Mucoadhesive dosage form is a pharmaceutical dosage form with prolonged gastric residence time which can increase bioavailability of drugs. An excipient with suitable swelling and bioadhesive characteristics plays important role to obtain good mucoadhesive dosage form. Our pre-eliminary study showed that chitosan-xanthan gum polyelectrolyte complex (CXPC) in ratio 1:1 exhibit suitable swelling index to be developed as mucoadhesive dosage forms. This research was performed to study CXPC characteristics as matrix for mucoadhesive granules dosage form matrix. In this study CXPC 1:1 was utilized as the matrix in the mucoadhesive granules with drug-CXPC ratio of 1:1, 1:2, and 1:3, using diltiazem HCl as a drug model. The granules were prepared by wet granulation method, and the in vitro bioadhesive properties of the granules, as well as the drug release profile, were evaluated. The results showed that formula containing diltiazem HCl and CXPC in ratio of 1:2 possessed a good bioadhesive ability up to 8-12 hours and showed controlled drug release profile up to 8 hours. The results can be concluded that the CXPC is a suitable excipient as a mucoadhesive matrix.

Bahasa Abstract

Sediaan mukoadhesif merupakan bentuk sediaan farmasi dengan waktu tinggal di lambung yang lebih panjang sehingga dapat meningkatkan bioavalilabilitas obat. Untuk membuat sediaan mukoadhesif ini diperlukan eksipien yang dapat menempel pada mukosa lambung dan memiliki daya mengembang yang sesuai untuk mengatur pelepasan obat dari sediaan. Berdasarkan studi pendahuluan diketahui bahwa kompleks polielektrolit kitosan-xanthan dengan perbandingan 1:1 memiliki daya mengembang yang sesuai untuk dikembangkan sebagai sediaan mukoadhesif. Penelitian ini bertujuan untuk meneliti kemampuan eksipien kompleks polielektrolit kitosan-gum xanthan (KPKX) sebagai matriks sediaan granul mukoadhesif tertahan di lambung. Pada penelitian ini KPKX 1:1 digunakan sebagai matriks pada granul mukoadhesif dengan perbandingan obat dengan KPKX (1:1, 1:2, dan 1:3), dengan diltiazem HCl sebagai model obat. Granul dibuat dengan metode granulasi basah, kemudian diuji kemampuan menempel secara in vitro, serta profil pelepasan obatnya. Hasil evaluasi menunjukkan bahwa formula yang mengandung diltiazem HCl dengan KPKX 1:2 mampu tetap menempel di mukosa lambung hingga 8-12 jam dan menunjukkan profil pelepasan obat yang terkendali hingga 8 jam. Penelitian ini dapat disimpulkan bahwa KPKX dapat merupakan eksipien yang sesuai untuk digunakan sebagai matriks mukoadhesif.


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