聚己内酯埋植剂的制备及药物通透性研究

Preparation and the drug permeability of polycaprolactone implant

目的制备聚己内酯（PCL）长效药物缓释制剂,优化药物缓释效果,并研究PCL埋植剂的药物通透性.方法 合成分子质量为（8～16）×104 u含有普朗尼克F68的PCL,用挤出法制备不同壁厚的PCL长效缓释埋植剂.将左炔诺孕酮（LNG）装入PCL管封装,制成LNG药囊.通过高效液相色谱法测定LNG的释放效果,考察PCL的分子质量及PCL管壁厚度对LNG通透性的影响.结果 当PCL分子质量为（8～16）×104u时,对LNG通透性无显著影响.PCL管壁厚在0.20～0.40 mm时,对LNG通透性亦无显著影响;当壁厚小于0.15 mm时,LNG通透性显著提高.结论 PCL埋植剂对LNG具有通透性,可通过改变PCL管壁厚度增加药物通透性.

Objective To prepare polycaprolactone （PCL） implant with long-term sustained release,optimize the drug delivery effect and observe the permeability of PCL for drug.Methods PCL implant with average molecular weight of （8-16）×104 u were synthesized and extruded into tubes.The tubular capsules were filled with levonorgestrel （LNG）,closed at both ends.The drug release of PCL implant was measured by HPLC.The drug permeability of PCL implant was evaluated with different molecular weight and thickness.Results The molecular weight of （8-16）×104 u showed no effect on the permeability of PCL implant for LNG.The thickness of 0.20-0.40 mm of PCL membranes showed no effect on the permeability for LNG.The PCL membranes with the thickness of less than 0.15 mm had the higher permeability than those with the thickness of 0.20-0.40 mm.Conclusions The PCL implant is permeable for LNG and the permeability can be increased by decreasing the thickness of membrane.