hydrocortisone sodium succinate | 125-04-2

• 物质功能分类: 原料药 - 激素及调节内分泌功能类药 - 肾上腺皮质激素类药
• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: hydrocortisone sodium succinate
• 英文别名: HSS；hydrocortisone 21-sodium succinate；sodium;4-[2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-oxoethoxy]-4-oxobutanoate
• CAS: 125-04-2
• 化学式: C₂₅H₃₃O₈*Na
• 分子量: 484.522
• InChiKey: HHZQLQREDATOBM-CODXZCKSSA-M

物化性质

• 熔点：
  169.0-171.2°
• 溶解度：
  H2O:50 mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  -2.13
• 重原子数：
  34
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.76
• 拓扑面积：
  141
• 氢给体数：
  2
• 氢受体数：
  8

安全信息

• WGK Germany：
  3
• RTECS号：
  GM9015000
• 储存条件：
  -20℃。

SDS

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Section 1. Chemical Product and Company Identification
Hydrocortisone Sodium Succinate Catalog
Common Name/
Number(s).
Trade Name
CAS# 125-04-2
Manufacturer
Commercial Name(s)
Hydrocortisone Sodium Succinate

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Section 3. Hazards Identification
Potential Acute Health Effects Slightly hazardous in case of skin contact (irritant), of eye contact (irritant), of ingestion, of inhalation.
Potential Chronic Health CARCINOGENIC EFFECTS: Not available.
Effects MUTAGENIC EFFECTS: Not available.
TERATOGENIC EFFECTS: Not available.
DEVELOPMENTAL TOXICITY: Not available.
Repeated or prolonged exposure is not known to aggravate medical condition.

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Section 4. First Aid Measures
Eye Contact Check for and remove any contact lenses. In case of contact, immediately flush eyes with plenty of water for at
least 15 minutes. Cold water may be used. Get medical attention if irritation occurs.
Skin Contact Wash with soap and water. Cover the irritated skin with an emollient. Get medical attention if irritation develops.
Cold water may be used.
Serious Skin Contact Not available.
Inhalation If inhaled, remove to fresh air. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get
medical attention.
Serious Inhalation Not available.
Ingestion Do NOT induce vomiting unless directed to do so by medical personnel. Never give anything by mouth to an
unconscious person. If large quantities of this material are swallowed, call a physician immediately. Loosen tight
clothing such as a collar, tie, belt or waistband.
Serious Ingestion Not available.

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Section 5. Fire and Explosion Data
Flammability of the Product May be combustible at high temperature.
Auto-Ignition Temperature Not available.
Flash Points Not available.
Flammable Limits Not available.
These products are carbon oxides (CO, CO2). Some metallic oxides.
Products of Combustion
Fire Hazards in Presence of Slightly flammable to flammable in presence of heat.
Various Substances
Explosion Hazards in Presence Risks of explosion of the product in presence of mechanical impact: Not available.
of Various Substances Risks of explosion of the product in presence of static discharge: Not available.
Fire Fighting Media SMALL FIRE: Use DRY chemical powder.
and Instructions LARGE FIRE: Use water spray, fog or foam. Do not use water jet.
Special Remarks on As with most organic solids, fire is possible at elevated temperatures.
Fire Hazards Material in powder form, capable of creating a dust explosion.
Special Remarks on Explosion Fine dust dispersed in air in sufficient concentrations, and in the presence of an ignition source is a potential dust
Hazards explosion hazard.
Hydrocortisone Sodium Succinate

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Section 6. Accidental Release Measures
Small Spill Use appropriate tools to put the spilled solid in a convenient waste disposal container. Finish cleaning by
spreading water on the contaminated surface and dispose of according to local and regional authority
requirements.
Large Spill Use a shovel to put the material into a convenient waste disposal container. Finish cleaning by spreading water
on the contaminated surface and allow to evacuate through the sanitary system.

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Section 7. Handling and Storage
Precautions Keep away from heat. Keep away from sources of ignition. Ground all equipment containing material. Do not
breathe dust. Keep away from incompatibles such as oxidizing agents.
Storage Keep container tightly closed. Keep container in a cool, well-ventilated area. Do not store above -20°C (-4°F).
Freeze.

