Development of a formulation of Pirodavir using 2-hydroxypropyl-β-cyclodextrin

被引:0
作者
Jef Peeters
Peter Neeskens
Marcus Eli Brewster
机构
[1] Johnson and Johnson,
[2] Chemical and Pharmaceutical Research,undefined
[3] Pharmaceutical Sciences,undefined
来源
Journal of Inclusion Phenomena and Macrocyclic Chemistry | 2007年 / 57卷
关键词
Pirodavir; Solubility; Cyclodextrins; Complexation capacity; Nasal formulation;
D O I
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学科分类号
摘要
Pirodavir, 4-[2-[1-(6-Methyl-3-pyridazinyl)-4-piperidinyl]ethoxy]benzoic acid ethyl ester, is an antiviral compound which has low aqueous solubility (<0.01 mg/ml). The compound is a weak base (pKa 5.8) with high lipophicity (logP 4.44). Ionization of the compound increases the solubility in acidic medium to 2.3 mg/ml at pH 2.4. However, a low pH is not acceptable for nasal application as this would induce irritation.
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页码:137 / 139
页数:2
相关论文
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