灯盏花素自微乳的制备及其溶出度评价

Preparation and Dissolution Evaluation of Breviscapine Self-microemulsion

目的:研究灯盏花素自微乳的处方与制备工艺,并对其质量、稳定性以及溶出度进行评价。方法:通过溶解度考察、配伍试验与伪三元相图的绘制,以自乳化时间、外观、粒径和稳定性为指标,筛选并优化处方与制备工艺,并对自微乳的形态、含量、稳定性以及溶出度进行评价。结果:所得灯盏花素自微乳的处方组成:辛酸/癸酸甘油三酯(GTCC,40%)、Cremophor RH-40(50%)、PEG-400(10%),载药量7.0 mg/g,外观澄清透明,平均粒径38.57nm,粒度分布均匀,Zeta电位-8.80 m V。溶出度结果表明在0.1 mol/L盐酸中90 min药物累积溶出度可达90.30%,是原料药的5.9倍。稳定性结果表明高温影响药物含量,应低温保存。结论:灯盏花素自微乳制备工艺简单,改善药物溶解性,有利于胃肠道吸收,符合主要指标要求,为进一步开发与研究奠定基础。

Objective： To study the prescription and preparation technology of breviscapine self-microemulsion for oral administration,and to evaluate the quality,stability and in vitro dissolution. Methods： The prescription and preparation technology were selected and optimized through the solubility experiment,compatibility test,and pseudo-ternary phase diagram method,using the self-emulsifying time,appearance,particle diameter and stability as indexes. The droplet morphous,drug content,stability and dissolution were evaluated. Results： The prescription composition of breviscapine self-microemulsion was caprylic / capric triglyceride（ GTCC,40%）,Cremophor RH-40（ 50%）,and PEG-400（ 10%）,with the drug loading of 7. 0 mg / g. The breviscapine self-microemulsion exhibited uniform and transparent,with the particle size of 38. 57 nm,Zeta potential of- 8. 80 m V. The results of dissolution indicated that the accumulative dissolution in 0. 1 mol / L hydrochloric acid was able to reach 90. 30% after 90 min,being 5. 9 times to that of the raw material medicine. The stability result showed that the content of breviscapine self-microemulsion was affected by high temperature,indicating it should be stored at low temperature. Conclusion： The preparation of breviscapine self-microemulsion is simple,which can increase the solubility of breviscapine in water and the absorption of breviscapine in the stomach and intestine,and conform to the main indexes of oral drug delivery system. It offers the basis for further research of breviscapine.