Hadinugroho Wuryanto, Foe Kuncoro, Tjahjono Yudy, Caroline Caroline, Esar Senny Yesery, Wijaya Hendy, Jessica Maria Annabella
Faculty of Pharmacy, Widya Mandala Surabaya Catholic University, Kalisari Selatan no. 1 Pakuwon City, Surabaya 60112, Indonesia.
ACS Omega. 2022 Sep 12;7(38):34045-34053. doi: 10.1021/acsomega.2c03147. eCollection 2022 Sep 27.
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 (3CHCl) (log = 3.73) tablet formulations. In addition, this study aims to determine the optimum of the 3CHCl tablet formula.
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.
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).
SLS, CS, and SLS-CS combinations affect the quality of tablet mass and tablets. The optimum tablet formula was 3CHCl (300 mg), Ne (9.38%), SLS (0.92%), CS (2.33%), MCC (5%), and SDL (ad 800 mg). 3CHCl has analgesic activity despite the presence of tablet excipients. The 3CHCl tablet is an innovative formulation and a new alternative for future analgesic drugs.
本研究确定月桂醇硫酸酯钠（SLS）作为表面活性剂、交联羧甲基纤维素钠（CS）作为崩解剂以及SLS - CS组合对2 - ((3 - (氯甲基)苯甲酰基)氧基)苯甲酸（3CHCl）（log = 3.73）片剂制剂的影响。此外，本研究旨在确定3CHCl片剂配方的最佳值。
根据单纯形格子设计通过直接压片法制备片剂。使用线性和二次模型在体外确定最佳的SLS和CS浓度，以实现更好的片剂崩解和溶解。
SLS和CS相同的线性和二次系数曲线表明，具有二次模型的SLS - CS组合系数可用于预测SLS - CS组合的效果。基于线性模型系数，SLS和CS增加了流动时间值（9.35；7.65）、卡尔指数（26.17；21.17）、硬度（9.84；7.44）、脆碎度（0.38；0.31）、崩解时间（5.74；2.62）和药物释放（84.28；58.65）。二次模型系数表明，SLS - CS组合增加了流动时间（0.60）、卡尔指数（2.00）、硬度（1.00）和崩解时间（1.04）。同时，它们降低了脆碎度（-0.02）和药物释放（-9.10）。
SLS、CS和SLS - CS组合影响片芯和片剂的质量。最佳片剂配方为3CHCl（300 mg）、Ne（9.38%）、SLS（0.92%）、CS（2.33%）、MCC（5%）和SDL（加至800 mg）。尽管存在片剂辅料，3CHCl仍具有镇痛活性。3CHCl片剂是一种创新制剂，是未来镇痛药的新选择。
