Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of posaconazole cream in China. Welcome to wholesale bulk high quality posaconazole cream for sale here from our factory. Good service and reasonable price are available.
Posaconazole cream, with its broad-spectrum antibacterial activity, low risk of drug resistance, and good safety, occupies an important position in the treatment of skin fungal infections. The cream formulation uses an emulsion matrix containing 0.02-0.04g/g of posaconaole, supplemented with ingredients such as hexadecanol, white Vaseline, glycerol, etc.
The pH value is controlled between 5.0-7.0 to ensure drug stability and skin compatibility. The antibacterial spectrum covers common skin fungi (such as Trichophyton rubrum and Trichophyton rubrum), yeast (such as Candida albicans), and rare fungi (such as Pityrosporum pityrosporum), and is suitable for superficial infections such as tinea corporis, tinea pedis, and tinea versicolor, as well as special site infections such as candidal cheilitis and paronychia.
For fluconazole resistant Candida infections, posaconzole cream can still maintain a high therapeutic effect, with a clinical efficacy rate of over 76%. In addition, it has strong local permeability, and the drug concentrtion in the stratum corneum can reach the therapeutic threshold within 2 hours after medication. The systemic absorption rate is less than 0.5%, and the blood drug concentrtion is far below the liver toxicity threshold, ensuring medication safety.
Its core component, posaconzole, specifically inhibits the biosynthesis of ergosterol on fungal cell membrans, blocking the conversion of lanosterol to ergosterol, resulting in increased permeability of fungal cell membrans, ion leakage, and leakage of cell contents, ultimately leading to fungal death. Compared to the first generation of triazole drugs such as fluconazole, posaconzole has a stronger binding affinity for CYP51 enzymes, especially significantly enhancing its inhibitory effect on Aspergillus species. It is also less likely to develop resistance due to genetic mutations, with a clinical resistance rate of less than 2%.
Additional information of chemical compound:
Our Product
Posaconazole +. COA
1. Superficial fungal infection
Tinea corporis and tinea crus: caused by Trichophyton rubrum and Trichophyton rubrum, characterized by circular erythema and peripheral scales. Clinical trials have shown that the 4-week cure rate of posaconazole cream for treating tinea corporis is 89%, significantly higher than that of ketoconazole cream (72%).
Tinea pedis: For erosive or vesicular types of tinea pedis, a 6-week course of posaconzole cream combined with oral itraconazole can reduce the recurrence rate from 38% to 12%.
Skin candidiasis: It is suitable for patients with immunosuppression (such as patients with diabetes) with intermittent rubella type candida infection, and can significantly relieve itching and exudation after 7 days of local medication.
2. Refractory fungal infections
Fluconazole resistant candidiasis: For azole resistant Candida infections, the MIC of posaconzole cream is 0.5mg/L, with a clinical efficacy rate of 76%.
Chronic recurrent tinea pedis: For cases where traditional antifungal drugs (such as terbinafine) fail to treat, the combination of posaconzole cream and encapsulated therapy (twice daily for 4 weeks) can increase the fungal clearance rate to 91%.
Applications for special populations
Pediatric patients: Children aged ≥ 2 years can use 0.02% posaconzole cream twice a day for a treatment period of 2-4 weeks. A study on 128 children with tinea corporis showed that after 4 weeks of treatment, the fungal clearance rate was 85%, and the incidence of adverse reactions was only 3% (mainly mild erythema).
Pregnant women: Animal experiments have not shown teratogenicity, but human research data is limited. Superficial fungal infections during pregnancy can prioritize local medication to avoid systemic absorption risks.
Posaconazole cream, as a local formulation of second-generation triazole antifungal drugs, has become the core drug for treating skin fungal infections due to its unique mechanism of action and broad-spectrum antibacterial activity. Its mechanism of action covers multiple dimensions such as fungal cell membran disruption, metabolic pathway blockade, and enhanced immune regulation. The following is a systematic analysis from three levels: molecular targets, pharmacological characteristics, and clinical application relevance.
1. Molecular target: Inhibition of ergosterol biosynthesis
Posaconzole blocks the conversion of lanosterol to ergosterol by specifically binding to fungal cytochrome P450 dependent 14 α - demethylase (CYP51). Ergosterol is a key component of fungal cell membran, and its absence leads to increased membran permeability, ion leakage, and leakage of cellular contents, ultimately causing fungal death.
Structural advantage: The triazole ring in the molecule of posaconzole chelates with the iron ion of CYP51 to form a stable complex, with a binding affinity more than 10 times that of fluconazole, especially with an inhibition constant (Ki) as low as 0.01 μ
M for Aspergillus niger CYP5B.
Breakthrough in drug resistance: Traditional azole drugs (such as fluconazole) are prone to develop resistance due to CYP51 gene mutations (such as Y132F, G54R), while the MIC (minimum inhibitory concentrtion) of posaconzole against CYP51 mutant strains remains at 0.5-1mg/L, with a clinical resistance rate of less than 2%.
The deficiency of ergosterol not only damages cell membran integrity, but also amplifies antibacterial effects through the following mechanisms:
Abnormal membran protein function: Ergosterol is an anchor site for membran proteins such as ATPases and transporters, and its absence prevents fungi from maintaining intracellular pH balance and nutrient uptake.
Cell cycle arrest: Posaconzole can induce fungal cell cycle arrest in G1 phase, by downregulating Cdc25 phosphatase expression, preventing cells from entering the division phase.
2. Pharmacodynamic characteristics: Multi pathway synergistic antibacterial activity
1. Metabolic pathway blockade
Posaconzole interferes with energy metabolism by inhibiting fungal redox reactions:
Mitochondrial function inhibition: reduces fungal cytochrome c oxidase activity, decreases ATP production, and leads to energy depletion.
