Formula and Preparation Optimization and Properties Study of Exendin W/O/W Multiple Emulsion / 中国药师

ABSTRACT

Objective:To optimize the formula and preparation of exendin W /O/W multiple emulsion , and study the main proper-ties in vitro to lay foundation for the development of exendin prolonged action preparation .Methods:Using multiple emulsion yield and centrifugal separation time as the comprehensive index , the formula and preparation of exendin multiple emulsion were optimized by or-thogonal tests, and the morphology, particle size, stability, encapsulation efficiency and drug release in vitro were studied.Results:The optimal formula was as follows:the volume ratio of W1 phase to O phase was 1:1.2, the quality percentage of emulsifierⅠin the O phase was 10％, poloxamer 407 in W2 phase was 10％, and the quantity ratio of W1/O to W2 phase was 1:1.The optimal prepara-tion conditions were as follows:the stirring speed for W1/O was 10000 r· min-1 , and the stirring time was 10 min, and that for W1/O/W2 was 2500 r· min-1 with the stirring time of 3 min.The multiple emulsion was spherical with the mean size of (46.3 ±2.6)μm, and the centrifugal and viscosity stability were both promising .The drug encapsulation efficiency was above 90％, and the drug release in vitro accorded with a Higuchi equation: Y=13.7930X+5.5981(r=0.9883), showing notable sustained and prolonged property .Conclusion:The optimal formula and preparation process of exendin multiple emulsion are simple with high drug content , good stability and notable sustained release property in vitro.