抗骨质疏松产品-骨元肽结肠靶向胶囊综合评价(之一).docVIP

抗骨质疏松产品－骨元肽结肠靶向胶囊的综合评价（之一） 李延平 刘义 吴科锋 邓亦峰 艾春梅 龚先玲 吕应年 崔燎（广东天然药物研究与开发重点试验室，湛江524023） 摘要 目的 综合评价抗骨质疏松产品－骨元肽结肠靶向胶囊。方法 抗骨质疏松试验采用新生SD大鼠成骨细胞体外培养法，测定MTT、ALK（E2）、骨钙素（BGP）、转化生长因子（TGF-β1）、碱性磷酸酶（ALK）；骨密度、24小时尿液中Ca、P含量；测定骨元肽分子量分布及大鼠在体结肠吸收率结果 骨元肽对新生SD大鼠成骨细胞有明显增殖作用，ALKComprehensive evaluation on colon targeting capsule of Guyuan peptide for anti-osteoporosis product LI Yan-ping，，Deng yifeng，Ahun-mei，Cui liao. （Guangdong key Laboratory for Research and Development of Natural Drugs，zhanjiang 524023，ChinaAbstract: Objective To perform comprehensive evaluation on colon targeting capsule of Guyuan peptide（GYP） for anti-osteoporosis action. Methods In vitro anti-osteoporosis product was investigated by MTT method, detecting alkaline phosphatase (ALK) and mineralized nodes in osteoblasts from SD rats. In vivo the rat models of osteoporosis were induced by ovariectomy and treated with three doses of colon targeting capsule of GYP (5.0, 20.0, 80.0mg.kg-1.d-1). The serum levels of estradiol (E2), osteocalcin (BGP), transforming growth factors (TGF-β1) and ALK, bone mineral density (BMD), and the contents of calcium (Ca) and phosphorus (P) in 24h urine were detected. The distribution and absorption of GYP’s MW in the colon of rats were also investigated. Results GYP enhanced cell proliferation, ALK activity and the number of mineralized nodes in rats’ osteoblasts. The colon targeting capsule of GYP were significantly increased the serum level of E2，TGF-β1，and BMD，decreased the serum level of ALK, BGP and the contents of Ca，P in 24h urine, and the capsules had no side effects and the shelf life of them reached 24 months. The Mw of G is between 189-1000 D, in which the component of 189-512D takes 68.5% or above. The average absorption rate is 49.61％ in the colon of rats.Conclusion The colon targeting capsule of Guyuan peptide is an effective and safe product with controllable quality for BMD enhancement, prevention and control of osteoporosis in middle-aged and senile groups. KEY WORDS：colon