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英文药名：Kiklin Granules 86.2％（Bixalomer）
中文药名：踢磷颗粒（比沙洛姆）
生产厂家：安斯泰来制药
キックリン顆粒86.2％
治疗类别名称
高磷血症治疗剂（磷酸结合性聚合物）
批准上市日期：2016年12月
商標名
Kiklin Granules 86.2％
一般名
ビキサロマー（Bixalomer）
本質
〔日本名〕ビキサロマーは、N,N,N’,N’-テトラキス（3-アミノプロピル）ブタン-1,4-ジアミンと 2-（クロロメチル）オキシランが1：2.1-2.4の比で反応して得られた架橋重合体である。
〔英名〕Bixalomer is a cross-linked polymer which is obtained by a reaction between N,N,N’,N’-tetrakis（3-aminopropyl）butane-1,4-diamine and 2-（chloromethyl）oxirane with a ratio of 1：2.1-2.4.
性状
是一种白色到粉末的黄色。几乎不溶于水和乙醇（99.5）。它是吸湿性的。
操作注意事项
注意：
因为这个产品质量是由干燥剂持有的目的，即准备工作后，不要离开盖子打开。
条件批准
在建立药品风险管理计划的顶部，要正确实施。
药效药理
1.药理作用
(1) 血浆磷浓度和Ca×P产品降血脂作用
在高磷减肥食品5/6肾切除慢性肾脏病鼠，Bikisaroma按3％的膳食管理，降低显著血浆磷浓度（AUC值）和Ca×P产品（AUC值）。此外，在腺嘌呤诱发慢性肾病大鼠，Bikisaroma由3％的膳食给药，显著降低血浆磷浓度（AUC值）和Ca×P产品（AUC值）。
(2) 血管钙化的抑制作用
维生素D的负载腺嘌呤诱发慢性肾病大鼠，Bikisaroma由2％的膳食给药，显著减少在主动脉钙的量。
(3) 继发性甲状旁腺功能改进作用
在高磷减肥食品5/6肾切除慢性肾脏病鼠，Bikisaroma按3％的膳食管理，降低显著血浆浓度PTH（AUC值）和甲状旁腺的重量比。此外，在腺嘌呤诱发慢性肾病大鼠，Bikisaroma由3％的膳食给药，显著降低血浆PTH浓度（AUC值）和甲状旁腺重量比。
(4) 肾性骨病进步抑制作用
在腺嘌呤诱发慢性肾病大鼠，Bikisaroma由3％的膳食管理，降低了股骨的间隙面积比和纤维化面积比。对于骨质面积比，没有观察到显著的变化，由于Bikisaroma施用。
(5) 血液的pH值，对碳酸氢根离子浓度的作用
在腺嘌呤诱发慢性肾病大鼠，Bikisaroma由3％的膳食管理，是提高血液pH值和血碳酸氢根离子浓度的降低。
2. 作用机理
Bikisaroma是胺官能磷酸结合性聚合物，通过促进磷排泄到粪便结合磷酸盐在胃肠道中，从而减少了从胃肠道磷的吸收的抑制血磷浓度的。
3. 生物等效性试验
Bikisaroma颗粒2,610mg/剂量（2,250mg/倍Bikisaroma）和三木佐吕间在胶囊2,250mg/次，三次8天由交叉法健康成年男性一天（第一天只有一天两次）的饮食口服前不久，它是由尿磷排泄生物等效性研究。作为结果，已经显示Bikisaroma颗粒被锯成佐吕间超过胶囊和生物等效。（见“药理学表”）
适应病症
在慢性肾脏疾病患者的高磷血症的改善
用法与用量
成人，一次500毫克一个（此药物580mg），为起始剂量作为Bikisaroma，仅有前一天口服给药三次餐。此后，根据血清磷浓度的程度的症状，但要调整，最高剂量为1天7,500mg（这种药物8,700mg）
包装规格
瓶装
100g
制造商
安斯泰来制药公司
完整使用资料附件：http://www.info.pmda.go.jp/go/pack/2190032D1027_1_02/
Astellas Launches Kiklin Granules, a Treatment for Hyperphosphatemia, in Japan
7, 2016 - Astellas Pharma Inc. (TSE: 4503; President and CEO: Yoshihiko Hatanaka, "Astellas") announced that it launched Kiklin® Granules 86.2% (generic name: bixalomer, "Kiklin® Granules"), an additional formulation of Kiklin® Capsules 250 mg ("Kiklin® Capsules"), for the indication of treatment of hyperphosphatemia in patients with chronic kidney disease ("CKD") in Japan today. Astellas expects to further contribute to hyperphosphatemia treatment by introducing Kiklin® Granules which can further improve the compliance with its more convenient dosing option into Japanese market.
Hyperphosphatemia occurs in patients whose renal function is decreased, since phosphorus is not sufficiently excreted into urine via the kidneys and consequently accumulates in the body. With continuous high blood phosphorus concentration, the risk of renal osteodystrophy characterized by a high tendency of bone pain and bone fracture is known to be increased. Additionally, high blood phosphorus concentration is associated with increased coronary artery calcification and subsequent cardiovascular events. Therefore, it is considered extremely important to maintain the serum phosphorus concentration at an appropriate level in CKD patients. Bixalomer is amine-functional polymers which decrease the serum phosphorus concentration by binding to phosphate in the gastrointestinal tract, thus inhibiting absorption of phosphate into the human body.
Bixalomer was discovered by Ilypsa, Inc., now a wholly-owned subsidiary of Amgen Inc. In April 2006, Astellas and Ilypsa, Inc. entered into a license agreement that grants Astellas exclusive rights to develop and commercialize bixalomer in Japan and then, Astellas conducted the development of bixalomer.
On June 26, 2012, Astellas launched Kiklin® Capsules for the indication of hyperphosphatemia in patients on dialysis with CKD in Japan. Astellas also received an approval for a supplemental new drug application of Kiklin® Capsules for the treatment of CKD patients not on dialysis with hyperphosphatemia on February 29, 2016.
Astellas and Sanwa Kagaku Kenkyusho Co.Ltd. co-promote Kiklin® Capsules and both company will co-promote Kiklin® Granules while Astellas is solely responsible for these distribution.
PRODUCT SUMMARY
Product name: Kiklin® Granules 86.2%
Generic name: Bixalomer
Indication:Treatment of hyperphosphatemia in patients with chronic kidney disease
Dosage regimen:The usual starting dose of Bixalomer for adults is 500mg (Granules 580mg) three times daily just before meals. The dose can be adjusted based on symptoms and serum phosphorus concentration. The maximum daily dose should not exceed 7,500mg (Granules 8,700mg).
Package: Kiklin® Granules 86.2%:100g
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