HYOSCYAMINE SULFATE | 5908-99-6

• 物质功能分类: 原料药 - 神经系统用药 - 拟胆碱药
• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 托烷生物碱
• 英文名称: HYOSCYAMINE SULFATE
• 英文别名: ATROPINE SULFATE；atropine sulphate monohydrate；DL-tropic acid tropane-3endo-yl ester; sulfate；DL-Tropasaeure-tropan-3endo-ylester; Sulfat
• CAS: 5908-99-6；5979-02-2；6835-16-1；73791-47-6
• 化学式: C₁₇H₂₃NO₃*H₂O*H₂O₄S
• 分子量: 405.469
• InChiKey: PVGPXGKNDGTPTD-ODJCEOKHSA-N

物化性质

• 熔点：
  189-192 °C (A)(lit.)
• 比旋光度：
  -0.6 º (per USP 25 ºC)
• 溶解度：
  H2O:2.5g/mL(在4℃下可稳定数天。)
• LogP：
  2.137 (est)

计算性质

• 辛醇/水分配系数(LogP)：
  0.45
• 重原子数：
  27.0
• 可旋转键数：
  4.0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  155.87
• 氢给体数：
  3.0
• 氢受体数：
  6.0

安全信息

• TSCA：
  Yes
• 危险等级：
  6.1
• 危险品标志：
  T+
• 安全说明：
  S1,S23,S26,S36/37/39,S45
• 危险类别码：
  R36/37/38,R43,R26/28
• WGK Germany：
  2
• 海关编码：
  29399900
• 危险品运输编号：
  UN 1544 6.1/PG 2
• 危险类别：
  6.1
• RTECS号：
  CK2455000
• 包装等级：
  II
• 储存条件：
  20°C

SDS

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Section 1. Chemical Product and Company Identification
Hyoscyamine sulfate
Common Name/
Trade Name
Hyoscyamine sulfate

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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 In case of contact, immediately flush skin with plenty of water for at least 15 minutes while removing
contaminated clothing and shoes. Cover the irritated skin with an emollient. Cold water may be used.Wash
clothing before reuse. Thoroughly clean shoes before reuse. Get medical attention immediately.
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.
Not available.
Flash Points
Flammable Limits Not available.
Products of Combustion These products are carbon oxides (CO, CO2), nitrogen oxides (NO, NO2...), sulfur oxides (SO2, SO3...).
Fire Hazards in Presence of Slightly flammable to flammable in presence of heat.
Various Substances
Risks of explosion of the product in presence of mechanical impact: Not available.
Explosion Hazards in
Risks of explosion of the product in presence of static discharge: Not available.
Presence of Various
Substances
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

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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 Poisonous solid.
Stop leak if without risk. Do not get water inside container. Do not touch spilled material. Use water spray
to reduce vapors. Prevent entry into sewers, basements or confined areas; dike if needed. Eliminate all
surface and allow to evacuate through the sanitary system.
Hyoscyamine sulfate

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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 ingest. Do not breathe dust. Wear suitable protective clothing. If ingested, seek medical advice
immediately and show the container or the label.
Keep container tightly closed. Keep container in a cool, well-ventilated area. Sensitive to light. Store in
Storage
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
a Large Spill used 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. Odor Not available.
Not available.
Taste
Molecular Weight 712.85 g/mole
Not available.
Color
Not available.
pH (1% soln/water)
Boiling Point Decomposes.
206°C (402.8°F)
Melting Point
Critical Temperature Not available.
Specific Gravity Not available.
Vapor Pressure Not applicable.
Vapor Density Not available.
Not available.
Volatility
Odor Threshold Not available.
Not available.
Water/Oil Dist. Coeff.
Ionicity (in Water) Not available.
Dispersion Properties See solubility in water.
Solubility Soluble in cold water.

