Pembentukan dan Karakterisasi Dispersi Padat Efavirenzs-Crospovidone
| Main Authors: | Noviza, Deni, Fajriani, Aisyah, Z, Erizal |
|---|---|
| Format: | Article info application/pdf eJournal |
| Bahasa: | ind |
| Terbitan: |
Fakultas Farmasi Universitas Andalas
, 2017
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| Online Access: |
http://jstf.ffarmasi.unand.ac.id/index.php/jstf/article/view/96 http://jstf.ffarmasi.unand.ac.id/index.php/jstf/article/view/96/79 |
Daftar Isi:
- 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 %).
- Efavirenz merupakan suatu non-nucleosid reverse transcriptase inhibitor (NNRTI) yang digunakan untuk mengatasi infeksi Human immunodeficiency virus (HIV) tipe 1. Efavirez termasuk ke dalam obat BCS Kelas II, dimana diperlukan upaya untuk meningkatkan kelarutan dan laju dissolusi untuk meningkatkan bioavailabilitas oralnya. Tujuan dari penelitian ini adalah meningkatkan kelarutan dari efavirenz dengan pembentukan dispersi padat dengan crospovidone sebagai pembawa. Pada penelitian ini dilakukan pembentukan dispersi padat efavirez – crospovidone dengan perbandingan efavirenz-crospovidone 1:1; 1;2 dan 2:1 (b/b), dengan metode pelarutan menggunakan etanol 96%. Karakteristik dispersi padat yang terbentuk dilakukan dengan analisis difraksi sinar-X, Fourtier Transform Infra Red, Scanning Electron Microscopy, Differential Scanning Calorimetry, analisis ukuran partikel dan uji kelarutan. Hasil uji kelarutan menunjukkan kelarutan dispersi padat 1:1 ; 1:2 ; 2:1 (12,207 μg/ml; 14,052 μg/ml ; 8,303 μg/ml) lebih tinggi dibandingkan campuran fisik 1:1 ; 1:2 ; 2:1 (9,378 μg/ml; 10,153 μg/ml ; 7,489 μg/ml) dan efavirenz murni memiliki kelarutan yang paling rendah (6,9765 μg/ml).