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Peningkatan Disolusi dan Stabilitas Efavirenz Menggunakan Beberapa Metode Dispersi Padat
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Efavirenz merupakan obat terapi AIDS yang memiliki beberapa bentuk polimorf. Beberapa bentuk polimorf akan memiliki perbedaan dalam disolusi dan stabiltasnya. Dispersi padat merupakan dispersi bahan aktif farmasi kedalam pembawa yang hidrofilik, yang bertujuan untuk meningkatkan disolusi dan stabilitasnya. Beberapa metode dispersi padat efavirenz pada penelitian sebelumnya yang berpotensi dalam meningkatkan kelarutan, disolusi, dan stabilitas efavirenz diantaranya hot melt extrusion, penguapan pelarut, pengeringan semprot, pengeringan beku, dan pengadukan (kneading). Diantara kelima metode dispersi padat yang dapat dirujuk diantara metode lainnya dalam meningkatkan kelarutan, disolusi, dan stabilitas adalah hot melt extrusion karena telah dilakukan uji kelarutan dan disolusi dengan peningkatan kelarutan rentang hingga 5,45 kali dan peningkatan disolusi hingga 9 kali dibandingkan efavirenz murni, serta pengujian stabilitas tetap stabil setelah dilakukan selama 1-6 bulan. Namun metode lainnya terkecuali penguapan pelarut (karena tidak meningkatkan profil disolusi meskipun stabil dalam penyimpanan 1 bulan), seperti pengeringan semprot, pengeringan beku, dan pengadukan (kneading) dapat dijadikan rujukan untuk pengembangan dispersi padat untuk meningkatkan kelarutan, disolusi, dan stabilitas efavirenz. Peningkatan stabilitas setelah penyimpanan salah satunya ditandai dengan stabil dalam bentuk amorf, stabil atau serupa dalam kelarutan, profil pelepasan dan kandungannya. Perbaikan stabilitas penyimpanan dispersi padat perlu disesuaikan antara parameter metode dispersi padat (terutama suhu dan perilaku mekanis) dengan sifat pembawa dan atau eksipien lain yang akan digunakan (seperti pelarut, plastizer dsb.).
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