Transdermal Delivery of Piroxicam by Surfactant Mediated Electroporation

A lipophilic, nonsteroidal antiinflammation drug, piroxicam, was administered by skin electroporation using short, high-voltage pulses. The transdermal delivery of piroxicam during the electroporation was buffered due to the higher partition in skin lipids than in aqueous environments, which is called entrapment. Entrapment is the main resistance to transdermal delivery of lipophilic drugs. Two types of surfactants were used to enhance the skin electroporation. Tween 80 （0.2 g/L） and sodium dodecyl sulphate （SDS, 3 mg/mL） improve the solubility and diffusion rate of the drug in the hydrophobic local transport regions and reduce the entrapment of piroxicam in the skin. The transdermal delivery rate of piroxicam is increased 30- to 50-fold. However, the entrapment of piroxicam in the skin still occurred when Tween 80 was added. The SDS provides higher and more stable transdermal delivery rates of piroxicam than Tween 80, and also reduces the entrapment of piroxicam in the skin.     

格列吡嗪控释微球的制备及体外释药性质

为研究口服药物控释微球的制备及其体外释药性质,以格列吡嗪为模型药物,采用喷雾干燥法制备具有恒速释药性质的微球.通过考察微球的收率、包封率以及体外释放特性,研究了载体材料、材料与药物比例以及药物释放环境对格列吡嗪控释微球释药性质的影响.结果表明,采用醋酸纤维素为载体材料,选用合适的配方,可制得具有零级释药动力学的格列吡嗪控释微球制剂,并且该制剂可以根据需要的条件在12 h或24 h内释放完毕.不同条件下微球的药物释放曲线线性拟合的相关系数在0.981～0.999之间.     

5-氟尿嘧啶结肠定位释药微囊的制备与释药特性

为制备结肠定位给药制剂,研究囊材溶剂、药物/囊材质量比对微囊性质和药物体外释放特性的影响。以水溶性抗癌药5-氟尿嘧啶为模型药物,选用丙烯酸树脂Eudrag itS100为材料制备了pH控制的结肠定位给药微囊。结果表明:采用液中干燥法制备的5-氟尿嘧啶微囊载药量为14.47%,微囊包封率为96.68%,在人工胃液、人工小肠液中10 h的累积释放率为18.5%。实验表明,微囊的体外释放特性具有结肠定位释药的特征。     

聚羟基丁酸酯缓释微粒作用下的埋植给药系统

制备了以壳聚糖水凝胶为基质的温度敏感型、可注射、并能够在体内生物降解的新型皮下埋植制剂,考察了该制剂中水溶性小分子药物的体外释放规律。为降低该类药物的释放速度,首先利用溶剂非溶剂法,以生物可降解的聚羟基丁酸酯为骨架,制备了抗癌药物5-氟尿嘧啶的微粒。在优化配比下,微粒收率达90%以上,包封率95%左右;然后将微粒温敏型水凝胶耦合制成复合给药系统。药物微粒化与温敏型水凝胶的耦合有效地控制了药物植入初期的“突释”问题,并将药物的释放周期延长至将近10个月。