L-thyroxine, sodium salt hexahydrate | 25416-65-3

• 物质功能分类: 分析化学 - 标准品 - 农残、兽药及化肥类
• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: L-thyroxine, sodium salt hexahydrate
• 英文别名: Sodium 4-[4-(2-amino-2-carboxyethyl)-2,6-diiodophenoxy]-2,6-diiodophenolate--water (1/1/1)；sodium;4-[4-[(2S)-2-amino-2-carboxyethyl]-2,6-diiodophenoxy]-2,6-diiodophenolate;hydrate
• CAS: 25416-65-3
• 化学式: C₁₅H₁₀I₄NO₄*6H₂O*Na
• 分子量: 906.948
• InChiKey: ANMYAHDLKVNJJO-LTCKWSDVSA-M

物化性质

• 熔点：
  207 °C
• 比旋光度：
  16 º (c=2,1M HCl/alcohol 1/4)
• 溶解度：
  极微溶于水，微溶于乙醇（96%）。溶于碱金属氢氧化物的稀溶液。
• 稳定性/保质期：
  <p>遵照规定使用和储存，则不会发生分解。</p>

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  96.6
• 氢给体数：
  3
• 氢受体数：
  6

安全信息

• 安全说明：
  S24/25
• WGK Germany：
  3
• 海关编码：
  29379000
• 危险品标志：
  Xn
• 危险类别码：
  R20/21
• 危险品运输编号：
  2811
• 包装等级：
  II
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335
• 储存条件：
  存放在0-6°C的阴凉干燥处。

SDS

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Section 1. Chemical Product and Company Identification
Levothyroxine Sodium Hydrate Catalog
T1281, T1432, T3183
Common Name/
Number(s).
Trade Name
CAS# 25416-65-3; 55-03-8
(anhydrous CAS number)
Manufacturer
Commercial Name(s)
Levothyroxine Sodium Hydrate

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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. Get medical attention.
Skin Contact In case of contact, immediately flush skin with plenty of water. Cover the irritated skin with an emollient. Remove
contaminated clothing and shoes. Wash clothing before reuse. Thoroughly clean shoes before reuse. Get
medical attention.
Serious Skin Contact Wash with a disinfectant soap and cover the contaminated skin with an anti-bacterial cream. Seek medical
attention.
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), nitrogen oxides (NO, NO2...). Some metallic oxides.
Fire Hazards in Presence of Slightly flammable to flammable in presence of open flames and sparks, of heat.
Various Substances Non-flammable in presence of shocks.
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 Not available.
Fire Hazards
Special Remarks on Explosion Not available.
Hazards
Levothyroxine Sodium Hydrate

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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. Wear suitable protective clothing. In case of insufficient ventilation, wear suitable respiratory
equipment. If you feel unwell, seek medical attention and show the label when possible. Avoid contact with skin
and eyes.
Keep container tightly closed. Keep container in a cool, well-ventilated area. Do not store above 8°C (46.4°F).
Storage
Refrigerate. Sensitive to light. Store in light-resistant containers.

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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. (crystalline powder. Powdered solid.) Odor Odorless.
Not available.
Taste
Molecular Weight 798.86 g/mole + xH2O
Off-white. White to yellowish.
Color
Not available.
pH (1% soln/water)
Boiling Point Not available.
Decomposition temperature: 207°C (404.6°F) - 210 C.
Melting Point
Critical Temperature Not available.
Specific Gravity Not available.
Not applicable.
Vapor Pressure
Vapor Density Not available.
Not available.
Volatility
Odor Threshold Not available.
Water/Oil Dist. Coeff. Not available.
Ionicity (in Water) Not available.
Dispersion Properties Not available.
Solubility Partially soluble in cold water.
Solubilitiy in Water: 0.15 g/l @ 25 C.
Levothyroxine Sodium Hydrate

