Seo S-A, Khang G, Rhee J M, Kim J, Lee H B
Department of Polymer Science and Technology, Chonbuk National University, Chonju, Korea.
J Microencapsul. 2003 Sep-Oct;20(5):569-79. doi: 10.1080/0265204031000148013.
In order to study the development of the delivery device of long-acting local anaesthetics for post-operative analgesia and control of chronic pain of cancer patient, fentanyl loaded poly(l-lactide-co-glycolide) (PLGA, molecular weight; 5000, 8000, 20,000, and 33,000 g/mole) microspheres (FMS) were studied. FMS were prepared by an emulsion solvent-evaporation method. The influence of several preparation parameters such as initial drug loading, PLGA concentrations, emulsifier concentrations, oil phase volume and mole ratio and molecular weight has been investigated on the fentanyl release patterns. Generally, the drug showed the biphasic release patterns, with an initial diffusion followed by a lag period before the onset of the degradation phase, but there were no lag times in the device. Fentanyl was slowly released from FMS over 10 days in vitro, with a quasi-zero order property. The release rate increased with increasing drug loading as well as increasing polymer concentration with a relatively small initial burst effect. From the results, FMS may be a good formulation to deliver the anaesthesia for the treatment of chronic pain.
为了研究用于术后镇痛和控制癌症患者慢性疼痛的长效局部麻醉剂给药装置的开发，对载有芬太尼的聚（左旋丙交酯-乙交酯）（PLGA，分子量分别为5000、8000、20000和33000 g/摩尔）微球（FMS）进行了研究。FMS采用乳液溶剂蒸发法制备。研究了几个制备参数，如初始药物载量、PLGA浓度、乳化剂浓度、油相体积、摩尔比和分子量对芬太尼释放模式的影响。一般来说，药物呈现双相释放模式，在降解阶段开始前，先是初始扩散，然后是一个滞后阶段，但在该装置中没有滞后时间。芬太尼在体外10天内从FMS中缓慢释放，具有准零级特性。释放速率随着药物载量的增加以及聚合物浓度的增加而增加，且初始突释效应相对较小。从结果来看，FMS可能是一种用于治疗慢性疼痛的良好麻醉剂给药制剂。
