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RISS 인기검색어
- 검색키워드
- 저자 : Jingshu Piao (검색결과 3 건)
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Pharmacokinetic study of mucoadhesive metformin pellets in rats
Jingshu Piao,Ji-Eun Lee,신대환,김진석 한국약제학회 2012 Journal of Pharmaceutical Investigation Vol.42 No.3
Previously, we have reported the preparation and characterization of mucoadhesive pellets of metformin hydrochloride using four high-viscosity polymers including hydroxymethylcellulose (HPMC), HPMC/carbopol, sodium carboxylmethylcellulose (Na-CMC) and sodium alginate (Na-Alg) (Piao et al., Arch Pharm Res 32:391–397, 2009). Here, pharmacokinetic and pharmacodynamic evaluation of these metformin pellets was performed. Metformin pellets were administered orally to normal and streptozotocininduced diabetic rats at 100 mg/kg dose and the blood concentration of metformin and blood glucose levels were determined. The area under the plasma concentration versus time curve from the Na-Alg-coated metformin pellets in normal rats was 69.93 ± 39.63 lg h/mL and it was the highest among tested, followed by Na-CMC-coated pellets (58.38 ± 5.19), HPMC/carbopol-coated pellets (52.24 ±5.29), HPMC-coated pellets (42.70 ± 14.29) and metformin aqueous solution (33.49 ± 2.04). The Cmax from the Na-Alg-coated metformin pellets in normal rats was 29.47 ±10.74 lg/mLand itwas the highest among tested, followed by Na-CMC-coated pellets (15.10 ± 2.73), HPMC/carbopolcoated pellets (11.38 ± 3.04), HPMC-coated pellets (11.29 ± 3.85) and metformin aqueous solution (6.92 ±0.83). The area under the effect versus time curve of the Na-Alg-coated pellets in diabetic rats was the highest as 670.01 ± 211.20 lg h/mL, followed by CMC-coated pellets (542.42 ± 116.93), HPMC-coated pellets (539.46 ±189.91), HPMC/carbopol-coated pellets (444.03 ± 90.30),and metformin aqueous solution (199.28 ± 31.07). These data show that the Na-Alg-coated pellets were found to be the best among tested as a new mucoadhesive formulation for metformin hydrochloride prepared by the powder layering technique with a centrifugal fluidizing-granulator.
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Development of Novel Mucoadhesive Pellets of Metformin Hydrochloride
Jingshu Piao,이지은,원권연,김동욱,이정석,James D. S. Park,김진석,Yuichi Nishiyama,Ikuo Fukui 대한약학회 2009 Archives of Pharmacal Research Vol.32 No.3
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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