[Optimization of preparation process of floating sustained-release pellets of capsaicin based on nanometer CaCO3 by central composite design-response surface method].
OBJECTIVE
To prepare floating sustained-release pellets of capsaicin based on nanometer CaCO3.


METHODS
The floating sustained-release pellets were prepared by the dropping method with sodium alginate as matrix. The effects of the concentration of sodium alginate, the ratio of capsaicin to sodium alginate and the ratio of nanometer CaCO3 to sodium alginate on pellets were detected in the single-factor test. On that basis, central composite design-response surface method were used to optimize the formula, with the floating capacity, drug-loading rate and in vitro drug release property of pellets as indicators.


RESULTS
In the optimal formula, CaCl2 accounted for 1.87%, the ratio of nanometer CaCO3 to sodium alginate was 2.16:1, and the ratio of capsaicin to sodium alginate was 2.36: 1, respectively. Capsaicin sustained-release pellets prepared under the conditions featured round granule, even particle size. It could float on artificial gastric fluid for over 15 hours, showing good sustained-release effect. Its accumulative drug-release percent of pellets in vitro at 12 h were 89.93%.


CONCLUSIONS
The floating sustained-release pellets of capsaicin show good floating capacity and sustained-release effect after being optimized with central composite design-response surface method.
Key Laboratory of New Drug Delivery System of Chinese Meteria Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing 210028, China. chenxy1190@163.com
Xiao-Yun
XY
Chen
Zhen-Hai
ZH
Zhang
Xin
X
Jin
Xiao-Bin
XB
Jia
D000464:Alginates / Q000737:chemistry; D002119:Calcium Carbonate / Q000737:chemistry; D002211:Capsaicin / Q000737:chemistry* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical / Q000295:instrumentation / Q000379:methods*; D003692:Delayed-Action Preparations / Q000737:chemistry* / Q000493:pharmacokinetics; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D053758:Nanoparticles / Q000737:chemistry; D010316:Particle Size
D000464:Alginates; D003692:Delayed-Action Preparations; D006603:Hexuronic Acids; D020723:Glucuronic Acid; D002119:Calcium Carbonate; D002211:Capsaicin