcial a los ISRS, especialmente en aquellas con historia de trastornos depresivos relacionados con la menopausia (AU)

We report a case of a woman with a depressive disorder with partial response to antidepressant treatment. Raloxifene, a Selective Estrogen Receptor Modulator (SERM) was added to the treatment, the patient achieving complete remission of her depressive symptoms. The interest of our case lies in the fact that it exemplifies the relationship between depressive disorders and hormonal changes during menopause. Furthermore, raloxifene may become a novel therapeutic option in some postmenopausal women who do not respond or only partially respond to SSRIs, especially in those with a history of depressive disorders related to menopause (AU)

Bioadhesive microspheres for bioavailability enhancement of raloxifene hydrochloride: formulation and pharmacokinetic evaluation.

Raloxifene hydrochloride (R-HCl), a BCS class II drug, remains a mainstay in the prevention and pharmacologic therapy of osteoporosis. Its absolute bioavailability, however, is 2% due to poor solubility and extensive first pass metabolism. The present study describes two simultaneous approaches to improve its bioavailability, complexation of R-HCl with cyclodextrin(s), and formulation of mucoadhesive microspheres of the complex using different proportions of carbopol and HPMC. Microspheres were pale yellow in color, free-flowing, spherical, and porous in outline. The particle size ranged between 3 and 15 µm, and entrapment efficiency was found to be within 81.63% to 87.73%. A significant improvement in the solubility of R-HCl was observed, and it differed with the combination of excipients used. X-ray diffraction and differential scanning calorimetry studies revealed that enhancement in drug solubility was resulted due to a change in its crystallinity within the formulation. Microspheres possessed remarkable mucoadhesion and offered controlled drug release, lasting up to 24 h. They produced a sharp plasma concentration-time profile of R-HCl within 30 min post-administration to Wistar rats. [AUC](0-24 h) was found to be 1,722.34 ng h/ml, and it differed significantly to that of pure drug powder (318.28 ng h/ml). More than fivefold increase in AUC and more than twofold increase in MRT were observed. FT-IR studies evidenced no interaction among drug and excipients. The results of this study showed that mucoadhesive microspheres could be a viable approach to improve the pharmacokinetic profile of R-HCl.

Development and validation of a quantitative assay for raloxifene by capillary electrophoresis.

The migration behavior of raloxifene was investigated by capillary electrophoresis (CE). The influence of different parameters (nature and concentration of the running buffer, pH and applied voltage) on migration time, peak symmetry and efficiency was systematically investigated. A buffer consisting of 20mM acetate buffer of pH 4.5 was found to provide a very efficient and stable electrophoretic system for the analysis of raloxifene. The optimized method was validated with respect to precision, linearity, limits of detection and quantification, accuracy and robustness. The applicability of the assay was demonstrated by analyzing this drug in human plasma and pharmaceutical preparations.