Preparation and Quality Evaluation of O/W-Type Nifedipine Transdermal Nanoemulsion / 中国药师

ABSTRACT

Objective:To optimize the formula of nifedipine nanoemulsion (NFNE) to lay foundation for the development of nifedipine transdermal preparation.Methods:The content of nifedipine as the index,the compositions in the formula were screened out by single factor experiments,and then the formula of NFNE was optimized by orthogonal tests with the ratio of emulsifier to co-emulsifier,ratio of mixed emulsifiers to oil phase and the amount of water as the influencing factors.N-Trimethyl chitosan (TMC) was used as the transdermal enhancer.The formula of TMC-NFNE was optimized by orthogonal tests with the degree of quaternization of TMC,the concentration of TMC solution and the amount of TMC solution as the influencing factors.The quality evaluation of TMC-NFME was determined including appearance,type identification,particle size and drug content.Results:The optimal formula was as follows7% ethyl oleate,32% Tween 80,16% alcohol,45%water and the mass ratio of TMC of 0.45%.The type of the emulsion was O/W.The content of NFNE,TMC20-NFNE,TMC40-NFNE and TMC60-NFNE was (12.76±0.22),(14.76±0.16),(12.26±0.18) and (12.92±0.27) mg·ml-1,respectively.The particle size was 13.62,17.10,16.26 and 17.25 nm,respectively.The morphology of the nanoemulsion was spherical.Conclusion:The optimal formula and preparation process of TMC-NFNE are simple with high drug content,which is worthy of further studies.