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  • Title: Further enhanced dissolution and oral bioavailability of docetaxel by coamorphization with a natural P-gp inhibitor myricetin.
    Author: Wei Y, Zhou S, Hao T, Zhang J, Gao Y, Qian S.
    Journal: Eur J Pharm Sci; 2019 Mar 01; 129():21-30. PubMed ID: 30590119.
    Abstract:
    The current study aims to improve the dissolution and oral bioavailability of a BCS IV drug docetaxel (DOC) by coamorphization with a natural P-gp inhibitor myricetin (MYR). A single-phase coamorphous form of DOC with MYR in a 1:1 molar ratio was prepared by solvent-evaporation method and characterized by differential scanning calorimetry, thermogravimetric analysis and powder X-ray diffraction. In comparison to crystalline DOC, amorphous DOC showed similar equilibrium aqueous solubility, temporary improvement in the intrinsic dissolution rate (IDR) and supersaturated dissolution; while coamorphous DOC-MYR exhibited a persistent enhanced IDR and prolonged highly supersaturated dissolution. In addition, coamorphous DOC-MYR demonstrated significantly superior physical stability compared to amorphous DOC under the long-term storage condition and accelerated condition. Compared with oral administration of crystalline DOC to rats, amorphous DOC showed a significant increase in Cmax (2.6-fold) and a marginal increase in AUC (1.3-fold) of DOC; but coamorphous DOC-MYR performed a 3.9-fold higher Cmax and 3.1-fold higher AUC. In conclusion, coamorphization of DOC with MYR was a promising approach to enhance both dissolution and oral absorption of poorly soluble and permeable DOC.
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