Alfuzosin hydrochloride, (R)- | 183658-25-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: Alfuzosin hydrochloride, (R)-
• 英文别名: (2R)-N-[3-[(4-amino-6,7-dimethoxyquinazolin-2-yl)-methylamino]propyl]oxolane-2-carboxamide;hydrochloride
• CAS: 183658-25-5
• 化学式: C19H28ClN5O4
• 分子量: 425.9
• InChiKey: YTNKWDJILNVLGX-PFEQFJNWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.77
• 重原子数：
  29
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  112
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• ALFUZOSIN HYDROCHLORIDE POLYMORPHS
  申请人：Anumula Reddy Raghupathi

  公开号：US20070049756A1

  公开（公告）日：2007-03-01

  Alfuzosin hydrochloride crystalline and amorphous polymorphic forms and processes for preparing them.

  阿尔福兹辛盐酸盐的晶态和非晶态多晶形式及其制备过程。
• Composition comprising alfuzosin
  申请人：Cimex Pharma AG

  公开号：EP1637129A1

  公开（公告）日：2006-03-22

  A monolithic composition includes alfuzosin in a polymeric matrix adapted to release 13-33% of the alfuzosin within 2 hours, 40-60% of the alfuzosin within 7 hours, and greater than 80% of the alfuzosin within 20 hours of administration. A unit dosage form includes: a heterogeneous mixture of alfuzosin hydrochloride anhydrate, lactose monohydrate, hydroxypropylmethylcellulose, polyvinylpyrrolidone and magnesium stearate, wherein the heterogeneous mixture is heterogeneously distributed throughout the unit dosage form. A manufacturing process includes: mixing a hydrophilic polymer and alfuzosin to provide a blend; granulating the blend to provide granules; drying the granules on a dryer to provide dried granules; sizing the dried granules to provide sized granules; mixing the sized granules with a lubricant to obtain a mixture; and compressing the mixture to obtain a tablet. A method of treating benign prostatic hyperplasia, includes administering to a patient the composition or unit dosage form once a day.

  一种单片组合物包括聚合基质中的阿夫唑嗪，该聚合基质可在给药后 2 小时内释放 13-33%的阿夫唑嗪、7 小时内释放 40-60%的阿夫唑嗪、20 小时内释放 80%以上的阿夫唑嗪。一种单位剂型包括：盐酸阿夫唑嗪水合物、一水乳糖、羟丙基甲基纤维素、聚乙烯吡咯烷酮和硬脂酸镁的异质混合物，其中异质混合物异质分布在整个单位剂型中。一种生产工艺包括：混合亲水性聚合物和阿夫唑嗪，以得到混合物；将混合物制粒，以得到颗粒；在干燥器上干燥颗粒，以得到干燥颗粒；对干燥颗粒进行定型，以得到定型颗粒；将定型颗粒与润滑剂混合，以得到混合物；以及压缩混合物，以得到片剂。一种治疗良性前列腺增生症的方法，包括每天一次给患者服用组合物或单位剂型。
• Alfuzosin tablets and synthesis
  申请人：Scheer Mathias

  公开号：US20060062845A1

  公开（公告）日：2006-03-23

  A monolithic composition includes alfuzosin in a polymeric matrix adapted to release 13-33% of the alfuzosin within 2 hours, 40-60% of the alfuzosin within 7 hours, and greater than 80% of the alfuzosin within 20 hours of administration. A unit dosage form includes: a heterogeneous mixture of alfuzosin hydrochloride, lactose monohydrate, hydroxypropylmethylcellulose, polyvinylpyrrolidone and magnesium stearate, wherein the heterogeneous mixture is heterogeneously distributed throughout the unit dosage form. A manufacturing process includes: mixing a hydrophilic polymer and alfuzosin to provide a blend; granulating the blend to provide granules; drying the granules on a dryer to provide dried granules; sizing the dried granules to provide sized granules; mixing the sized granules with a lubricant to obtain a mixture; and compressing the mixture to obtain a tablet. A method of treating benign prostatic hyperplasia, includes administering to a patient the composition or unit dosage form once a day.
• CONTROLLED RELEASE FORMULATIONS OF AN ALPHA-ADRENERGIC RECEPTOR ANTAGONIST
  申请人：Vishnubhotla Nagaprasad

  公开号：US20080206338A1

  公开（公告）日：2008-08-28

  The present invention relates to controlled release formulations comprising an alpha-adrenergic receptor antagonist. More particularly, the present invention relates to controlled release matrix formulation comprising alfuzosin hydrochloride and a combination of hydrophilic and hydrophobic polymers prepared by direct compression.
• ALFUZOSIN FORMULATIONS, METHODS OF MAKING, AND METHODS OF USE
  申请人：Arnold Kristin

  公开号：US20100092556A1

  公开（公告）日：2010-04-15

  Alfuzosin compositions comprising a tablet core of alfuzosin and a release-retarding matrix comprising about 40 to about 80% (by weight) hydroxypropyl methyl cellulose with a maximum apparent viscosity of about 5600 cP, based on the total weight of the tablet core; and an extended-release coating substantially surrounding the tablet core comprising a release-retarding coating material, wherein the compositions are bioequivalent to the reference dosage form of NDA #021287 (UROXATRAL) are disclosed. Methods of making and using the alfuzosin compositions are also disclosed.