3种鼻喷雾剂中混悬液的理化性质和喷雾性能比较

Comparison of physicochemical properties and spray performances among three suspensions in nasal sprays

目的:比较临床上用于治疗变应性鼻炎的一种布地奈德鼻喷雾剂中的含药混悬液(A)和2种糠酸莫米松鼻喷雾剂中的含药混悬液(B和C)的理化性质和喷雾性能。方法:采用流变仪、粒度分析仪、HPLC、喷雾模式和喷雾形态分析仪测定流变学性质、粒径大小和分布、物理稳定性、溶出度和喷雾性能。结果:3种鼻喷雾剂中的混悬液都具有良好的物理稳定性,皆为假塑性流体,A的黏度和触变性显著小于B和C;A,B和C中药物颗粒的D90分别为56.30,145.43和90.33μm;在3 cm处,喷雾面积分别为740.28,341.27和604.39 mm^(2);喷雾液滴的D90分别为73.66,138.11和109.16μm;喷雾液滴的可呼吸分数均<2.00%,即至少98.00%的雾滴>10μm,符合《中华人民共和国药典》的有关标准;A中药物溶出度最高,为2.15%。结论:与B和C相比,A的药物颗粒和喷雾液滴较小,黏度和触变性也较小,溶出度较高。

Objective:To compare the physicochemical properties and spray performances of suspensions in one budesonide nasal spray(A)and two mometasone furoate nasal sprays(B and C)for treatment of allergic rhinitis.Methods:The rheological property was measured by a rheometer.The particle/droplet size and distribution were measured by the particle/droplet size measurement system.The dissolution rates were measured by HPLC.The spray pattern and plume geometry were measured by the spray pattern and plume geometry measurement system.Results:The three suspensions in nasal sprays had good physical stability and they were all pseudoplastic fluids.The viscosity and thixotropy of suspension A were significantly lower than that of B and C.The particle sizes(D90)of A,B and C were 56.30,145.43 and 90.33μm,respectively.The spray areas of A,B and C at 3 cm were 740.28,341.27,604.39 mm^(2),respectively.The droplet sizes(D90)of A,B and C at 3 cm were 73.66,138.11 and 109.16μm,respectively.The respirable fractions of the droplets of all three nasal sprays were less than 2.00%.In other words,at least 98%of the droplets were larger than 10μm,so the droplet sizes of all three nasal sprays met the standard of Chinese Pharmacopoeia.The drug dissolution rate in A was the highest,which was 2.15%.Conclusion:Compared with B and C,A has smaller drug particles,smaller spray droplets,lower viscosity,lower thixotropy and higher dissolution rate.