【摘要】：目的:制備他克莫司類脂囊泡(Tac-NS)并進(jìn)行體外表征。方法:采用薄膜水化-超聲法制備Tac-NS。以包封率(EE%)、載藥量、平均粒徑及粒徑分布(PDI)的綜合評(píng)分為指標(biāo),設(shè)計(jì)正交試驗(yàn)對(duì)硬脂山梨坦(Span-60)濃度、Span-60與膽固醇的摩爾比、Span-60與脫氧膽酸鈉(SDC)的摩爾比進(jìn)行優(yōu)化�？疾焖芓ac-NS的外觀形態(tài)、平均粒徑、PDI、Zeta電位及EE%,并通過體外經(jīng)皮滲透試驗(yàn)比較Tac-NS與Tac和NS物理混合物的累積經(jīng)皮滲透量(Q)、累積皮膚滯留量(Qs)。結(jié)果:最優(yōu)處方為Span-60 0.025mol/L,Span-60與膽固醇的摩爾比10∶1,Span-60與SDC的摩爾比15∶1,藥載比5%。所制Tac-NS形態(tài)圓整、分散均勻、很少有聚集,平均粒徑為(233.0±6.48)nm,PDI為0.266±0.021,Zeta電位為(-41.7±0.32)m V,EE%為(76.83±4.61)%。經(jīng)皮滲透試驗(yàn)表明,24 h后Tac-NS的Qs值約為物理混合物的2.4倍,而二者Q值相當(dāng)。結(jié)論:成功制得EE%高、粒徑小、分布均勻、透皮效果較為理想的Tac-NS。
[Abstract]:Objective: to prepare tacrolimus-like vesicles (Tac-NS) and characterize them in vitro. Methods: Tac-NS. was prepared by thin film hydration-ultrasound method. Taking EE%, drug loading, average particle size and size distribution of (PDI) as indexes, the orthogonal test was designed to determine the concentration of stearosortan (Span-60), the molar ratio of Span-60 to cholesterol, and the concentration of stearic sorbitan (Span-60) and the molar ratio of Span-60 to cholesterol. The molar ratio of Span-60 to sodium deoxycholate (SDC) was optimized. The appearance, average diameter, PDI,Zeta potential and EE%, of the prepared Tac-NS were investigated. The cumulative transdermal permeation of Tac-NS, Tac and NS was compared by in vitro transdermal permeation test. The cumulative skin retention of (Q), was compared with that of the physical mixture of Tac-NS and Tac and NS. Results: the optimal formulation was Span-60 0.025 mol / L, the molar ratio of Span 60 to cholesterol was 10 渭 1, the molar ratio of Spana 60 to SDC was 15 mol / L, and the drug loading ratio was 5%. The morphology of the prepared Tac-NS was round and uniform, with little aggregation. The average particle size was (233.0 鹵6.48) nm,PDI, the mean diameter was 0.266 鹵0.021, the Zeta potential was (- 41.7 鹵0.32) MV, and the EE% was (76.83 鹵4.61)%. The results of percutaneous permeation test showed that the Qs value of Tac-NS was about 2.4 times higher than that of physical mixture after 24 h, and the Q value of them was the same as that of physical mixture. Conclusion: the Tac-NS. with high EE%, small particle size, uniform distribution and better transdermal effect has been successfully prepared.
【作者單位】： 深圳市福田區(qū)第二人民醫(yī)院藥劑科;廣東醫(yī)學(xué)院附屬福田醫(yī)院藥劑科;
【分類號(hào)】：R943

【參考文獻(xiàn)】

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