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Co-amorphous palbociclib-organic acid systems with increased dissolution rate, enhanced physical stability and equivalent biosafety.


ABSTRACT: The preparation of co-amorphous drug systems by adding a small molecular excipient is a promising formulation in the modern pharmaceutical industry to improve the solubility, dissolution rate, and bioavailability of poorly soluble drugs. In this study, palbociclib co-amorphous systems with organic acids (succinic, tartaric, citric, and malic acid) at molar ratios of 1 : 1 were prepared by co-milling and characterized by differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR) and solid-state nuclear magnetic resonance (SS-NMR). These solid-state investigations have confirmed the formation of co-amorphous salts between PAL and organic acids. The solubility, dissolution rate and stability of the four co-amorphous drug systems were significantly improved compared with these of crystalline and amorphous palbociclib. The biosafety of the co-amorphous drug systems was the same as that of palbociclib without affecting the efficacy of the drug and eliciting toxic side effects. These comprehensive approaches for the palbociclib-acid co-amorphous drug systems provided a theoretical basis for its clinical applications.

SUBMITTER: Zhang M 

PROVIDER: S-EPMC9060427 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature

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Co-amorphous palbociclib-organic acid systems with increased dissolution rate, enhanced physical stability and equivalent biosafety.

Zhang Man M   Xiong Xinnuo X   Suo Zili Z   Hou Quan Q   Gan Na N   Tang Peixiao P   Ding Xiaohui X   Li Hui H  

RSC advances 20190129 7


The preparation of co-amorphous drug systems by adding a small molecular excipient is a promising formulation in the modern pharmaceutical industry to improve the solubility, dissolution rate, and bioavailability of poorly soluble drugs. In this study, palbociclib co-amorphous systems with organic acids (succinic, tartaric, citric, and malic acid) at molar ratios of 1 : 1 were prepared by co-milling and characterized by differential scanning calorimetry (DSC), fourier transform infrared spectros  ...[more]

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