摘要
目的制备苦参碱固体自微乳颗粒,并对其进行质量评价。方法通过固体吸附材料的优选,制备了苦参碱固体自微乳颗粒,建立了HPLC法测定颗粒中苦参碱及其体外溶出度的方法;对溶解后微乳的类型、pH值、Zeta电位、粒径进行研究。结果选择微粉硅胶与甘露醇质量比2∶1为固体吸附材料,每克苦参碱微乳液需加微粉硅胶0.42g,微晶纤维素0.21g,50℃恒温干燥后成淡黄色的苦参碱自微乳颗粒,遇水快速形成澄明的液体,平均粒径79nm,pH值为7.95,Zeta电位1.34mV,载药量23.51mg/g,45min内累积溶出94.2%以上。结论苦参碱固体自微乳的制备工艺简单,制剂稳定,可为水难溶性药物的开发提供一个新方法、新思路。
Objective To develop the matrine solid self-microemulsifying drug delivery syetem （S-SMEDDS） and to evaluate its quality. Methods The matrine solid self-microemulsifying granule was prepared through the optimization of solid adsorption material, the HPLC method and dissolution test were used to determine the drug content in matrine S-SMEDDS, and the particle form, pH value, Zeta potential, and particle size were studied after it was dissolved. Results The ratio of micro powder silica gel and mannitol （2∶1） was selected as the solid adsorption material, and 1 g of matrine micro-emulsion needed to add 0.42 g of micronized silica gel and 0.21 g of microcrystalline cellulose. The color of the matrine microemulsion particle was pale yellow after 50 ℃ constant temperature drying. Transparent liquid was formed quickly after it was dissolved. The average particle size was 79 nm, the pH value was 7.95, the Zeta potential was 1.34 mV, the drug loading was 23.51 mg/g, and the cumulative dissolution was over 94.2% within 45 min. Conclusion The preparation technology of matrine S-SMEDDS is simple and stable, and provides a means for the research and development of dissolvable drugs.
出处
《现代药物与临床》
CAS
2013年第4期511-514,共4页
Drugs & Clinic