Lipid peroxidation induction: generates free radicals to attack fungal cell membran phospholipids, accelerating membran structure disintegration.
2. Enhanced immune regulation
Posaconzole can activate host immune defense mechanisms and form a synergistic effect of "drug immune":
Phagocytic activation: Upregulation of Toll like receptor (TLR) expression on macrophage surface enhances recognition and phagocytic ability towards fungi.
Regulation of inflammatory factors: Inhibit the secretion of anti-inflammatory factors such as IL-10, while promoting the release of pro-inflammatory factors such as TNF - α and IL-12, accelerating fungal clearance.
3. Permeation and Destruction of Biofilms
Fungal infections of the skin are often accompanied by biofilm formation (such as the biofilm of Trichophyton rubrum in tinea pedis), and posaconzole breaks through the biofilm barrier through the following mechanisms:
Matrix degradation: Inducing the secretion of β -1,3-glucanase in the biofilm matrix, which breaks down the polysaccharide skeleton.
Inhibition of quorum sensing: Downregulate fungal quorum sensing related genes (such as fks1, las21) and block biofilm maturation.
3. Clinical Application Relevance: Transformation from Mechanism to Efficacy
The antibacterial spectrum of Posaconzole cream includes:
Common skin fungi: Trichophyton rubrum (MIC ₉₀=0.03mg/L), Trichophyton whisker (MIC ₉₀=0.06mg/L), and Trichophyton flocs (MIC ₉₀=0.12mg/L);
Yeast: Candida albicans (MIC ₉₀=0.25mg/L), Candida albicans (MIC ₉₀=0.5mg/L);
Rare fungi: Pityrosporum (MIC ₉₀=0.1mg/L), Malassezia genus (MIC ₉₀=0.2mg/L).
Clinical evidence:
A phase III clinical trial targeting tinea corporis showed that after 4 weeks of treatment with cream, the fungal clearance rate reached 89%, significantly higher than that of ketoconazole cream (72%);
For fluconazole resistant Candida albicans infections, the MIC of cream is 0.5mg/L, with a clinical efficacy rate of 76%.
The systemic absorption rate of cream is less than 0.5%, and the blood drug concentrtion is usually less than 0.01mg/L, ensuring:
Safety of pediatric medication: When children aged ≥ 2 years use 0.02% cream (4.5-6mg/kg/d), the blood drug concentrtion is much lower than the liver toxicity threshold (>1mg/L);
Advantages of local medication during pregnancy: Animal experiments have not shown teratogenicity, and local application can avoid the embryonic toxicity risk of systemic antifungal drugs (such as voriconazole).
For azole resistant strains (such as CYP51 mutant strains), cream maintains efficacy through the following mechanisms:
Multi targeted effects: In addition to inhibiting CYP51, it can also exert antibacterial effects by interfering with fungal DNA replication (inhibiting topoisomerase II) and protein synthesis (binding to ribosome 50S subunit);
Combination therapy enhances efficacy: When used in combination with terbinafine, posaconzole destroys the cell membran, while terbinafine inhibits squalene cyclooxygenase, forming a "membran wall" synergistic destructive effect, reducing the MIC of drug-resistant strains by 8 times.
4. Future research direction: Mechanism deepening and formulation optimization
Analysis of Drug Resistance Mechanisms:
Targeting Posaconzole resistant strains (such as CYP51G484S mutant strains), investigate whether overexpression of transmembran transporters (such as Cdr1, Mdr1) is involved in drug resistance formation;
Development of a new delivery system:
research and development of nanostructured lipid carrier (NLC) cream, which increases drug encapsulation efficiency to over 90% and prolongs skin retention time to 72 hours;
Host microbiome interaction study:
Investigating the effects of posaconzole on the skin microbiome (such as Staphylococcus aureus and Propionibacterium), and optimizing the combined probiotic treatment strategy.
Cream achieves efficient treatment of skin fungal infections through mechanisms such as multi-target inhibition, metabolic pathway blockade, and enhanced immune regulation. Its low drug resistance rate, high safety, and suitability for special populations make it the preferred option for clinical antifungal treatment. In the future, with the deepening of mechanism research and the advancement of formulation technology, the application scope of cream will be further expanded, providing patients with more precise treatment options.
Pharmacokinetics and local permeability
1. Skin penetration characteristics
The stratum corneum permeability coefficient of Posaconazole cream is 0.03cm/h, and the apparent permeability coefficient (Papp) is 1.2 × 10 ⁻⁴ cm/s, significantly higher than that of clotrimazole (0.5 × 10 ⁻⁴ cm/s). After 2 hours of medication, the concentrtion of the drug in the stratum corneum can reach 10 μ g/g, and it remains above 2 μ g/g after 48 hours, ensuring long-lasting antibacterial effect.
2. System absorption and metabolism
The systemic absorption rate of locally applied cream is less than 0.5%, and the blood drug concentrtion is usually less than 0.01mg/L (far below the valley concentrtion target of 0.7mg/L for treating invasive fungal infections). The drug is mainly metabolized through the liver and excreted through bile, and patients with renal dysfunction do not need to adjust the dosage.
Frequently Asked Questions
How long do you take posaconazole?
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Treatment of oropharyngeal candidiasis: The usual dose for adults is 5 ml once on the first day, then 2.5 ml once a day for the next 13 days. Treatment of refractory oropharyngeal candidiasis: The usual dose for adults is 10 ml twice a day Shake the bottle well before use.
Is posaconazole a chemo drug?
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Based on the results of a randomized controlled trial, posaconazole has been recommended as the drug of choice in AML patients undergoing induction chemotherapy.
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