Abstract：
PURPOSE:To better understand the nature of drug-excipient interactions we have studied the phase behavior of amorphous binary and ternary mixtures of citric acid, indomethacin and PVP, as model systems. METHODS:We have prepared amorphous mixtures by co-melting or coprecipitation from solvents, and have measured glass transition temperatures with differential scanning calorimetry. RESULTS:Citric acid and indomethacin in the amorphous state are miscible up to 0.25 weight fraction of citric acid, equivalent to about 2 moles of citric acid and 3 moles of indomethacin. Phase separation, as reflected by two Tg values, occurs without crystallization leading to a saturated citric acid-indomethacin amorphous phase and one essentially containing only citric acid. PVP-citric acid and PVP-indomethacin form non-ideal miscible systems at all compositions. A ternary system containing 0.3 weight fraction of PVP produces a completely miscible system at all citric acid-indomethacin compositions. The use of 0.2 weight fraction of PVP, however, only produces miscibility up to a weight fraction of 0.4 citric acid relative to indomethacin. The two phases above this point appear to contain citric acid in PVP and citric acid in indomethacin, respectively. CONCLUSIONS:Two components of an amorphous solid mixture containing citric acid and indomethacin with limited solid state miscibility can be solubilized as an amorphous solid phase by the addition of moderate levels of PVP.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Lu Q,Zografi Gdoi
10.1023/a:1011983606606subject
Has Abstractpub_date
1998-08-01 00:00:00pages
1202-6issue
8eissn
0724-8741issn
1573-904Xjournal_volume
15pub_type
杂志文章abstract：PURPOSE:Formulate phospho-sulindac (P-S, OXT-328) in a Pluronic hydrogel to be used as a topical anti-inflammatory agent and study its efficacy, safety and pharmacokinetics in an arthritis model. METHODS:LEW/crlBR rats with Freund's adjuvant-induced arthritis were treated with P-S formulated in Pluronic hydrogel (PSH)...
journal_title：Pharmaceutical research
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：1992-04-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：1994-09-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：1998-05-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：1990-10-01 00:00:00
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更新日期：2010-09-01 00:00:00
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更新日期：2009-10-01 00:00:00
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更新日期：1997-09-01 00:00:00
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更新日期：2016-10-01 00:00:00
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更新日期：2011-09-01 00:00:00
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更新日期：2015-02-01 00:00:00
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更新日期：2020-02-19 00:00:00
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更新日期：2009-03-01 00:00:00
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更新日期：2015-02-01 00:00:00
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更新日期：2014-11-01 00:00:00
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更新日期：2004-10-01 00:00:00
