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目的应用高效液相色谱法考察粉雾剂在肺部递送效率和药物的释放情况。方法以壳聚糖为载体,用喷雾干燥技术制备硫酸沙丁胺醇粉雾剂,乳糖制剂做参比。采用新一代药用撞击器,测定粉雾剂的排空率及有效部位沉积率;用“桨法”初步考察粉雾剂缓释能力。结果壳聚糖载体中药物的有效部位沉积率55%~65%,比乳糖制剂(11%)有显著性提高;在1min内药物经乳糖载体可释放出80%,壳聚糖载体中释放出等量药物需20min,说明壳聚糖粉雾剂缓释效果明显。结论本方法稳定,可靠,可用于吸入式药物在肺部分布情况的研究。
OBJECTIVE To study the delivery efficiency and drug release of powder aerosol in lungs by high performance liquid chromatography. Methods Chitosan was used as a carrier. Spray drying technology was used to prepare albuterol sulfate aerosol and lactose preparation. A new generation of medical impactor was used to measure the emptying rate of powder aerosol and the effective deposition rate. The “propeller method” was used to study the sustained release capacity of powder aerosol. Results The effective deposition rate of the drug in chitosan carrier was 55% -65%, which was significantly higher than that of lactose preparation (11%). The drug was released by lactose carrier at 80% in 1 min and released by chitosan carrier The same amount of drug required 20min, indicating that chitosan powder aerosol slow release effect is obvious. Conclusion The method is stable and reliable and can be used to study the distribution of inhaled drugs in the lungs.