Objective To evaluate the pharmacokinetics(PK)properties of extended release formulations of buspirone hydrochloride in Beagle dogs.Methods A randomized,two period,two treatment,two sequence crossover bioequivalence s...Objective To evaluate the pharmacokinetics(PK)properties of extended release formulations of buspirone hydrochloride in Beagle dogs.Methods A randomized,two period,two treatment,two sequence crossover bioequivalence study was designed;six healthy Beagle dogs were randomly divided into two groups,each group was orally given buspirone tablets or buspirone extended capsule containing 15 mg buspirone hydrochloride.Blood samples(about 1 mL)were collected in heparinized tubes before dosing and at 0.33,0.67,1,2,3,4,6,8,10,12,18,24 h after administration,and were then immediately centrifuged at 3000 rpm for 15 min.The pharmacokinetics(PK)properties of the drugs were evaluated using the liquid chromatographic-tandem mass spectrometric(LC-MS/MS)method.Results The mean tmax was 4.7,0.8 h and Cmax values was 1.8,6.9 μg·L-1,respectively for the sustained-release test(capsule)and reference formulation(tablet).When compared to the tablets,the residence time of the sustained capsules was dramatically prolonged and Cmax was reduced(P<0.01).The initial release speed was slow and stable.The bioavailability was similar to the common tablets.Conclusions The sustained capsule had showed good pharmacokinetics property of sustained-release in the Beagle dogs.展开更多
文摘Objective To evaluate the pharmacokinetics(PK)properties of extended release formulations of buspirone hydrochloride in Beagle dogs.Methods A randomized,two period,two treatment,two sequence crossover bioequivalence study was designed;six healthy Beagle dogs were randomly divided into two groups,each group was orally given buspirone tablets or buspirone extended capsule containing 15 mg buspirone hydrochloride.Blood samples(about 1 mL)were collected in heparinized tubes before dosing and at 0.33,0.67,1,2,3,4,6,8,10,12,18,24 h after administration,and were then immediately centrifuged at 3000 rpm for 15 min.The pharmacokinetics(PK)properties of the drugs were evaluated using the liquid chromatographic-tandem mass spectrometric(LC-MS/MS)method.Results The mean tmax was 4.7,0.8 h and Cmax values was 1.8,6.9 μg·L-1,respectively for the sustained-release test(capsule)and reference formulation(tablet).When compared to the tablets,the residence time of the sustained capsules was dramatically prolonged and Cmax was reduced(P<0.01).The initial release speed was slow and stable.The bioavailability was similar to the common tablets.Conclusions The sustained capsule had showed good pharmacokinetics property of sustained-release in the Beagle dogs.