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Section 8. Exposure Controls/Personal Protection
Engineering Controls Use process enclosures, local exhaust ventilation, or other engineering controls to keep airborne levels below
recommended exposure limits. If user operations generate dust, fume or mist, use ventilation to keep exposure to
airborne contaminants below the exposure limit.
Personal Protection Safety glasses. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent. Gloves.
Personal Protection in Case of Splash goggles. Full suit. Dust respirator. Boots. Gloves. A self contained breathing apparatus should be used
a Large Spill to avoid inhalation of the product. Suggested protective clothing might not be sufficient; consult a specialist
BEFORE handling this product.
Exposure Limits Not available.

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Section 9. Physical and Chemical Properties
Physical state and appearance Solid. (Powdered solid.) Odor Not available.
Taste Not available.
Molecular Weight 484.52 g/mole
White. Off-white.
Color
Not available.
pH (1% soln/water)
Boiling Point Not available.
Not available.
Melting Point
Critical Temperature Not available.
Specific Gravity Not available.
Vapor Pressure Not applicable.
Vapor Density Not available.
Volatility Not available.
Odor Threshold Not available.
Water/Oil Dist. Coeff. Not available.
Ionicity (in Water) Not available.
Dispersion Properties See solubility in water.
Solubility Soluble in cold water.
Hydrocortisone Sodium Succinate

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Section 10. Stability and Reactivity Data
The product is stable.
Stability
Instability Temperature Not available.
Excess heat, incompatible materials, moisture
Conditions of Instability
Reactive with oxidizing agents.
Incompatibility with various
substances
Corrosivity Not available.
Special Remarks on Not available.
Reactivity
Special Remarks on Not available.
Corrosivity
Polymerization Will not occur.

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Section 11. Toxicological Information
Routes of Entry Inhalation. Ingestion.
Toxicity to Animals LD50: Not available.
LC50: Not available.
Chronic Effects on Humans Not available.
Other Toxic Effects on Slightly hazardous in case of skin contact (irritant), of ingestion, of inhalation.
Humans
Special Remarks on Not available.
Toxicity to Animals
Special Remarks on May cause adverse reproductive effects and birth defects (teratogenic) based on animal test data.
Chronic Effects on Humans
Special Remarks on other Acute Potential Health Effects:
Toxic Effects on Humans Skin: May cause skin irritation.
Eyes: May cause eye irritation.
Inhalation: May cause respiratory tract irritation.
Ingestion: May cause nausea and vomiting. May affect respiration, cardiovascular system.
Chronic Potential Health Effects:
Ingestion: Prolonged or repeated ingestion may cause weight loss, nausea, vomiting. It may also affect the blood
(anemia), adrenal gland.

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Section 12. Ecological Information
Ecotoxicity Not available.
BOD5 and COD Not available.
Possibly hazardous short term degradation products are not likely. However, long term degradation products may
Products of Biodegradation
arise.
The product itself and its products of degradation are not toxic.
Toxicity of the Products
of Biodegradation
Special Remarks on the Not available.
Products of Biodegradation
Hydrocortisone Sodium Succinate

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Section 13. Disposal Considerations
Waste Disposal Waste must be disposed of in accordance with federal, state and local environmental
control regulations.

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Section 14. Transport Information
DOT Classification Not a DOT controlled material (United States).
Not applicable.
Identification
Not applicable.
Special Provisions for
Transport
DOT (Pictograms)

