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

Wuryanto Hadinugroho; Kuncoro Foe; Yudy Tjahjono; Caroline Caroline; Senny Yesery Esar; Hendy Wijaya; Maria Annabella Jessica

doi:10.1021/acsomega.2c03147

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

ACS Omega. 2022 Sep 12;7(38):34045-34053. doi: 10.1021/acsomega.2c03147. eCollection 2022 Sep 27.

Authors

Wuryanto Hadinugroho¹, Kuncoro Foe¹, Yudy Tjahjono¹, Caroline Caroline¹, Senny Yesery Esar¹, Hendy Wijaya¹, Maria Annabella Jessica¹

Affiliation

¹ Faculty of Pharmacy, Widya Mandala Surabaya Catholic University, Kalisari Selatan no. 1 Pakuwon City, Surabaya 60112, Indonesia.

Abstract

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 (3CH₂Cl) (log P = 3.73) tablet formulations. In addition, this study aims to determine the optimum of the 3CH₂Cl 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 3CH₂Cl (300 mg), Ne (9.38%), SLS (0.92%), CS (2.33%), MCC (5%), and SDL (ad 800 mg). 3CH₂Cl has analgesic activity despite the presence of tablet excipients. The 3CH₂Cl tablet is an innovative formulation and a new alternative for future analgesic drugs.