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本研究制备了一种新型的干粉吸入剂载体,并用于噻托溴铵的吸附和脱附应用。合成的药用花形载体乳糖微粒呈结晶态,含微-介-大孔均匀分布的孔结构,且具有高孔隙率、高载药量和高药物释放效率的优点。在噻托溴铵吸附研究中,采用溶液吸附法结合的噻托溴铵分子集中分布在花形微粒的内部,载体形貌变化小,测得的药物吸附量为5%(w/w,固体质量比),而采用结晶吸附法结合的噻托溴铵分子集中分布在花形微粒的外部,载体形貌变化大,测得的药物吸附量为49%(w/w)。此外,在载体的几何形貌影响下,采用溶液吸附法制备的制剂,其药物释放速率先快后慢;而采用结晶吸附法制备的制剂,其药物释放速率先慢后快。因此,该乳糖微粒可作为一种新型的药用载体,用于干粉吸入剂。
In this study, a new type of dry powder inhaler carrier was prepared and applied to the adsorption and desorption of tiotropium bromide. The synthetic medicinal flower-shaped carrier lactose particles are crystalline and contain micro-mesoporous macropores with uniformly distributed pore structure, and have the advantages of high porosity, high drug loading and high drug release efficiency. In the study of Tiotropium bromide adsorption, the Tiotropium bromide molecules adsorbed by solution adsorption concentrated on the interior of the flower-shaped particles, and the change of the carrier morphology was small. The measured drug adsorption was 5% (w / w, solid mass ), While the Tiotropium bromide molecules adsorbed by crystal adsorption concentrated on the outer part of the flower-shaped particles, and the morphology of the carrier changed greatly. The adsorbed amount of the drug was 49% (w / w). In addition, under the influence of the carrier morphology, the preparation prepared by solution adsorption method showed a faster and slower drug release rate. The drug release rate of the preparation prepared by the crystal adsorption method first and then slowed down. Therefore, the lactose particles can be used as a new type of pharmaceutical carrier for dry powder inhalers.