Formulation development and evaluation of Silybum marianum tablets

• Published in: Rodriguésia Vol. 71
• Main Authors: Cianchino, Valeria Andrea, Favier, Laura Silvina, Ortega, Claudia Alicia, Peralta, Cecilia, Cifuente, Diego Alberto
• Format: Journal Article
• Language: English; Portuguese
• Published: Instituto de Pesquisas Jardim Botânico do Rio de Janeiro 2020
• Subjects: direct compression; ECOLOGY; ethanolic extract; herbal tablets; PLANT SCIENCES; quality controls; Silybum marianum; controles de calidad; Silybum marianum; quality controls; ethanolic extract; herbal tablets; compresión directa; extracto etanólico; comprimidos herbarios; direct compression
• ISSN: 0370-6583; 2175-7860; 2175-7860
• DOI: 10.1590/2175-7860202071044

Abstract In popular medicine Silybum marianum is used as a hepatoprotective agent. Silymarin is the major constituent. The present work deals with the formulation and evaluation of S. marianum tablets from ethanolic extract by direct compression. The ethanolic extract was obtained from seeds by soxhlet extraction. Two pharmaceutical formulations were prepared using fluid extract as an active principle, and Aeroperl® 300 Pharma as a carrier. In order to improve flow ability and compressibility, co-processed excipients MicroceLac® 100 and FlowLac® 90 were employed. Pre-compression and post-compression parameters were evaluated according to USP 34-NF 29. Besides, silymarin was determined by NMR spectral data. Both formulations showed excellent rheological properties and the best biopharmaceutical parameters were observed in F2 (S. marianum ethanolic extract, aeroperl® 300 Pharma, flowLac® 90, glycolate starch and magnesium stearate) in terms of the friability (0.82 %) and the disintegration time (8.05 min). Resumen En medicina popular, Silybum marianum se usa como agente hepatoprotector. La silimarina es su componente principal. El presente trabajo trata de la formulación y evaluación de tabletas de S. marianum a partir de extracto etanólico por compresión directa. El extracto etanólico se obtuvo de las semillas mediante extracción con soxhlet. Se prepararon dos formulaciones farmacéuticas usando extracto fluido como principio activo y Aeroperl® 300 Pharma como vehículo. Para mejorar la capacidad de flujo y la compresibilidad, se emplearon excipientes coprocesados MicroceLac® 100 y FlowLac® 90. Los parámetros de precompresión y postcompresión se evaluaron de acuerdo con USP 34-NF 29. Además, la silimarina se determinó mediante datos espectrales de RMN. Ambas formulaciones mostraron excelentes propiedades reológicas y los mejores parámetros biofarmacéuticos se observaron en F2 (S. marianum ethanolic extract, aeroperl® 300 Pharma, flowLac® 90, glicolado de almidón y estearato de magnesio) en términos de friabilidad (0,82%) y el tiempo de desintegración (8,05 min).