Ketoconazole
Time: 2022-10-26 12:24:33; Reading: 0

Ketoconazole

Synonyms

Piperazine, 1-acetyl-4-(4-((2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)-, cis-;

Category

Non-ionic surfactant

> Amine

>> Heteroaromatic Amine

>>> Imidazole and its Derivatives

Chemical Numbering System

CASRN: 65277-42-1

EINECS: 265-667-4

Molecular Formula & Molecular Weight

Molecular Formula: C26H28Cl2N4O4

Molecular Weight: 531.43

Structure

Properties

Appearance    (1), solid.

Solubility    insoluble in water.

Stability    stable.

Risk    Solid form: flammable material; irritation, irritation to skin, eye, respiratory system. Harmful products of combustion are CO, CO2, nitrogen oxides and so on. Contact with strong oxidants, can cause to burn.

GHS (Rev.9) label:  

Animal Toxicity

Table 1 Animal toxicity values

dog intravenous LD50

23.3mg/kg[1]

dog oral LD50

178mg/kg[1]

guinea pig intravenous LD50

23.3mg/kg[1]

guinea pig oral LD50

178mg/kg[1]

mouse intraperitoneal LD50

2937mg/kg[1]

mouse intravenous LD50

32mg/kg[1]

mouse oral LD50

618mg/kg[1]

mouse subcutaneous LD50

> 4000mg/kg[1]

rat intraperitoneal LD50

1474mg/kg[1]

rat intravenous LD50

86mg/kg[1]

rat oral LD50

166mg/kg[1]

rat subcutaneous LD50

> 2400mg/kg[1]

Human Toxicity

Table 2 Human toxicity values

child oral TDLo

450mg/kg/90D[1]

man oral LDLo

45mg/kg/17D-I[1]

man oral TDLo

49mg/kg/17D-I[1]

women oral LDLo

264mg/kg/66D[1]

women oral LDLo

412mg/kg/15W[1]

women oral TDLo

60mg/kg[1]

Ecology    may be hazardous to environment. Water body should be given special attention.

Biodegradability    biodegradable.

Characteristics    excellent antimicrobial, anti-infective abilities. Broad spectrum antifungal. Has severe hepatotoxicity. Not to be used in personal care products.

Synthesis

 

Quality Standards & Test Methods

1, Physical and chemical indexes

Item

Physical and chemical indexes

Solid

Actives, %, ≥

95.0

Test Methods

(1), Actives

GB/T 13173 Surface active agents -- Detergents -- Testing methods

2, Hazardous substances indexes

Item

Hazardous substances indexes

Solid

Heavy metals (as Pb), mg/kg, ≤

20

As, mg/kg, ≤

3

Test Methods

(1), Heavy metals (as Pb)

Safety and Technical Standards for Cosmetics (2015 Edition)

GB/T 30799 The test method of food detergents -- Determination of heavy metals

(2), As

Safety and Technical Standards for Cosmetics (2015 Edition)

GB/T 30797 The test method of food detergents -- Determination of total arsenic

3, Product standards

(1), Chinese standards

(1a), Chinese Pharmacopoeia (2020 Edition) Ketoconazole

4, Further explanation

(a), On physical and chemical indexes: firstly, shall be indicated carbon atom distribution; secondly, shall be indicated average molecular weight.

Major Uses

1, Typical applications

Use as antifungal agent.

2, Medicine

Use as pharmaceutical ingredient (antifungal agent). (This section is for reference only, should be implemented according to local Pharmacopoeia.)

Manufacturers

 

References

[1]: ChemIDplus. 65277-42-1, Ketoconazole