Abstract：
:The addition of polysorbate 20 (T20) is required to achieve "sink" conditions during a dissolution test for tablets with candesartan cilexetil (CC). Polysorbate 20 (0.35%-0.7% w/w) added to 0.05 mol/L of phosphate buffer pH 6.5 dramatically increased the apparent solubility of the drug from 0.8 μg/ml even to 353 μg/ml, while its effect in lower pH or in water was much smaller (20 μg/ml in pH 4.5). The increased concentration of phosphate salts (0.2 mol/l) at pH 6.5 in the presence of 0.7% of polysorbate 20, resulted in further increase of candesartan cilexetil solubility to 620 μg/ml. The change of pH from 1.2 to 7.4 resulted in a 1.5-fold increase of the activation energy and, depending on temperature, 8-14-fold decrease of the degradation rate. When polysorbate 20 increased the activation energy 2-fold, independent of pH, it protected candesartan cilexetil from degradation; however, this effect was temperature dependent and was very small at 310 K-the degradation rate in pH 6.5 decreased by 13% only. It was calculated that in the phosphate buffer pH 6.5 with polysorbate, one can expect during 24 h the degradation at the level of 9.3%, thus a flow-through dissolution apparatus was recommended for testing prolonged release dosage forms.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Hoppe K,Sznitowska Mdoi
10.1208/s12249-014-0109-8subject
Has Abstractpub_date
2014-10-01 00:00:00pages
1116-25issue
5issn
1530-9932journal_volume
15pub_type
杂志文章abstract：:Nanoparticles, of the poorly water-soluble drug, itraconazole (ITZ), were produced by the Advanced Evaporative Precipitation into Aqueous Solution process (Advanced EPAS). This process combines emulsion templating and EPAS processing to provide improved control over the size distribution of precipitated particles. Spe...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
pub_type： 传,历史文章,新闻
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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更新日期：2006-01-01 00:00:00
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pub_type： 杂志文章
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pub_type： 杂志文章,评审
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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