Paracetamol Ketoconazole Raw Materials Powder

CAS:65277-42-1

MF: C26H28Cl2N4O4

MW: 531.43

EINECS:265-667-4

Specification​: 99% min Ketoconazole Powder

Sample: Ketoconazole Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Ketoconazole Powder Usage and Synthesis.

Ketoconazole is indicated for the treatment of the following systemic fungal infections:

1. candidiasis, chronic cutaneous mucosal candidiasis, oral candida infection, urinary tract candida infection, chronic, recurrent vaginal candidiasis for which topical therapy is ineffective.

2. Dermatophytosis.

3. Coccidioidomycosis.

4. Histoplasmosis.

5. Colouring fungal disease.

6. Coccidioidomycosis parapsilosis. Skin fungal diseases, lichen planus and ringworm caused by skin fungi and yeasts can be treated with this product when topical treatment or oral ashwagandha is ineffective, or when it is difficult to accept ashwagandha treatment for severe and persistent skin fungal infections.

Uses and functions of Ketoconazole.

A broad-spectrum antifungal agent that is a CYP3A4 inhibitor.

Ketoconazole is a broad spectrum antifungal agent used to treat candidiasis,chronic mucocutaneous candidiasis,oralthrush,candiduria,blastomycosis,coccidioidomycosis,histoplasmosis,chromomycosis,and paracoccidioidomycosis.It is used to identifyp-glycoprotein/CYP3A-limited bioavailability in the monkey model,to study interleukin 1 mediated antitumor effects,and drug interactions in vivo.

Pharmacological Effects of Ketoconazole Raw Materials.

1.Pharmacology ketoconazole belongs to the pyrrole class antifungal drugs, on the deep infection of fungi such as Candida, colouring fungi, Coccidioides, histoplasmosis, sporotrichum, etc. are antibacterial, on Trichophyton mentagrophytes, etc. also have antibacterial activity.

Ketoconazole has a weaker effect on Aspergillus, Schenk's sporotrichum, some dark spore family, Trichoderma spp.

Ketoconazole by interfering with the activity of cytochrome P-450, thus inhibiting the biosynthesis of ergosterol, the main sterol of fungal cell membrane, damage to the fungal cell membrane and change its permeability, so that important intracellular material leakage. Ketoconazole can inhibit the biosynthesis of triacylglycerol and phospholipids in fungi, inhibit the activity of oxidase and peroxidase, and cause intracellular hydrogen peroxide accumulation leading to cellular submicroscopic degeneration and cell necrosis. For Candida albicans, it can inhibit the process of transformation from spore to invasive mycelium.

2. Toxicological long-term toxicity experiments in animals show that ketoconazole can cause a significant increase in alkaline phosphatase and degeneration of hepatocytes.

Production method of Ketoconazole Raw Powder.

A mixture of 2.4 parts of 1-acetyl-4-(4-hydroxyphenyl)piperazine, 0.4 parts of 78% sodium hydride, 75 parts of dimethyl sulphate, and 22.5 parts of benzene was stirred at 40°C for 1h, then 4.2 parts of 2-(2,4-dichlorobenzene-2-(1H-imidazol-1-ylmethyl)-1,3-dioxopentanepen-4-ylmethyl methanesulphonate were added, and the mixture was stirred at 100°C overnight. The reaction product was post-treated to give 3.2 parts of ketoconazole.