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Epidendrum coryophorum belongs to the Orchidaceae family. Traditional uses of some species for this genus include infusions of the leaves used for kidney problems, treat influenza, conjunctivitis, liver pain, relieve kidney symptoms, and hypoglycemic effect. This work's objective was to determine the phytochemical profile of the ethanolic extract of Epidendrum coryophorum leaves and to evaluate the potential anti-inflammatory activity in vitro of the extract employing the erythrocyte membrane stabilization method. The phytochemical screening carried out in this work suggested phenols, coumarins, flavonoids, tannins, steroids, and sterols in the ethanolic extract of Epidendrum coryophorum leaves. Cardiotonic glycosides and carbohydrates were also found. The ethanolic extract's UV-Vis spectrum showed absorption maxima at 268 nm and 332 nm, which could correspond to flavonoids of the flavonoid classes, 3-OH substituted flavonols, or isoflavones. The quantitative determination of total phenols of the ethanolic extract was carried out using the Folin-Ciocalteu method. The total phenolic content expressed as mg Gallic acid equivalent (G.A.E.) per gram of extract was found to be 19,96 mgGAE/g of Epidendrum coryophorum. The ethanolic extract of Epidendrum coryophorum leaves showed hemolysis inhibition values ​​of 18,19% at 1,0 mg/mL, 38,98% at 1,5 mg/mL and 40,94% at 2,5 mg/mL compared with aspirin (positive control) giving values ​​of 65,33% at 1,0 mg/mL, 72,26% at 1,5 mg/mL and 73,75% at 2,5 mg/mL. The values ​​obtained for inhibition of hemolysis with ethanolic extract, compared with the values ​​obtained with a pure anti-inflammatory, are significant and demonstrate anti-inflammatory activity in Epidendrum coryophorum. Keywords: Epidendrum coryophorum, total phenolic content, microencapsulation, anti-inflammatory activity

We investigated a spray drying process for preparing water-soluble salts of high molecular weight chitosan (CH) intended for pharmaceutical excipient applications. CH was derived from chitin of marine lobster origin (Panulirus argus). The effects of organic acid (acetic or lactic acid) and the ratio (difference) of inlet/outlet air temperature (140/90 °C or 160/100 °C) on spray drying were studied. The yield of spray-dried CH salt powders ranged from 50% to 99% in laboratory and industrial-scale processes. The spray-dried dry powder of CH salts consisted of spherical agglomerated particles with an average diameter of 36.2 ± 7.0 µm (CH acetate) and 108.6 ± 11.5 µm (CH lactate). After dispersing the spray-dried CH salt powder samples in purified water, the mean particle sizes obtained for the CH acetate salts were 31.4 nm (batch A001), 33.0 nm (A002) and 44.2 nm (A003), and for the CH lactate salts 100.8 nm (batch L001), 103.2 nm (L002) and 121.8 nm (L003). The optimum process conditions for spray drying were found: an inlet air temperature of 160 ± 5 °C, an outlet temperature of 100 ± 5 °C and an atomizer disk rotational speed of 18,200 min−1. The X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) results confirmed the amorphous state of the CH salts. The 1H nuclear magnetic resonance (NMR) and Fourier transform infrared (FT-IR) spectra of CH acetate and lactate salts verified that the spray drying process does not affect the polymer backbone. In conclusion, both laboratory and industrial-scale spray drying methods for preparing water-soluble acid salts of CH are reproducible, and the physicochemical properties of the corresponding CH acid salts are uniform.

