Search

The aim of this study is to determine the impact caused by direct compression on the crystalline state of two prototypes of Rupatadine fumarate 10 mg tablets. The tablets were manufactured through direct compression. Five grams powdered tablets samples were taken randomly for analysis through DSC, TGA and XRD. The results were analyzed by making a comparison between their crystalline characterization and the one shown by the active pharmaceutical ingredient, excipients, the placebo and the powdered formula before compression. The active pharmaceutical ingredient showed a melting point at 201.38 °C, which decreased 2 – 3 °C in the tablets’ thermograms. Placebos presented an endotherm at 228 °C characteristic of amorphous lactose’s melting point. The only thermal change presented between the tablets and the other samples is the crystallization of amorphous lactose around 172 – 176 °C. X-ray diffractograms showed an increased intensity for the peaks of α - lactose monohydrate after compression and no changes regarding the active pharmaceutical ingredient. The comparison done between the analyses, confirmed that compression didn’t impact the crystalline state of Rupatadine fumarate. However mechanical treatment and the influence of the excipients caused the fusion peak to shift towards lower temperatures. Lactose’s crystal lattice suffered the greatest impact caused by compression, which generated the crystallization of the amorphous region present in that raw material. Nevertheless, such modification doesn’t alter the prototypes’ aptitude for being developed into a final solid pharmaceutical form and it is not a situation that affects the product’s quality. UCR::Vicerrectoría de Investigación::Unidades de Investigación::Ciencias de la Salud::Instituto de Investigaciones Farmacéuticas (INIFAR)

Bactris gasipaes es una palmera de la cual se obtiene una fruta conocida comúnmente en Costa Rica como Pejibaye, es autóctona de América Central, muy común en la alimentación de Costa Rica, por su alto contenido de almidón en su fruto. La semilla es un producto de desecho industrial. El presente estudio busca caracterizar la composición de la misma para analizar sus aplicaciones farmacéuticas. UCR::Vicerrectoría de Investigación::Unidades de Investigación::Ciencias de la Salud::Instituto de Investigaciones Farmacéuticas (INIFAR)

The Bactris gasipaes is a native palm from Central America which its fruit is known as pejibaye, its wood is also used for the manufacture of various utensils, the marrow of its tender stems is edible and it is called palmetto, it is used in the preparation of salads and other dishes. The pejibaye is cultivated in Costa Rica and part of the diet, this due to its high content of starch and mainly by content of antioxidant substances. The objective of the present study is to identify the main phytochemical groups and quantify the main markers in order to associate them with cosmetic or medicinal functions in pharmaceutical products. Materials and Methods: The mature fruits of Bactris gasipaes were peeled and separated the seeds of the mesocarp, were dried, milled and subdivisions were made with low, medium and high polarity solvents, then a phytochemical screening was carried out according to the Guidelines for the Quality Control of Products of Natural Origin of the World Health Organization, additionally the antioxidant properties were evaluated, the concentration of total phenols, total carotenoids content, the content and type of saturated and unsaturated fatty acids and the physicochemical properties of the aqueous extract were determined. The study found a low concentration of phenolic compounds such as condensed and non-condensed tannins and the main phytochemical groups such as: carotenoids, terpenes, fats, carbohydrates and alkaloids and the absence of Anthocyanins. The antioxidant power that was 45.56 ± 1.96 g/mol Trolox Eq/g dry fruit, an EC 50 0.293 mg/Lfor the mesocarp oil, the total phenols found are 0.628 ± 0.12 mg/Gof dry sample (equivalents of Gallic acid), which shows that the main antioxidant components are lipophilic, so they can be useful in formulations such as emollients, anti-aging effect, anti-wrinkle, nourishing and moisturizing for the skin, and as a sunscreen. The mesocarp oil contains unsaturated fats (78.6% ± 1.2 µg/g): oleic, linoleic and Palmitoleic and Palmitic acid, respectively 58.3 ± 1.8, 14.5 ± 1.2, 4.5 ± 0.3 and 20.8 ± 1.4 µg/g. The acidity index is 4.32 ± 0.10 which is beneficial to maintain the cutaneous acid mantle and thus favor the normal flora of the skin, although this property represents a challenge in the formulation of Carbomer-based gels. The aqueous extract is hyperosmotic, 2333 ± 9.54 mOs/kg, and has a high electrical conductivity (1492 ± 5.56 S/cm) due to the presence of polyelectrolytes and a high concentration of reducing sugars according to the obtained brix degrees (13.45 ± 0.01), finally mesocarp oil at 0.1% w/w shows an absorption of ultraviolet radiation of 25% at wavelengths between 260 nm and 400 nm, which could also be useful for formulating compositions for sun protection UCR::Vicerrectoría de Investigación::Unidades de Investigación::Ciencias de la Salud::Instituto de Investigaciones Farmacéuticas (INIFAR)

