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- W2125992078 abstract "The pharmaceutical cocrystal approach can be used to modify the properties of paliperidone. We report here two novel cocrystals, paliperidone 4-hydroxybenzoic acid cocrystal (1, 1 : 1, w/w) and paliperidone 4-aminobenzoic acid cocrystal (2, 1 : 1, w/w), with CCDC numbers of 855981 and 948923, which were constructed using paliperidone with 4-hydroxybenzoic acid and 4-aminobenzoic acid, respectively. The experimental results of the dissolution studies revealed that both 1 and 2 showed much faster dissolution rates than the original active pharmaceutical ingredient (API) in simulated gastric fluid media (pH = 1.2). The pharmacokinetic (PK) studies of 1, 2 and the original API were conducted using beagle dogs. 1 has a slightly higher maximal serum concentration, and both of the cocrystals presented considerably faster absorption rates after a single-dose oral administration to beagle dogs compared to the original API. Observed improvements suggested their potential application to the treatment of acute schizophrenia." @default.
- W2125992078 created "2016-06-24" @default.
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- W2125992078 date "2014-06-26" @default.
- W2125992078 modified "2023-09-23" @default.
- W2125992078 title "Dissolution and pharmacokinetic properties of two paliperidone cocrystals with 4-hydroxybenzoic and 4-aminobenzoic acid" @default.
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- W2125992078 doi "https://doi.org/10.1039/c4ce00784k" @default.
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