Abstract：
:A drug's solubility in a polymeric excipient is an important parameter that dictates the process window of hot-melt extrusion (HME) and product stability during storage. However, it is rather challenging to experimentally determine the solubility and there is very few published work in this field. In this study, the solubility of a model drug acetaminophen (APAP) in a pharmaceutical grade polymer poly(ethylene oxide) (PEO) at HME processing temperature was measured utilizing rheological analysis, hot-stage microscopy and differential scanning calorimetry (DSC). The results from three methods were consistent and the solubility was found to increase from 14% at 80°C to 41% at 140°C. The apparent drug solubility at room temperature was estimated to be less than 10% through glass transition temperature (T(g)) measurement using DSC and dynamic mechanical thermal analysis (DMTA). A "phase diagram" was constructed based on the experimental data and could be explored to design the HME process and formulation. Very few assumptions were made in the experimental study and result analysis, and the methods described here can be applied to investigate other drug-polymer systems to obtain the important thermodynamic data.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Yang M,Wang P,Suwardie H,Gogos Cdoi
10.1016/j.ijpharm.2010.10.026subject
Has Abstractpub_date
2011-01-17 00:00:00pages
83-9issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(10)00801-Xjournal_volume
403pub_type
杂志文章abstract：:Dry powder inhalers (DPIs) are widely used to deliver respiratory medication as a fine powder. This study investigates the physical mechanism of DPI operation, assessing the effects of geometry, inhalation and powder type on dose fluidisation. Patient inhalation through an idealised DPI was simulated as a linearly inc...
journal_title：International journal of pharmaceutics
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pub_type： 临床试验,杂志文章,随机对照试验
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