CAJ | 학술논문

为提高β-桉油醇的生物利用度与肝靶向性,将其包封为脂质体.利用超临界 CO_2 沉析技术,将脂质体膜材与β-桉油醇制成脂质体混悬液,再经真空干燥,制备了冻干β-桉油醇脂质体,并对脂质体形态、粒径、包封率、载药量、稳定性等各项理化参数进行测定与表征.考察了超临界CO_2压力、温度、共溶剂乙醇在CO_2中摩尔分数[x(CH_3CH_2OH)]等因素对脂质体制备的影响,在压力为 30 MPa,温度为338 K、x (CH_3CH_2OH) =15%条件下,脂质体包封率为87.2%,载药量为 5.9%,平均粒径为448.5 nm.所制备的冻干β-桉油醇脂质体具有良好的复水性能,包封率、溶出度、稳定性等理化性质均符合中国药典的规定,为β-桉油醇的肝靶向药物开发提供了固体制剂中间体.
위제고β-안유순적생물이용도여간파향성,장기포봉위지질체.이용초림계 CO_2 침석기술,장지질체막재여β-안유순제성지질체혼현액,재경진공간조,제비료동간β-안유순지질체,병대지질체형태、립경、포봉솔、재약량、은정성등각항이화삼수진행측정여표정.고찰료초림계CO_2압력、온도、공용제을순재CO_2중마이분수[x(CH_3CH_2OH)]등인소대지질체제비적영향,재압력위 30 MPa,온도위338 K、x (CH_3CH_2OH) =15%조건하,지질체포봉솔위87.2%,재약량위 5.9%,평균립경위448.5 nm.소제비적동간β-안유순지질체구유량호적복수성능,포봉솔、용출도、은정성등이화성질균부합중국약전적규정,위β-안유순적간파향약물개발제공료고체제제중간체.
b-eudesmol was incorporated into liposome in order to improve its bioavailability and target delivery to hepatic cells. The liposome suspension of b-eudesmol was formed by supercritical carbon dioxide (SC-CO_2) precipitation technology and was dried by vacuum freezing. The physicochemical properties of the freeze-dried liposome of b-eudesmol, such as the structure, size, entrapment efficiency and drug loading content, were measured. The effects of pressure, temperature of SC-CO_2 and mole fraction of cosolvent ethanol in SC-CO_2 (x(CH_3CH_2OH)) on liposome formation process were discussed. Under the found optimum operation conditions of 30 MPa, 338 K and x(CH_3CH_2OH)=15%, the entrapment efficiency, loading content and average size of the prepared liposome are 87.2%, 5.9% and 448.5 nm, respectively. The freeze-dried liposome of β-eudesmol has the good performance of redispersion in buffer solution. The physicochemical properties of the prepared liposome of β-eudesmol, such as entrapment efficiency, dissolution rate and stability, accord with the provisions of Chinese pharmacopoeia. The results show that the prepared liposome of β-eudesmol can be used as a solid immediate for the drug of liver cancer.