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Section 15. Other Regulatory Information and Pictograms
No products were found.
Federal and State
Regulations
California California prop. 65: This product contains the following ingredients for which the State of California has found
to cause cancer which would require a warning under the statute: No products were found.
Proposition 65
Warnings
California prop. 65: This product contains the following ingredients for which the State of California has found
to cause birth defects which would require a warning under the statute: No products were found.
Other Regulations EINECS: This product is on the European Inventory of Existing Commercial Chemical Substances (EINECS No.
204-725-5).
Canada: Listed on Canadian Domestic Substance List (DSL).
China: Not listed on National Inventory.
Japan: Listed on National Inventory (ENCS).
Korea: Listed on National Inventory (KECI).
Philippines: Not listed on National Inventory (PICCS).
Australia: Listed on AICS.
WHMIS (Canada) Not controlled under WHMIS (Canada).
Other Classifications
DSCL (EEC) This product is not classified according Not applicable.
to the EU regulations.
Health Hazard
HMIS (U.S.A.) 1 National Fire Protection
1 Flammability
1 Association (U.S.A.)
Fire Hazard
1 0 Reactivity
Health
Reactivity
0
Specific hazard
Personal Protection
E
WHMIS (Canada)
(Pictograms)
DSCL (Europe)
(Pictograms)
Hydrocortisone Sodium Succinate
TDG (Canada)
(Pictograms)
ADR (Europe)
(Pictograms)
Protective Equipment
Gloves.
Lab coat.
Dust respirator. Be sure to use an
approved/certified respirator or
equivalent.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

氢化可的松琥珀酸钠简介

氢化可的松琥珀酸钠，化学名为：11β，17-二羟基-21-(3-羧基-1-羟丙氧基)孕甾-4-烯-3，20-二酮钠盐。目前的传统生产工艺是以中间体氢化可的松琥珀酸酯及氢氧化钠为原料，在丙酮溶剂中进行化学反应，并在高温条件下回流。反应完成后通过分馏去除丙酮，再调节pH值后过滤得到氢化可的松琥珀酸钠。

背景

气管炎和哮喘是影响人类健康的严重呼吸道疾病，且发病率逐年上升，尤其可以侵扰各年龄段人群。氢化可的松琥珀酸钠属于糖皮质激素类药物，具有很强的抗炎作用，主要用于治疗急性肾上腺皮质功能不全、哮喘急性发作及休克等病症，特别适用于重症患者。相较于传统的醇性制剂，氢化可的松琥珀酸钠吸收快、药效迅速且副作用较少，价格低廉，更加适合临床使用。

应用

2008年，中华医学会呼吸病学分会哮喘学组发布的《支气管哮喘防治指南》建议严重急性哮喘发作时静脉给予氢化可的松琥珀酸钠400～1000mg/d。同年，中华医学会儿科学分会呼吸学组也发布了《儿童支气管哮喘诊断与防治指南》，强调全身应用糖皮质激素是治疗儿童重症哮喘发作的首选方法，严重患儿可静脉注射氢化可的松琥珀酸钠5～10mg/(kg•次)，每4～8小时重复使用一次，一般2～5天内停药。卫生部于2011年发布的《糖皮质激素类药物临床应用指导原则》同样推荐严重急性哮喘发作时静脉给予氢化可的松琥珀酸钠200～1000mg/d。由于地塞米松半衰期较长、起效时间慢且对HPA轴抑制作用较强等缺点，上述三个指南均不推荐使用地塞米松。

应用

氢化可的松琥珀酸钠具有很强的抗炎作用，主要用于急性肾上腺皮质功能不全和哮喘急性发作及休克等症状的治疗。此药物特别适合重症患者的治疗需求。

药理作用

该品为氢化可的松的盐类化合物，在水溶性方面优于氢化可的松，无需额外使用乙醇助溶剂即可实现大剂量给药或局部注射。其主要药理作用包括抗炎、抗过敏和抑制免疫反应等。

制备方法

一种氢化可的松琥珀酸钠的制备方法如下：

1. 在极性溶剂中，将氢化可的松琥珀酸酯与缓冲溶液在0-80℃条件下反应1-4小时，控制pH值为5-8，反应完毕后静置1～4小时，使温度降至40℃以下；
2. 搅拌下缓慢加入碱性溶液，直到pH值达到7.5-11.0，过滤得到白色或类白色的氢化可的松琥珀酸钠。

用途

用作医药中间体。

反应信息

• 作为反应物：
  描述：

  hydrocortisone sodium succinate 生成 氢化可的松 、 可的松 、 4-雄烯-11β-醇-3,17-二酮 、 cortisone sodium succinate
  参考文献：
  名称：

