Optimasi Formula Tablet Gastroretentive Mucoadhesive Levofloksasin Menggunakan Kombinasi Matriks Xanthan Gum dan Guar Gum

Afifa Naila Nabila, Prof. Dr. Akhmad Kharis Nugroho, M. Si., Apt.; Dr. Teuku Nanda Saifullah Sulaiman, M. Si., Apt.

2019 | Skripsi | S1 FARMASI

Levofloksasin merupakan pengembangan dari florokuinolon yang memiliki aktivitas antibakteria dengan spektrum luas. Salah satu penggunaan levofloksasin adalah untuk terapi infeksi Helicobacter pylori (H. pylori) pada mukosa lambung. Penelitian ini bertujuan untuk 1) mengidentifikasi pengaruh proporsi matriks mucoadhesive terhadap sifat fisik tablet dan 2) memperoleh formula optimum tablet gastroretentive mucoadhesive levofloksasin. Tablet dibuat dengan metode granulasi basah dengan menggunakan kombinasi xanthan gum dan guar gum sebagai matriks gastroretentive mucoadhesive. Kombinasi xanthan gum dan guar gum diharapkan mampu memberikan respon optimum pada kekuatan mucoadhesive dan pelepasan obat diperlambat (sustained release). Optimasi formula dirancang menggunakan metode Simplex Lattice Design dalam software Design Expert versi 11. Evaluasi tablet secara in vitro meliputi keragaman bobot, kekerasan tablet, kerapuhan tablet, swelling index, kekuatan mucoadhesive, dan uji disolusi. Formula optimum diverifikasi menggunakan metode analisis One Sample T-test. Hasil penelitian menunjukkan bahwa kombinasi xanthan gum dan guar gum memberikan pengaruh signifikan terhadap kekerasan, kerapuhan, swelling index, kekuatan mucoadhesive, dan disolusi obat (p-value < 0,05). Proposi optimum xanthan gum (23,53% b/b) dengan guar gum (26,47%b/b) memberikan sifat sinergis dalam meningkatkan kekuatan mucoadhesive dan memberikan profil pelepasan obat diperlambat.

Levofloxacin is a derivative form of the fluoroquinolone antimicrobials which has broad-spectrum antibacterial activity. Levofloxacin is used for Helicobacter pylori (H. pylori) infection treatment in the gastric mucosa. The aims of this study were 1) to identify the influence of the matrix proportion on tablet's physical properties and 2) to obtain an optimum formula of gastroretentive mucoadhesive levofloxacin tablet. The tablet was made by wet granulation method using a combination of xanthan gum and guar gum as mucoadhesive gastroretentive matrix. The combination of xanthan gum and guar gum is expected to provide an optimum response to mucoadhesive strength and sustained release dissolution profile. Formula optimization was designed based on Simplex Lattice Design method using Design Expert version 11 software. In vitro evaluation of tablets included weight variation, hardness, friability, swelling index, mucoadhesive strength, and dissolution test. The optimum formula was verified by One Sample T-test analysis. The results showed that the combination of xanthan gum and guar gum significantly influence the hardness, the friability, the swelling index, the mucoadhesive strength, and drug dissolution characteristic (p-value < 0.05). The optimum proportion of xanthan gum (23.53% b/b) with guar gum (26.47% b/b) provided synergistic properties in increasing mucoadhesive strength and optimize the sustained release drug dissolution profile.

Kata Kunci : levofloxacin, gastroretentive mucoadhesive, xanthan gum, guar gum