Reformulación de un ingrediente farmacéutico activo herbario (IFAH) gastrorresistente a partir de Portulaca oleracea L. con vistas a la elaboración de formas farmacéuticas sólidas seguras y eficaces
Date
2018
Authors
Guerrero Medina, Yuliet
Journal Title
Journal ISSN
Volume Title
Publisher
Universidad Central ‘‘Marta Abreu’’ de Las Villas. Facultad de Química Farmacia. Departamento de Farmacia
Abstract
En el presente trabajo se utilizó el sólido pulverulento (SP) de Portulaca Oleracea L. en
el intervalo de tamaño de partícula comprendido entre 0,1-0,5 mm. Se evaluó sus
características organolépticas, determinándose que el mismo presenta color verde
claro, olor característico y forma irregular de las partículas. Se elaboraron 6
formulaciones de granulados donde se utilizó el SP a una concentración del 50 %, en
tres de ellas se empleó como aglutinante Eudragit L 30D-55 (dispersión acuosa al 30%)
y en las restantes el acetoftalato de celulosa al 10% disuelto en etanol - acetona (3:1).
Para las formulaciones elaboradas con cada tipo de aglutinante se varió la mezcla de
lubricantes utilizados (mezcla 1: dióxido de silicio coloidal al 1% y estearato de
magnesio al 0,2%; mezcla 2: almidón de maíz al 1% y estearato de magnesio al 0,2% y
mezcla 3: carbonato de magnesio al 1% y estearato de magnesio al 0,2%). En todos
los casos se empleó como desintegrante almidón de maíz al 15 % y como vehículo
lactosa. Todos los granulados formulados y elaborados resultaron ser muy
higroscópicos. Al caracterizar químico – física y tecnológicamente los granulados
pudimos concluir que las propiedades reológicas de los mismos cuando se les añade
agentes antifricción mejoran de manera apreciable, siendo consideradas de excelente
cuando se emplean las mezclas almidón - estearato de magnesio y carbonato de
magnesio - estearato de magnesio. Las variantes de granulados donde se utiliza como
solución aglutinante la dispersión acuosa de Eudragit L 30D-55 y lubricadas con las
mezclas almidón - estearato de magnesio y carbonato de magnesio - estearato de
magnesio son consideradas las óptimas por presentar una distribución normal de
tamaño de partícula, mejores propiedades reológicas, menor riesgo de toxicidad y ser
más económicas por el no empleo de solventes orgánicos.
In the present work, the powdery solid (SP) of Portulaca Oleracea L. was used in the range of particle size comprised between 0.1-0.5 mm. Its organoleptic characteristics were evaluated, determining that it has a light green color, characteristic odor and irregular shape of the particles. Six formulations of granules were elaborated where the SP was used at a concentration of 50%, in three of them it was used as a binder Eudragit L 30D-55 (aqueous dispersion at 30%) and in the rest the dissolved 10% cellulose acetophthalate in ethanol - acetone (3: 1). For the formulations made with each type of binder, the mixture of lubricants used was mixed (mixture 1: 1% colloidal silicon dioxide and 0.2% magnesium stearate, mixture 2: 1% corn starch and magnesium stearate) 0.2% and mixture 3: magnesium carbonate at 1% and magnesium stearate at 0.2%). In all cases, 15% corn starch was used as a desintegrant and as a lactose vehicle. All the formulated and processed granules turned out to be very hygroscopic. By chemically and technologically characterizing the granulates we were able to conclude that the rheological properties of these when added antifriction agents improve appreciably, being considered excellent when the mixtures are used starch - magnesium stearate and magnesium carbonate - stearate magnesium. The granular variants where the aqueous dispersion of Eudragit L 30D-55 is used as a binder solution and lubricated with the mixtures starch magnesium stearate and magnesium carbonate magnesium stearate are considered optimal because they present a normal distribution of particle size, better rheological properties, less risk of toxicity and be more economical by not using organic solvents.
In the present work, the powdery solid (SP) of Portulaca Oleracea L. was used in the range of particle size comprised between 0.1-0.5 mm. Its organoleptic characteristics were evaluated, determining that it has a light green color, characteristic odor and irregular shape of the particles. Six formulations of granules were elaborated where the SP was used at a concentration of 50%, in three of them it was used as a binder Eudragit L 30D-55 (aqueous dispersion at 30%) and in the rest the dissolved 10% cellulose acetophthalate in ethanol - acetone (3: 1). For the formulations made with each type of binder, the mixture of lubricants used was mixed (mixture 1: 1% colloidal silicon dioxide and 0.2% magnesium stearate, mixture 2: 1% corn starch and magnesium stearate) 0.2% and mixture 3: magnesium carbonate at 1% and magnesium stearate at 0.2%). In all cases, 15% corn starch was used as a desintegrant and as a lactose vehicle. All the formulated and processed granules turned out to be very hygroscopic. By chemically and technologically characterizing the granulates we were able to conclude that the rheological properties of these when added antifriction agents improve appreciably, being considered excellent when the mixtures are used starch - magnesium stearate and magnesium carbonate - stearate magnesium. The granular variants where the aqueous dispersion of Eudragit L 30D-55 is used as a binder solution and lubricated with the mixtures starch magnesium stearate and magnesium carbonate magnesium stearate are considered optimal because they present a normal distribution of particle size, better rheological properties, less risk of toxicity and be more economical by not using organic solvents.
Description
Keywords
Portulaca Oleracea L., Plantas Medicinales, Sólidos Pulverulentos Herbarios, Granulación, Efecto Hipocolesterolémico