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The Research on Effect-enhancing and Toxicity-reducing of Rhubarb Total Anthraquinones Caused by Oral Colon-specific Drug Delivery System When Producing Purgative Efficacy

Lin Zhang, Xiaodong Gu, Hongwei Wei, Xigang Liu, Pei Liu, Jinhua Chang, Qiang Fu, Cuizhe Liu

In the present study, we aimed to prepare rhubarb total anthraquinones oral colon-specific drug delivery granules (RTA-OCDD-GN) for delivering rhubarb free anthraquinones to colon. RTA-OCDD-GN was successfully prepared through a double-layer coating process using chitosan as an inner layer and Eudragit S100 as an outer enteric coating layer. The pharmacodynamics and toxicological results showed that RTA-OCDD-GN could produce considerable purgative efficacy with half dosage of rhubarb medical material (RMM), and significantly reduce the nephrotoxicity of anthraquinones compared with RMM. The comparative pharmacokinetics results in vivo gave a preliminary explanation to the mechanism of toxicity attenuation of RTA-OCDD-GN. Taken together, the oral colon-specific delivery system was a useful media to achieve the effect-enhancing and toxicity attenuation of orally administrated rhubarb total anthraquinones.