Polymorphism analysis of pharmaceutical raw materials is considered one of the most relevant evaluations that should be done. As we know, different crystal forms from the same molecule have differences in terms of their physicochemical properties. According to the crystal form used, researchers can obtain benefits for the development of a new product or it can also imply a disadvantage for the formulation of the product. The present study focuses on the identification of crystalline forms in Rupatadine Fumarate raw material samples. The active pharmaceutical ingredient is an antihistaminic, classified as a second-generation selective H1 receptor, which shows advantages in terms of solubility in contrast with the free base and the trichloride form. Analytical techniques employed were: X ray diffraction, differential scanning calorimetry, thermogravimetric analysis, and infrared spectroscopy. The results were analyzed all together and compared with the information found in literature. Based on the results obtained, it was demonstrated that the analyzed drug samples don´t present any other polymorphic form besides A form, which is the only one reported in literature. UCR::Vicerrectoría de Investigación::Unidades de Investigación::Ciencias de la Salud::Instituto de Investigaciones Farmacéuticas (INIFAR)

There are more than 700 species of the genus Rubus, popularly known as Mora (tropical highland blackberry). In Costa Rica, the species Rubus adenotrichus has been characterized by its high content of antioxidant substances, becoming one of the most cultivated species and that may have characteristics to be used in cosmetics or medicine. The objective of the present study is to identify the main phytochemical groups and to quantify the main markers in order to associate them with cosmetic or medicinal functions in pharmaceutical products. Ripe fruits of Rubus adenotrichius were fractionated with solvents of low, medium and high polarity, followed by a phytochemical screening according to the World Health Organization Guidelines for the Control of Quality of Products of Natural Origin. The antioxidant properties were evaluated by means of the H-ORAC and DPPH test; the concentration of total phenols by Folin-Ciocalteau and antocinanins by differential pH was determined. Finally, the physicochemical properties of the aqueous extract, such as pH, specific gravity, Brix grades, conductivity, and osmolarity was determined and an absorption spectrum from 260 to 700 nm was obtained. Phenolic compounds were found as condensed and non-condensed tannins, anthocyanins, flavonoids, terpenes, and alkaloids as major phytochemical groups, a high antioxidant power measured in H-ORAC 311 ± 7.63 μg/mol Trolox Equivalent/g of dry fruit, and EC 50 118.46 mg/L for the aqueous extract. The total phenols found was 20.85 ± 0.27 mg/g of dry sample of gallic acid equivalents which makes the Rubus adenotrichus fruit an excellent component for bacteriostatic, anti-aging, anti-wrinkle, nourishing and moisturizing formulations, and the astringent effect also allows its application to small superficial wounds on the skin. Likewise, the acidic pH of 3.55 ± 0.1 is beneficial for maintaining the cutaneous acid mantle thereby favoring the normal flora of the skin, but may be a problem for the formulation of carbomer-based gels or the incorporation of preservatives. The aqueous extract is hyperosmotic (559.66 ± 3.21 mOs/kg) and has a high electrical conductivity (285 ± 2 μS/cm) due to the presence of electrolytes and a considerable amount of sugars, according to Brix degrees (7.543° ± 0.005°). Finally, the 4% w/w aqueous extract shows an absorption of ultraviolet radiation of 25% in the wavelengths from 260 to 400nm, by which it also could be useful for formulating compositions for sun protection. UCR::Vicerrectoría de Investigación::Unidades de Investigación::Ciencias de la Salud::Instituto de Investigaciones Farmacéuticas (INIFAR)

