Formula and Preparation Optimization and Properties Study of Exendin W/O/W Multiple Emulsion
10.3969/j.issn.1008-049X.2018.01.024
- VernacularTitle:艾塞那肽W/O/W复乳的处方工艺优化及性质考察
- Author:
Jun WANG
1
;
Junqiao XING
Author Information
1. 武汉大学人民医院药学部 武汉430060
- Keywords:
Exendin;
Multiple emulsion;
Formula and preparation optimization;
Sustained release
- From:
China Pharmacist
2018;21(1):100-104
- CountryChina
- Language:Chinese
-
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.