[In vitro and in vivo pharmaceutical behaviors of lycopene microcapsules].
OBJECTIVE
To evaluate in vitro release of lycopene microcapsules. Pharmacokinetic parameters of lycopene microcapsule and lycopene powder as reference were estimated after a single dose of oral administration to dogs. The relationship between in vitro dissolution and in vivo absorption was investigated.


METHODS
The content of lycopene in the release medium was determined by UV spectroscopy method. Health hybrid male dogs were used as experiment subjects and lycopene powder used as standard to estimate the pharmacokinetics of lycopene microcapsules. HPLC method was used to assay the concentration of lycopene in dog plasma. Pharmacokinetics parameters were estimated by 3P87 program. The drug release percentage in stimulated intestinal fluid was compared with the absorption at a given time point.


RESULTS
The release profiles of lycopene from microcapsule showed that the lycopene gelatin microcapsule exhibited enteric property. The pharmacokinetics parameters estimated after oral administration of lycopene powder and lycopene microcapsule in a single dose of 2.5 mg x kg(-1) body weight to dogs were 7.30 h, 15.06 h for T1/2alpha; 28.10 h, 46.76 h for T1/2beta; 22.32 h, 41.03 h for T(max); 1.67 microg x h x L(-1), 2.08 microg x h x L(-1) for AUC(0-infinity), respectively. The concentration-time curves could be fitted to a two-compartment model for both the lycopene powder and the lycopene microcapsule analyzed by 3P87 program. The relationship between in vitro dissolution and in vivo absorption was found to have good correlation (r = 0. 981 9) was found.


CONCLUSIONS
It could be concluded that lycopene microcapsule was a sustained release dosage form. The result of release in vitro could be used to predict the absorption in vivo.
Wang
Hui-Juan
HJ
Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.
Li
Xin-Ru
XR
Huang
Yan-Qing
YQ
Zhang
Yun-Long
YL
Hu
Xin
X
Liu
Yan
Y
D000284:Administration, Oral; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D002214:Capsules; D002338:Carotenoids / Q000008:administration & dosage / Q000493:pharmacokinetics*; D003692:Delayed-Action Preparations; D004285:Dogs; D000077276:Lycopene; D008297:Male
D000975:Antioxidants; D002214:Capsules; D003692:Delayed-Action Preparations; D002338:Carotenoids; D000077276:Lycopene