The preparation of curcumin sustained-release solid dispersion by hot melt extrusion--------Ⅱ. Optimization of preparation process and evaluation in vitro and in vivo.
Summary of "The preparation of curcumin sustained-release solid dispersion by hot melt extrusion--------Ⅱ. Optimization of preparation process and evaluation in vitro and in vivo."
The purpose of this study was to optimize hot melt extrusion(HME) preparation process and evaluate in vitro and in vivo for developing curcumin sustained-release solid dispersion, to explore the possibility of HME for one-step preparation of insoluble drug sustained-release solid dispersion. The effect of three process parameters- barrel temperature, screw speed and cooling rate - were systematically studied. Physical state of curcumin sustained-release solid dispersion was characterized by DSC, XRD, FTIR. It was found that curcumin - Eudragit RS/RL system exhibited a good miscibility. Curcumin in the solid dispersion existed in an amorphous state and had molecular interactions with carriers. Stability studies showed no apparent difference of physical state of solid dispersion after 6 months. The mechanism of the curcumin release in sustained-release solid dispersion was a diffusion and dissolution coexisting action. Pharmacokinetics study showed the relative bioavailability of the curcumin in sustained-release solid dispersion to curcumin were 223.44%. The curcumin sustained-release solid dispersion have been successfully prepared by HME, significantly extending the half-life, ensuring a stable and effective blood concentration, and improving the bioavailability of curcumin. In conclusion, HME can be used to prepared sustained-release solid dispersion of a poorly water-soluble drug as a promising method.
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Journal Details
This article was published in the following journal.
Name: Journal of pharmaceutical sciences
ISSN: 1520-6017
Pages:
Links
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/31794699
- DOI: http://dx.doi.org/10.1016/j.xphs.2019.11.020
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