Chitosan (CS) microparticles loaded with dexamethasone were prepared by spray drying, followed by coating with a pH-dependentinterpolymer complex based on poly(acrylic acid)/poly(vinyl pyrrolidone) using an water-in-oil emulsion technique. The aim ofthis research was to evaluate the influence of PAA/PVP coating on the release of dexamethasone from loaded chitosanmicroparticles, in simulated gastric fluid (SGF, pH = 1 2) and simulated intestinal fluid (SIF, pH = 6 8). The release ofdexamethasone from uncoated loaded CS microparticles was similar in both fluids, and almost complete release of the drug wasachieved in 5 hours. In the coated loaded CS microparticles, the release of dexamethasone in SGF was reduced considerably,very close to zero, due to the interpolymer complex formation at low pH, demonstrating that this system applied aspH-dependent coating has a potential as a site-specific delivery system. Fil: García Couce, Jomarien. Universidad de La Habana; Cuba Fil: Bada Rivero, Nancy. Universidad de La Habana; Cuba Fil: López Hernández, Orestes D.. Universidad Técnica de Ambato; Ecuador Fil: Nogueira, Antonio. Centro de Investigacion y Desarrollo de Drogas; Cuba Fil: Caracciolo, Pablo Christian. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Mar del Plata. Instituto de Investigaciones en Ciencia y Tecnología de Materiales. Universidad Nacional de Mar del Plata. Facultad de Ingeniería. Instituto de Investigaciones en Ciencia y Tecnología de Materiales; Argentina Fil: Abraham, Gustavo Abel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Mar del Plata. Instituto de Investigaciones en Ciencia y Tecnología de Materiales. Universidad Nacional de Mar del Plata. Facultad de Ingeniería. Instituto de Investigaciones en Ciencia y Tecnología de Materiales; Argentina Fil: Ramón Hernández, José A.. Universidade Federal do Rio de Janeiro; Brasil Fil: Peniche, Carlos. Universidad de La Habana; Cuba

El estudio de estabilidad del aceite microencapsulado y sin microencapsular se realizó por el método de vida de estante a las temperaturas de 2-8 °C, y temperatura ambiente, respectivamente, durante doce meses. Los parámetros analizados al pool de aceite fueron: características organolépticas, índice de acidez, peróxido, saponificación, contenido de vitamina A y conteo microbiológico. Mientras que al aceite microencapsulado se le evaluaron las características organolépticas, la eficiencia de encapsulación, contenido de humedad, aceite superficial, contenido de vitamina A y conteo microbiológico. Los resultados evidenciaron una disminución superior al 5% en el contenido de vitamina A en el aceite sin microencapsular, a diferencia del aceite microencapsulado. Se logró el enmascaramiento del olor intenso a pescado, y los restantes parámetros evaluados se encontraron dentro de los límites establecidos.El aceite de hígado de tiburón microencapsulado resultó estable física, química y microbiológicamente por doce meses, mientras que el aceite sin microencapsular solo seis meses. El proceso de microencapsulación no solo mejoró sus características organolépticas, sino también favoreció su estabilidad lográndose un mayor período de vida útil.

El citrato de calcio y magnesio es una materia prima de calidad farmacéutica obtenida a partir de dolomitas cubanas, con la finalidad de ser empleada en la producción de formas terminadas para suplir calcio y magnesio en personas con deficiencias de estos minerales. Como parte de la optimización del proceso tecnológico de obtención, se estudió el tiempo de filtración con el objetivo de evaluar el comportamiento a escalas superiores. Para ello se realizó un estudio de desescalado para determinar las condiciones en la escala de banco, empleando como criterio de escalado mantener igual consumo de potencia por unidad de volumen. A través de la ecuación fundamental de la filtración, se determinó el tiempo de esta operación. El estudio de filtración dio como resultados que el valor de la resistencia del medio filtrante era Rm= 6,08 × 10(10) m-1 y la resistencia de la torta a= 1,239 × 10(10) m/kg-1 a una diferencia de presión constante (Dp= 9,99 × 10(4) kg/m·s²). Mientras que el tiempo medio de filtración fue de 494,6 s (8,24 ± 3,0 min). En conclusión, los resultados mostraron que el tiempo de filtración es adecuado para el proceso tecnológico estudiado, y el estudio de escalado demostró la viabilidad del proceso de filtración.Calcium and magnesium citrate is a raw material of pharmaceutical quality obtained from Cuban dolomites to be used in those people with deficiency in these two minerals. As part of the technological process optimization, the filtering time was studied to evaluate the possible behaviour at higher scales. To this end, one scale-down study was made to determine the conditions at bench scale by keeping the same power consumption per volume unit. The fundamental filtering equation allowed determining the time for this operation. The results of this study showed that the resistance value of the filtering material was Rm= 6.08 · 10(10) m-1 and the resistance of the mass was a= 1.239 · 10(10) m·kg-1 at constant pressure (Dp= 9.99 × 10(4) kg/m·s²). The filtration time was 494.6 s (8,24 ± 3,0 min). The results showed that the filtration time was correct for the studied technological process and the scale up study demonstrated the feasibility of the filtration process.