  60Co辐射的皮质类固醇的辐射分解方案。

  摘要：

  已在以下皮质类固醇中鉴定出60钴的放射降解产物：可的松，醋酸可的松，氢化可的松，醋酸氢化可的松，氢化可的松琥珀酸钠，乙酸异氟泼酮，甲基强的松龙，乙酸甲基泼尼松龙，泼尼松龙，醋酸泼尼松龙和泼尼松。已经确定了两种主要的降解过程：损失D环上的皮质类固醇侧链以产生C-17酮，以及将C-11醇（如果存在）转化为C-11酮。在几种皮质类固醇中还发现了由影响侧链的其他变化产生的较小降解产物。这些化合物通常作为加工杂质或降解化合物与皮质类固醇结合。尚未发现60Co辐射特有的新的辐射分解化合物。已显示大多数皮质类固醇对60Co辐射稳定。放射降解的速率为0.2-1.4％/ Mrad。

  DOI：

  10.1002/jps.2600720108
• 作为产物：
  描述：

  丁二酸酐 、 氢化可的松 在 4-二甲氨基吡啶 、 碳酸氢钠 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 、 丙酮 、 水 为溶剂， 反应 9.0h， 以97%的产率得到hydrocortisone sodium succinate
  参考文献：
  名称：

  一种氢化可的松琥珀酸钠的制备方法

  摘要：

  本发明公开了一种氢化可的松琥珀酸钠的制备方法。该方法以琥珀酸酐和氢化可的松为原料制备得到氢化可的松琥珀酸单酯；然后以氢化可的松琥珀酸单酯等为原料在低温下进行反应，反应完成后采用‑20℃左右的丙酮对反应液进行处理，得到氢化可的松琥珀酸钠。该方法采用的工艺条件是低温下生成钠盐，再将反应液加入大量丙酮中，再过滤，滤饼用丙酮带水，最后真空干燥丙酮，避免了高温蒸水的过程，使产品稳定，收率高，产品状态好，在反应时，纯度就能达到97％以上，纯化后，产品完全符合中国药典标准。丙酮能回收利用，也节省了生产成本。所以此方案适合工业化大生产，产品质量也好。

  公开号：

  CN109970834A
• 作为试剂：
  描述：

  雄烯二酮 在 α-MEM 、 normal cultured human breast epithelial cells from early lactation milk 、 阿米卡星 、 hydrocortisone sodium succinate 、 fetal calf serum 、 insulin 作用下， 反应 8.0h， 以1.0%的产率得到雌酚酮
  参考文献：
  名称：

  Androstenedione metabolism in epithelial cells derived from early-lactation human milk

  摘要：

  Epithelial cells derived from duct epithelium were cultured from early lactation human milk in medium supplemented with 15% fetal calf serum, insulin (0.3 u/ml), cortisol 21-sodium succinate (6 micrograms/ml) and amikacin (50 micrograms/ml). The capacity of these cells to metabolize androstenedione to estrone, estradiol and C19 metabolites was studied during continuous culture. After extraction of the medium, the products were subjected to phenolic partition and separated by thin-layer and paper chromatography, followed by recrystallization to constant specific activity. The study demonstrated a progressive increase in the formation of estrone and testosterone over the first 24 h in culture, while estradiol formation showed an initial 2-4 h lag, then increased slowly. The C19 compounds identified were androsterone, 5 alpha-androstanedione, epiandrosterone, dihydrotestosterone and etiocholanolone. 5 alpha-Androstanedione and androsterone were the major 5 alpha-reduced metabolites. Since these cells are derived from normal duct epithelium, their metabolic characteristics may be more representative of normal breast tissue than those of tissue removed from patients with pathological breast disorders.

  DOI：

  10.1016/0039-128x(83)90137-x

文献信息

• [EN] ACC INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE L'ACC ET UTILISATIONS ASSOCIÉES
  申请人：GILEAD APOLLO LLC

  公开号：WO2017075056A1

  公开（公告）日：2017-05-04

  The present invention provides compounds I and II useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.

