新诺明钠 | 4563-84-2

• 物质功能分类: 原料药 - 人工合成抗感染类药 - 磺胺类药及增效剂
• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 新诺明钠
• 中文别名: 磺胺甲恶唑钠
• 英文名称: Sodium N-(5-methylisoxazol-3-yl)sulphanilamidate
• CAS: 4563-84-2
• 化学式: C10H11N3NaO3S
• 分子量: 276.27
• InChiKey: CFNQJJGJKVHAME-UHFFFAOYSA-N

物化性质

• 溶解度：
  DMSO：55mg/mL（199.81毫摩尔）；

计算性质

• 辛醇/水分配系数(LogP)：
  0.99
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  107
• 氢给体数：
  2
• 氢受体数：
  6

制备方法与用途

简介

新诺明钠又名磺胺甲噁唑钠，为白色或微黄色结晶或粉末。无臭，遇光色渐变暗。易溶于水，微溶于乙醇。长时间置于湿空气中会缓慢吸收CO2而析出SMZ。本品属广谱抑菌剂，用于革兰氏阳性菌和阴性菌，尤其是沙门氏杆菌、变形杆菌、大肠杆菌等具有抑菌作用。

理化性质

新诺明钠为白色或微黄色结晶或粉末，无臭。遇光色渐变暗。易溶于水，微溶于乙醇。长时间置于湿空气中会缓慢吸收CO2而析出SMZ。

应用

新诺明钠属广谱抑菌剂，用于革兰氏阳性菌和阴性菌，尤其是沙门氏杆菌、变形杆菌、大肠杆菌等具有抑菌作用。其作用机理主要是影响二氢叶酸形成，最终抑制蛋白质合成，从而抑制细菌生长和繁殖。抗菌作用较其他磺胺药强，对猪弓形虫病、猪水肿病和畜禽球虫病等都有较好的疗效；可用于禽霍乱、禽副伤寒、禽慢性呼吸道病等。与抗菌增效剂TMP合用时，抗菌作用可增强数倍至数十倍。

生物活性

Sulfamethoxazole sodium是一种用于治疗细菌感染的抗生素。

文献信息

• Composition for coelomic administration, its preparation, and ingredients for use therein
  申请人：SHIONOGI & CO., LTD.

  公开号：EP0055609A1

  公开（公告）日：1982-07-07

  A pharmaceutical or veterinary composition for coelomic administration comprising sulfamethoxazole and trimethoprim with a base material(s), having a phospholipid included therein so that the tendency of solidification at the step of mixing of the said components in the manufacture of the said composition is prevented whilst solving the problem of delayed disintegration. When trimethoprim is used in the form of its salt or together with an organic acid in the manufacture of the said composition, the absorption rate of trimethoprim can be improved.

  一种用于腔肠给药的药物或兽药组合物，由磺胺甲噁唑和曲甲氧苄啶与一种或多种基质材料组成，其中含有磷脂，这样可以防止在制造上述组合物时混合上述成分时出现凝固的趋势，同时解决延迟崩解的问题。在制造上述组合物时，如果以盐的形式或与有机酸一起使用曲甲氧苄啶，则可提高曲甲氧苄啶的吸收率。
• Azacycloalkane derivatives, absorption promoters containing the derivatives as the effective ingredient and external preparation containing the absorption promoters
  申请人：HISAMITSU PHARMACEUTICAL CO., INC.

  公开号：EP0241050A2

  公开（公告）日：1987-10-14

  An azacycloalkane derivative useful for promoting the absorption of a medicine, an absorption promoting agent comprising at least one of the azacycloalkane derivatives as the effective ingredient for promoting the absorption and an external preparation containing the absorption promoting agent, the derivative being represented by the following formula wherein A is -CH2-or -S-for example, B is sulfur or oxygen, R is -SR" in which R" is an alkyl group or alkylthioalkyl group for example, or -OR" in which R" is as defined above, an alkyl group or substituted amino group, R' is a hydrogen atom, alkyl group or alkyloxy group for example, m is an integer of 0-5 and n is an integer of 1-15.

