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KMID : 0043320090320030391
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Archives of Pharmacal Research
2009 Volume.32 No. 3 p.391 ~ p.397
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Development of Novel Mucoadhesive Pellets of Metformin Hydrochloride
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Kim Jin-Seok
Fukui Ikuo
Nishiyama Yuichi
Park James D.S.
Lee Jung-Suk
Kim Dong-Wook
Weon Kwon-Yeon
Lee Ji-Eun
Piao Jing-Shu
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Abstract
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Mucoadhesive polymer-coated pellets containing metformin hydrochloride were prepared by the powder-layering technique using a centrifugal fluidizing (CF)-granulator. Four high-viscosity polymers were applied to make the pellets: 1) hydroxymethylcellulose (HPMC), 2) sodium alginate (Na-Alg), 3) HPMC/Carbopol, and 4) sodium carboxylmethylcellulose (Na-CMC). The physical crushing test, mucoadhesive test, zeta-potential test, in vitro release study and observation of gastroretention state of the dosage form were performed to investigate the pellets. The strong adhesive interaction between the Na-CMC-coated pellets and the mucin disc was obtained by mucoadhesive test. Na-Alg was most effective among the polymers used in changing the value of zeta potential of the mucin solution by the interaction between a polymer and a mucin particle. Results from drug dissolution study showed that over 95% of the drug from all the four pellets was released before 2 h, while Na-CMC- and Na-Alg-coated pellets showed a moderate sustained-release in SGF (simulated gastric fluid) and SIF (simulated intestine fluid), respectively. In conclusion, Na-CMC and Na-Alg seem to be promising candidates for mucoadhesive formulation and further studies to improve the sustained-release property are underway for achieving the ultimate goal of once-a-day formulation of metformin hydrochloride.
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KEYWORD
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Powder-layering, CF-granulator, Mucoadhesion, Polymer, Pellets, Metformin hydrochloride
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