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Section 10. Stability and Reactivity Data
The product is stable.
Stability
Instability Temperature Not available.
Excess heat, incompatible materials, light
Conditions of Instability
Not available.
Incompatibility with various
substances
Corrosivity Not available.
Special Remarks on Light Sensitive
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 (Maternal effects on fertility, fetotoxicity) based on animal 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 by mechanical action.
Inhalation: May cause respiratory tract irritation.
Ingestion: May cause digestive tract irritation. May affect metabolism, thyroid, urinary sytem, behavior
(excitement, headache, coma), cardiovascular system (increased pulse rate),

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

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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 Not available.
Other Classifications WHMIS (Canada) Not controlled under WHMIS (Canada).
DSCL (EEC) This product is not classified according S24/25- Avoid contact with skin and eyes.
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)
TDG (Canada)
(Pictograms)
Levothyroxine Sodium Hydrate
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

简介

L-甲状腺素钠是甲状腺的主要激素之一。它主要控制耗氧速率和总代谢速率，促进一般组织代谢、提高神经兴奋性和身体发育。主要用于治疗甲状腺机能减退、粘液性水肿及克汀病等。

左甲状腺素钠（L-T4）的作用较为迟缓但持久，起效较慢，患者容易耐受。通常每天服用一次，方便且剂量易于掌握。

用途

L-甲状腺素钠是一种有用的化学研究品。其游离型甲状腺素参与维持代谢稳态，是甲状腺激素的一种。它作为甲状腺球蛋白的氨基酸残基合成和储存成分，而甲状腺球蛋白则是甲状腺滤泡胶体的主要蛋白质成分。合成与分泌受垂体激素（TSH）调节。在外周组织中，L-甲状腺素钠会脱碘生成活性代谢物——甲磺酸。尽管D型左甲状腺素钠的活性较小，但它已被用于治疗高脂血症。

反应信息

• 作为反应物：
  描述：

  L-thyroxine, sodium salt hexahydrate 在 盐酸 作用下， 以 甲醇 、 二甲基亚砜 为溶剂， 以96%的产率得到甲状腺素
  参考文献：
  名称：

  Conjugates

  摘要：

  一种化合物，其化学式表示为##STR1##，其中X是一个间隔基团。该化合物可用于将具有醇基团或胺基团的化合物与具有硫醇基团的化合物结合。该化合物可用于将生物活性基团（如抗原）与蛋白质（如酶）结合，从而提供用于酶放大免疫分析方法的酶标记抗原，用于分析样品液中的分析物或代谢物。该化合物还可用于将材料（如蛋白质）固定到固体支持上。

  公开号：

  US05294536A1
• 作为产物：
  描述：

  liothyronine sodium 、 D-甲状腺素 生成 L-thyroxine, sodium salt hexahydrate
  参考文献：
  名称：

  Pharmaceutical preparation comprising an active dispersed on a matrix

  摘要：

  本发明涉及制药技术领域，描述了一种新型的有利的活性成分制备方法。该新型制备方法适用于生产大量的药物剂型。在新型制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油三酯和脂肪酸酯等一种或多种赋形剂组成的基质中。

  公开号：

  US20070122474A1

文献信息

• Levothyroxine compositions having unique triiodothyronine Tmax properties
  申请人：——

  公开号：US20030181524A1

  公开（公告）日：2003-09-25

  The present invention generally relates to stable pharmaceutical compositions, and methods of making and administering such compositions. In one aspect, the invention features stabilized pharmaceutical compositions that include pharmaceutically active ingredients such as levothyroxine (T4) sodium and liothyronine (T3) sodium (thyroid hormone drugs), preferably in an immediate release solid dosage form. Also provided are methods for making and using such immediate release and stabilized compositions.

  本发明一般涉及稳定的制药组合物，以及制备和给予这种组合物的方法。在一个方面，本发明涉及稳定的制药组合物，包括药物活性成分，例如左旋甲状腺素（T4）钠和甲状腺素（T3）钠（甲状腺激素药物），最好是以即时释放固体剂量形式。还提供制备和使用这种即时释放和稳定组合物的方法。
• Resorufin derivatives
  申请人：Boehringer Mannheim GmbH

  公开号：US04954630A1

  公开（公告）日：1990-09-04

  The present invention provides resorufin derivatives of the general formulae: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5, which can be the same or different, are hydrogen, halogen, carboxyl, carboxamido, lower alkoxycarbonyl, cyano or nitro groups or lower alkyl or lower alkoxy radicals, which can be substituted by carboxyl, carboxamido, lower alkoxycarbonyl, cyano or nitro groups, and wherein R.sup.4 and R.sup.5 can together also represent an anellated aromatic residue, Z is a bridge member, A is the residue of a ligand and n is a whole number of from 1 to 200. The present invention also provides processes for the preparation of these resorufin derivatives, as well as intermediates for the preparation thereof.