  本发明提供了化合物I和II，这些化合物可用作乙酰辅酶A羧化酶（ACC）的抑制剂，以及它们的组合物和使用方法。
• [EN] COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF SHP2<br/>[FR] COMPOSÉS ET COMPOSITIONS POUR INHIBER L'ACTIVITÉ DE SHP2
  申请人：NOVARTIS AG

  公开号：WO2016203404A1

  公开（公告）日：2016-12-22

  The present invention relates to compounds of formula I. The compounds are inhibitors of the Src Homolgy-2 phosphatase (SHP2) and thus useful in the treatment of Noonan Syndrome, Leopard Syndrome and cancer.

  本发明涉及式I的化合物。这些化合物是Src同源-2磷酸酶（SHP2）的抑制剂，因此在努南综合征、豹纹综合征和癌症的治疗中有用。
• TRIAZOLE ACC INHIBITORS AND USES THEREOF
  申请人：Gilead Apollo, LLC

  公开号：US20170166584A1

  公开（公告）日：2017-06-15

  The present invention provides triazole compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.

  本发明提供了三唑化合物，可用作乙酰辅酶A羧化酶（ACC）的抑制剂，以及其组合物和使用方法。
• BIODEGRADABLE ORGANIC RADICAL-FUNCTIONALIZED POLYCARBONATES FOR MEDICAL APPLICATIONS
  申请人：International Business Machines Corporation

  公开号：US20160220705A1

  公开（公告）日：2016-08-04

  Paramagnetic, amphiphilic, biocompatible polymers were prepared comprising a carbonate repeat unit bearing a paramagnetic organic radical, more specifically a nitroxyl radical. The radical polymers can be produced in one step from a precursor polymer bearing an active ester side chain by treating the precursor polymer with a radical-bearing nucleophile. The precursor polymer can be prepared by organocatalyzed catalyzed ring opening polymerization (ROP) of a cyclic carbonate monomer bearing an active ester side chain. The radical polymers can be non-toxic and partially biodegradable. The radical polymers have utility as contrast enhancing agents in a medical imaging application and/or as therapeutic agents for treating a medical condition. The radical polymers can also serve as carriers for therapeutic agents (e.g., drugs) and/or medical image enhancing agents (e.g., NIRF dyes).

  具有顺磁性、两性亲疏性、生物相容性的聚合物已经制备好，其中包含一个带有顺磁性有机自由基的碳酸酯重复单元，更具体地说是一个亚硝基自由基。这种自由基聚合物可以通过将带有活性酯侧链的前体聚合物与带有自由基的亲核试剂处理而一步制备而成。前体聚合物可以通过有机催化的环氧化聚合（ROP）来制备，该环氧化单体带有活性酯侧链。这种自由基聚合物可能是无毒且部分可生物降解的。这种自由基聚合物在医学成像应用中可用作增强对比剂，和/或作为治疗医疗状况的治疗剂。这种自由基聚合物还可以作为治疗剂（例如药物）和/或医学图像增强剂（例如NIRF染料）的载体。
• [EN] COMBINATION OF CHIMERIC ANTIGEN RECEPTOR THERAPY AND AMINO PYRIMIDINE DERIVATIVES<br/>[FR] THÉRAPIE COMBINÉE PAR RÉCEPTEUR ANTIGÉNIQUE CHIMÉRIQUE ET DÉRIVÉS D'AMINO PYRIMIDINE
  申请人：NOVARTIS AG

  公开号：WO2016164580A1

  公开（公告）日：2016-10-13

  The invention provides compositions and methods for treating diseases associated with expression of CD19, e.g., by administering a recombinant T cell comprising the CD19 CAR as described herein, in combination with a BTK inhibitor, e.g., an amino pyrimidine derivative described herein. The invention also provides kits and compositions described herein.

  这项发明提供了用于治疗与CD19表达相关疾病的组合物和方法，例如，通过给予包含本文所述的CD19 CAR的重组T细胞，结合一种BTK抑制剂，例如，本文所述的氨基嘧啶衍生物。该发明还提供了本文所述的试剂盒和组合物。