[Optimization of a novel mucoadhesive drug deliver system with ion-exchange resin core loaded with berberine hydrochloride using central composite design methodology].
A novel mucoadhesive microcapsule with drug-resin complex core loaded with berberine hydrochloride (BH) was developed and optimized. Drug-ion exchange resin (IER) complex was prepared by static method which stirring IER in drug solution at certain conditions. The influences of different IERs, different temperature, pH values and concentrations of drug solution on the drug loading were investigated. IER complex was coated by emulsion-solvent evaporation method. The coating fluid formulation was optimized using central composite design-response surface methodology, where the ratio between Carbopol 934 and IER (X1), the ratio between Eudragit and IER (X2) and the ratio between Eudragit RL and RS (X3) were taken as independent variables. Time of cumulative release 85% (Y1) and percentage of gastric retention (Y2) were taken as response variables. Drug loading achieved a high level and more drug available in the condition of IER (IRP 88), 37 degrees C, pH 5 and 1.0 mg x mL(-1) drug solution. When X1 = 0.75, X2 = 0.9, X3 = 0.6, the time of cumulative release reached 85% at 300 min, the highest percentage of gastric retention in the range of this experiment were procured.
Chen
Fei
F
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
Zhang
Yue
Y
Liu
Qiang
Q
Pang
Ming-zhi
MZ
Yang
Xing-gang
XG
Pan
Wei-san
WS
D000179:Acrylates / Q000737:chemistry; D000818:Animals; D001599:Berberine / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D002214:Capsules; D003692:Delayed-Action Preparations; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems; D004655:Emulsions; D005753:Gastric Mucosa / Q000378:metabolism*; D006863:Hydrogen-Ion Concentration; D007475:Ion Exchange Resins / Q000737:chemistry*; D008297:Male; D011108:Polymers / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D013696:Temperature
D000179:Acrylates; D002214:Capsules; D003692:Delayed-Action Preparations; D004655:Emulsions; D007475:Ion Exchange Resins; D011108:Polymers; D001599:Berberine; C058665:Eudragit RL; C453622:carbopol 934P