Characterization of Albendazole Amorphous Solid Dispersion, In Vitro Dissolution Behavior and Preliminary Pharmacodynamics
OUYANG Cang-hong1, HU Chun-hui2*, XIONG De-qing1, WANG Li-na3
1. The Third Affiliated Hospital of Zunyi Medical University, Zunyi 563000, China; 2. Medical College of Qinghai University, Xining 810001, China; 3. Zunyi Medical University, Zunyi 563000, China
Abstract：OBJECTIVE To design and prepare a stable amorphous solid dispersion with enhanced solubility based on molecular interaction between albendazole (ABZ) and polymer. METHODS The wide angle X-ray diffraction (WXRD), liquid nuclear magnetic resonance (1H-NMR), Fourier transform infrared spectroscopy (FT-IR) were used to study the intermolecular interactions between ABZ and polymer to explain crystallization mechanism of ABZ at molecular level. RESULTS The hydrogen bonding between amino group on the carbamate in ABZ and the carbonyl group of HPMC-AS stabilized the amorphous solid dispersion(ASD) from crystallization of ABZ. In addition, the dissolution performance of the ASD in vitro and pharmacodynamics in rats with secondary hepatic alveolar hydatidosis were much better than those of other polymer combinations, especially those of the marketed form of ABZ (Shikechangchongqing). CONCLUSION The ASD combined with ABZ and HPMC-AS can effectively improve drug dissolution behavior in vitro and pharmacodynamics in vivo leading to enhanced therapeutic effect in the rat model.
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2020, Vol. 55 
