Blephamide S.O.P. | 52-21-1

• 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: Blephamide S.O.P.
• 英文别名: inflamase forte；inflamase mild；Prednefrin；Econopred；Omnipred；Prednisolone-21-acetate；[2-(11,17-dihydroxy-10,13-dimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-yl)-2-oxoethyl] acetate
• CAS: 52-21-1
• 化学式: C₂₃H₃₀O₆
• 分子量: 402.488
• InChiKey: LRJOMUJRLNCICJ-UHFFFAOYSA-N

物化性质

• 熔点：
  240-244 °C
• 比旋光度：
  D25 +116° (dioxane)
• 沸点：
  579.8±50.0 °C(Predicted)
• 密度：
  1.28±0.1 g/cm3(Predicted)
• 溶解度：
  几乎不溶于水，微溶于乙醇 (96%) 和二氯甲烷。
• 稳定性/保质期：

  稳定，不与强氧化剂相容。

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.7
• 拓扑面积：
  101
• 氢给体数：
  2
• 氢受体数：
  6

安全信息

• 危险品标志：
  T
• 安全说明：
  S45
• 危险类别码：
  R25
• WGK Germany：
  3
• 海关编码：
  2937210000
• 危险品运输编号：
  UN 2811 6.1/PG 3
• RTECS号：
  TU4152500
• 储存条件：
  本品应密封存放在阴凉干燥的地方。

SDS

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Section 1. Chemical Product and Company Identification
Prednisolone acetate Catalog
YY1423, P1219, PR100
Common Name/
Number(s).
Trade Name
CAS# 52-21-1
Manufacturer
RTECS TU4152500
SPECTRUM CHEMICAL MFG. CORP.
TSCA TSCA 8(b) inventory:
Prednisolone acetate
Commercial Name(s) Prednisolone 21-Acetate; Cormalone; Cortpred; Meticortelone
CI# Not available.
acetate; Nisolone; Prediacortine; Perdicort
(11beta)-11,17,21-Trihydroxypregna-1,4-diene-3,20-dione acetate
Synonym
IN CASE OF EMERGENCY
Chemical Name
(11.beta.)-
Chemical Family Not available. CALL [phone]
Chemical Formula C21H26O5
SPECTRUM CHEMICAL MFG. CORP.

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Section 2.Composition and Information on Ingredients
Exposure Limits
TWA (mg/m3) STEL (mg/m3) CEIL (mg/m3)
Name CAS # % by Weight
1) Prednisolone acetate 52-21-1 100
Not applicable.
Toxicological Data
on Ingredients

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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.
CARCINOGENIC EFFECTS: Not available.
Potential Chronic Health
Effects MUTAGENIC EFFECTS: Not available.
TERATOGENIC EFFECTS: Not available.
DEVELOPMENTAL TOXICITY: Classified Reproductive system/toxin/female, Reproductive system/toxin/male
[POSSIBLE].
Repeated or prolonged exposure is not known to aggravate medical condition.
Prednisolone acetate

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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. 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.
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.
Products of Combustion These products are carbon oxides (CO, CO2).
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.
Risks of explosion of the product in presence of static discharge: Not available.
of Various Substances
SMALL FIRE: Use DRY chemical powder.
Fire Fighting Media
and Instructions LARGE FIRE: Use water spray, fog or foam. Do not use water jet.
Not available.
Special Remarks on
Fire Hazards
Special Remarks on Explosion Not available.
Hazards

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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.
Prednisolone acetate

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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.
Storage Keep container tightly closed. Keep container in a cool, well-ventilated area.

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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. (Solid crystalline powder.) Odor Odorless.
Taste Not available.
Molecular Weight 402.49 g/mole
Color White.
pH (1% soln/water) Not available.
Boiling Point Not available.
Melting Point Decomposes. (237°C or 458.6°F)
Critical Temperature Not available.
Not available.
Specific Gravity
Vapor Pressure Not applicable.
Vapor Density Not available.
Volatility Not available.
Odor Threshold Not available.
Not available.
Water/Oil Dist. Coeff.
Ionicity (in Water) Not available.
See solubility in water, methanol, acetone.
Dispersion Properties
Solubility Soluble in methanol, acetone.

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Section 10. Stability and Reactivity Data
Stability The product is stable.
Not available.
Instability Temperature
Conditions of Instability Not available.
Incompatibility with various Not available.
substances
Corrosivity Non-corrosive in presence of glass.
Prednisolone acetate
Special Remarks on Not available.
Reactivity
Special Remarks on Not available.
Corrosivity
Polymerization No.

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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).
Chronic Effects on Humans
Excreted in maternal milk in human.
Special Remarks on other Acute Potential Health Effects:
Toxic Effects on Humans Skin: May cause skin irritation. It may be absorbed through the skin.
Eyes: Dust may cause eye irritation.
Inhalation: Dust may cause respiratory tract irritation.
Ingestion: May cause gastrointestinal tract irritation. May also affect behavior (toxic psychosis), metabolism
(anorexia), and urinary system. This material is readily absorbed from the gastrointestinal tract. Ingestion of a
massive single dose is unlikely to cause adverse effects.
Chronic Potential Health Effects:
Prolonged or repeated exposure by inhalation, ingestion, or skin contact may cause allergic reaction (possible
hypersensitization).
Other symptoms of chronic overdose effects may include, acne or other skin problems, weight loss or weight
gain, hip or shoulder pain, fullness in face, fluid retention associated with sodium retention, potassium
loss,swelling of feet or lower legs, excess or abnormal thirst, menstrual irregularities, nausea, vomiting, irregular
heartbeat, muscle cramps, weakness, osteoporosis, increased susceptibility to infection, psychosis, and eye
problems. May also affect urinary system (polyuria), liver, adrenal gland.

