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[Relativities between lattice changes and the function of dissolution improvement of poorly soluble drug silymarin
Feng-qian Li1, Jin-hong Hu, Hui Wang
1Department of Pharmaceutical Sciences, Changhai Hospital, Second Military Medical University, Shanghai 200433, China.
Aim:
To investigate the lattice mechanisms involved in the increased dissolution effect of polyethylene glycol (PEG 6,000) dispersion system on poorly soluble drug silymarin (SILY).
Methods:
Fusion method was used to prepare the solid dispersions of SILY with PEG 6,000. Evaluation of the improvement of dissolution was performed with dissolution studies in vitro. X-ray powder diffraction combined with diffraction peak pattern-fitting procedure were applied to quantitatively analyze the changes of lattice parameters. The interaction of SILY and PEG 6,000 was also determined with Fourier transform-infrared (FT-IR) spectroscopy.
Results:
The dissolution rate of SILY was considerably increased when formulated in solid dispersion of PEG 6,000 as compared to pure SILY. The datum from the X-ray diffraction showed the changes in the lattic spacings and particular diffraction peaks (position and the intensity) of PEG 6,000 and SILY. These could explain the increased rate of SILY released from solid dispersion system. The information of FT-IR spectroscopy showed the absence of well-defined drug-polymer interaction.
Conclusion:
The dissolution improvement of poorly soluble SILY from solid dispersion of PEG 6,000 can be illuminated by the changes of the lattice parameters of PEG 6,000 and the drug.