Effects of alendronate on bone mineral density and bone metabolic markers in patients with liver transplantation

Introduction The purpose of this study was to evaluate the effects of alendronate (ALN) on bone mineral density (BMD) and bone turnover markers in patients with orthotopic liver transplantation (OLT). Methods In the prospective, controlled, open study with 24 months of follow-up, 98 patients with OLT were randomised to receive ALN 70 mg weekly or no ALN; calcium (Ca) 1,000 mg daily and 0.5 mcg calcitriol daily were provided to all patients. Lumbar spine (LS) and hip BMDs were measured at 6-month intervals by dual-energy X-ray absorptiometry (DEXA). Spinal radiographs were obtained to assess vertebral fractures. Additionally, bone turnover markers, serum parathyroid hormone (PTH) and biochemical parameters were determined every 3 months. Results Compared with the control group, the ALN group showed significant increases in BMD of the LS (5.1±3.9% vs 0.4±4.2%, p<0.05 at 12 months, 8.9±5.7% vs 1.4±4.9%, p<0.05 at 24 months), femoral neck (4.3±3.8% vs −1.1±3.1%, p<0.05 at 12 months, 8.7±4.8% vs 0.6±4.5%, p<0.05 at 24 months) and total femur (3.6±3.8% vs −0.6±4.0%, p<0.05 at 12 months, 6.2±3.8% vs 0.3±4.6%, p<0.05 at 24 months). In the ALN group, osteocalcin and urinary deoxypyridinoline (DPD) decreased significantly at the sixth month, with no further change, by −35.6% and −63.0%, on average, respectively (p<0.05). In the control group, a significant increase in biochemical markers of bone turnover was observed in comparison to baseline values (p<0.05). PTH increased within reference levels without a difference between groups. Two nonvertebral fractures (4.2%) and nine vertebral fractures (18.8%) in the control group and three vertebral fractures (6.8%) in the ALN group occurred during the follow-up. The weekly ALN was well tolerated, and no severe side effects occurred. Conclusion This is the first randomised study including a control group to demonstrate that weekly ALN was able to significantly increase BMD in patients with OLT when compared with Ca and calcitriol alone. However, ALN did not appear to offer protection against fractures. This study was awarded the “Novartis Young Investigator Award” at the Second Joint Meeting of the European Calcified Tissue Society and the International Bone and Mineral Society, Geneva, 25–29 June 2005.     

醋氨己酸锌在大鼠的药代动力学

测定了醋氨已酸锌(ZAC)在大鼠体内的药代动力学。结果表明:大鼠poZAC吸收迅速,给药后1.5h即可达峰,其后稍快下降。3个剂量组的吸收峰时及半衰期基本一致,T_1/2约在1.5h,峰浓度、AUC及CL/F呈剂量依赖关系。ZAC在大鼠的药代动力学模型为一室模型。组织分布的实验结果表明:服药2h后药物可广泛分布于各组织中,主要集中在胃、肠;肾、肝、血浆及肺次之;心、脾、脑较低;肌肉、子宫未检出。6h后胃中含锌量稍降,肺中含量变化不大,其它组织的药物浓度普遍明显下降,表明该药在组织中不易蓄积。ZACpo后主要经粪排出,尿及胆汁仅排出少量药物。     

牛蒡子化学成分的研究

从牛蒡(Arctium lappa L.)子乙醚和丙酮提取物中,经硅胶柱层析,低压柱层析和制备性薄层层析分离到一个甾体化合物,胡萝卜甙(daucosterol,Ⅰ)和四个已知木脂素:牛蒡子甙元(arctigenin,Ⅱ)、牛蒡子甙(arctiin,Ⅲ)、罗汉松脂素(matairesinol,Ⅳ)和牛蒡酚F(lappaol F,Ⅴ)。一个新木脂素,命名为新牛蒡素乙(neoarctin B,Ⅵ)。根据光谱(UV,IR,¹H-NMR,¹³C-NMR,DEPT,2D-NMR和MS)分析,推定了其化学结构为式Ⅵ。     

差示—线性组合导数光谱法测定扑咳灵片中扑尔敏和溴化丙胺太林

本文提出了差示一线性组合导数光谱法用于测定混合组分体系的基本原理和实验方法。并试用本法消除了扑尔敏、溴化丙胺太林、灵芝粉及附加剂之间的相互干扰,从而分别测定了扑咳灵片巾扑尔敏和溴化丙胺太林的含量,其平均回收率分别为100.2±1.49％(CV)和99.89±1.03％(CV)。其精密度、准确度均好。     

巴戟天和恩施巴戟的蒽醌化合物

从巴戟天(Morinda officinalis How.)根的氯仿提取物中,分离得八个蒽醌化合物,其中二个为新化合物,它们的结构为1,6-二羟基-2,4-二甲氧基蒽醌(1,6-dihydroxy-2,4-dimethoxyanthraquinone,V),1,6-二羟基-2-甲氧基蒽醌(1,6-dihydroxy-2-methoxy-anthraquinone,Ⅵ)。从恩施巴戟(Damnacanthus indicus Linn.)根的氯仿提取物中,分离得七个蒽醌化合物,其中一个为新化合物,其结构为1,4-二甲氧基-2α-羟基蒽醌(1,4-dimethoxy-2-hydroxyanthraquinone,ⅩⅢ)。