Pharmacokinetics of a novel nifedipine and pH-sensitive N-succinyl chitosan/alginate hydrogel bead in rabbits.
BACKGROUND
A novel N-succinyl chitosan/alginate hydrogel bead was prepared by the ionic gelation method for controlled delivery of nifedipine (NF).


OBJECTIVE
The delivery behavior of NF from the hydrogel bead was studied in rabbit body.


METHODS
Nitrendipine was used as the internal standard and the concentration of NF in serum was determined by reversed-phase high-performance liquid chromatography.


RESULTS
The assay was linear from 5 to 755 ng/mL. The limit of quantitation for NF was 5 ng/mL in serum, and the recovery was greater than 90%. The method was used to determine the concentration-time profiles of NF in the serum. The pharmacokinetic parameters were calculated by Drug and Statistics (ver 1.0) program. The mean Cmax was 320.2 ± 71.3 μg/L, the mean Tmax was 3.2 ± 0.5 hours, the mean t1/2 was 6.60 ± 2.17 hours, the mean AUC0-24 was 2.03 ± 0.25 mg h/L, the mean AUC0-∞ was 2.50 ± 0.36 mg h/L, the mean MRT0-24 was 8.57 ± 0.19 hours, and the mean MRT0-∞ was 15.2 ± 1.8 hours.


CONCLUSIONS
The pharmacokinetic characteristics were found by a two-compartment model following the oral administration of NF-loaded N-succinyl chitosan/alginate hydrogel beads in rabbits.
Zhu
Xu-Jiang
XJ
Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences, Lanzhou, PR China.
Yuan
Wei
W
Li
Ping
P
Liu
Xia
X
He
Jun-Quan
JQ
D000284:Administration, Oral; D000464:Alginates / Q000737:chemistry*; D000818:Animals; D019540:Area Under Curve; D002121:Calcium Channel Blockers / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D048271:Chitosan / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D020100:Hydrogels; D006863:Hydrogen-Ion Concentration; D008863:Microspheres; D009543:Nifedipine / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D011817:Rabbits
D000464:Alginates; D002121:Calcium Channel Blockers; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D006603:Hexuronic Acids; D020100:Hydrogels; C118639:N-succinyl-chitosan; D020723:Glucuronic Acid; D048271:Chitosan; D009543:Nifedipine