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Section 10. Stability and Reactivity Data
Stability The product is stable.
Instability Temperature Not available.
Conditions of Instability Excess heat
Incompatibility with various Not available.
substances
Corrosivity Non-corrosive in presence of glass.
Special Remarks on Not available.
Reactivity
Hyoscyamine sulfate
Not available.
Special Remarks on
Corrosivity
Polymerization Will not occur.

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Section 11. Toxicological Information
Routes of Entry Inhalation. Ingestion.
LD50: Not available.
Toxicity to Animals
LC50: Not available.
Chronic Effects on Humans Not available.
Hazardous in case of ingestion.
Other Toxic Effects on
Slightly hazardous in case of skin contact (irritant), of inhalation.
Humans
Special Remarks on Not available.
Toxicity to Animals
Special Remarks on Not available.
Chronic Effects on Humans
Special Remarks on other May cause skin, eye, and respiratory tract irritation.
Toxic Effects on Humans Harmful if swallowed. May cause constipation. May affect behavior/central nervous system, respiratory
system (dyspnea), cardiovascular system, vision. An anticholinergic agent. It can cause blurred vision,
photophobia, vasodilation, rapid and weak pulse, tachydardia, hyperpyrexia, excitement, muscular
incoordination, convulsions, agitation, restlessness, disturbed gait and speech, hallucinations, delirium, and
pupil dilation, bradycardia.

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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 of Biodegradation
products may arise.
The products of degradation are less toxic than the product itself.
Toxicity of the Products
of Biodegradation
Not available.
Special Remarks on the
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.

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Section 14. Transport Information
DOT Classification CLASS 6.1: Poisonous material.
UNNA: 1544 : Alkaloid salt, solid, n.o.s. (Hyoscyamine sulfate) PG: III
Identification
Special Provisions for Not available.
Transport
DOT (Pictograms)
Hyoscyamine sulfate

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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
Proposition 65 found to cause cancer which would require a warning under the statute: No products were found.
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 OSHA: Hazardous by definition of Hazard Communication Standard (29 CFR 1910.1200).
WHMIS (Canada) CLASS D-1B: Material causing immediate and serious toxic effects (TOXIC).
Other Classifications
DSCL (EEC) R25- Toxic if swallowed. S45- In case of accident or if you feel unwell,
seek medical advice immediately (show the
label where possible).
Health Hazard
HMIS (U.S.A.) 2 National Fire Protection
1 Flammability
1 Association (U.S.A.)
Fire Hazard
2 0 Reactivity
Health
Reactivity
0
Specific hazard
Personal Protection
E
WHMIS (Canada)
(Pictograms)
DSCL (Europe)
(Pictograms)
TDG (Canada)
(Pictograms)
ADR (Europe)
(Pictograms)
Protective Equipment
Gloves.
Lab coat.
Dust respirator. Be sure to use an
approved/certified respirator or
equivalent.
Safety glasses.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

药理作用

硫酸阿托品是一种典型的M胆碱受体阻断药。一般剂量时它能解除胃肠平滑肌痉挛、抑制腺体分泌、扩大瞳孔、升高眼压、产生眼调节麻痹效应，同时还能使心率加快、支气管扩张。大剂量使用时，则会对血管平滑肌发挥影响，扩张血管、解除痉挛性收缩，从而改善微循环。与其它颠茄生物碱相比，它对心脏、肠和支气管平滑肌的作用更强且更持久。

生物活性

硫酸阿托品硫酸盐单水合物是一种竞争性毒蕈碱型乙酰胆碱受体拮抗剂，其IC50值为2.5 nM。

靶点

Target	Value
mAChR	2.5 nM

体外研究

硫酸阿托品增加神经递质多巴胺的释放至100-500 mM，对体外玻璃体的影响为250 mg。它还可以诱导大脑皮层扩散性抑制（SD），并减少电生理反应ERG b和d波，导致RPE电势衰减振荡，并逆转了ERG c波。在视网膜中，阿托品仅在产生严重非特异性副作用的剂量下才抑制近视。

