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不同药物混合比例干粉制剂中花粉状载体的吸入性能:与乳糖载体的比较。

Inhalation performance of pollen-shape carrier in dry powder formulation with different drug mixing ratios: comparison with lactose carrier.

机构信息

School of Chemical and Biomedical Engineering, Nanyang Technological University, 62 Nanyang Drive, Singapore.

出版信息

Int J Pharm. 2010 Feb 15;386(1-2):6-14. doi: 10.1016/j.ijpharm.2009.10.047. Epub 2009 Nov 14.

Abstract

In this study, the drug delivery performance of pollen-shape hydroxyapatite (HA) carriers is assessed and compared with conventional lactose (LA) carriers. Budesonide (Bd) is used as the model drug. Three drug mixing ratios of 2:1, 10:1 and 45:1 (carrier:drug, w/w) are used. The attachment of the drug with the carrier is characterized by sieving test. It is found that the drug content in the blends with HA particles is higher than the blends with LA. In vitro inhalation experiments are also conducted in an Andersen cascade impactor (ACI) equipped with a Rotahaler at gas flow rates of 30 and 60 L/min. The HA blends show high emitted dose (ED) of 82-90% at 30 L/min while the LA blends are observed to have ED of 69-82% at the same conditions. The high emission of the HA blends also allows high fine particle fraction (FPF) of 10-18% while the FPF of the LA blends are 3-15%. At a gas flow rate of 60 L/min, all the HA and LA blends show compatible ED (83-95% for HA blends and 82-84% for LA blends) and FPF (19-41% for HA blends and 21-34% for LA blends).

摘要

在这项研究中,评估了花粉状羟基磷灰石(HA)载体的药物输送性能,并与传统乳糖(LA)载体进行了比较。布地奈德(Bd)被用作模型药物。使用三种药物混合比(载体:药物,w/w),分别为 2:1、10:1 和 45:1。通过筛分试验来表征药物与载体的结合情况。结果发现,与 LA 颗粒相比,HA 颗粒混合物中的药物含量更高。还在配备 Rotahaler 的 Andersen 级联冲击器(ACI)中进行了体外吸入实验,气流速率为 30 和 60 L/min。在 30 L/min 时,HA 混合物的发射剂量(ED)高达 82-90%,而在相同条件下,LA 混合物的 ED 为 69-82%。HA 混合物的高发射率还允许高达 10-18%的细颗粒分数(FPF),而 LA 混合物的 FPF 为 3-15%。在气流速率为 60 L/min 时,所有 HA 和 LA 混合物均显示出相似的 ED(HA 混合物为 83-95%,LA 混合物为 82-84%)和 FPF(HA 混合物为 19-41%,LA 混合物为 21-34%)。

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