Pembentukan dan Karakterisasi Dispersi Padat Efavirenzs-Crospovidone

ABSTRACT: Efavirenz is a non-nucleosid reverse transcriptase inhibitor (NNRTI) approved for the treatment of human immunodeficiency virus (HIV) type I infection. Acording to BCS, efavirenz is classified into class II, which is necessary to increase its solubility and dissolution rate to enhance its oral bioavailability. One way to achieve that is solid dispersion formation. In this research, preparation of solid dispersion of efavirenz - crospovidone with solvent method using ethanol 96% had been done. The solid dispersion characterization of was carried out using X-ray diffraction, Differential Thermal Analysis (DTA), Scanning Electron Microscopy (SEM), Fourier Transform Infrared (FTIR) and particle size distribution analysis. The result were compared to physical mixture and pure compound. The solubility test was performed in CO2-free aquadest using an orbital shaker while dissolution rate was studied in CO2-free aquadest with Sodium Lauryl Sulphate (SLS) 0.5 % w/v. The result of solubility test showed that solubility of solid dispersions 1:1 ; 1:2 ; 2:1 (12,2071µg/mL ; 14,0522µg/mL ; 8303µg/mL) were higher than the physical mixture 1:1 ; 1:2 ; 2:1 (9,3786µg/mL ; 10,1532µg/mL ; 7,4899µg/mL) and pure efavirenz have the lowest solubility (6,9765µg/mL). From the results of the one-way ANOVA test for dissolution efficiency of the seven samples showed different results where the significance of the ANOVA is 0.000 (P<0.05), where the dissolution efficiency of solid dispersion 1:1 ; 1:2 ; 2:1 (42.9456 % ; 35.3712 % ; 48.1877 %) were lower than pure efavirenz (47.2471 %) , where as the physical mixture of 1:1 ; 2:1 and 1:2 shows the highest dissolution efficiency (62.9245 % ; 55.9456 % and 54.5427 %).
Keyword: efavirenz; crospovidone; solid dispersion; solubility
Penulis: Deni Noviza, Aisyah Fajriani, Erizal Z
Kode Jurnal: jpfarmasidd170130

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