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
