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KMID : 0043319960190040280
Archives of Pharmacal Research
1996 Volume.19 No. 4 p.280 ~ p.285
Preparation and in Vitro Release of Melatonin-Loaded Multivalent Cationic Alginate Beads
Lee Beom-Jin

Min Geun-Hong
Kim Tae-Wan
Abstract
The sustained release dosage form which delivers melatonin (MT) in a circadian fashion over 8 h is of clinical value for those who have disordered circadian rhythms because of its short halflife. The purpose of this study was to evaluate the gelling properties and release characteristics of alginate beads varying multivalent cationic species . The surface morphologies of Ca- and Ba-alginate beads were also studied using scanning electron microscope (SEM). MT, an indole amide pineal hormone was used as a model drug. The $Ca^{++}, \; Ba^{++}, \; Zn^{++}, \; Al^{++}\; and\; Fe^{+++}\; ions\; except\; Mg^{++}$ induced gelling of sodium alginate. The strength of multivalent cationic alginate beads was as follows: $Al^{+++}\llFe^{+++} concentration was optimal in terms of trapping efficiency of MT and gelling strength of Ca-alginate beads. In the gastric fluid, Ca-alginate beads gelled at 0.2 M concentration had higher bead strength, resulting in the most retarded release when compared to other concentrations. In the intestinal fluid, the decreased release of Ca-alginate beads prepared at 0.2 M concentration was also observed. However, release profiles of Ca-alginate beads were quite similar regardless of concentration. Either too low or high concentrations may not be useful for gelling and curing of alginate beads. Optimal concentrations must be decided in terms of trapping efficiency and release and profiles of drug followed by curing time and gelling strength of alginate beads.
KEYWORD
Melationin, Multivalent cationic alginate beads, SEM, Release, profiles, Trapping efficiency
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