SOLID SITOSTANOL FORMULATIONS INHIBIT CHOLESTEROL UPTAKE

植物固醇（例如谷甾烷醇）通过抑制小肠吸收来降低人体血清胆固醇水平。尽管谷甾烷醇具有最小的毒性并且本身不被吸收，但先前使用这种植物甾烷醇降低胆固醇的尝试由于其在水和食用油中的低溶解度而变得复杂。 使用一种创新的质谱方法来取代传统的长期临床试验，一种新的水性谷甾烷醇制剂已被证明可以减少人体胆固醇吸收37%。重要的是，这仅用300 mg谷甾烷醇就实现了，该量比先前报道的有效量少5至10倍。为了开发商业制剂的组成和剂量大小，本研究将通过质谱法评价作为人体胆固醇吸收抑制剂的各种固体谷甾烷醇制剂。 这里描述的工作将产生一种灵活的固体制剂，可用于膳食补充剂的片剂或作为食品成分的固体添加剂。 该制剂的多功能性和公认的谷甾烷醇安全性将为血清胆固醇轻度升高的个体提供更好的治疗，这是目前常规药物无法治疗的人群。建议的商业应用：植物甾醇可以作为胆固醇吸收抑制剂，因为它们是安全的，耐受性良好。该提案描述了制备可用作膳食补充剂或食品成分的固体谷甾烷醇制剂的研究。

Plant sterols, such as sitostanol, lower the level of human serum cholesterol by inhibiting its absorption from the small intestine. Even though sitostanol has minimal toxicity and is not absorbed itself, previous attempts to use this plant stanol for cholesterol lowering have been complicated by its low solubility in water and dietary oils. Using an innovative mass spectrometry method to replace conventional long-term clinical trials, a new aqueous sitostanol formulation has been shown to reduce human cholesterol absorption by 37%. Importantly, this was achieved with only 300 mg of sitostanol, an amount that is 5- to 10-fold less than that previously reported to be effective. In order to develop a composition and dose size for a commercial preparation, this study will evaluate by mass spectrometry various solid sitostanol formulations as inhibitors of human cholesterol absorption. The work described here will produce a flexible solid formulation that can be used in a tablet for a dietary supplement or as a solid additive for a food ingredient. The versatility of this formulation and the acknowledged safety of sitostanol will provide better therapy for individuals with mildly elevated serum cholesterol, a group that is currently not served by conventional pharmaceuticals. PROPOSED COMMERCIAL APPLICATIONS: Plant sterols can serve as cholesterol absorption inhibitors since they are safe and well tolerated. This proposal describes studies to prepare a solid sitostanol formulation that can be used as a dietary supplement or as a food ingredient.