[关键词]
[摘要]
目的 制备去甲泽拉木醛(DMZ)醇质体及其凝胶剂,并考察其制剂性能和体外透皮特性。方法 采用注入法制备DMZ醇质体,并对其粒径、包封率、分析方法学及体外释放行为进行研究。采用改良的Franz扩散池进行醇质体凝胶的体外透皮试验。结果 DMZ醇质体外观为淡黄乳状液,平均粒径为(365.2±14.4)nm,包封率为(72.30±2.31)%。醇质体凝胶中DMZ的体外透皮行为符合Higuchi方程(Q=80.198 t1/2-71.641,r=0.986 8),其24 h的累积渗透量是普通凝胶的3.94倍。结论 醇质体凝胶可良好地改善DMZ的透皮行为,为雷公藤有效成分的局部透皮制剂的开发提供依据。
[Key word]
[Abstract]
Objective To prepare the ethosomes-based gel of demethylzeylasteral (DMZ) and to investigate its properties and transdermal absorption behavior. Methods The infusion method was used to prepare DMZ ethosomes. The particle size, entrapment efficiency (EE), analysis methodology, and in vitro release behavior were examined, respectively. The in vitro transdermal absorption of ethosomes-based gel of DMZ was evaluated by Franz diffusion cells. Results The DMZ ethosomes was yellowish emulsion. The average particle size of the ethosomes was (365.2 ± 14.4) nm and the EE was (72.30 ± 2.31)%. The cumulative permeation curve of DMZ in ethosomes-based gel was consistent with Higuchi equation (Q = 80.198 t1/2-71.641, r = 0.986 8). Compared with common gel, the ethosomes-based gel had 3.94 times higher cumulative permeation amount in 24 h. Conclusion The prepared ethosomes- based gel of DMZ could enhance the transdermal permeation, which provides evidence for the development of transdermal drug delivery system of DMZ.
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[基金项目]
浙江省重大科技专项重点社会发展项目(2010C13014);浙江省“重中之重”学科(针灸推拿学)开放基金项目(ZTK2010A13)