Yano Tetsuo, Yamada Mei, Konda Tomoyuki, Shiozaki Makoto, Inoue Daisuke
Research Center, Ajinomoto Pharmaceuticals Co., Ltd., 1-1 Suzuki-cho, Kawasaki-ku, Kawasaki-shi, Kanagawa, 210-8681, Japan,
J Bone Miner Metab. 2014 Nov;32(6):653-9. doi: 10.1007/s00774-013-0543-9. Epub 2013 Dec 20.
Clinical evidence suggests that, compared with alendronate, risedronate reduces fracture risk faster and more potently, with less bone mass gain. We tested the hypothesis that risedronate improves bone quality faster than alendronate using calcium-deficient, ovariectomized (OVX) rats. Female Sprague-Dawley rats at 24 weeks of age were divided into sham-operated and OVX groups and fed a low-calcium (0.05%) diet under paired feeding. After 12 weeks, OVX rats were divided into five groups and treated with vehicle, risedronate (3.5 and 17.5 μg/kg/week, s.c.) or alendronate (7 and 35 μg/kg/week, s.c.). Rats were killed 6-8 weeks later and the bone architecture and strength of the left femur were evaluated by micro-computed tomography and a three-point bending test. Trabecular bone mineral density (BMD), number and thickness were significantly lower in OVX rats than in the sham-operated group. Cortical BMD, bone area (Ct.Ar), and thickness (Ct.Th) were similarly decreased. Risedronate significantly improved Ct.Ar (+8%) and Ct.Th (+9%) at 6 weeks, while alendronate only caused a significant improvement in Ct.Ar (+8% at 6 weeks) and only at the higher dose. At 8 weeks, both risedronate and alendronate significantly increased trabecular BMD compared with the vehicle. Bone strength parameters showed a significant correlation between Ct.Ar and Ct.Th. Risedronate significantly improved maximum load at 6 weeks, while alendronate failed to produce any significant changes. Our results suggest that risedronate is superior to alendronate at improving cortical bone architecture and strength, and that enhanced bone quality partly accounts for risedronate's efficacy.
临床证据表明,与阿仑膦酸盐相比,利塞膦酸盐能更快、更有效地降低骨折风险,且骨量增加较少。我们使用缺钙、卵巢切除(OVX)大鼠检验了利塞膦酸盐比阿仑膦酸盐更快改善骨质量的假设。24周龄的雌性斯普拉格-道利大鼠分为假手术组和OVX组,并在配对喂养下给予低钙(0.05%)饮食。12周后,将OVX大鼠分为五组,分别给予赋形剂、利塞膦酸盐(3.5和17.5μg/kg/周,皮下注射)或阿仑膦酸盐(7和35μg/kg/周,皮下注射)治疗。6-8周后处死大鼠,通过微计算机断层扫描和三点弯曲试验评估左股骨的骨结构和强度。OVX大鼠的小梁骨矿物质密度(BMD)、数量和厚度显著低于假手术组。皮质骨BMD、骨面积(Ct.Ar)和厚度(Ct.Th)也同样降低。利塞膦酸盐在6周时显著改善了Ct.Ar(增加8%)和Ct.Th(增加9%),而阿仑膦酸盐仅在较高剂量时才使Ct.Ar有显著改善(6周时增加8%)。在8周时,与赋形剂相比,利塞膦酸盐和阿仑膦酸盐均显著增加了小梁骨BMD。骨强度参数显示Ct.Ar和Ct.Th之间存在显著相关性。利塞膦酸盐在6周时显著提高了最大负荷,而阿仑膦酸盐未产生任何显著变化。我们的结果表明,在改善皮质骨结构和强度方面,利塞膦酸盐优于阿仑膦酸盐,骨质量的提高部分解释了利塞膦酸盐的疗效。