The determination of the spatial configuration of the compounds structures used in the production of drugs is of utmost importance due to the different physical characteristics that each have in their solid state and therefore the different qualities of each one for its use as pharmaceutical raw material. This study aimed to identify the polymorphic crystalline form of Etoricoxib raw material, a non-steroidal anti-inflammatory drug (NSAIDs) selective inhibitor of cyclooxygenase 2 (COX2) enzyme widely used in the present, which was done through four different instrumental analytical techniques: X-ray diffractometry, differential scanning calorimetry, thermogravimetry and infrared spectroscopy, comparing and studying the results obtained from the analysis with those found in the literature. Using the data obtained with these four techniques it was demonstrated that the study sample exists predominantly in the 1 anhydrous Etoricoxib form. UCR::Vicerrectoría de Investigación::Unidades de Investigación::Ciencias de la Salud::Instituto de Investigaciones Farmacéuticas (INIFAR) UCR::Vicerrectoría de Docencia::Salud::Facultad de Farmacia

The method was validated by ultraviolet spectrophotometry for the determination of levofloxacin 500 mg tablets using dissolution profiles to establish therapeutic equivalence. The parameters were satisfactory according to accuracy and precision in a linear range between 2,0 μg/mL and 8.0μg/mL. Both, the relative error and relative standard deviation were less than 2%, the recovery was on average of 98,5%, the quantification limit (QL) obtained was 0,47 μg/mL. The effect of filters Varian ® Full FlowTM of 70 microns used in the dissolution equipment autosampler Varian ® 7010 and the effect of light were evaluated. For the effect of the filter, three concentrations levels were evaluated (3, 5, 7 μg/mL); no change in the recovery were observed applying a T-test (both sides, 95% limit of confidence). The effect of light was explored exposing levofloxacin standard’s to natural and artificial light for 0, 6, 24, 48, 62 and 86 hours. We find that after 24 hours the response have significance’s changes. With a both-sides, 95 % limit confidence ANOVA, the homocedasticity (Leven’s test) and normality test (Shapiro-Wilk) were checked. In conclude the developed method can be used to determine levofloxacine in tablets for profile dissolution, and the filter used does not affect, but light effect is important, and samples must not be handle for more than 24 hours. UCR::Vicerrectoría de Investigación::Unidades de Investigación::Ciencias de la Salud::Instituto de Investigaciones Farmacéuticas (INIFAR) UCR::Vicerrectoría de Docencia::Salud::Facultad de Farmacia

Determining the spatial configuration of the structures of compounds used in the production of medicines is extremely important due to the different characteristics of each of them in its solid state and therefore its different qualities of each for use as pharmaceutical raw material. This study aimed to identify the phase of the solid state of Atorvastatin hemi-dihydrate, a lipid-lowering medication HMG-CoA reductase widely use in the present and their characterization by four different instrumental analytical techniques: X-ray diffractometry, differential scanning calorimetry, thermogravimetry and infrared spectroscopy, comparing the obtained analytical results with those found in the literature. Using data obtained from these four techniques are able to show that the study sample exists predominantly in the 27 form of amorphic hemi-dihydrate calcic atorvastatin. Universidad de Costa Rica/[]/UCR/Costa Rica UCR::Vicerrectoría de Investigación::Unidades de Investigación::Ciencias de la Salud::Instituto de Investigaciones Farmacéuticas (INIFAR)

Introduction: Since 2009 the University of Costa Rica, through the Faculty of Pharmacy, is dedicated to promote a model of development in cosmetics in small and medium industries in rural or poorest areas of Costa Rica, in which female heads of household are leading the company,. aA successful example of this model is microenterprise Biosphere, located in the province of Alajuela, canton of San Carlos, District Fortune, which produces cosmetics based on hot springs and peloids obtained in the surroundings of the Arenal Volcano, which are characterized and formulated at the Institute of Pharmaceutical Research (INIFAR). Objective: Formulate a cream based on hot springs with renewable natural resources, cosmetic features, and high in content of minerals and high in content of minerals and not physicochemically unstable due to this composition. Methods: the raw materials and formulations were characterized by physicochemical tests such as pH, rheology, density, and organoleptic tests, and a formula were selected due to this characterized attributes. Results and conclusions: an stable formulation at high mineral content, HLB 6.82 , thixotropic adequate bed-wetting characteristics, pH 5.0 -7.0 , and without overheating with the friction, useful as the base was obtained for massage spas were obtain. UCR::Vicerrectoría de Investigación::Unidades de Investigación::Ciencias de la Salud::Instituto de Investigaciones Farmacéuticas (INIFAR)

