The Drug Development And Quality Control For Osteoporosis

Osteoporosis is a systemic skeletal disorder characterized by low bone mass and micro architectural deterioration of bone tissue, leading to enhanced bone fragility. The clinical consequences of osteoporosis are vertebral and peripheral fractures. Postmenopausal osteoporosis affects women after menopause and results from an accelerated rate of bone loss mainly due to estrogen deficiency. Thus, there is an increase in bone turnover, resulting in a decrease in bone mass and bone mineral density. The bone loss is more accelerated during the first years after menopause, and continues at a slower rate for the lifetime. It is considerable for human healthy and life quality, and to develop new medicinal products and its quality control for the treatment and/or prevention of postmenopausal osteoporosis. In this project, zolendronic acid-a third generate bisphosphonate was synthesised, two kinds of novel 6-amio-purine-9-substituted bisphosphonic acid are designed and obtained, and their characteristics of inhibiting hydroxyapatite dissolution in vitro were investigated. Another novel antiosteoprosis agent named Strontium ranelate was also developed in our project. It is the first antiosteoporotic drug that has significant effects on treatment of increasing bone formation and decreasing bone resorption simultaneously. This rebalances bone turnover in favor of the formation of new and stronger bone and provides early and sustained antifracture efficacy. The quality of these drugs above were studied and the evaluation methods were established. The novel platform for bisphosphonate assay was constructed.Bisphosphonate as potent bone resorpton inhibitor is play an important role in osteoporosis treatment, but some adverse affects are occurred in long term use. Etidronate belongs to the first generation BP. It can affect mineralization at therapy dose. The second generation BPs which containing an amino group have shown significantly increased potency compared to other...