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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.
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 differentiated 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, The pharmacokinetics (PK) properties of the drugs were evaluated using the liquid chromatographic-tandem mass spectrometry (LC-MS / MS) method. Results The mean tmax was 4.7, 0.8 h and Cmax values were 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 sustained capsules was dramaticall The initial release speed was slow and stable. The bioavailability was similar to the common tablets. Conclusions The sustained-release capsule had showed good pharmacokinetics property of sustained-release in the Beagle dogs.