Petrangolini Giovanna, Corti Fabrizio, Ronchi Massimo, Arnoldi Lolita, Allegrini Pietro, Riva Antonella
Research and Development Department, Indena SpA, 20139 Milan, Italy.
Evid Based Complement Alternat Med. 2021 Nov 27;2021:7563889. doi: 10.1155/2021/7563889. eCollection 2021.
To evaluate in vitro solubility, bioaccessibility, and cytotoxic profile, together with a pharmacokinetic profile by oral administration to healthy volunteers of a novel food-grade berberine formulation (BBR-PP, i.e., berberine Phytosome®).
An in vitro increase of solubility in simulated gastric and intestinal fluids and an improved bioaccessibility at intestinal level along with a lower cytotoxicity with respect to berberine were observed with BBR-PP. The pharmacokinetic profile of the oral administration to healthy volunteers confirmed that berberine Phytosome® significantly ameliorated berberine absorption, in comparison to unformulated berberine, without any observed side effects. The berberine plasma concentrations observed with both doses of BBR-PP were significantly higher than those seen after unformulated berberine administration, starting from 45 min (free berberine) and 30 min (total berberine). Furthermore, BBR-PP improved berberine bioavailability (AUC) was significantly higher, around 10 times on molar basis and with observed dose linearity, compared to the unformulated berberine.
These findings open new perspectives on the use of this healthy berberine formulation in metabolic discomforts.
通过对健康志愿者口服一种新型食品级小檗碱制剂（BBR-PP，即小檗碱磷脂复合物），评估其体外溶解度、生物可及性和细胞毒性概况以及药代动力学概况。
观察到BBR-PP在模拟胃液和肠液中的体外溶解度增加，在肠道水平的生物可及性提高，且相对于小檗碱细胞毒性更低。对健康志愿者口服给药的药代动力学概况证实，与未制剂化的小檗碱相比，小檗碱磷脂复合物显著改善了小檗碱的吸收，且未观察到任何副作用。两种剂量的BBR-PP所观察到的小檗碱血浆浓度均显著高于未制剂化小檗碱给药后的浓度，从45分钟（游离小檗碱）和30分钟（总小檗碱）开始。此外，与未制剂化的小檗碱相比，BBR-PP改善后的小檗碱生物利用度（AUC）显著更高，以摩尔为基础约高10倍，且具有剂量线性关系。
这些发现为这种健康的小檗碱制剂在代谢不适中的应用开辟了新的前景。