The effects of spray-drying process and acidic solvent system on physicochemical properties of chitosan salts were investigated. Chitosan used in spray dryings was obtained by deacetylation of chitin from lobster (Panulirus argus) origin. The chitosan acid salts were prepared in a laboratory-scale spray drier, and organic acetic acid, lactic acid, and citric acid were used as solvents in the process. The physicochemical properties of chitosan salts were investigated by means of solid-state CP-MAS (13)C nuclear magnetic resonance (NMR), X-ray powder diffraction (XRPD), differential scanning calorimetry, and Fourier transform infrared spectrometry (FTIR) and near-infrared spectroscopy. The morphology of spray-dried chitosan acid salts showed tendency toward higher sphericity when higher temperatures in a spray-drying process were applied. Analysis by XRPD indicated that all chitosan acid salts studied were amorphous solids. Solid-state (13)C NMR spectra revealed the evidence of the partial conversion of chitosan acetate to chitin and also conversion to acetyl amide form which appears to be dependent on the spray-drying process. The FTIR spectra suggested that the organic acids applied in spray drying may interact with chitosan at the position of amino groups to form chitosan salts. With all three chitosan acid salts, the FTIR bands at 1,597 and 1,615 cm(-1) were diminished suggesting that -NH groups are protonated. The FTIR spectra of all chitosan acid salts exhibited ammonium and carboxylate bands at 1,630 and 1,556 cm(-1), respectively. In conclusion, spray drying is a potential method of preparing acid salts from chitosan obtained by deacetylation of chitin from lobster (P. argus) origin.

Un tema de gran interés para la industria farmacéutica moderna lo constituye sin duda, la búsqueda de tecnologías para la obtención de formas farmacéuticas para la administración y transporte de citostáticos, antiinflamatorios, péptidos y hormonas, entre otros fármacos, que impliquen una reducción de su toxicidad o una liberación controlada del principio activo para lograr con ello un aumento de su eficacia. En el presente trabajo se estudió la influencia del flujo de líquido de alimentación, del flujo de aire de atomización y de secado, y se evaluaron diferentes características fisicoquímicas y morfológicas (tamaño, forma, porosidad y distribución de tamaño de partículas, eficiencia de encapsulación del principio activo) de microesferas de tramadol. Como resultado se obtuvo que es posible lograr microesferas con un tamaño de 18,93 ± 2,31 µm con forma esférica, una superficie no porosa, y se demostró mediante difractometría de rayos X la encapsulación del tramadol en el polímero.An interesting subject for pharmaceutical industry is the search of technologies to achieve pharmaceutical ways for administration and transportation of cytostatics, anti-inflammatories, peptides and hormones among other drugs implicating a reduction of its toxicity or a contolled releasing of active principle to increase its effectiveness. In present paper authors studied the influence of fluid flow in feeding, of atomization air and of driying; different physicochemical and morphological features (size, shape, porosity and distribution in the particles size, and the effectiveness of active principle encapsulation) of Tramadol's microspheres. As result, it was possible to achieve microspheres of 18.93 ± 2.31 µm with an spherical shape, a non-porous surface demostrating it by X-ray difractometry and Tramadol encapsulation in the polymer.

