天然乳化剂阿拉伯胶对绿原酸自微乳体内外性能的影响

Effect of Natural Emulsifier Acacia Senegal on in vivo and in vitro Performance of Chlorogenic Acid Self-microemulsion

目的:研究天然乳化剂阿拉伯胶对绿原酸自微乳体内外性能的影响。方法:以阿拉伯胶逐步取代含非离子型乳化剂的绿原酸自微乳(简称"传统绿原酸自微乳")中的聚山梨酯80制成含阿拉伯胶的绿原酸自微乳(简称"新型绿原酸自微乳"),评价两种自微乳的外观、乳滴形态、粒径、电导率、p H值、稳定性、体外释放度和肠吸收动力学指标。结果:新型绿原酸自微乳采用阿拉伯胶取代了聚山梨酯80处方量的50%。传统和新型绿原酸自微乳的微乳液外观澄明,乳滴为近似球形,粒径分别为(24.53±3.03)、(35.51±5.91)nm,电导率分别为(195.6±0.3)、(189.5±0.4)μs/cm,p H分别为3.87±0.02、4.08±0.03(n=3)。与传统绿原酸自微乳比较,新型绿原酸自微乳在十二指肠、空肠、回肠中的吸收速率常数、有效渗透系数和吸收量均略有增加(P>0.05),在结肠中的上述指标均明显降低(P<0.05)。结论:新型绿原酸自微乳可保持传统绿原酸自微乳的性能,并能增加绿原酸在小肠的吸收。

OBJECTIVE： To study the effect of natural emulsifier acacia senegal on in vivo and in vitro performance of chloro- genic acid self-microemulsion. METHODS： Chlorogenic acid self-microemulsion containing acacia senegal （＂new chlorogenic acid self-microemulsion＂） was prepared by using acacia senegal to gradually replace polysorbate 80 in chlorogenic acid self-microemul- sion containing nonionic emulsifier （＂traditional chlorogenic acid self-microemulsion＂ ）. The appearance, morphology, particle size, conductivity, pH value, stability, in vitro release and intestinal absorption kinetics of the 2 kinds self-microemulsions were evaluated. RESULTS： 50% of polysorbate 80 was replaced by acacia senegal in new chlorogenic acid self-microemulsion. The tradi- tional and new chlorogenic acid self-microemulsions had clear appearance, and approximately spherical drops. Particle sizes were （24.53 ±3.03）, （35.51± 5.91） nm; dectrical conductivities were （195.6± 0.3）, （189.5 ± 0.4） μs/cm; and pH were 3.87±0.02, 4.08 ± 0.03 （n=3）, respectively. Compared with traditional chlorogenic acid self-microemulsion, the absorption rate constant, ef- fective permeability coefficient and absorption amount of the new one in duodenum, jejunum, ileum were increased a little （P〉 0.05）; the above indexes in colon were obviously decreased （P〈0.05）. CONCLUSIONS： The new chlorogenic acid self-micro- emulsion can maintain the performance of traditional one, and increase absorption of chlorogenic acid in small intestine.