氢溴酸右美沙芬热敏型鼻用凝胶的制备及体外释放

Preparation of the dextromethorphan hydrobromide thermosensitive nasal gel and study on the drug release in vitro

目的制备氢溴酸右美沙芬热敏型鼻用凝胶,并对其体外释放行为进行考察。方法以热敏型材料泊洛沙姆407为主要辅料制备氢溴酸右美沙芬滴鼻液,采用立式扩散池对该制剂的体外释放行为进行研究。结果该制剂中含泊洛沙姆407质量分数为20%、PEG6000质量分数为2.5%时,室温下为液态,加热至33℃转变为半固状凝胶;药物从凝胶中的释放符合Higuchi方程(r>0.99)。结论该制剂制备简单,与一般鼻用制剂相比具有延长药物在鼻腔内的滞留时间、减少药液流失和避免对咽部的刺激等优点,具有开发前景。

Objective To prepare the dextromethorphan hydrobromide(DMH) thermosensitive gel for nasal drug delivery,and study the drug release in vitro.Methods Themosensitive material Poloxamer407 was used as the main excipient to prepare the nasal drop and a vertical diffusion cell was adopted to study the drug release.Result The solution containing 20%(w) poloxamer407 and 2.5%(w) PEG6000 is liquid state at room temperature,then undergoes a phase transition to a semisolid gel when being heated up to 33 ℃;drug release from poloxamer vehicle followed the Higuchi equation kinetics(r>0.99).Conclusion The preparation,with the unique advantages comparing to traditional nasal preparations,is simple to produce and shows great prospect.