Posaconazole Raw Materials Powder 171228-49-2

CAS:171228-49-2

MF: C37H42F2N8O4

MW: 700.78

EINECS:682-747-8

Specification: 99% min Posaconazole Powder

Sample: Posaconazolel Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Posaconazole Powder Usage and Synthesis.

Clinically, it can be used for the treatment of Aspergillosis, Splintering Bacteriosis and Fusarium Bacteriosis, and can also be used for the treatment of some fluconazole-resistant Candida spp. infections.

Studies have shown that Posaconazole is broadly effective in the treatment of dark filamentous mycoses and improves the survival of dermatophyte infected individuals in a dose-dependent manner.

Posaconazole, as a second-line agent, is 44% to 78% effective against amphotericin B or itraconazole-resistant invasive Aspergillosis, and 71% effective against Mycobacterium avium subsp. japonicum infections.

Posaconazole is available as an oral suspension, with a recommended dose of 200 mg orally with meals four times daily for 7 to 10 days, after which this dose may be maintained or changed to 400 mg orally twice daily.Steady-state blood levels are obtained within 7 to 10 days.

Uses and functions of Posaconazole.

Posaconazole exerts its antifungal activity by inhibiting ergosterol biosynthesis.

Ergosterol is an important component of fungi necessary for maintaining the structural integrity of cell membranes and for the function of some membrane-associated proteins, as well as an essential trace substance in the fungal cell cycle.

Posaconazole blocks ergosterol synthesis by inhibiting the fungal pigment P45014 alpha-demethylase and causing the accumulation of 14 alpha-methylsterols, among others, and the extent of the blockage is related to the susceptibility of the test strains and the dosage of posaconazole.

Mutant strains of Candida albicans are resistant to itraconazole (ITC), fluconazole (FLC), and voriconazole (VRC) due to mutations in the 14α-demethylase enzyme, but are still sensitive to this product.

Posaconazole inhibits sterol biosynthesis in Aspergillus fumigatus and Aspergillus flavus more effectively than ITC.

Pharmacological Effects of Posaconazole Raw.

Posaconazole is derived from itraconazole. It is currently in phase III clinical trials.

Pharmacological effects are the same as those of azoles, but compared with itraconazole, its inhibition of sterol C14 demethylation is stronger, especially for Aspergillus.

Studies on dosage and dosing regimens have shown that the rate of absorption and elimination is consistent with a single-compartment model, and that the relative bioavailability of the oral suspension is significantly different between doses, and that split doses (every 12 hours or every 6 hours) significantly increase bioavailability, with a protein-binding rate of 98% to 99%.

Bioavailability of the suspension was increased relative to tablets, and food significantly increased the rate and extent of drug absorption. Results of a study examining the effect of abnormal renal function on the pharmacokinetics of the drug showed that it was not cleared by haemodialysis and was not affected by haemodialysis.

Single-dose studies have shown that no dose adjustment is necessary in patients with varying degrees of chronic kidney disease. Half-life is approximately 25 hours and is metabolised mainly by the liver.

Usage and dosage of Bulk Posaconazole Powder.

Posaconazole different dosage forms, different specifications of the dosage may vary, please read the specific instructions for use of the drug, or follow doctor's advice.

Posaconazole Oral Suspension:

The recommended dose is 400mg (10ml) twice a day with a meal or with 240ml of nutritional supplement.