Formulasi, Karakterisasi dan Efek Pengurangan Iritasi Lambung Self-Emulsifying Drug Delivery System Asam Mefenamat

Abstract

Background: Mefenamic acid is a non-steroidal anti-inflammatory drugs (NSAID). The effects of non-steroidal anti-inflammatory drugs (NSAID) are known to disrupt the gastric mucosa, triggering inflammation of the gastric mucosa. To reduce the effects of local irritation on the stomach, Self-Emulsifying Drug Delivery System (SEDDS) preparations are made. Objective: To formulate, characterize and reduce the local gastric irritation effect of self-emulsifying drug delivery system mefenamic acid (SEDDS). Method: The formulation of SEDDS preparations with variations in mefenamic acid doses (50, 100, 150, and 200 mg) and types of oils (sunflower oil, soyabean oil, and oleic acid) with a ratio of Tween 80 and PEG 400 was 2.5 : 1, then taken as a formula with soluble SEDDS to continue the characterization test including organoleptics, pH, density, particle size, zeta potential, content and solution. Furthermore, the stability test of the preparation was carried out including organoleptics, phase separation, particle size, pH and solution. Followed by testing the anti-inflammatory effect, and gastric irritation effect using rat test animals consisting of 3 groups with 6 rats each. Results: From the results of the study, the F12 formula (containing 50 mg of mefenamic acid and oleic acid oil) was taken as the best formula. From the characterization results, it was obtained that the particle size was 591.48±6.99 nm, the level was 101.23±5.70%, and the potential zeta was -7.16±0.32 mV. From the dissolution results, SEDDS was obtained 74.51% faster than suspension. In the antiinflammatory effect test, the AUC percent of SEDDS inflammation was obtained ± 123.45220.7458 %h, suspension 156.3363±1.2644 %h and aquadest 383.2299±0.8501 %h and the effect of gastric irritation of SEDDS was obtained with a total degree of lesion formed only 1 of erosion while in suspension the total degree of lesion formed 3 of erosion and 1 in the form of ulcer. Conclusion: Based on the results of the study, it can be concluded that the SEDDS F12 formula of mefenamic acid compared to mefenamic acid suspension has a reduction in gastric irritation effects and anti-inflammatory effects that are better than mefenamic acid suspension although not significant.