Development of novel mucoadhesive pellets of metformin hydrochloride
| Autor: | Jingshu Piao, Kwon-Yeon Weon, Ji-Eun Lee, Yuichi Nishiyama, Ikuo Fukui, Dong-Wook Kim, Jin-Seok Kim, James D. S. Park, Jung Suk Lee |
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| Rok vydání: | 2009 |
| Předmět: |
Alginates
Polymers Chemistry Pharmaceutical Sodium Acrylic Resins Pellets chemistry.chemical_element Capsules Methylcellulose Dosage form Hypromellose Derivatives Glucuronic Acid Hardness Drug Discovery Mucoadhesion Zeta potential Animals Hypoglycemic Agents Dissolution testing Drug Carriers Chromatography Viscosity Chemistry Hexuronic Acids Organic Chemistry Mucins Adhesiveness Metformin Rats Kinetics Solubility Gastric Mucosa Carboxymethylcellulose Sodium Delayed-Action Preparations Molecular Medicine Polyvinyls Powders Drug carrier |
| Zdroj: | Archives of Pharmacal Research. 32:391-397 |
| ISSN: | 1976-3786 0253-6269 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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