Posaconazole powder is a derivative of itraconazole, which has a broader antibacterial spectrum and stronger effects compared to itraconazole. However, phase III clinical trials are currently underway, and only some formulations have been approved by the FDA. The pharmacological effects of pure Posaconazole are basically the same as other azole products, that is, it inhibits the synthesis of cholesterol in fungal cell walls to cause obstacles in fungal cell membrane biosynthesis, changes cell membrane permeability, and thus inhibits fungal growth. Compared with itraconazole, it has a stronger inhibitory effect on the demethylation of steroid C14, especially on Aspergillus.
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TEST ITEM |
SPECIFICATION |
RESULTS |
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Appearance |
White to Offwhite powder. |
White powder |
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Melting point |
167~171℃ |
167.5-168.0C |
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Specific optical rotation |
-28.5.-24.5. |
-27.2° |
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Identification |
The retention time o the major peak of the test solution corresponds to that of the standard solution,as obtained in the Assay. |
Conform |
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The infrared absorption spectrum of this product should corresponds to the reference spectrum |
Conform |
|
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Crystallinity |
There are characteristic peaks at 7.7°±0.2° 9.9°±0.2°,17.8°±0.2°,19.5°±0.2°,20.0°±0.2° (Crystal form 1). |
Conform |
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Water content (%w/w) |
≤0.5% |
0.1% |
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Residue on ignition |
≤0.1% |
0.02% |
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Related substances |
QR0005DS-IN-01:≤0.10% |
Not detected |
|
QR0005DS-IN-02:≤0.10% |
0.01% |
|
|
QR0005DS-IM-08:≤0.10% |
Not detected |
|
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QR0005DS-IN-02-IM-06:≤0.10% |
Not detected |
|
|
Other maximum unknown impurity ≤0.10% |
0.02% |
|
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Total impurities:≤0.40% |
0.07% |
|
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Enantiomeric and |
QR0005DS-IM-02:≤0.10% |
0.01% |
|
QR0005DS-IM-03:≤0.10% |
Not detected |
|
|
QR0005DS-IM-04:≤0.10% |
Not detected |
|
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QR0005DS-IM-01+QR0005DS-IM-05+QR0005DS-IM-06:≤0.10% |
Not detected |
|
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QR0005DS-IM-07:≤0.10% |
0.02% |
|
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Totalisomer impurities:≤0.50% |
0.04% |
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Residual solvents |
Methanol:≤3000 ppm |
31 ppm |
|
Dichloromethane:≤600 ppm |
53 ppm |
|
|
Acetone:≤5000 ppm |
Not detected |
|
|
Ethanol:≤5000 ppm |
Not detected |
|
|
Dimethyl sulfoxide:≤5000 ppm |
Not detected |
|
|
Benzene |
≤2 ppm |
Not detected |
|
Heavy metals |
≤10 ppm |
Conform |
|
Bacterial endotoxin |
≤0.25 EU/mg |
Conform |
|
Microbial limit |
Total Aerobic Microbial Count (TAMC):≤10²cfu/g |
10 cfu/g |
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Total molds and Yeast Count (TYMC):≤10¹cfu/g |
<10 cfu/g |
|
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Escherichia Coli:Absence |
Not detected |
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|
Assay |
C37H₄₂F₂N₈O4:98.0%-102.0%(on the anhydrous basis) |
101.0% |
|
Conclusion |
Conform to Enterprise Standard |
What is the difference between posaconazole and voriconazole?
Posaconazole and voriconazole belong to the second generation of triazole antifungal agents, both of which can inhibit lanosterol 14α- demethylase (CYP51), a key enzyme for ergosterol synthesis on fungal cell membrane, thus interfering with the growth of fungal cells. Both of them can prevent the development of invasive fungal diseases, and still have antibacterial activity against some drug-resistant and emerging pathogens.
