2011Zhongguo xin yao zazhiRequires access

Preparation and in vitro-in vivo correlation in Beagle dogs of levetiracetam sustained-release tablets

Lijuan Mao

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Abstract

Objective:To prepare levetiracetam sustained release tablets,and investigate in vitro-in vivo correlation in Beagle dogs.Methods:Mixed HPMC and EC matrix was used to prepare levetiracetam sustained release tablets.The in vitro release characteristics and in vivo pharmacokinetics in dogs of the tablets were investigated.Results:Higuchi model was optimal for the description of drug release profile.The mean elimination half-lives(t1/2) after administration of conventional tablets,reference sustained release tablets and our sustained release tablets were(2.09±0.45),(5.35±0.76) and(7.44±1.48)h,respectively.The peak levels were(1.184±0.38),(3.87±0.37) and(4.07±0.56)h;AUCs were calculated to be(175.40±15.47),(240.93±19.73) and(251.47±13.22)μg·h·mL-1,respectively.Conclusion:The levetiracetam sustained release tablets exhibit the sustained release characteristics in vitro,and show a good correction in vitro release and in vivo absorption.

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Objective:To prepare levetiracetam sustained release tablets,and investigate in vitro-in vivo correlation in Beagle dogs.Methods:Mixed HPMC and EC matrix was used to prepare levetiracetam sustained release tablets.The in vitro release characteristics and in vivo pharmacokinetics in dogs of the tablets were investigated.Results:Higuchi model was optimal for the description of drug release profile.The mean elimination half-lives(t1/2) after administration of conventional tablets,reference sustained release tablets and our sustained release tablets were(2.09±0.45),(5.35±0.76) and(7.44±1.48)h,respectively.The peak levels were(1.184±0.38),(3.87±0.37) and(4.07±0.56)h;AUCs were calculated to be(175.40±15.47),(240.93±19.73) and(251.47±13.22)μg·h·mL-1,respectively.Conclusion:The levetiracetam sustained release tablets exhibit the sustained release characteristics in vitro,and show a good correction in vitro release and in vivo absorption.

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Available abstract

Objective:To prepare levetiracetam sustained release tablets,and investigate in vitro-in vivo correlation in Beagle dogs.Methods:Mixed HPMC and EC matrix was used to prepare levetiracetam sustained release tablets.The in vitro release characteristics and in vivo pharmacokinetics in dogs of the tablets were investigated.Results:Higuchi model was optimal for the description of drug release profile.The mean elimination half-lives(t1/2) after administration of conventional tablets,reference sustained release tablets and our sustained release tablets were(2.09±0.45),(5.35±0.76) and(7.44±1.48)h,respectively.The peak levels were(1.184±0.38),(3.87±0.37) and(4.07±0.56)h;AUCs were calculated to be(175.40±15.47),(240.93±19.73) and(251.47±13.22)μg·h·mL-1,respectively.Conclusion:The levetiracetam sustained release tablets exhibit the sustained release characteristics in vitro,and show a good correction in vitro release and in vivo absorption.

Key concepts: Beagle, Levetiracetam, In vivo, Pharmacokinetics, Pharmacology, In vitro, Immediate release, Absorption (acoustics)

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