用于改变红曲米中洛伐他汀释放曲线以治疗高胆固醇血症的藻酸盐-明胶制剂。
Alginate-gelatin formulation to modify lovastatin release profile from red yeast rice for hypercholesterolemia therapy.
作者信息
Leone Gemma, Consumi Marco, Pepi Simone, Lamponi Stefania, Bonechi Claudia, Tamasi Gabriella, Donati Alessandro, Rossi Claudio, Magnani Agnese
机构信息
Department of Biotechnology, Chemistry & Pharmacy, University of Siena, via Aldo Moro 2, Siena 53100, Italy.
出版信息
Ther Deliv. 2017 Oct;8(10):843-854. doi: 10.4155/tde-2017-0025.
AIM
The preparation of a delivery system able to guarantee a delayed release of lovastatin from red yeast rice (RYR) is mandatory to counteract cholesterol biosynthesis effectively.
MATERIALS & METHODS: Polymeric formulations were prepared mixing alginate and gelatin, in different ratios, with RYR. The effect of different composition on stiffness, viscosity, swelling behavior and mesostructure of matrices was analyzed.
RESULTS
Formulations obtained combining polymers in comparable amount (i.e., 60/40 and 50/50) guaranteed a delayed release of lovastatin from RYR, a prolonged inhibitory activity toward 3-hydroxy-3-methylglutaryl-coenzyme A reductase and a decreased cholesterol synthesis.
CONCLUSION
The formulation obtained combining 60% gelatin and 40% of alginate showed physicochemical properties suitable to lead a lovastatin release profile compatible with cholesterol biosynthesis.
目的
制备一种能够保证洛伐他汀从红曲米（RYR）中延迟释放的递送系统，对于有效对抗胆固醇生物合成是必不可少的。
材料与方法
将藻酸盐和明胶按不同比例与红曲米混合制备聚合物制剂。分析了不同组成对基质的硬度、粘度、溶胀行为和介观结构的影响。
结果
以相当量（即60/40和50/50）混合聚合物得到的制剂保证了洛伐他汀从红曲米中的延迟释放、对3-羟基-3-甲基戊二酰辅酶A还原酶的延长抑制活性以及胆固醇合成的减少。
结论
由60%明胶和40%藻酸盐混合得到的制剂显示出适合导致与胆固醇生物合成相容的洛伐他汀释放曲线的物理化学性质。
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