Optimization of the Preparation Technology of Nicotine-?-cyclodextrin Inclusion Compound by Orthogonal Test and Quality Evaluation / 中国药房

ABSTRACT

OBJECTIVE:To prepare nicotine-?-CD inclusion compound and evaluate its quality.METHODS:The inclusion complex was prepared by saturated water solution method,and the preparation conditions were optimized by orthogonal test with the ratio of nicotine to?-CD(A),the inclusion temperature(B),the inclusion time(C)as factors and with the inclusion rate and the yield as indexes for evaluation.The formation of the inclusion complexes were verified by inclusion equilibrium constant analysis and its dissolution characteristics in vitro were investigated.The stability of nicotine-?-CD inclusion compound and the mixture of nicotine and?-CD were studied by conducting high-temperature,high humidity and high light tests.RESULTS:The optimum preparation conditions for the inclusion compound were established asA was 13, B was 60℃and C was 2 hours.The inclusion rate of nicotine reached 65.28%;the yield was 79.55%,and the slow-release rate at 150 min was 92.26%.Under different temperature,humidity and high light conditions,the content of nicotine was always significantly higher in the inclusion complex than in the mixture.CONCLUSIONS:The inclusion technology is simple and the conditions were easily controllable,and the prepared nicotine-?-CD inclusion compound enjoys good stability and sustained-release property.