  本发明提供了一般式为：##STR1##的雷索鲁芬衍生物，其中R.sup.1，R.sup.2，R.sup.3，R.sup.4和R.sup.5可以相同也可以不同，可以是氢，卤素，羧基，羧酰胺基，较低的烷氧基羰基，氰基或硝基或较低的烷基或较低的烷氧基基团，可以被羧基，羧酰胺基，较低的烷氧基羰基，氰基或硝基基团取代，其中R.sup.4和R.sup.5还可以共同表示一个接环芳香残基，Z是桥接成员，A是配体残基，n是从1到200的整数。本发明还提供了制备这些雷索鲁芬衍生物的方法，以及其制备中间体。
• Immediate release pharmaceutical compositions
  申请人：——

  公开号：US20030194436A1

  公开（公告）日：2003-10-16

  The present invention generally relates to stable pharmaceutical compositions, and methods of making and administering such compositions. In one aspect, the invention features stabilized pharmaceutical compositions that include pharmaceutically active ingredients such as levothyroxine (T4) sodium and liothyronine (T3) sodium (thyroid hormone drugs), preferably in an immediate release solid dosage form. Also provided are methods for making and using such immediate release and stabilized compositions.

  本发明通常涉及稳定的药物组合物、制备和使用该组合物的方法。在一方面，本发明涉及稳定的药物组合物，其中包括药效成分，例如左甲状腺素（T4）钠和甲状腺素（T3）钠（甲状腺激素类药物），优选为立即释放的固体剂量形式。此外，还提供了制备和使用此类立即释放和稳定组合物的方法。
• Levothyroxine compositions and methods
  申请人：——

  公开号：US20030199585A1

  公开（公告）日：2003-10-23

  The present invention generally relates to stable pharmaceutical compositions, and methods of making and administering such compositions. In one aspect, the invention features stabilized pharmaceutical compositions that include pharmaceutically active ingredients such as levothyroxine (T4) sodium and liothyronine (T3) sodium (thyroid hormone drugs), preferably in an immediate release solid dosage form. Also provided are methods for making and using such immediate release and stabilized compositions.

  本发明通常涉及稳定的药物制剂，以及制备和给药这种制剂的方法。在一个方面，本发明涉及稳定的药物制剂，包括药物活性成分，例如左甲状腺素（T4）钠和左旋甲状腺素（T3）钠（甲状腺激素药物），最好是以立即释放的固体剂量形式。还提供了制备和使用这种立即释放和稳定的制剂的方法。
• Levothyroxine Formulations
  申请人：Jiang Zhi-Qiang

  公开号：US20130053445A1

  公开（公告）日：2013-02-28

  A levothyroxine composition includes levothyroxine sodium and mannitol. The composition is a solid. The composition may include from 100 to 500 micrograms levothyroxine sodium and from 1 to 5 milligrams mannitol. The composition may include from 100 to 200 micrograms levothyroxine sodium, and the mass ratio of mannitol to levothyroxine sodium in the composition may be at most 40:1. The composition may include about 500 micrograms levothyroxine sodium, and the mass ratio of mannitol to levothyroxine sodium in the composition may be at most 10:1.

  一种左旋甲状腺素组合物包括左旋甲状腺素钠和甘露醇。该组合物为固体。该组合物可以包含100至500微克左旋甲状腺素钠和1至5毫克甘露醇。该组合物可以包含100至200微克左旋甲状腺素钠，且组合物中甘露醇与左旋甲状腺素钠的质量比最多为40:1。该组合物可以包含约500微克左旋甲状腺素钠，且组合物中甘露醇与左旋甲状腺素钠的质量比最多为10:1。