Para administrar por vía oral compuestos oleosos como los extractos lipídicos de origen natural, los aceites esenciales volátiles y las vitaminas liposolubles, se hace necesario presentarlos en forma de cápsulas blandas. Una alternativa a esta forma de presentación es la microencapsulación, que ofrece una solución para modificar el estado físico y presentarlos en una forma sólida para su administración por vía oral. Esta alternativa permite enmascarar el olor y sabor desagradable de productos que van a ser administrados por vía oral, además de proteger de la oxidación a los ácidos grasos presentes. El secado por aspersión es uno de los métodos más utilizados a escala industrial para la obtención de microcápsulas. Debido a su creciente uso en la industria farmacéutica, en el presente trabajo se recopila el estado del arte en el uso de esta tecnología para la microencapsulación de sustancias oleosas.To administer oral oily compounds such as lipid extracts of natural origin, volatile essential oils and liposoluble vitamins, it is necessary that presentation be in soft capsulae. An alternative to this form of presentation is the microencapsulation being a solution to modify the physical state and to achieve a solid form for its oral administration. This alternative allows masking the smell and the unpleasant flavor of oral products ant also to protect the oxidation of fatty acids present. The aspersion dry is one of the more used methods at industrial scale to microcapsulae achievement. Because of its increasing use in pharmaceutical industry in present paper is gathered the art of state in the use of this technology for oily substances microencapsulation.

Aim: The objective of this work was to develop and validate a method for determining the degree of molar deacetylation of chitosan acetate and chitosan lactate, as well as to study the stability of both salts. Materials and Methods: A spectrophotometric method was validated according to internationally-established quantitative techniques. Three industrial batches of chitosan acetate and chitosan lactate, obtained by spray drying, were stored under shelf life conditions for twelve months. Organoleptic characteristics, the degree of molar deacetylation, pH, loss on drying and microbiological count were determined at the beginning and end of the study. Results and Discussion: The statistical data proved that the two methods complied with international standards for the validation of analytical techniques. It was shown that the procedures developed were linear, specific, precise and accurate, so they can be used for the purposes of quality control and stability study of the polymer salts. Salts remained in powder form, with a light-yellow to dark-yellow coloration. Values of loss on drying (2.5 - 5.2 %) of chitosan salt using acetic or lactic acid, as a solvent, indicated the good quality of spray-dried particles of chitosan. Similar behavior was obtained regarding pH. The two salts stayed within the parameters that determine their quality, both in the initial stage and after twelve months at room temperature. Conclusion: Spray drying chitosan acetate and chitosan lactate, stored at room temperature in a dry place, in double polyethylene bags and multilayer paper bags, kept their physical, chemical and microbiological characteristics for a period of twelve months.

Didanosine (ddI) is a water-soluble antiretroviral used in the treatment of HIV that undergoes fast gastric degradation to an inactive hypoxanthine. Therefore, its oral bioavailability is relatively low (20–40%). In this work, we investigated for the first time a scalable open-loop spray-drying method with co-current flow for the encapsulation of ddI (model drug) within particles of the biocompatible polyester poly(epsilon-caprolactone). The average diameter of the particles was 36–118 μm and the morphology spherical. The encapsulation efficiency ranged from 60% to 100% with yields of up to 65%. ATR/FT-IR analysis indicated that most of the drug was encapsulated within the particles. In vitro release assays showed that the particles released the drug within 120 min. Finally, oral administration to rats led to a statistically significant 2.5-fold increase of the bioavailability with respect to a ddI aqueous solution, highlighting the potential of this technology to encapsulate efficiently other hydrophilic antiretrovirals and, by doing so, to overcome different biopharmaceutical drawbacks associated with the oral administration. Fil: Seremeta, Katia Pamela. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: Reyes Tur, María I.. AICA Laboratories; Cuba Fil: Martínez Pérez, Sandra. LIORAD Laboratories; Cuba Fil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina Fil: Taira, Carlos Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina Fil: López Hernández, Orestes D.. Ambato Technical University. Faculty of Food Science and Engineering; Ecuador Fil: Sosnik, Alejandro Dario. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Technion - Israel Institute of Technology; Israel

