Pembentukan dan Karakterisasi Dispersi Padat Kandesartan Sileksetil-HPMC dengan Teknik Solvent Co-Evaporation
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Abstract
Candesartan cilexetil (CC) merupakan agen antihipertensi yang sangat efektif tetapi memiliki kelarutan yang buruk sehingga bioavailabilitasnya terbatas. Penelitian ini bertujuan untuk meningkatkan CC terdisolusi melalui pembuatan dispersi padat dengan hidroxypropylmethylcellulose (HPMC). Dispersi padat CC-HPMC dibuat menjadi 3 formula, yaitu 2:1, 1:1 dan 1:2 (b/b) menggunakan metode solvent co-evaporation. CC tunggal, campuran fisik dan dispersi padat yang terbentuk kemudian dikarakterisasi secara fisikokimia dan pengaruh variasi konsentrasi HPMC diselidiki terhadap laju disolusi. Hasil PXRD menunjukkan penurunan intensitas puncak pada dispersi padat. Analisis termal dengan DSC memperlihatkan titik leleh yang lebih rendah pada dispersi padat. Morfologi dispersi padat menggambarkan bentuk yang berbeda dibandingkan dengan CC tunggal dan campuran fisik. Spektrum inframerah menunjukkan sedikit pergeseran pada bilangan gelombang gugus fungsi tetapi tidak terbentuk gugus fungsi baru. Disolusi dispersi padat meningkat secara signifikan, hasil uji disolusi setelah 60 menit masing-masing untuk CC tunggal, campuran fisik, dispersi padat F1, F2, dan F3 adalah 32,46 ± 0,26; 67,76 ± 0,07; 61,22 ± 0,20; 71,74 ± 0,20; dan 78,58 ± 020 (μg/ml). Kesimpulannya, sistem dispersi padat CC-HPMC mampu memodifikasi sifat fisikokimia dan meningkatkan disolusi hingga 2,42 kali CC tunggal. Selain itu, peningkatan konsentrasi HPMC berdampak positif pada peningkatan CC yang terdisolusi.
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