Evaluation of Callinectes Chitosan as a Superdisintegrant in Metronidazole Tablet

Abstract

Objective: The objective of this study is to evaluate callinectes chitosan as a superdisintegrant in tablet formulation; superdisintegrants are incorporated into tablets at concentrations below 5% of tablet weight to effect prompt break-up of tablets after administration. Methods:Chitosan was extracted from shells of Callinectes gladiator. The polymer was characterized and then used as a disintegrant (in comparison with Ac-Di-Sol ® and corn starch) at concentrations of 2, 4 and 8% for the formulation of metronidazole tablets. The micromeritic properties of granules; and mechanical and release properties of the tablets were studied.Results: A yield of 36.7% chitosan having degree of deacetylation of 62.7% was obtained from the crab shell. Fourier Transform Infrared absorption bands at 1495 and 3240 cm -1 typical of N-H bending and stretching respectively; and endothermic peak of 159 °C typical of melting of chitosan were obtained. No adverse interaction between the chitosan and metronidazole was observed. The disintegration times of tablets containing 2, 4 and 8% chitosan were 12.2, 10.4 and 9.3 min respectively. Conclusion:Callinectes chitosan is suitable for use as a superdisintegrant in tablets. It appears to be superior to corn starch as disintegrant although less effective compared to Ac-Di-Sol ® . However, the relative cheapness and ready availability of chitosan would make it to be preferred to Ac-Di-Sol ® .

Evaluation of Chitosan-Microcrystalline Cellulose Blends as Direct Compression Excipients

“…The materials used include metronidazole powder (Hopkins and Williams, England), Merck Art 2330 microcrystalline cellulose (E. merck, Darmstadt), and chitosan obtained from shells of Callinectes gladiator having degree of deacetylation of 62.7% and viscosity of 2.88 mPas at 2% concentration, spindle #1, and 60 rpm [ 11 ]. Others are α -lactose monohydrate (Riedel De Haen Seelze, Hannover), magnesium stearate (BDH Poole, England), and talc (BDH Poole, England).…”

PHARMACEUTICAL EQUIVALENCE OF METRONIDAZOLE TABLETS USING THE FLOW-THROUGH CELL (USP APPARATUS 4) AND MEDIA OF PHYSIOLOGICAL pH RANGE

“…Several authors have reported a significant in vitro/in vivo correlation (IVIVC) between data obtained with the flow-through cell and human behaviour [8,9], which makes it a suitable option to estimate the release of the drug in the human body. On the other hand, in vitro dissolution studies with new metronidazole formulations have been reported, including release data with USP Apparatus 4 [10][11][12]. The aim of this work was to test four metronidazole commercial formulations, three generic drug products and the reference under the hydrodynamic environment of the flow-through cell (USP Apparatus 4) and dissolution media of physiological relevance (pH 1.2, 4.5, and 6.8) to document whether these formulations meet standard criteria to waiver in vivo studies and consider them pharmaceutical equivalents.…”

Pengaruh Variasi Konsentrasi Chitosan Sebagai Bahan Penghancur Terhadap Sifat Fisik Sediaan Orally Disintegrating Tablet (ODT) Paracetamol

“…Hal ini disebabkan fakta bahwa ketika kitosan dalam jumlah tinggi, penyerapan air ke dalam tablet menghasilkan pembentukan gel dari pada disintegrasi. Hasil ini konsisten dengan penelitian yang menunjukkan waktu hancur meningkat dengan konsentrasi kitosan 27 .…”

“…Setiap formula memenuhi persyaratan bahwa tidak kurang dari 80% bahan harus larut dalam waktu 30 menit 13 . Tingkat kelarutan konsisten dengan literatur; semakin rendah laju disolusi, semakin besar kandungan kitosan 27 . Hal ini berkorelasi dengan laju disintegrasi, semakin cepat tablet larut semakin cepat proses disolusinya 29 .…”