Posaconazole is a derivative of itraconazole, which has a wide antibacterial spectrum, covering candida, Aspergillus, most zygotic bacteria, Tricholoma, etc. Voriconazole is a derivative of fluconazole. Like fluconazole, voriconazole can inhibit 14α‐ demethylase to hinder lanosterol demethylation, and at the same time, it can also inhibit 24 methylene dihydrolanosterol demethylase of some yeasts and filamentous fungi, so it has a broader antibacterial spectrum than fluconazole.
What is the difference between posaconazole and voriconazole?
1. Aspergillus
For invasive aspergillosis, current guidelines recommend that posaconazole is more suitable for prevention, while voriconazole is more suitable for treatment. Although some studies have shown that the new dosage form of posaconazole is not inferior to voriconazole in the treatment of invasive aspergillosis, there is no initial evidence of posaconazole in the treatment of invasive aspergillosis due to the lack of large-scale clinical research.
In 2016, the American Society of Infectious Diseases' new edition of Guidelines for the Diagnosis and Treatment of aspergillosis recommended posaconazole and voriconazole for the prevention of invasive aspergillosis infection, and posaconazole was recommended for the prevention of GVHD in HSCT recipients. The guidelines all recommend voriconazole as the first choice drug and posaconazole as the first-line drug treatment failure patients.
2. Candida
For candida infection, clinical studies in recent years have also shown that posaconazole has a better preventive effect. The increased resistance of candida to fluconazole is related to the existence of filamentous fungi. Therefore, in terms of preventive drugs, according to the Expert Consensus on Diagnosis and Treatment of Adult Candidiasis in China, posaconazole oral suspension is the first choice, followed by voriconazole, itraconazole, micafungin and caspofungin.
3: Mucor
For Mucor infection, "Guidelines for Diagnosis and Treatment of Mucor in Europe in 2019" recommended: among patients with neutropenia or graft-versus-host disease, the primary prevention of posaconazole sustained-release tablets is moderately recommended, while the recommended evidence of posaconazole suspension prevention is low; However, voriconazole has a general effect on Mucor infection.
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| 171228-49-2 Posaconazole | 137234-62-9 Voriconazole |
Our company can provide various Posaconazole, Voriconazole etc. If you are interested, please contact us via email:sales6@faithfulbio.com
What is the difference between the adverse reactions of Posaconazole and Voriconazole?
All azole antifungal drugs have a certain degree of hepatotoxicity. The mild hepatotoxicity is characterized by a slight increase in transaminase, and hepatitis, cholestasis and fulminant liver failure may occur in severe cases.
In clinic, voriconazole can be stopped because of its serious hepatotoxicity, visual impairment, QT interval extension and other adverse reactions. And studies have shown that long-term use of voriconazole is related to skin phototoxicity/skin cancer and skeletal fluorosis.
Posaconazole is often used to treat patients with liver injury caused by voriconazole because of its lower hepatotoxicity. By switching to Posaconazole treatment, the liver function indexes of patients gradually return to normal. Compared with voriconazole, posaconazole has better application safety.
Prevention is greater than cure. Patients with high risk factors of IFD, such as allogeneic hematopoietic stem cell transplantation, patients with acute leukemia (including MDS) undergoing initial induction or salvage chemotherapy, patients with expected neutropenia lasting more than 10 days, and severe aplastic anemia with severe neutropenia or receiving antithymglobulin (ATG) therapy or hematopoietic stem cell transplantation, should receive antifungal preventive treatment.
Whether voriconazole powder or posaconazole powder is chosen, therapeutic drug concentration monitoring (TDM) should be carried out to reduce the failure rate of antifungal prevention or treatment.
Posaconazole oral suspension and which drugs should not be taken at the same time?
The oral suspension made from posaconazole powder is a very convenient antifungal product,which can inhibit the synthesis of fungal cell membrane and play an antifungal role, and is used to treat fungal infections sensitive to Posaconazole. Posaconazole oral suspension and the following drugs should not be taken at the same time:
1. Immunosuppressants metabolized by CYP3A4 (such as sirolimus, tacrolimus and cyclosporine): The whole blood concentration of immunosuppressants metabolized by CYP3A4 should be monitored frequently during the treatment of Posaconazole and after stopping the treatment, and the dose of immunosuppressants metabolized by CYP3A4 should be adjusted accordingly.
