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Development of novel mucoadhesive pellets of metformin hydrochloride

Authors
Piao, JingshuLee, Ji-EunWeon, Kwon-YeonKim, Dong-WookLee, Jung SukPark, James D. S.Nishiyama, YuichiFukui, IkuoKim, Jin-Seok
Issue Date
Mar-2009
Publisher
PHARMACEUTICAL SOC KOREA
Keywords
Powder-layering; CF-granulator; Mucoadhesion; Polymer; Pellets; Metformin hydrochloride
Citation
ARCHIVES OF PHARMACAL RESEARCH, v.32, no.3, pp.391 - 397
Journal Title
ARCHIVES OF PHARMACAL RESEARCH
Volume
32
Number
3
Start Page
391
End Page
397
URI
https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/13817
DOI
10.1007/s12272-009-1312-0
ISSN
0253-6269
Abstract
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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