Evaluation of tetrandrine sustained release calcium alginate gel beads in vitro and in vivo.
An approach for the preparation of tetrandrine sustained release calcium alginate gel beads was described. In vitro the release of tetrandrine from sustained release dosage forms went on a time of 12 hours which fitted non-Fickian diffusion with matrix erosion significantly. In vivo the plasma concentration of tetrandrine extended preparation given in dogs reached Cmax 2.67+/-0.69 microg/ml approximately at 5.67+/-0.58 h after oral administration. The AUC0-->24 and AUC0-->infinity were 24.64+/-6.77 mg.h/l and 29.75+/-5.30 mg.h/l, respectively. The elimination half-time was 9.6+/-2.40 h. While a favorable correlation existed between in vitro and in vivo with a correlative coefficient of 0.9798 through linear regression. An investigation on the quantitative relationship between in vitro release and in vivo absorption is a highly necessary work guided for manufacture, optimization and in vivo evaluation of sustained release dosage by means of in vitro release or dissolution tests.
Ma
Yan
Y
College of Chinese Traditional Medicine, Guangzhou University of Chinese Medicine, Guangzhou, People's Republic of China. mygzhtcm@163.com
Li
Wei-Zhong
WZ
Guan
Shi-Xia
SX
Lai
Xiao-Ping
XP
Chen
Da-Wei
DW
D000284:Administration, Oral; D000464:Alginates; D000818:Animals; D044182:Benzylisoquinolines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D003692:Delayed-Action Preparations; D004285:Dogs; D005782:Gels; D020723:Glucuronic Acid; D006603:Hexuronic Acids; D066298:In Vitro Techniques; D007408:Intestinal Absorption; D012995:Solubility; D013997:Time Factors
D000464:Alginates; D044182:Benzylisoquinolines; D003692:Delayed-Action Preparations; D005782:Gels; D006603:Hexuronic Acids; C009438:tetrandrine; D020723:Glucuronic Acid