Estudio comparativo de divisibilidad de diferentes formulaciones de prednisona / Comparative study on the divisibility of different prednisone formulations

El objetivo de este trabajo fue estudiar la influencia de la divisibilidad en comprimidos de prednisona 30 mg. La división de comprimidos se utiliza a menudo en la práctica farmacéutica para ajustar las dosis administradas. La prednisona es un corticoesteroide (glucocorticoide) utilizado en el tratamiento de sustitución en la insuficiencia adrenal incluyendo entre otras la enfermedad de Addison. Como medicamento de referencia se utilizó Dacortin 30 mg, el cual se comparó con dos medicamentos genéricos. Se estudiaron diferentes características farmacotécnicas para evaluar la calidad de los comprimidos estudiados, tales como la disgregación y la resistencia a la rotura. Atendiendo al estudio de fraccionamiento de comprimidos, se determinó la diferencia sobre el peso teórico esperado (pérdida de masa media tras el fraccionamiento de cada marca comercial). La liberación del principio activo se estudió mediante el ensayo de velocidad de disolución en fracciones de comprimidos. Los resultados de las tres presentaciones comerciales fueron estudiados y analizados estadísticamente con un nivel de confianza de un 95 %. (AU)

The objective of this work was to study the influence of the division in prednisone tablets 30 mg. The division of tablets is often used in pharmaceutical practice to adjust the administered doses. Prednisone is a corticosteroid (glucocorticoid) used in the substitution treatment in adrenal insufficiency including, among others, Addison’s disease. As a reference drug, Dacortin 30 mg was used, and compared with two generic drugs. Different pharmacotechnic characteristics were studied to evaluate the quality of the tablets studied, such as disintegration, and the resistance to crushing. Based on the study of tablet fractionation, the difference over the expected theoretical weight was determined (loss of average mass after the fractionation of each trademark). The release of the active substance was carried out with dissolution rate study in fractions of tablets. The results of the three commercial formulations were studied and statistically analyzed with a confidence level of 95 %. (AU)

Study of Different Chitosan/Sodium Carboxymethyl Cellulose Proportions in the Development of Polyelectrolyte Complexes for the Sustained Release of Clarithromycin from Matrix Tablets.

This study investigated the combination of different proportions of cationic chitosan and anionic carboxymethyl cellulose (CMC) for the development of polyelectrolyte complexes to be used as a carrier in a sustained-release system. Analysis via scanning electron microscopy (SEM) Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) confirmed ionic interactions occur between the chitosan and carboxymethyl cellulose chains, which increases drug entrapment. The results of the dissolution study in acetate buffer (pH 4.2) showed significant increases in the kinetic profiles of clarithromycin for low proportions of chitosan/carboxymethyl cellulose tablets, while the tablets containing only chitosan had high relaxation of chitosan chains and disintegrated rapidly. The Korsmeyer-Peppas kinetic model for the different interpolymer complexes demonstrated that the clarithromycin transport mechanism was controlled by Fickian diffusion. These results suggest that the matrix tablets with different proportions of chitosan/carboxymethyl cellulose enhanced the ionic interaction and enabled the prolonged release of clarithromycin.

Self-Micellizing Technology Improves the Properties of Ezetimibe and Increases Its Effect on Hyperlipidemic Rats.

The aim of this work was to develop ezetimibe self-micellizing solid dispersions using Kolliphor® RH40 (MS-K) as a surfactant incorporating ezetimibe (EZ) into the croscarmellose hydrophilic carrier. Different ezetimibe:Kolliphor® ratios were studied to select micellar systems that improve the dissolution properties of ezetimibe. The different formulations were characterized by means of solid state analysis by SEM, powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), and dissolution studies. These physicochemical studies showed a decrease from the crystalline structure of ezetimibe (EZ) to its amorphous state in the micellar systems (MS-K). A rapid dissolution profile was observed in these micellar systems compared to the drug raw material and physical mixture. Efficacy studies were conducted using a high-fat diet that induced hyperlipidemic rats. The micellar system selected (MS-K 1:0.75) revealed a significant improvement in serum levels of total cholesterol (TC), low-density lipoproteins (LDL), and triglycerides (TG) compared to ezetimibe raw material. The histopathological examination of liver tissue also showed that this micellar system exhibited more beneficial effects on liver steatosis compared to ezetimibe raw material (EZ-RM) and the high-fat diet group (HFD). This study suggests that EZ micellar systems using Kolliphor® RH40 could enhance the antihyperlipidemic effect of ezetimibe and reduce liver steatosis.

