ABSTRACT
AIM: To examine the pharmacodynamics of a self-developed oral colon-specific delivery coated tablets of 4-aminosalicylic acid (4-ASA) on rats. METHODS: Ulcerative colitis rat model was developed by intrarectal administration of 2, 4, 6-trinitrobenzenesulfonic acid (TNBS) in alcohol. Rats were divided randomly into healthy control group, TNBS control group, TNBS + lower dose (coated tablets) group, TNBS +medium dose (coated tablets) group, TNBS + higher dose (coated tablets) group, TNBS + sulfasalazine (SASP) group, TNBS + medium dose non-coated tablet group. Several indices including macroscopic change,histological damage, and tissue myeloperoxidase (MPO) activity were examined after 5 consecutive oral drug administration to assess pharmacodynamics of the coated tablets. RESULTS: An experimental ulcerative colitis in rats was induced by TNBS. Compared with 4-ASA non-coated tablet group, decreased macroscopic and histological damage score and lower MPO activity were observed after the oral administration of 4-ASA coated tablets or SASP. There was no significant difference between the effects on the indices of higher dose of coated tablets and SASP (P ＞ 0.05) CONCLUSION: The self-made 4-ASA oral colon-specific delivery coated tablet showes higher effect than non-coated tablets to treat ulcerative colitis in rats.
ABSTRACT
Se estudiaron diferentes formulaciones de tabletas de pimozida en dosis de 1 y 4 mg, diseñadas con el objetivo de obtener una formulación que cumpla con los parámetros establecidos en la Farmacopea de los Estados Unidos XXII para el control de la calidad del producto terminado, así como los requerimientos necesarios para su revestimiento. Entre las formulaciones establecidas la denominada PP cumplió con los parámetros de calidad establecidos, antes y posterior al revestimiento. Los resultados obtenidos en el estudio de vida en estante de las tabletas revestidas fabricadas a escala semiindustrial demostraron que hasta 1 año posterior a la fabricación, éstas cumplen con las especificaciones establecidas en la Farmacopea, lo cual soporta la factibilidad para su escalado al nivel industrial.
Different formulations of Pimozide 1 and 4 mg tablets designed to obtain a formulation that meets the parameters established by the United States Pharmacopeia XXII for controlling the quality of the finished product, as well as the necessary requirement for its coating, were studied. Among these formulations, the so-called PP fulfilled the established quality parameters before and after coating. The results obtained in the shelf life study of the coated tablets made at semiindustrial scale showen that even one year after their making they meet the specifications established by the Pharmacopeia, which supports the feasibility for their scale-up at industrial level.