quinidine; sulfate | 6119-70-6

• 物质功能分类: 原料药 - 抗寄生虫病药 - 抗疟药
• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 金鸡纳生物碱
• 英文名称: quinidine; sulfate
• 英文别名: Chinidin; Sulfat；Chinidin; Sulfat-Dihydrat；(S)-[(2R,4S,5R)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-(6-methoxyquinolin-4-yl)methanol;sulfuric acid;hydrate
• CAS: 6119-70-6；6151-39-9；6183-68-2；6485-42-3；6591-63-5
• 化学式: 2C₂₀H₂₄N₂O₂*2H₂O*H₂O₄S
• 分子量: 782.956
• InChiKey: ZYCWGZVLCXRARB-KAIFKDDSSA-N

物化性质

• 熔点：
  ~225 °C (dec.)(lit.)
• 比旋光度：
  -245 º (c=2, 0.1M HCl)
• 溶解度：
  溶于氯仿和无水乙醇（2:1）的混合物。
• LogP：
  3.44
• 稳定性/保质期：

  常温常压下稳定，为白色精细粉末。

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  130
• 氢给体数：
  4
• 氢受体数：
  9

安全信息

• TSCA：
  Yes
• 危险品标志：
  Xn
• 安全说明：
  S24,S37,S45
• 危险类别码：
  R22,R42/43
• WGK Germany：
  3
• 海关编码：
  29392000
• 危险品运输编号：
  UN 2811
• RTECS号：
  VA8440000
• 危险性防范说明：
  P280,P305+P351+P338,P310
• 危险性描述：
  H302,H315,H319,H332,H335

SDS

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Section 1. Chemical Product and Company Identification
Quinidine sulfate dihydrate Catalog
QU105
Common Name/
Number(s).
Trade Name
CAS# 6591-63-5
Manufacturer
RTECS VA5950000
SPECTRUM CHEMICAL MFG. CORP.
TSCA TSCA 8(b) inventory:
Quinidine sulfate dihydrate
Commercial Name(s) Not available.
CI# Not available.
Synonym 6'-Methoxycinchonan-9-ol sulfate
IN CASE OF EMERGENCY
Not available.
Chemical Name
Chemical Family Not available. CALL [phone]
(C20H24N2O2)2.H2SO4.2H2O
Chemical Formula
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) Quinidine sulfate dihydrate 6591-63-5 100
Toxicological Data Quinidine sulfate dihydrate
on Ingredients LD50: Not available.
LC50: Not available.

---

Section 3. Hazards Identification
Potential Acute Health Effects Very hazardous in case of ingestion. Hazardous in case of eye contact (irritant), of inhalation.
Potential Chronic Health Very hazardous in case of ingestion.
Effects Hazardous in case of skin contact (irritant), of eye contact (irritant), of inhalation.
CARCINOGENIC EFFECTS: Not available.
MUTAGENIC EFFECTS: Not available.
TERATOGENIC EFFECTS: Not available.
DEVELOPMENTAL TOXICITY: Not available.
Quinidine sulfate dihydrate

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Section 4. First Aid Measures
Eye Contact Check for and remove any contact lenses. Immediately flush eyes with running water for at least 15 minutes,
keeping eyelids open. Cold water may be used. Do not use an eye ointment. Seek medical attention.
Skin Contact No known effect on skin contact, rinse with water for a few minutes.
Serious Skin Contact Not available.
Inhalation Allow the victim to rest in a well ventilated area. Seek immediate medical attention.
Serious Inhalation Not available.
Ingestion Do not induce vomiting. Loosen tight clothing such as a collar, tie, belt or waistband. If the victim is not
breathing, perform mouth-to-mouth resuscitation. Seek immediate medical attention.
Serious Ingestion Not available.

---

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...), sulfur oxides (SO2, SO3...).
Fire Hazards in Presence of Not available.
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 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 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.
Quinidine sulfate dihydrate

---

Section 7. Handling and Storage
Precautions Keep away from heat. Keep away from sources of ignition. Empty containers pose a fire risk, evaporate the
residue under a fume hood. Ground all equipment containing material. Do not breathe dust. Avoid contact with
eyes 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.
Storage Keep container dry. Keep in a cool place. Ground all equipment containing material. Keep container tightly
closed. Keep in a cool, well-ventilated place. Combustible materials should be stored away from extreme heat
and away from strong oxidizing agents.

---

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 Splash goggles. Lab coat.
Personal Protection in Case of Splash goggles. Full suit. Boots. Gloves. Suggested protective clothing might not be sufficient; consult a
a Large Spill specialist BEFORE handling this product.
Exposure Limits Not available.

---

Section 9. Physical and Chemical Properties
Physical state and appearance Solid. (Crystals solid.) Odor Odorless.
Taste Bitter.
Molecular Weight 782.96 g/mole
Color White.
pH (1% soln/water) Not available.
Not available.
Boiling Point
Melting Point Decomposes. (120°C or 248°F)
Not available.
Critical Temperature
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, methanol.
Solubility Soluble in methanol.
Partially soluble in cold water.