2. CYP3A4 substrates (such as pimozide and quinidine): Posaconazole can increase the plasma concentration of the above drugs, thus leading to prolonged QTc interval and rare torsade de pointes ventricular tachycardia.
3. HMG-CoA reductase inhibitors metabolized by CYP3A4 (statins): Increasing the concentration of HMG-CoA reductase inhibitors in plasma may be associated with rhabdomyolysis. Posaconazole and HMG-CoA reductase inhibitors mainly metabolized by CYP3M are prohibited to be taken at the same time.
4. Ergot alkaloids: Posaconazole can increase the plasma concentration of ergot alkaloids (ergotamine and dioxygenamine), which may lead to ergot poisoning. Therefore, the combination of posaconazole and ergot alkaloids is prohibited.
5. Benzodiazepines metabolized by CYP3A4: The combination of Posaconazole and other benzodiazepines metabolized by CYP3A4 (such as alprazolam and triazolam) will lead to the increase of plasma concentration of these benzodiazepines.
6. Anti-HIV drugs (such as efavirenz, ritonavir and fosanavir): Because HIV protease inhibitors are CYP3A4 substrates, it is expected that posaconazole will increase the plasma concentration of these antiretroviral agents. Efavirenz and fosanavir can also reduce the plasma concentration of posaconazole.
7. Phenytoin: The combination of phenytoin and posaconazole will lead to the increase of plasma concentration of phenytoin.
8. Gastric acid inhibitors/neutralizers (such as cimetidine and esomeprazole): It can reduce the plasma concentration of posaconazole.
9. Changchun Alkaloids: Posaconazole can increase the plasma concentration of Changchun Alkaloids, leading to neurotoxicity and other serious adverse reactions.
10. Calcium channel blockers metabolized by CYP3A4 (for example, verapamil, diltiazem, nifedipine, nicardipine, felodipine): Posaconazole may increase the plasma concentration of calcium channel blockers metabolized by CYP3A4.
11. Digoxin: Posaconazole may increase the plasma concentration of digoxin.
12. Gastrointestinal prokinetic drugs (such as metoclopramide): metoclopramide can reduce the plasma concentration of posaconazole. If metoclopramide is used at the same time, it is recommended to closely monitor the breakthrough fungal infection.
13. Vincristine: Posaconazole combined with vincristine can cause serious intestinal obstruction.
14. Midazolam: The combination of this product and Midazolam will increase the plasma concentration of Midazolam by about 5 times. However, the increase of midazolam plasma concentration will enhance and prolong hypnosis and sedation.
15. Rifamycin antibacterial drugs (rifampicin, rifabutin), specific anticonvulsants (phenytoin, carbamazepine, phenobarbital, primidone), efavirenz and cimetidine: during the combined treatment, the concentration of posaconazole can be significantly reduced; Therefore, the combined use of posaconazole must be avoided unless the benefits to patients outweigh the risks.
If you need to use other drugs (including prescription or over-the-counter drugs, natural products and vitamins) during taking this product, you must first get the doctor's permission.
A variety of shipping methods for you to choose
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Transportation Time |
Shipping method |
Cargo weight requirements |
Advantage |
|
3-7 days |
DHL,Germany DHL,Germany DPD, |
Suitable for under 50kg. |
We have warehouses in Germany and California, USA, |
|
7-15 days |
By Air |
Suitable for more than 50kg. |
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|
15-60 days |
By Sea |
Suitable for more than 500kg. |
Our strengths:
Our company has passed FDA and ISO19001 quality management system certification. And we have internal cooperation agreements with multiple factories and laboratories in China,Can provide you with a good price.Our company can provide various Posaconazole, Voriconazole etc. If you are interested, please contact us via
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