A soy peptone obtained with enzyme papain as a hydrolyzing agent was characterized. The physicochemical evaluation of the nutritive base attained at pilot and industrial scale showed the following characteristics: loss due to desiccation, 1.93%; aminic nitrogen, 1.71%; total nitrogen, 8.63%; chlorides (as NaCl), 5.45%; and pH, 6.94. For the functional evaluation of the pilot and industrial batches (3), developed soy peptone and another one taken as a reference from the Biotécnica Internacional firm (México), was incorporated to a mixture of bases. There were no significant differences (p0.05) in the absorbance values at 640 nm obtained in the promotion of the growth between the developed product and that of reference for Staphylococcus aureus ATCC 25923. For Streptococcus pyogenes ATCC 19615, it was observed a mild superiority (significant difference for p0.05) starting from the 5th hour of incubation in favor of the industrial batches compared with the reference soy peptone. It was proved that the promotion of the growth in the soy triptone agar and broth media and in malt extract agar for the evaluated microorganisms was similar or higher (significant differences for p0.05) in those prepared with the experimental soy peptone, in comparison with the formulated with the reference base.

La industria farmacéutica moderna busca constantemente tecnologías para la obtención de transportadores de diferentes fármacos como citostáticos, antiinflamatorios, péptidos y hormonas, entre otros, que impliquen una reducción de su toxicidad y una liberación sostenida o controlada para lograr el efecto terapéutico con una sola dosis. Dentro de estas tecnologías se destaca el empleo de microesferas biodegradables de ácidos polilácticos como sistemas poliméricos matriciales de liberación controlada. En el presente trabajo se exponen aspectos relevantes relacionados con la tecnología de obtención de microesferas mediante secado por aspersión conocido también como Spray drying, el cual tiene como ventajas una alta eficiencia de encapsulación además de ser un método rápido, continuo, relativamente sencillo con respecto a otros existentes, y principalmente brinda la posibilidad de ser escalado hasta nivel de producción.The modern pharmaceutical Industry search constantly technologies for obtaining drugs targeting as antineoplasics, peptides and hormones, among other that imply a toxicity reduction, and sustained or controlled release to achieve the therapeutic effect with a single dose. These technologies employment of biodegradable microspheres of polylactic acids as matricial polymeric systems for controlled release. This work related aspects with the technology of microspheres obtaining by Spray drying which has as advantages, a high encapsulation efficiency, continuous method, relatively simple it offers the possibility of being scale up until production level.

Se estudiaron las condiciones de la deshidratación por aspersión de un hidrolizado papaínico proveniente del músculo animal, y se demostró que el parámetro de mayor influencia directa sobre la densidad aparente del polvo resultó la concentración de sólidos totales (43 %), seguidamente de la temperatura en la entrada de la cámara (140 °C) y velocidad del atomizador (21 500 rev/min), ambos de forma inversa. La densidad aparente alcanzó aproximadamente 400 kg m-3 en comparación con la obtenida antes del estudio de 50 kg m-3. Se comprobó que mejores resultados, en cuanto a la densidad aparente, se obtuvieron al deshidratar el hidrolizado a 122 °C en la entrada de la máquina y 90 °C en la salida en comparación con 140 °C en la entrada del equipo. Se demostró que el producto obtenido posee características físico-químicas y bioquímicas favorecedoras del crecimiento de diferentes especies microbianas de colecciónThe spraying dehydration conditions of a Papaic hydrolisate from an animal muscle were studied, and it was proved that the parameter with the highest direct influence on the apparent density of the powder was the concentration of total solids (43 %), followed by the temperature at the inlet of the chamber (140 °C) and the speed of the atomizer (21 500 rev/min), both in an inverse form. The apparent density reached approximately 400 kg m-3 compared with the obtained before the study of 50 kg m-3. As to the apparent density, better results were obtained on dehydrating the hidrolisate at 122 °C in the inlet of the machine and at 90 °C in the outlet, in comparison with 140 °C in the inlet of the equipment. It was proved that the product obtained had physical, chemical and biochemical characteristics that favored the growth of different microbial species of collection