摘要
目的筛选酮洛芬羟丙基-β-环糊精(KP-HP--βCD)凝胶剂的最佳处方,比较该凝胶剂与酮洛芬(KP)游离药物凝胶的离体皮肤渗透性,探讨包合物作为载体对KP经皮渗透的影响。方法以高温下KP含量变化作为稳定性指标,采用正交实验设计确立最佳处方。采用改良双室渗透池作为离体皮肤的渗透试验装置,测定KP在接受液内的累积透过药量和皮肤内的滞留药量。结果pH为7.0、每100 g凝胶剂中助溶剂丙二醇用量20mL、抗氧化剂NaHSO3为0.3 g时,包合物凝胶剂黏度适中,稳定性最好。包合物凝胶剂经皮渗透过程符合零级释放动力学,与游离KP凝胶剂相比,前者药物透过皮肤速率明显减慢,透皮24 h后,药物在皮肤内滞留量约为后者的2.5倍。结论KP-HP--βCD包合物凝胶剂处方设计合理,性质稳定。以包合物为KP载体、卡波姆为基质的凝胶剂具有促进药物进入皮肤的作用。
Objective To choose the best formulation of ketoprofen-hydroxypropyl-β-cyclodextrin （KP-HP-β-CD） compound gel, and to compare the transcutaneous permeation of KP-HP-β-CD inclusion compound gel with the free drug in gel. Methods Orthogonal design was used to observe the change of contents in high temperature for different formulation to choose the best formulation. The drug accumulated permeation percentage through the skin and the drug resident percentage using the improved double permeation ceils in vitro. Results Viscosity was proper and the concentration change was least when pH was 7.0 with adding 20 mL propylene glycol and 0.3 g NaHSO3. The rate of the transcutaneous permeation of inclusion compound gel is rather slowing down, and the drug resident percentage in the skin was 2.5 times compared with the free drug gel after 24 hours. Conclusion The formulation is reasonable, the property is stable, and the inclusion compound as the carrier has the ability to enhance the transcutaneous permeation of KP.
出处
《福建医科大学学报》
2007年第5期437-439,443,共4页
Journal of Fujian Medical University
基金
福建省科技厅青年科技人才资助项目(2004J045)
关键词
酮基布洛芬
包合物
凝胶剂
正交法
经皮渗透
ketoprofen
inclusion compound
gel
orthogonal design
transcutaneous permeation
