盐酸法舒地尔半水合物 | 186694-02-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 中文名称: 盐酸法舒地尔半水合物
• 中文别名: 盐酸法舒地尔水合物；法舒地尔；盐酸法舒地尔
• 英文名称: Fasudil hydrochloride hydrate
• 英文别名: 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline;hydrate;dihydrochloride
• CAS: 186694-02-0
• 化学式: C28H38Cl2N6O5S2
• 分子量: 673.7
• InChiKey: AACOJGPCMIDLEY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.46
• 重原子数：
  43
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  142
• 氢给体数：
  5
• 氢受体数：
  11

反应信息

• 作为反应物：
  描述：

  盐酸法舒地尔半水合物 以 水 为溶剂， 生成 盐酸法舒地尔
  参考文献：
  名称：

  Sustained release oral preparations of fasudil hydrochloride

  摘要：

  本发明揭示了一种口服缓释制剂，其包含从含有盐酸法舒地尔和其水合物的组中选择的至少一种活性成分。本发明还揭示了一种评估口服缓释制剂的方法，其中评估是针对所述活性成分的缓释能力进行的。

  公开号：

  US06699508B1

文献信息

• Process for producing an oral sustained-release preparation of fasudil hydrochloride
  申请人：ASAHI KASEI PHARMA CORPORATION

  公开号：US20040131679A1

  公开（公告）日：2004-07-08

  Disclosed is an oral sustained-release preparation which contains at least one active ingredient selected from the group consisting of fasudil hydrochloride and a hydrate thereof, the preparation comprising at least one sustained-release coated particle comprising a core having a surface and a coating formed on the surface of the core, wherein the core contains the active ingredient and the coating comprises a coating base material and a specific insoluble auxiliary material, and wherein the preparation exhibits, with respect to the active ingredient, a specific dissolution rate, as measured by the dissolution test. By using the oral sustained-release preparation of the present invention, it becomes possible to surely control the release of fasudil hydrochloride from the preparation, so that the effect of the active ingredient is maintained for a long period of time. Therefore, the burden of the patient who has to take the preparation can be decreased and the compliance with respect to the administration of the preparation can be improved. Also disclosed is a method for evaluating an oral sustained-release preparation containing the active ingredient, wherein the evaluation is conducted with respect to the sustained-release ability of the active ingredient.

  本发明公开了一种口服缓释制剂，其含有从羟氯喹硫酸盐和其水合物组成的群中选择的至少一种活性成分，该制剂包括至少一种缓释包被粒子，其包括具有表面的核心和形成在核心表面上的涂层，其中核心含有活性成分，涂层包括涂层基材料和特定的不溶性辅助材料，且该制剂展现出特定的溶解速率，如溶解测试所测量的。通过使用本发明的口服缓释制剂，可以确保控制羟氯喹硫酸盐的释放，从而使活性成分的效果持续较长时间。因此，可以减轻服用制剂的患者的负担，并提高对制剂的管理的遵从性。还公开了一种评估口服缓释制剂的方法，该方法与活性成分的缓释能力有关。
• Oral sustained-release preparation of fasudil hydrochloride
  申请人：Sugi Tomokazu

  公开号：US20060280793A1

  公开（公告）日：2006-12-14

  Disclosed is an oral sustained-release preparation which contains at least one active-ingredient selected from the group consisting of fasudil hydrochloride and a hydrate thereof, the preparation comprising at least one sustained-release coated particle comprising a core having a surface and a coating formed on the surface of the core, wherein the core contains the active ingredient and the coating comprises a coating base material and a specific insoluble auxiliary material, and wherein the preparation exhibits, with respect to the active ingredient, a specific dissolution rate, as measured by the dissolution test. By using the oral sustained-release preparation of the present invention, it becomes possible to surely control the release of fasudil hydrochloride from the preparation, so that the effect of the active ingredient is maintained for a long period of time. Therefore, the burden of the patient who has to take the preparation can be decreased and the compliance with respect to the administration of the preparation can be improved. Also disclosed is a method for evaluating an oral sustained-release preparation containing the active ingredient, wherein the evaluation is conducted with respect to the sustained-release ability of the active ingredient.

  本发明揭示了一种口服缓释制剂，其含有选择自fasudil盐酸盐和其水合物的活性成分中的至少一种，该制剂包括至少一个缓释包衣颗粒，该颗粒包括一个具有表面的核心和形成在核心表面上的涂层，其中核心含有活性成分，而涂层包括涂层基材料和特定的不溶辅助材料，并且该制剂在溶解试验中表现出与活性成分相关的特定溶解速率。通过使用本发明的口服缓释制剂，可以确保控制fasudil盐酸盐从制剂中的释放，从而使活性成分的效果长时间保持。因此，可以减轻服用制剂的患者的负担，并提高对制剂的管理的遵从性。本发明还揭示了一种评估含有活性成分的口服缓释制剂的方法，其中评估是针对活性成分的缓释能力进行的。