  一种用于促进药物吸收的氮杂环烷烃衍生物，一种包含至少一种氮杂环烷烃衍生物作为促进吸收有效成分的吸收促进剂，以及一种含有该吸收促进剂的外用制剂，该衍生物由下式表示 其中 A 是-CH2-或-S-例如，B 是硫或氧，R 是-SR"，其中 R "是烷基或烷硫烷基（例如），或-OR"，其中 R "如上定义，是烷基或取代的氨基，R'是氢原子、烷基或烷氧基（例如），m 是 0-5 的整数，n 是 1-15 的整数。
• Adhesive device for transdermal administration of an active agent
  申请人：NITTO DENKO CORPORATION

  公开号：EP0452837A2

  公开（公告）日：1991-10-23

  A medical adhesive comprising a plaster layer containing the following ingredients, characterized in that the ingredient ② is incorporated in a larger amount than the ingredient ⑤ and in an amount not less than 25% by weight relative to the total amount of the ingredients ①∼⑤, and the plaster layer is a W/O type : ① a medicinal ingredient, ② a hydrophobic polymer having a glass transition temperature (Tg) of -65°C to 35°C, ③ a percutaneous absorption-promoting agent, ④ water, and ⑤ a hydrophilic polymer which is soluble or capable of swelling in water; and a medical adhesive which comprises a porous base layer in the plaster layer or in contact with the plaster layer, which enable stable release of the medicinal ingredient, the percutaneous absorption-promoting agents and so on and sustaining of the pharmacological effects over a long period.

  一种医用粘合剂，由含有下列成分的石膏层组成，其特征在于，成分②的掺入量大于成分⑤，且相对于成分①∼⑤的总掺入量不低于 25%（重量百分比），石膏层为 W/O 型： 药物成分、 一种疏水性聚合物，其玻璃转化温度（Tg）为-65°C 至 35°C、 经皮吸收促进剂、 水，以及 可溶于水或能在水中溶胀的亲水性聚合物；以及 一种医用粘合剂，由石膏层中的多孔基底层或与石膏层接触的多孔基底层组成，可使药物成分、促进经皮吸收剂等稳定释放，并长期保持药理作用。
• Aerosol composition containing a film-forming hydroxycarboxylic acid polymer
  申请人：TAKEDA CHEMICAL INDUSTRIES, LTD.

  公开号：EP0521455A2

  公开（公告）日：1993-01-07

  The present invention relates to an aerosol composition which comprises a biodegradable hydroxycarboxylic acid polymer as a film-forming component. This aerosol composition produces the following effects, among others: (1) application to the injured site by spraying will not cause pain; (2) it is biocompatible and resists peeling off after application; (3) it is not readily dissolved in or washed away with water; and (4) it can be allowed to remain on the skin after application since it is biodegradable.

  本发明涉及一种气溶胶组合物，它由可生物降解的羟基羧酸聚合物作为成膜成分。 除其他外，这种气雾剂组合物具有以下效果：(1) 喷洒到受伤部位不会引起疼痛；(2) 具有生物相容性，喷洒后不易脱落；(3) 不易溶于水或被水冲走；(4) 由于可生物降解，喷洒后可留在皮肤上。
• REVERSIBLE, THERMALLY GELLING WATER-BASE MEDICINAL COMPOSITION
  申请人：Wakamoto Pharmaceutical Co., Ltd.

  公开号：EP0694310A1

  公开（公告）日：1996-01-31

  A heat-reversible water-base medicinal composition for ophthalmology, dermatology and the body cavity, which comprises an effective dose of a medicine for pharmacological therapy or diagnosis, methyl-cellulose, citric acid and polyethylene glycol and has the pH of 3 to 10. The composition is highly flowable before administration or application, but gels rapidly by the effect of the body temperature at the affected part after administration or application.

  一种用于眼科、皮肤科和体腔的热可逆水基药物组合物，由有效剂量的药物治疗或诊断用药、甲基纤维素、柠檬酸和聚乙二醇组成，pH 值为 3 至 10。该组合物在给药或使用前流动性很好，但在给药或使用后，受影响部位的体温会使其迅速凝胶化。