体内研究

1毫克/千克腹腔注射硫酸阿托品可以在训练小鼠后立即防止抗胆碱酯酶诱导的记忆力增强，而甲基阿托品则没有此效果。犬中，阿托品能有效防止心动过缓和第二度心脏传导阻滞，导致交替脉和高血压。在大鼠中，在10 nM新斯的明存在下，阿托品对处理引起的乙酰胆碱输出无影响；但在100 nM和1000 nM新斯的明存在时会更大、更长时间地增加这种效果。与先用生理盐水处理的大鼠相比，阿托品不仅阻止了CGS诱导的快速眼动（REM）睡眠增加，还倾向于降低REM睡眠时间。它还能减少正常大鼠和去肾上腺髓质大鼠由运动引起的垂体催乳素释放分别达50%和90%，同时减少正常大鼠的疲劳时间67%。

化学性质

硫酸阿托品为无色结晶或白色结晶粉末，熔点为190-194℃。其1克晶体能溶于0.4毫升水、2.5毫升沸醇、5毫升醇、2.5毫升甘油、420毫升氯仿和3000毫升乙醚。无气味，有风化性遇光易变质，味道极其苦涩且剧毒。

用途

硫酸阿托品是一种抗胆碱药，用于解除平滑肌痉挛及抑制腺体分泌。适用于胃与十二指肠溃疡、胃肠道和肾绞痛、胆绞痛等病症的治疗；还常被用于散瞳检查及验光、角膜炎、虹膜睫状体炎以及麻醉前给药等场景，此外也可用在有机磷杀虫剂中毒、感染性休克以及锑制剂引起的急性心源性脑缺血综合症等情况。

生产方法

硫酸阿托品可以通过合成法或植物提取法制备。

1. 合成法：将阿托品乙醇溶液经过活性炭脱色，然后在冷冻条件下加入硫酸调节pH值为5-6。随后加入乙醚，待析出结晶后进行过滤，并用冷冻的乙醇及乙醚各洗一次，最后干燥即得产物。
2. 植物提取法：将唐古特山莨菪根粉碎过筛并碱化至pH大于10以上，采用甲醛酯提取。使用20%硫酸调节所得甲醛酯溶液的pH为3-4后进行分离操作。取硫酸溶液，调pH至10以上后用四氯化碳萃取，进一步分离，从四氯化碳溶液中析出莨菪碱结晶。在无水乙醇中的莨菪碱溶液加入2%氢氧化钠的无水乙醇溶液，在室温下完成消旋反应。过滤除去碳酸氢钠，向滤液中加入20%硫酸的无水乙醇溶液使其成盐，经活性炭脱色后减压回收乙醇，并添加丙酮结晶出产品。

反应信息

• 作为反应物：
  描述：

  HYOSCYAMINE SULFATE 、 alkaline earth salt of/the/ methylsulfuric acid 生成 (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 2-phenylprop-2-enoate
  参考文献：
  名称：

  Hesse, Justus Liebigs Annalen der Chemie, 1893, vol. 277, p. 306

  摘要：

  DOI：
• 作为产物：
  描述：

  Atropine 在 硫酸 作用下， 以 乙醇 为溶剂， 反应 0.5h， 以92%的产率得到HYOSCYAMINE SULFATE
  参考文献：
  名称：

  一种硫酸阿托品的合成方法

  摘要：

  本发明属于化学合成领域，具体涉及一种硫酸阿托品的制备方法。先制备托品酯，然后制备阿托品，再成盐制得硫酸阿托品，最后经精制得到产品。在制备托品酯的过程中，严格控制反应温度105‑111℃，结晶温度0‑5℃，以提高托品酯的收率。在还原反应制备阿托品的过程中，采用钯炭作为催化剂，并严格控制反应温度10‑15℃，有效地提高其产品质量。通过配制成硫酸乙醇溶液来稀释硫酸，控制其滴加速度，确保硫酸阿托品的质量稳定。

  公开号：

  CN113321648B

文献信息

• METHODS AND COMPOSITIONS FOR TREATING INFECTION
  申请人：UNIVERSITY OF ROCHESTER

  公开号：US20150238473A1

  公开（公告）日：2015-08-27

  Provided herein are compositions and methods for treating or preventing infection.