Costa Rica is a volcanic country, containing a variety of peloids with different physicochemical properties; also its main source of income is the tourism. Most of their abundant natural resources have not been characterized and even used yet, this need offer the opportunity to study the physicochemical characteristics of peloids near the Arenal Volcano which may be related to its therapeutic properties, despite of this is a tourist attraction area characterized by hot springs, hotels and spas, it has a low socioeconomic and industrial development, and industrialization of products would create new jobs, and promote the health and wellness tourism, producing a productive linkage. Objective The physicochemical characterization of the Peloids near the Arenal Volcano Costa Rica and relate them to their therapeutic properties. Methods Peloids were characterized by tests such as pH, rheology, density, DSC, X-ray diffraction and thermal conductivity. Results and conclusions Peloids where characterized primarily as kandites billaminars, with a thixotropic flow, high in Fe2O3 , Al2O3, SIO2, Na2O, TiO2, ZrO2 minerals, an acid 4,70 pH, allowing them for the formulation of masks and other anti-psoriasis and anti-acne pharmaceutical forms. UCR::Vicerrectoría de Investigación::Unidades de Investigación::Ciencias de la Salud::Instituto de Investigaciones Farmacéuticas (INIFAR) UCR::Vicerrectoría de Docencia::Salud::Facultad de Farmacia

Desde el año 2009 la Universidad de Costa Rica por medio de la Facultad de Farmacia se ha dedicado a promover un modelo de desarrollo en la pequeña y mediana industria cosmética, para las zonas rurales o más pobres de Costa Rica, en la que las mujeres jefas de hogar lideran la empresa. Un ejemplo exitoso de este modelo es la microempresa Ditutto S.A, de las montañas de Acosta, la cual produce cosméticos a base de leche de cabra, en coordinación con el Instituto de Investigaciones Farmacéuticas, donde son evaluados y formulados. Este modelo ha hecho que la empresa genere empleo local, aumente su producción y ventas, y exporte a países como Canadá. Se plantea el modelo socioeconómico empleado y los resultados del mismo, entre los años 2009 al 2013, como un ejemplo del vínculo Empresa-Universidad-Sociedad. Universidad de Costa Rica/[]/UCR/Costa Rica UCR::Vicerrectoría de Investigación::Unidades de Investigación::Ciencias de la Salud::Instituto de Investigaciones Farmacéuticas (INIFAR)

La monitorización terapéutica de fármacos (MTF) es una herramienta válida para optimizar la farmacoterapia ,permitiendo el ajuste en la dosificación de medicamentos,tomando en cuenta las características individuales de cada paciente. El uso de la MTF ha sido indicado en el caso de falta de respuesta terapéutica o presencia de efectos adversos a dosis terapéuticas, ya sea por interacciones entre fármacos, presencia de particularidades genéticas concernientes a polimorfismos metabólicos y condiciones fisiológicas especiales, como sucede con los pacientes pediátricos y geriátricos. El tratamiento de pacientes con epilepsia, es una de las áreas donde el MTF ha hecho muchas contribuciones significativas y algunas de las razones que justifican su aplicación son: a) Que las crisis convulsivas ocurren en intervalos irregulares, lo que hace difícil el establecer una dosis óptima para su tratamiento; b) que los síntomas clínicos y los signos tóxicos pueden ser difíciles de detectar e interpretar y c) que los marcadores fisiológicos intermediarios de esta patología no están claramente definidos. La monitorización de fármacos antiepilépticos como fenobarbital y fenitoína no es algo nuevo; pues desde finales de la década de los 60’s, se inició como un procedimiento de investigación, el cual ya se perfilaba como una futura aplicación para un manejo mejor de la epilepsia. UCR::Vicerrectoría de Investigación::Unidades de Investigación::Ciencias de la Salud::Instituto de Investigaciones Farmacéuticas (INIFAR)