[Study on release mechanism of berberine hydrochloride-loaded carboxymethyl konjac glucomannan pellets for colonic delivery].
OBJECTIVE
To study release mechanism of berberine hydrochloride (BH) from carboxymethyl konjac glucomannan pellets for colonic delivery.


METHODS
The pellets were prepared by ionotropic gelation technique. The effects of the kinds of enzyme and enzyme concentration of dissolution media on the release of BH and the erosion properties of the pellets were studied.


RESULTS
Compared with the dissolution media without enzymes, the release of BH and the erosion of the pellets were increased obviously in the media with rat cecal and colonic content or beta-mannase, the degradation of the carrier material of pellets by enzymes was the main factor which result in the erosion of the pellets. With the increased of beta-mannase concentration, the release of BH and the erosion of the pellets increased, the amount relationships of the release of BH and the erosion of the pellets were approximately 1:1. The release of BH exhibit Peppas equation, the n value was more than 1.


CONCLUSIONS
The release mechanism of BH from the pellets was enzymatic erosion-controlled, which indicates the potential of the pellets to serve as a colon-specific drug delivery system.
Zhang
Yu
Y
School of Pharmacy, Henan University, Kaifeng 475004, China.
Ling
Chun-Sheng
CS
Hou
Shi-Xiang
SX
D000818:Animals; D001599:Berberine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001692:Biological Transport / Q000187:drug effects; D003106:Colon / Q000378:metabolism*; D016503:Drug Delivery Systems / Q000379:methods*; D008351:Mannans / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D044902:beta-Mannosidase / Q000494:pharmacology
D008351:Mannans; D001599:Berberine; C022901:(1-6)-alpha-glucomannan; D044902:beta-Mannosidase