双氯芬酸钠泊洛沙姆凝胶体外释放的影响因素研究

Factors influencing the in vitro release of diclofenac sodium from poloxamer gels

目的:以双氯芬酸钠为模型药,研究泊洛沙姆407(P407)制剂体外释放的影响因素。方法:采用无膜释放法考察不同P407浓度、振荡频率、温度、等渗调节剂、附加剂等对凝胶溶蚀和药物释放的影响。结果:随振荡频率的增加及等渗调节剂PBS,NaC l或葡萄糖的添加,凝胶溶蚀和药物释放增加;P407浓度增加及处方中加入羟甲基纤维素钠(CMC-Na)、羟丙甲纤维素(HPMC)、甲基纤维素(MC)、羧甲基壳聚糖(O-CMC)等抑制了凝胶溶蚀和药物释放;温度升高药物释放加快而对凝胶溶蚀没有明显影响。结论:药物释放主要取决于凝胶溶蚀,可通过调节处方中影响凝胶溶蚀及药物扩散的因素来控制药物从407凝胶中的释放。

Objective：To study the factors that influence the release of diclofenac sodium from poloxamer 407 gels. Methods： The non-membrane model was used for study, and the following factors were included for comparison including poloxamer 407 concentration, shaking frequency, temperature, isotonic agents, and additives. Results： The release rate was increased with the rise of shaking frequency, and the addition of isotonic agents such as PBS, NaCl or glucose. The erosion and the drug release rate were decreased with the increase of poloxamer 407 concentration or the addition of sodium carboxymethyl cellulose （CMC-Na）, hydroxylpropylmethyl cellulose （HPMC）, methyl cellulose （MC） or O-carboxym- ethyl chitosan （O-CMC）. An increase in temperature did not alter the erosion but improve the drug release rate. Conclusion： The release rate mainly depends on the erosion of the gels and can be regulated by the influencing factors in the gel formulation.