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http://dx.doi.org/10.4333/KPS.2003.33.3.179

Release and Characterization of Multiple Coated Pellets Containing Melatonin  

Kang, Bok-Ki (Department of Polymer Science and Technology, Chonbuk National University)
Khang, Gil-Son (Department of Polymer Science and Technology, Chonbuk National University)
Kim, Jong-Min (Department of Advanced Organic Materials Engineering, Chonbuk National University)
Jeung, Sang-Young (Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology)
Lee, Hai-Bang (Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology)
Cho, Sun-Hang (Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology)
Publication Information
Journal of Pharmaceutical Investigation / v.33, no.3, 2003 , pp. 179-185 More about this Journal
Abstract
Melatonin (MT) is an indole amide pineal hormone. It has not only very short half-life but also pH-sensitive property. The sustained release dosage form which delivers MT in a circadian fashion over 8 h is clinical value. The purpose of this study is to prepare sugar beads using multiple coating methods and enteric-coated in a sustained release to evaluate in vitro release characteristics in simulated gastric and intestinal fluids. The $Eudragit^{\circledR}$ as a polymer, sustained release membrane, and triethylcitrate (TEC) as a plasticzer were used. Multi-coated melatonin delivery system was composed of sugar, various excipients, $Eudragit^{\circledR}$ and enteric materials (e.g. hydroxy propyl methyl cellulose phthalate, HPMCP), and prepared by fluid bed coater. The dissolution test was carried out using the basket method at a stirring speed of 100 rpm at $37^{\circ}C$ in simulated gastric (pH 1.2) and intestinal fluid (pH 7.4). The released amount of MT was determined by High performance liquid chromatography method. The morhologies of surface and cross section of multi-coated beads were observed by scanning electron microscope. Size of multi-coated sugar beads was ranged over $1000{\sim}1300\;{\mu}m$. The release rate of MT from coated beads was limited in simulated gastric fluid (pH 1.2), but it was sustained in intestinal fluid (pH 7.4) during $3{\sim}8$ hours. The MT beads may provide small-intestine-targeted device for oral delivery. Studies on animal and relative experiment are in process.
Keywords
Melatonin (MT); Multi-coated beads; Enteric coating; Control release;
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