Solid State Mechanochemical Simultaneous Activation of the Constituents of the Silybum marianum Phytocomplex with Crosslinked Polymers

Simultaneous improvement of solubilization kinetics of main flavolignans of Silybum marianum extract was obtained cogrinding with two crosslinked polymers: micronized crospovidone, PVP-CL1 and sodium carboxymethylcellulose, Ac-Di-Sol1 in the 1:3 active-to-polymer weight ratio. By this process it was assessed that the main extract components lost its crystalline structure, and the powder surface area was increased by 2.1- and 1.7-fold in the coground products with Ac-Di-Sol1 and PVP-CL1, respectively. This activated status of the dry extract remained stable over a period of 2 years. Solubilization kinetics resulted ameliorated both in terms of entire dry extract and in terms of single components. The in vivo studies on rats confirmed that this solubilization improvement corresponded to an effective oral bioavailability enhancement.