  本文提供了用于治疗或预防感染的组合物和方法。
• Cathinone Derivatives, Pharmaceutical Formulations, and Methods
  申请人：The Corporation of Mercer University

  公开号：US20220056029A1

  公开（公告）日：2022-02-24

  Compounds, such as cathinone derivatives, and pharmaceutical formulations that include the compounds. The compounds may have a first selectivity for a first receptor subtype that is at least 10 times greater than a second selectivity for a second receptor subtype from the same class of receptors. Methods of treating patients, which may include administering to a patient a pharmaceutical formulation that includes a compound, such as a cathinone derivative.

  化合物，例如卡西酮衍生物，以及包括这些化合物的制药配方。这些化合物可能对于同一类别的第二个受体亚型的第一选择性至少比第二选择性高10倍。治疗患者的方法，可能包括向患者施用包括化合物（例如卡西酮衍生物）的制药配方。
• PROPHYLACTIC OR THERAPEUTIC AGENT FOR OCULAR DISEASE ACCOMPANIED BY OPTIC NERVE DISORDER
  申请人：Santen Pharmaceutical Co., Ltd

  公开号：EP2251009A1

  公开（公告）日：2010-11-17

  The present invention provides a novel pharmaceutical use of 2-phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof. 2-Phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof exhibits an excellent suppressive effect on retinal ganglion cell death in a pharmacological test using rats, and is therefore useful as a prophylactic or therapeutic agent for an eye disease accompanied by optic nerve disorder.

  本发明提供了一种 2-苯基-1,2-苯并异硒唑-3(2H)-酮或其盐的新型药物用途。在用大鼠进行的药理试验中，2-苯基-1,2-苯并异硒唑-3(2H)-酮或其盐对视网膜神经节细胞的死亡有很好的抑制作用，因此可用作伴有视神经障碍的眼病的预防或治疗药物。
• PREVENTIVE AND/OR REMEDY FOR HAND AND FOOT SYNDROME
  申请人：ONO Pharmaceutical Co., Ltd.

  公开号：EP2554184A1

  公开（公告）日：2013-02-06

  The agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity can be provided. The agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity can be safely administered to the patients with Hand-Foot Syndrome, and has shown the superior preventive and/or treatment effect against Hand-Foot Syndrome.

  可以提供由具有抗胆碱能活性的化合物组成的预防和/或治疗手足综合征的制剂。由具有抗胆碱能活性的化合物组成的预防和/或治疗手足综合征的制剂可安全地用于手足综合征患者，并显示出对手足综合征具有卓越的预防和/或治疗效果。
• Lens incorporating myopia control optics and muscarinic agents
  申请人：Johnson & Johnson Vision Care, Inc.

  公开号：EP2693259A1

  公开（公告）日：2014-02-05

  Ophthalmic devices, such as contact lenses, may incorporate myopia control optics in combination with therapeutic agents also known to control myopia to create a drug delivery mechanism to inhibit or arrest the progression of myopia in individuals. Any number of contact lenses incorporating myopia control optics may be combined with a therapeutic agent such as atropine, atropine sulphate monohydrate, and/or pirenzepine or dopamine agonists

  眼科设备（如隐形眼镜）可将近视控制光学元件与已知可控制近视的治疗剂结合在一起，形成一种药物输送机制，以抑制或阻止个人近视的发展。任何一种含有近视控制光学元件的隐形眼镜都可以与治疗剂如阿托品、一水硫酸阿托品和/或哌仑西平或多巴胺激动剂结合使用。