---

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
Quinidine sulfate dihydrate
Corrosivity Non-corrosive in presence of glass.
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 Eye contact. Inhalation. Ingestion.
Toxicity to Animals LD50: Not available.
LC50: Not available.
Chronic Effects on Humans Not available.
Other Toxic Effects on Very hazardous in case of ingestion.
Humans Hazardous in case of inhalation.
Special Remarks on Not available.
Toxicity to Animals
Special Remarks on Human: passes through the placenta, excreted in maternal milk.
Chronic Effects on Humans
Special Remarks on other Not available.
Toxic Effects on Humans

---

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.
Toxicity of the Products The products of degradation are more toxic.
of Biodegradation
Special Remarks on the Not available.
Products of Biodegradation

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Section 13. Disposal Considerations
Waste Disposal

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

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Section 15. Other Regulatory Information and Pictograms
TSCA 8(b) inventory: Quinidine sulfate dihydrate
Federal and State
Regulations
California
Proposition 65
Warnings
Other Regulations Not available..
WHMIS (Canada) Not controlled under WHMIS (Canada).
Other Classifications
DSCL (EEC) R36- Irritating to eyes.
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
j
WHMIS (Canada)
(Pictograms)
DSCL (Europe)
(Pictograms)
TDG (Canada)
(Pictograms)
ADR (Europe)
(Pictograms)
Protective Equipment
Not applicable.
Lab coat.
Not applicable.
Splash goggles.

---

SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

药理作用

奎宁是一种喹啉类衍生物，能够与疟原虫的DNA结合形成复合物，抑制DNA复制和RNA转录，进而抑制原虫的蛋白质合成。其作用较氯喹弱。此外，奎宁还能降低疟原虫的耗氧量，并干扰疟原虫内的磷酸化酶活性，从而影响其糖代谢。在某些情况下，奎宁还会引起疟色素聚集，但这种聚集发展缓慢，很少形成大团块，并且往往伴随着细胞死亡。通过电子显微镜观察可见到原虫核和外膜的肿胀以及含有血细胞颗粒的小空泡。此外，在血液中一定浓度的奎宁可导致寄生红细胞提前破裂，从而阻止裂殖体成熟。

本品对红外期疟疾无效，但长期使用可以根治恶性疟疾，但它并不能直接作用于恶性疟原虫的配子体，因此不能中断传播。

药物相互作用

1. 制酸药和含铝制剂：会延缓或减少奎宁的吸收。
2. 抗凝血药物：与奎宁合用后，抗凝作用增强。
3. 肌肉松弛剂（如琥珀胆碱、筒箭毒碱）：与奎宁同用可能会引起呼吸抑制。
4. 奎尼丁：与奎宁合用时，金鸡纳反应增加。
5. 尿液碱化剂（如碳酸氢钠）：可增加肾小管对奎宁的重吸收，导致血药浓度和毒性上升。
6. 维生素K：与奎宁合用能增加其吸收。
7. 某些药物组合（布克利嗪、赛克利嗪、美克利嗪、吩噻嗪类、噻吨类、曲美苄胺及氨基苷类抗生素）：可导致耳鸣和眩晕。
8. 硝苯地平：与奎宁合用时，游离的奎宁浓度增加。

不良反应

1. 奎宁每日用量超过1g或连续使用较长时间常会引起金鸡纳反应，包括耳鸣、头痛、恶心、呕吐及视力听力减退等症状。严重者可能会出现暂时性耳聋，停药后通常可以恢复。
2. 24小时内剂量大于4g时，可直接损害神经组织并收缩视网膜血管，导致视野缩小、复视和弱视等现象。
3. 大剂量中毒时，上述症状会进一步加重，并可能出现心肌抑制、传导延迟、心肌收缩力减弱以及外周血管扩张等症状。血压骤降、呼吸减慢或变浅、发热、烦躁及谵妄等情况也可能出现，最终因呼吸麻痹而死亡。
4. 奎宁的致死剂量约为8g。
5. 少数患者对奎宁高度敏感，即使少量使用也会引起严重的金鸡纳反应。孕妇应禁用。

标准溶液

硫酸奎宁荧光标准物质主要用于荧光光谱类仪器的校准与检验、分析方法的确证评价以及材料荧光性能评估等。

用途

• 校准仪器和装置
• 评价方法
• 工作标准
• 质量保证/质量控制
• 其他用途

文献信息

• PERCUTANEOUS ABSORPTION ENHANCER AND TRANSDERMAL PREPARATION USING THE SAME
  申请人：TOA Eiyo Ltd.

  公开号：EP2298352A1

  公开（公告）日：2011-03-23

  Provided are a percutaneous absorption enhancer excellent in an enhancing effect on percutaneous absorption of a wide range of drugs and excellent in compatibility with an adhesive base, and a transdermal preparation using the percutaneous absorption enhancer. The percutaneous absorption enhancer includes a sulfosuccinate or a salt thereof and an alkyl glycoside or an alkyl thioglycoside.

  本发明提供了一种经皮吸收促进剂，它对多种药物的经皮吸收具有极佳的促进作用，并且与粘合剂基质具有极佳的相容性，还提供了一种使用该经皮吸收促进剂的透皮制剂。经皮吸收促进剂包括磺基琥珀酸酯或其盐和烷基糖苷或烷基硫代糖苷。
• DISINTEGRATING PARTICLE COMPOSITION AND ORALLY RAPIDLY DISINTEGRATING TABLET
  申请人：FUJI CHEMICAL INDUSTRY CO., LTD.

  公开号：EP2465539A1

  公开（公告）日：2012-06-20

  There has been a need for an orally rapidly disintegrating tablet which has a good texture and taste in the oral cavity, such a sufficient hardness as not giving any worry of being chipped or dusted during production or transportation and good disintegrating properties in the oral cavity and can sustain a sufficient hardness even under humid conditions after opening. Disclosed are a disintegrating particle composition which is prepared by dispersing, in the presence of water, mannitol, xylitol, an inorganic excipient, a disintegrating agent and carmellose and drying, and an orally rapidly disintegrating tablet which comprises said disintegrating particle composition, an active substance and a disintegrating agent. The disintegrating tablet has a good texture and taste, an appropriate hardness and good disintegrating properties and can sustain a sufficient hardness under humid conditions.

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