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Tablet Formulation of 2-((3-(Chloromethyl)benzoyl)oxy)benzoic Acid by Linear and Quadratic Models

[Image: see text] Purpose: This research determines the effect of sodium lauryl sulfate (SLS) as a surfactant, croscarmellose sodium (CS) as a disintegrating agent, and SLS–CS combinations on 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid (3CH(2)Cl) (log P = 3.73) tablet formulations. In addition, thi...

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Detalles Bibliográficos
Autores principales: Hadinugroho, Wuryanto, Foe, Kuncoro, Tjahjono, Yudy, Caroline, Caroline, Esar, Senny Yesery, Wijaya, Hendy, Jessica, Maria Annabella
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9520729/
https://www.ncbi.nlm.nih.gov/pubmed/36188286
http://dx.doi.org/10.1021/acsomega.2c03147
Descripción
Sumario:[Image: see text] Purpose: This research determines the effect of sodium lauryl sulfate (SLS) as a surfactant, croscarmellose sodium (CS) as a disintegrating agent, and SLS–CS combinations on 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid (3CH(2)Cl) (log P = 3.73) tablet formulations. In addition, this study aims to determine the optimum of the 3CH(2)Cl tablet formula. Methods: The tablets are manufactured through direct compression according to the simplex lattice design. The optimal SLS and CS concentration was determined in vitro using linear and quadratic models to achieve better tablet disintegration and dissolution. Results: The same linear and quadratic coefficient profiles of SLS and CS indicate that the combined coefficient of SLS–CS with a quadratic model can be used to predict the effect of the SLS–CS combination. Based on the linear model coefficients, SLS and CS increase the value of flow time (9.35; 7.65), Carr index (26.17; 21.17), hardness (9.84; 7.44), friability (0.38; 0.31), disintegrating time (5.74; 2.62), and drug release (84.28; 58.65). The quadratic model coefficient shows that SLS–CS combinations increase flow time (0.60), Carr index (2.00), hardness (1.00), and disintegrating time (1.04). Meanwhile, they decrease friability (−0.02) and drug release (−9.10). Conclusions: SLS, CS, and SLS–CS combinations affect the quality of tablet mass and tablets. The optimum tablet formula was 3CH(2)Cl (300 mg), Ne (9.38%), SLS (0.92%), CS (2.33%), MCC (5%), and SDL (ad 800 mg). 3CH(2)Cl has analgesic activity despite the presence of tablet excipients. The 3CH(2)Cl tablet is an innovative formulation and a new alternative for future analgesic drugs.