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KMID : 0369820120420030133
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Jorunal of Korean Pharmaceutical Sciences
2012 Volume.42 No. 3 p.133 ~ p.137
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Pharmacokinetic study of mucoadhesive metformin pellets in rats
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Piao Jing Shu
Lee Ji-Eun
Shin Dae-Hwan
Kim Jin-Seok
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Abstract
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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 streptozotocin-induced 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 μg 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 μg/mL and it was the highest among tested, followed by Na-CMC-coated pellets (15.10 ± 2.73), HPMC/carbopol-coated 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 μg 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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KEYWORD
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Metformin hydrochloride, Type II diabetes, Mucoadhesive polymer-coated pellet, Pharmacokinetics, Pharmacodynamics
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