Graff Sandrine, Chaumeil Jean-Claude, Boy Pierre, Lai-Kuen René, Charrueau Christine
Laboratoire de Pharmacie Galénique EA 2498, Université Paris Descartes, Paris, France.
Biol Pharm Bull. 2008 Feb;31(2):266-72. doi: 10.1248/bpb.31.266.
Saccharomyces boulardii is a nonpathogenic yeast with proven health benefits, some of them depending on its viability. However, the living yeast is sensitive to environmental conditions and its viability is less than 1% in the faeces after oral administration. Therefore, we assessed the survival conditions of S. boulardii in aqueous suspension and in its freeze-dried form and we formulated microspheres with the former and tablets with the latter in order to preserve the viability of the probiotic. While the viability of the yeast in aqueous suspension could be maintained for one year at -20 degrees C and +5 degrees C, increasing the temperature led to almost total mortality within 14 d at +40 degrees C and 4 d at +60 degrees C. The viability of the freeze-dried yeast was preserved for one year at +25 degrees C without moisture. With 75% relative humidity, the mortality was significant at 28 d at +25 degrees C and almost total within 1 d at +60 degrees C. In vitro, whereas less than 1% of non-encapsulated or non-tabletted S. boulardii survived after 120 min at pH 1.1, both formulations in microspheres and direct compression enabled to protect the yeast from degradation in HCl and to release it viable at pH 6.8. However, despite a similar release profile from both dosage forms, the compression led to a significant decrease in the viability of the freeze-dried yeast. In conclusion, although both formulations are efficient in protecting S. boulardii in acidic condition, microspheres provide a higher entrapment efficiency and a faster release of the viable probiotic in intestinal condition than matrix tablets.
布拉氏酵母菌是一种具有已证实健康益处的非致病性酵母,其中一些益处取决于其活性。然而,活酵母对环境条件敏感,口服后在粪便中的活性低于1%。因此,我们评估了布拉氏酵母菌在水悬浮液和冻干形式下的存活条件,并分别用前者制备微球、后者制备片剂,以保持益生菌的活性。酵母在水悬浮液中的活性在-20℃和+5℃下可维持一年,温度升高则导致在+40℃下14天内几乎全部死亡,在+60℃下4天内几乎全部死亡。冻干酵母的活性在+25℃无水分条件下可保存一年。相对湿度为75%时,在+25℃下28天死亡率显著,在+60℃下1天内几乎全部死亡。在体外,未包封或未制成片剂的布拉氏酵母菌在pH 1.1条件下120分钟后存活的不到1%,而微球和直接压片这两种制剂都能保护酵母在盐酸中不降解,并使其在pH 6.8时以活的状态释放。然而,尽管两种剂型的释放曲线相似,但压片导致冻干酵母的活性显著降低。总之,虽然两种制剂在酸性条件下都能有效保护布拉氏酵母菌,但与基质片剂相比,微球在肠道条件下具有更高的包封效率和更快的活益生菌释放速度。