吡嘧司特钾鼻喷剂的制备与质量控制研究

Preparation and quality control of pemirolast potassium nasal spray

目的：本文制备适应症为过敏性鼻炎的吡嘧司特钾鼻喷剂并制定制剂的质量控制标准。方法根据吡嘧司特钾的理化性质以及鼻腔给药特点优化处方组成，并根据《中国药典》2010年版二部附录中对鼻用制剂及喷雾剂的要求，对制剂pH、性状、装量、每瓶总喷次、每喷喷量、沉降体积比及含量测定方法等进行考察，制定质量控制标准。结果吡嘧司特钾鼻喷剂的处方为：0.1％吡嘧司特钾，0.8％羧甲基纤维素钠，0.01％苯扎溴铵，pH调节剂为冰醋酸，溶剂为5％甘露醇溶液。该制剂为白色混悬液，pH值为7.0。平均装量为（25.12±0.16）mL，各瓶装量均大于23.75 mL（95％）；各瓶总喷次均大于160喷，每喷喷量均大于0.1400 g／揿；沉降体积比为1，以上检测项目等均符合规定，质量可控。吡嘧司特钾对照品的标准曲线为Y＝81085X＋15264，r＝0.9998，线性范围为0.5～25.0μg／mL。吡嘧司特钾对照品的鼻喷剂样品平均回收率为99.39％、精密度符合要求。吡嘧司特钾鼻喷剂供试品中吡嘧司特钾的含量为标示量的99.2％。结论本文制备得到的制剂制备方法简单，稳定性好，使用方便，质量可控，为进一步开发该药的鼻腔局部给药制剂提供了研究基础。

Objective To prepare pemirolast potassium nasal spray which could be used in treatment of allergic rhinitis and make a quality control standard for the preparation.Methods The preparation materials of nasal spray was selected which could meet the physical and chemical properties of pemirolast potassium as well as the characteristics of intranasal administration.The quality control standards for pemirolast potassium nasal spray was made according to the nasal spray quality standards for the formulation pH, property, loading capacity, total bottle spray times, puff volume, sedimentation volume ratio and detection of content of “Chinese Pharmacopoeia” two section （2010 edition）.Results The formulation prescription of pemirolast potassium nasal spray was：0.1% potassium pemirolast, 0.8% CMC-Na, 0.01% benzalkonium bromide, glacial acetic acid （ pH adjusting agent） and the solution was 5% mannitol.The formulation was a white suspension, pH=7.The mean value of installed capacity was （25.12 ＆#177;0.16） mL and installed capacity of each bottle was above 23.75 mL（95%）; total spray times of each bottle was above 160 sprays and spray volume was above 0.140 0 g/press; sedimentation volume ratio was 1, the above testing programmes of quality standard met the requirements and were controlled.The standard curve of pemirolast potassium reference substance was Y=81085X＋15264（r=0.999 8）, linearity range was 0.5～25.0μg/mL.The average recovery rate of pemirolast potassium sample was 99.39%, and precision met the requirements.The pemirolast potassium content of test sample was 99.2% of labeled amount.Conclusion The formulation prescription of pemirolast potassium nasal spray is suitable and the preparation is possessed several advantages such as stability, well-distributed spray, application convenience and quality controlled.Therefore, nasal administrated formulation of pemirolast potassium is potentially in further.