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Section 12. Ecological Information
Ecotoxicity Not available.
BOD5 and COD Not available.
Products of Biodegradation Possibly hazardous short term degradation products are not likely. However, long term degradation products may
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

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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.
Prednisolone acetate

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

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Section 15. Other Regulatory Information and Pictograms
TSCA 8(b) inventory: Prednisolone acetate
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.
200-134-1).
Canada: Listed on Canadian Domestic Substance List (DSL).
China: Not listed on National Inventory.
Japan: Not listed on National Inventory (ENCS).
Korea: Listed on National Inventory (KECI).
Philippines: Mot listed on National Inventory (PICCS).
Australia: Listed on AICS.
WHMIS (Canada) CLASS D-2A: Material causing other toxic effects (VERY TOXIC).
Other Classifications
DSCL (EEC)
R62- Possible risk of impaired fertility. S36- Wear suitable protective clothing.
R63- Possible risk of harm to the
unborn child.
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)
TDG (Canada)
(Pictograms)
Prednisolone acetate
ADR (Europe)
(Pictograms)
Protective Equipment
Gloves.
Lab coat.
Dust respirator. Be sure to use an
approved/certified respirator or
equivalent. Wear appropriate respirator
when ventilation is inadequate.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

醋酸泼尼松龙 糖皮质激素类药物

醋酸泼尼松龙是一种糖皮质激素类药物，能够与细胞内的糖皮质激素受体结合，形成复合物，进入细胞核，与DNA结合，调节基因的转录和蛋白合成，从而发挥其药理作用。它主要具有抗炎、抗过敏及免疫抑制等作用。在中枢神经系统中，小剂量兴奋而大剂量则会抑制。

这种药物主要用于治疗各种过敏性、炎症性和自身免疫性疾病，还用于器官移植中的免疫抑制治疗。局部使用时，眼部可能出现结膜充血和角膜水肿；皮肤上则可导致萎缩、毛细血管扩张及色素沉着等不良反应。

研发历史

醋酸泼尼松龙是由美国制药公司默克（Merck）于1955年开发的。通过在泼尼松龙的C21位置添加一个醋酸基团，使得其亲脂性增强，更容易穿过细胞膜，提高生物利用度和药效。相比泼尼松龙，它具有更强的抗炎作用；与氢化可的松相比，则是前者的5.3倍。

作用机制 化学结构与特性

醋酸泼尼松龙的化学结构类似于强的松，在C11位置有一个双键，使其抗炎效果增强约3～5倍。它通过抑制炎症反应中的组织水肿、纤维沉积和毛细血管扩张以及吞噬细胞游走来发挥其抗炎作用；在抗过敏机制方面，则是通过减少肥大细胞及嗜碱性粒细胞的释放，并抑制IgE介导的炎症介质合成与释放。

生物活性

醋酸泼尼松龙是一种中效糖皮质激素，其作用与泼尼松相同。口服吸收快且完全，在1小时内达到血药浓度峰值；血浆蛋白结合率为90%～95%，半衰期约为200分钟，并可进入胎儿循环和乳汁。

用法用量

• 口服：每次5~10毫克，每日3~4次；维持量为每日5~10毫克。
• 静滴：使用磷酸钠或琥珀酸钠配制，每次10~25毫克溶于5%或10%葡萄糖注射液中，以500毫升溶液进行滴注。
• 肌内或关节腔内注射：采用醋酸酯形式，每次剂量为5~50毫克。

药物相互作用

与其它糖皮质激素类药物联用时可能增强疗效及不良反应；与非甾体抗炎药合用会增加消化道溃疡的风险；与某些降血糖药物或胰岛素联合使用时会减弱其效果；与利尿剂配伍使用则可能导致低钾血症风险增加；与雌激素并用时有促进水肿可能；与洋地黄同服时需警惕洋地黄中毒情况；同时应用疫苗也可能影响免疫反应。

化学性质

醋酸泼尼松龙呈白色或类白色的结晶粉末，微溶于水但易溶于乙醇、氯仿及乙酸乙酯中而不溶解于石油醚。其化学结构包括四环烷酮结构，并具有抗炎、抗过敏和免疫抑制等生物活性。可通过从动物肾上腺皮质提取或人工合成获得。

用途

适用于治疗类风湿关节炎、风湿热、红斑狼疮、硬皮病、皮肌炎以及急性淋巴白血病等多种疾病。

反应信息

• 作为产物：
  描述：

  [2-(9-bromo-11,17-dihydroxy-10,13-dimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl)-2-oxoethyl] acetate 在 甲酸 、 2,2'-azobis(2-methylpropionamidine) hydrochloride 、 甲酸铵 作用下， 以 2-甲基四氢呋喃 为溶剂， 以83%的产率得到Blephamide S.O.P.
  参考文献：
  名称：

  9-卤代甾体化合物的脱卤方法及应用

  摘要：

  本发明提供了一种9‑卤代甾体化合物的脱卤方法及应用，涉及化学合成技术领域。9‑卤代甾体化合物的脱卤方法，包括如下步骤：化合物I与氢供体和偶氮类自由基引发剂反应，得到9‑卤代甾体化合物的9位脱卤产物化合物II。本发明提供的9‑卤代甾体化合物的脱卤方法，氢供体采用次磷酸及次磷酸盐、甲酸及甲酸盐、有机硅氢化物、肼类化合物或环己烯中的一种或几种的组合，引发剂采用偶氮类自由基引发剂，反应中未使用铬、二价铬盐、三价铬盐或氢化三丁基锡等毒性较大，对环境造成严重污染的试剂，绿色环保，合成工艺简便易行，提高了生产适用性。

  公开号：

  CN112142813A