萘夫西林钠 | 7177-50-6

• 物质功能分类: 原料药 - 抗生素类药物 - 青霉素类药
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 中文名称: 萘夫西林钠
• 英文名称: Nafcillin sodium, United States PharmacopeiaReference Standard
• CAS: 7177-50-6
• 化学式: C21H24N2NaO6S
• 分子量: 455.5
• InChiKey: RKBDQTFFBRQMPN-KMFBOIRUSA-N

物化性质

• 溶解度：
  H2O中可溶50mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  1.28
• 重原子数：
  31
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  122
• 氢给体数：
  3
• 氢受体数：
  7

安全信息

• 危险品标志：
  Xn,Xi
• 安全说明：
  S26,S36
• 危险类别码：
  R36/37/38
• WGK Germany：
  3
• 海关编码：
  29411099

制备方法与用途

生物活性

Nafcillin sodium (CL 8491) 可逆的抑制 β-内酰胺酶，Kd为33 mM。

靶点

Target	Value
β-lactamase	33 mM(Kd)

体外研究

Nafcillin sodium通过Ser-70与β-内酰胺酶形成一个共价的酰基酶中间体，使β-内酰胺酶灭活。超过80 mM浓度时，200秒内，Nafcillin显示出对β-内酰胺酶完全的抑制作用 。除去过量Nafcillin，被抑制的酶能够被完全重激活，速率常数为2×10Nafcillin sodium对青霉素耐药的葡萄球菌具有活性。在体外，具有抗葡萄球菌活性的最小必需浓度范围为0.2微克/毫升到2微克/毫升。

体内研究

Nafcillin (100 mg/kg; s.c.) exhibits bactericidal activity against methicillin-susceptible Staphylococcus aureus (MSSA) and methicillin-resistant S. aureus (MRSA), with MIC s of 0.5 μg/mL and 64.0 μg/mL for S. aureus strains Xen-29 and Xen-1, respectively, in mice.

Animal Model:	CD-1 female mice (20-25 g), with MRSA- and MSSA-infected
Dosage:	100 mg/kg
Administration:	Subcutaneous injection
Result:	Protected 100% of the healthy mice with MSSA infections.

文献信息

• EMULSION-TYPE EXTERNAL PREPARATION, AND METHOD FOR PRODUCTION THEREOF
  申请人：Tanoue Yasuhisa

  公开号：US20100256238A1

  公开（公告）日：2010-10-07

  Disclosed are: an emulsion-type external preparation in which the precipitation of crystals of an alkali metal salt or an alkali earth metal salt of a carboxylic acid-type pharmaceutical active ingredient compound or a hydrate of the salt cab be prevented effectively, which is mildly irritative, and in which the decrease in the content of the active ingredient can be prevented; and a method for producing the emulsion-type external preparation. Specifically disclosed are: an emulsion-type external preparation produced by mixing an emulsion and a treated acidic water-soluble polymer solution, wherein the emulsion is produced by emulsifying the following components (a) and (b): (a) an aqueous phase comprising a pharmaceutical active ingredient compound having a carboxylate group and taking the form of an alkali metal salt or an alkali earth metal salt and an aqueous solvent; and (b) an oily phase comprising at least one oily component selected from the group consisting of a fatty acid ester, hydrocarbon, an animal or plant oil, a hydrogenated oil thereof and a natural wax, and wherein the treated acidic water-soluble polymer solution is prepared by treating the whole or a part of an acidic water-soluble polymer with a basic substance in an aqueous solvent; and a method for producing the emulsion-type external preparation. Also specifically disclosed are: an emulsion-type external preparation produced by mixing an emulsified composition comprising a pharmaceutical active ingredient compound having a carboxylate group and taking the form of an alkali metal salt or an alkali earth metal salt with a solution comprising an acidic water-soluble polymer treated with a basic substance; and a method for producing the emulsion-tube external preparation.

  本发明涉及一种乳液型外用制剂，能够有效地防止羧酸类药物活性成分化合物的碱金属盐或碱土金属盐或其水合物晶体的沉淀，具有轻微的刺激性，并且可以防止药物活性成分含量的减少；以及一种制备乳液型外用制剂的方法。具体而言，本发明揭示了一种由乳化剂和处理过的酸性水溶性聚合物溶液混合制成的乳液型外用制剂，其中乳化剂是由以下组分（a）和（b）乳化制成的：（a）包含具有羧酸基并呈碱金属盐或碱土金属盐形式的药物活性成分化合物和水溶剂的水相；以及（b）包含至少一种从脂肪酸酯，烃，动植物油，其氢化物和天然蜡组成的油相。处理过的酸性水溶性聚合物溶液是通过在水溶剂中用碱性物质处理整个或部分酸性水溶性聚合物制备的。本发明还具体揭示了一种由具有羧酸基并呈碱金属盐或碱土金属盐形式的药物活性成分化合物的乳化组合物和经碱性物质处理的酸性水溶性聚合物溶液混合制成的乳液型外用制剂，以及制备乳液型外用制剂的方法。