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Issue 7, 2019
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Co-amorphous palbociclib–organic acid systems with increased dissolution rate, enhanced physical stability and equivalent biosafety

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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.

Graphical abstract: Co-amorphous palbociclib–organic acid systems with increased dissolution rate, enhanced physical stability and equivalent biosafety

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Supplementary files

Article information


Submitted
26 Nov 2018
Accepted
23 Jan 2019
First published
29 Jan 2019

This article is Open Access

RSC Adv., 2019,9, 3946-3955
Article type
Paper

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

M. Zhang, X. Xiong, Z. Suo, Q. Hou, N. Gan, P. Tang, X. Ding and H. Li, RSC Adv., 2019, 9, 3946
DOI: 10.1039/C8RA09710K

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