STUDI INHIBISI EKSTRAK MENIRAN (PHYLLANTHUS NIRURI) TERHADAP METABOLISME NEVIRAPINE SECARA IN VITRO

• Main Author: Permata, Gilang
• Format: Final Project
• Language: Indonesia
• Online Access: https://digilib.itb.ac.id/gdl/view/70329
• Institution: Institut Teknologi Bandung

Nevirapine is one of anti-HIV agents classified as NNRTI (Non Nucleoside Reverse Transcriptase Inhibitors). Metabolism of nevirapine involves liver microsome enzymes (CYPs 450). Co-administration of nevirapine with immunostimulant, such as meniran (Phyllanthus niruri L.) extracts may cause drug interactions. This study was to evaluate inhibition of nevirapine metabolism in vitro originated by meniran extracts in male Wistar rat liver microsomes. Liver microsomes were isolated from male Wistar rat using differential centrifuge. In vitro inhibition study of meniran extracts was perfomed by incubation of nevirapine (0.19; 1.88; 9.39; 18.78; 28.16; 37.55; 56.33 ?M) in liver microsomes in the absence or presence of meniran extracts (7.5 and 15 ?g/mL) for 5 min, and terminated by addition of acetonitrile. Remaining nevirapine concentrations were analyzed by HPLC. Km and Vmax values were calculated. Km and Vmax values of nevirapine metabolism in the absence of the extracts were 207.4 ?M and 6997 ?M.mg-1 protein.hr-1, respectively. Whereas Km and Vmax values in the presence of the extracts decreased: 146.9 ?M and 4575 ?M.mg-1 protein.hr-1 for 7.5 ?g/mL extracts; 40.02 ?M and 2583 ?M.mg-1 protein.hr-1 for 15 ?g/mL extracts. Inhibition constant of meniran extract was 7.885 ?g/mL. In vitro study of meniran extracts showed un-competitive inhibition to enzyme metabolizing nevirapine.