Diseño y preparación de formas farmacéuticas sólidas de Benznidazol para el tratamiento de la Enfermedad de Chagas / Design and Preparation fo Pharmaceutical Solid Dosage Forms of Benznidazole for the Treatment of Chagas Disease

INTRODUCCIÓN: En Argentina se emplea el benznidazolcomo terapéutica de primera línea para el tratamiento etiológico del Chagas. Desde su lanzamiento (hace más de 40 años), sólo se dispone de comprimidos convencionales de 100 mg; no se han desarrollado nuevas formas farmacéuticas que aumenten la eficacia y seguridad, ni alternativas con dosis pediátricas. OBJETIVOS: Desarrollar formas farmacéuticas de benznidazol que ofrezcan ventajas farmacoterapéuticas. MÉTODOS: Preformulación y diseño de nuevas formulaciones de benznidazol, con caracterización físico-química y selección de las formulaciones más favorables. Frente a la discontinuidad de producción del ingrediente activo benznidazol, se desarrolló una metodología de extracción a partir de 8520/8520/nica alternativa comercial disponible. RESULTADOS: Se obtuvieron nuevas formulaciones de comprimidos de 50 y 100 mg debenznidazol, con una rápida disolución del producto de referencia. Además, se obtuvieron formulaciones masticables de 50 mg bajo la forma de hidrogeles azucarados, con un efectivo enmascaramiento del mal sabor. Todas las formulaciones cumplieron los ensayos de evaluación de las propiedades farmacotécnicas y biofarmacéuticas, superando los perfiles de referencia. CONCLUSIONES: Se desarrollaron nuevas alternativas farmacéuticas de benznidazol de rápida disolución, que podrían mejorar el tratamiento etiológico de la enfermedad(especialmente en pediatría) y convertirse en herramientas aptas para su explotación comercial

INTRODUCTION: In Argentina, benznidazole is the drug of choice for the etiological treatment of Chagas disease. Since it was launched (more than 40 years ago), there are only 100 mg tablets available; the development included neither new pharmaceutical forms improving efficacy and safety, nor a pediatric dosage option. OBJECTIVES: To develop pharmaceutical form sof benznidazole with pharmacotherapeutic advantages. METHODS: Preformulation and design of new formulation sof benznidazole, with physicochemical characterization and selection of the most favorable formulations. Due to the discontinuity in the production of the active ingredient benznidazole, a specific methodology was developed in order to obtain it from the only commercially available alternative. RESULTS: New benznidazole tablet formulations were obtained (50 and 100 mg), with a rapid dissolution of the reference product, as well as chewable formulation sof 50 mg as sugar hydrogels featuring an effective taste masking. All formulations passed the evaluation tests for pharmacotechnical and biopharmaceutical properties, out performing the reference profiles. CONCLUSIONS:New fast-dissolving pharmaceutical dosage forms of benznidazole were developed, which could improve the etiological treatment of the disease (especially in the pediatric field) and become a proper tool for its commercial exploitation

Implementación de una técnica in house para la producción de geles de plaquetas a partir de hemocomponentes de donantes voluntarios / Implementation of an in house technique to produce platelets gel from blood components from volunteer blood donors

Se implementó una técnica para producir geles de fibrina y geles de plaquetas a partir de hemocomponentes de banco de sangre, en el Hospital Nacional de Niños de Costa Rica. Se aplicaron nueve combinaciones de, tres volúmenes de gluconato de calcio al 10% y tres volúmenes del sobrenadante de trombina obtenido a partir de plasma fresco congelado (PFC), con un volumen definido de PFC (plasma pobre en plaquetas) o, el mismo volumen de concentrado de plaquetas (CP). Se midieron los tiempos de gelificación in vitro, obteniéndose que la combinación 6 mL PRP/PPP más 0.5 mL de gluconato de calcio al 10% más 1.5 mL trombina, parece ser la más adecuada. Las pruebas de tamizaje de la coagulación son útiles para explicar tiempos de gelificación tardíos.

Antimicrobial activity of four different dental gel formulas on cariogenic bacteria evaluated using the linear regression method

The antimicrobial activity of four different dental gel formulas was evaluated on theree microorganisms associated with cariogenesis: Streptococcus mutans, Lactobacillus casei and Actinomyces viscosus. The preliminary antimicrobial activity evaluation was performed using an agar diffusion method. In addition, the formulas were challenged using each microorganism with subsequent determinations of survivors at time intervals of 1, 5, 10, 20 and 30 minutes. The decimal reduction time (D-value) calculated from the obtained curves (logCFU/mL vs. time) was employed for the antimicrobial activity comparison of the formulas. The selected method for survivor enumeration was validated according to official compendia...

Determinação do 17ß-estradiol nas formas farmacêuticas gel e adesivo transdérmico / Determination of 17ß-estradiol in dosage formulations: gel and patch

Desenvolveu-se um método espectrofotométrico na região do vísivel para doseamento de 17ß-estradiol em gel e adesivo transdérmico, utilizando-se sulfanilamida diazotada como reagente. O azo-composto formado apresentou absorção máxima em 480 nm, sendo a reação linear na faixa de concentração de 10,0 a 28,0 µg/mL. Quando aplicado a amostras comerciais mostrou-se preciso e exato...

In-vitro and in-vivo evaluation of formulated lidocaine dental gels and ointments

In this research, lidocaine HCl and lidocaine were formulated on different gel and ointment bases. Eight formulations of lidocaine and lidocaine HCl ointment and gel [four as 2% gel, one as 5% gel and three as 5% ointment] were prepared and tested for their release in Sorensen's phosphate buffer pH 7.4 using USP dissolution test apparatus at 37C +/- 0.5C and compared with four commercially available products; namely, xylocaine 2% jelly, xylonor 5% gel, xylocaine 5% ointment [Astra, Sweden] and xylocaine 5% ointment [Astra, Cid]. In vitro results showed that formula I [lidocaine HCl 2.0 g in carbopol gel base] and formula IV [lidocaine HCl 2.0 g in carboxymethyl cellulose gel base] gave the highest extent of release of the prepared gel formulae. Formula VII [lidocaine 5 g in emulsifying ointment base containing liquid paraffin and bees wax] gave the highest extent of release among all the prepared ointment formulae. The local anesthetic effect of the prepared lidocaine gel and ointment was evaluated in vivo using albino mice