压力定量吸入气雾剂处方优化技术的研究进展

Advances of Formulation Optimization Techniques in Pressurized Metered Dose Inhalers

压力定量吸入气雾剂(pMDI)起效迅速、全身不良反应少、应用方便。目前正逐步采用环保型抛射剂氢氟烷烃(HFA)替代传统氟利昂(CFC),但因HFA所具有的独特性质,pMDI面临了诸多问题,如许多用于CFC处方中的辅料和药物在HFA中溶解度差、药物在HFA中的稳定性差等,这使得重新开发新型HFA-pMDI并进一步优化其性能成为必然。本文从处方前和制剂因素两方面,综述了pMDI在制剂技术优化方面的进展,并结合最新研究成果,提出未来pMDI的发展疗向。

Pressurized metered dose inhalers （pMDI） have advantages of rapid action, less side-effect and convenient for application. Nowadays, hydrofluoroalkane （HFA） which is friendly to environment will gradually substitute for the traditional propellant chlorofluorocarbon （CFC）. However, the unique physicochemical property of HFA exerts much problems for formulation, such as poor solubility of excipients and drugs which were used in formulations with CFC propellants, poor stability of drugs dissolved in HFA and so on. In conclusion, it is inevitable that we should optimize and re-develop novel pMDI with HFA propellant. The advances of formulation optimization techniques in pMDI from preformulation and formulation aspects are reviewed and the trend ofpMDI is suggested in this paper.