摘要
目的:对硝苯地平纳米乳(NFNE)的处方进行优化,为研发硝苯地平透皮吸收制剂奠定基础。方法:以纳米乳的溶药量为指标,通过单因素初步筛选处方组成;以乳化剂与助乳化剂的质量比、混合乳化剂与油相的质量比及含水量为因素,采用正交试验优选NFNE的处方;N-三甲基壳聚糖(TMC)作为透皮吸收促进剂,以TMC的季铵化程度、TMC水溶液浓度及TMC水溶液用量为因素,采用正交试验研究TMC的加入对NFNE的影响。通过外观、粒径、类型鉴别及溶药量等方面对NFNE优选处方进行质量评价。结果:NFNE最优的处方组成为油酸乙酯-吐温80-无水乙醇-水,用量分别为7%、32%、16%、45%,TMC的质量比为0.45%。NFNE、TMC20-NFNE、TMC40-NFNE、TMC60-NFNE均为O/W型乳剂,溶药量分别为(12.76±0.22),(14.76±0.16),(12.26±0.18),(12.92±0.27)mg·ml^(-1),平均粒径分别为13.62,17.10,16.26,17.25 nm,外观均为圆球形。结论:优化的硝苯地平纳米乳处方及制备工艺简单,溶药量大,值得进一步研究。
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 follows： 7% 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, TMCA0-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.
出处
《中国药师》
CAS
2017年第4期668-673,共6页
China Pharmacist