Estudio comparativo de divisibilidad de diferentes formulaciones de prednisona / Comparative study on the divisibility of different prednisone formulations

El objetivo de este trabajo fue estudiar la influencia de la divisibilidad en comprimidos de prednisona 30 mg. La división de comprimidos se utiliza a menudo en la práctica farmacéutica para ajustar las dosis administradas. La prednisona es un corticoesteroide (glucocorticoide) utilizado en el tratamiento de sustitución en la insuficiencia adrenal incluyendo entre otras la enfermedad de Addison. Como medicamento de referencia se utilizó Dacortin 30 mg, el cual se comparó con dos medicamentos genéricos. Se estudiaron diferentes características farmacotécnicas para evaluar la calidad de los comprimidos estudiados, tales como la disgregación y la resistencia a la rotura. Atendiendo al estudio de fraccionamiento de comprimidos, se determinó la diferencia sobre el peso teórico esperado (pérdida de masa media tras el fraccionamiento de cada marca comercial). La liberación del principio activo se estudió mediante el ensayo de velocidad de disolución en fracciones de comprimidos. Los resultados de las tres presentaciones comerciales fueron estudiados y analizados estadísticamente con un nivel de confianza de un 95 %

The objective of this work was to study the influence of the division in prednisone tablets 30 mg. The division of tablets is often used in pharmaceutical practice to adjust the administered doses. Prednisone is a corticosteroid (glucocorticoid) used in the substitution treatment in adrenal insufficiency including, among others, Addison's disease. As a reference drug, Dacortin 30 mg was used, and compared with two generic drugs. Different pharmacotechnic characteristics were studied to evaluate the quality of the tablets studied, such as disintegration, and the resistance to crushing. Based on the study of tablet fractionation, the difference over the expected theoretical weight was determined (loss of average mass after the fractionation of each trademark). The release of the active substance was carried out with dissolution rate study in fractions of tablets. The results of the three commercial formulations were studied and statistically analyzed with a confidence level of 95 %

Estudio comparativo de disgregación de diferentes formulaciones de olanzapina / Comparative study on the disintegration of different olanzapine formulations

Las formas de dosificación bucodispersables son productos farmacéuticos que se disgregan y disuelven rápidamente en la saliva cuando se colocan en la boca. Hay distintos tipos de formulaciones y procesos de fabricación que pueden emplearse para su elaboración. En este trabajo, se estudia las diferencias entre los genéricos bucodispersables con 10 mg de olanzapina comercialmente disponibles en España y Zyprexa Velotab reconocido como innovación galénica. Se han analizado distintos aspectos, tales como forma y tamaño, formulación cualitativa, tiempo de disgregación in vitro en saliva artificial y material de acondicionamiento. Entre todos los productos analizados, Zyprexa Velotab fue el que tuvo una ultrarrápida disgregación en 3 segundos y el menor residuo de dispersión (AU)

Orally dispersable dosage forms are pharmaceutical products that disintegrate and dissolve rapidly in saliva when placed in the mouth. There are several types of formulations and manufacturing technologies, which may be used to produce orodispersibles. This work investigates different generic 10 mg olanzapine orodispersible products commercially available in Spain and the innovative Zyprexa Velotab manufactured by Eli Lilly & Co. Several aspects such as the shape and size, qualitative formulation, in vitro disintegration time in artificial saliva and packaging are analyzed. Among all the products tested Zyprexa Velotab showed an ultra fast disintegration in 3 seconds and the lowest dispersión (AU)