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目的:优选盐酸川芎嗪脂质体的制备工艺,为川芎嗪的临床应用提供参考。方法:采用HPLC测定盐酸川芎嗪含量,流动相甲醇-0.2%三乙胺水溶液(加冰乙酸调节p H 5.0)(60∶40),检测波长295 nm。利用薄膜分散法制备盐酸川芎嗪脂质体,以包封率为评价指标,磷脂和胆固醇为膜材,通过正交试验考察水合时间、胆固醇和磷脂质量比、盐酸川芎嗪和磷脂质量比、磷脂质量分数对制备工艺的影响,考察脂质体包封率、形态、粒径、稳定性和Zeta电位。结果:最佳制备工艺条件为水合时间30 min,胆固醇-磷脂(1∶2),盐酸川芎嗪-磷脂(1∶15),磷脂质量分数3%;盐酸川芎嗪脂质体包封率(70.27±0.58)%,外观接近球形,粒径(22.9±6.8)nm,Zeta电位(-29.79±1.24)m V,于4℃保存2周后稳定性良好。结论:优选的制备工艺合理、稳定,可促进盐酸川芎嗪的体内吸收并延长其作用时间。
OBJECTIVE: To optimize the preparation of Ligustrazine Hydrochloride liposomes and provide a reference for the clinical application of Ligustrazine. Methods: The content of ligustrazine hydrochloride was determined by HPLC. The mobile phase consisted of methanol - 0.2% triethylamine in water (pH = 5.0 with glacial acetic acid) (60:40). The detection wavelength was 295 nm. Ligustrazine hydrochloride liposomes were prepared by membrane dispersion method. The encapsulation efficiency was taken as the evaluation index, and phospholipid and cholesterol were used as membrane materials. The hydration time, mass ratio of cholesterol and phospholipid, the mass ratio of ligustrazine to phospholipid, phospholipid The influence of mass fraction on the preparation process was investigated. The entrapment efficiency, morphology, particle size, stability and Zeta potential of liposomes were investigated. Results: The optimal preparation conditions were as follows: hydration time 30 min, cholesterol-phospholipid 1: 2, ligustrazine-phospholipid 1:15, phospholipid 3%, tetramethylpyrazine hydrochloride liposome encapsulation efficiency 70.27 ± 0.58)%, the appearance was close to spherical, the particle size was (22.9 ± 6.8) nm and the zeta potential was (-29.79 ± 1.24) mV, and the stability was good after storage for 2 weeks at 4 ℃. Conclusion: The optimal preparation process is reasonable and stable, which can promote the absorption of tetramethylpyrazine hydrochloride in vivo and prolong its action time.