Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of fluconazole gel 0.5 in China. Welcome to wholesale bulk high quality fluconazole gel 0.5 for sale here from our factory. Good service and reasonable price are available.
Fluconazole gel 0.5 is a topical antifungal topical preparation, which uses fluconazole as the core active ingredient to play a bactericidal role by inhibiting the synthesis of ergosterol on fungal cell membrane. The gel dosage form is prepared with water-soluble matrix (such as carbomer, hydroxyethyl cellulose) or oil-based matrix (such as polyethylene glycol, white vaseline), and can achieve continuous penetration by adjusting the drug release rate. Its advantage lies in its ability to directly act on the site of infection, increase local drug concentration, while reducing systemic absorption and lowering the risk of systemic adverse reactions such as liver toxicity and gastrointestinal reactions. For example, when treating oral candidiasis, the gel can evenly adhere to the oral mucosa, form a protective film and slowly release drugs, extending the action time to 4-6 hours.
Additional information of chemical compound:
| Product Name | Fluconazole Gel | Fluconazole Tablet | Fluconazole Suspension | Fluconazole Injection | Fluconazole Capsule |
| Product Type | Gel | Tablets | Liquid | Injection | Capsules |
| Product Purity | ≥99% | ≥99% | ≥99% | ≥99% | ≥99% |
| Product Specifications | Customizable | Customizable | Customizable | Customizable | Customizable |
| Product Package | Customizable | Customizable | Customizable | Customizable | Customizable |
Our product form
Fluconazole +. COA
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Certificate of Analysis |
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Compound name |
Fluconazole | |
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CAS No. |
86386-73-4 | |
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Grade |
Pharmaceutical grade | |
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Quantity |
Customized | |
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Packaging standard |
Customized | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
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Lot No. |
20250109001 |
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MFG |
Jan 12th 2025 |
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EXP |
Jan 8th 2029 |
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Structure |
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| TEST STANDARD | GB/T24768-2009 Industry. Stnndard | |
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Item |
Enterprise standard |
Analysis result |
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Appearance |
White or almost white powder |
Conformed |
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Water content |
≤4.5% |
0.30% |
| Loss on drying |
≤1.0% |
0.15% |
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Heavy Metals |
Pb≤0.5ppm |
N.D. |
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As≤0.5ppm |
N.D. | |
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Hg≤0.5ppm |
N.D. | |
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Cd≤0.5ppm |
N.D. | |
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Purity (HPLC) |
≥99.0% |
99.5% |
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Single impurity |
<0.8% |
0.48% |
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Residue on ignition |
<0.20% |
0.064% |
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Total microbial count |
≤750cfu/g |
80 |
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E. Coli |
≤2MPN/g |
N.D. |
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Salmonella |
N.D. | N.D. |
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Ethanol (by GC) |
≤5000ppm |
400ppm |
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Storage |
Store in a sealed, dark and dry place at-20 degrees |
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Cryptococcus infection is a deep fungal disease caused by fungi of the Cryptococcus genus, which can affect multiple organs and systems in animals, including the meninges, lungs, skin, skeletal system, and blood. Among the Cryptococcus genus, Cryptococcus neoformans and Cryptococcus graminearum are the main pathogens that cause infections, widely distributed in nature such as soil, pigeon manure, beehives, milk, fruits, etc. Animals often contract infections by inhaling aerosolized Cryptococcus spores from the environment. Fluconazole gel 0.5 as an important triazole antifungal drug, plays a crucial role in the treatment of cryptococcal infections.
Conventional use in the treatment of Cryptococcus infection
1. The treatment of cryptococcal meningitis
(1) Induction therapy
In the initial treatment stage of cryptococcal meningitis, it is often used as a sequential treatment drug after induction therapy with amphotericin B combined with flucytosine. For HIV infected patients, the 2010 IDSA Clinical Practice Guidelines for Cryptococcus recommend fluconzole (800 mg/d, oral, for at least 8 weeks) as a sequential treatment after 2 weeks of treatment with amphotericin B (0.7-1.0 mg/(kg · d), intravenous drip) combined with flucytosine (800 mg/d, oral).
There are also studies showing that high-dose fluconzole (800 mg, once a day or 600 mg, once/12 hours) alone or in combination with amphotericin B and flucytosine can achieve good early bactericidal activity in the treatment of HIV related cryptococcal meningitis.
The Malawi Ministry of Health's comprehensive management guidelines for HIV infected children and adults recommend fluconzole as the first-line treatment for secondary cryptococcal meningitis in adult patients with HIV infection: 1200 mg/d for 14 days, followed by 400 mg/d for 42 days, and then 200 mg/d for life.
(2) Consolidate and maintain treatment
After completing the induction period treatment, enter the consolidation and maintenance treatment phase. For patients with good initial combined antifungal induction therapy for 2 weeks and normal renal function, the 2010 IDSA Clinical Practice Guidelines for Cryptococcus Disease recommend sequential administration of fluconzole 800 mg (12 mg/(kg · d)) orally for 8 weeks. Afterwards, depending on the patient's condition, fluconzole can be used for consolidation and maintenance treatment (400-800 mg/d, oral, course of treatment 6-18 months).
In order to prevent the recurrence of cryptococcal meningitis in AIDS patients, after completing a course of basic treatment, it can be maintained at 200 mg/time, once a day, for 10 to 12 weeks or indefinitely.
2. Treatment of non central nervous system cryptococcal infections
(1) Pulmonary cryptococcosis
For patients with pulmonary cryptococcosis with normal immune function, if there are no symptoms but the lung tissue cryptococcosis culture is positive, medication can be avoided, close observation can be conducted, or fluconzole can be used for 3-6 months. For patients with mild to moderate symptoms and positive culture, fluconzole or itraconazole should be used for 6-12 months. If oral administration is not possible, amphotericin B can be given.
For patients with immune dysfunction and HIV negative pulmonary cryptococcosis, the recommended treatment plan is the same as that for patients with normal immune function.Patients who are HIV positive and have mild to moderate respiratory symptoms should use fluconzole, itraconazole, or fluconzole plus flucytosine for life; For critically ill patients, they are treated according to the central nervous system cryptococcal infection protocol.
(2) Skin Cryptococcus infection
When infected with Cryptococcus, the dosage and course of treatment can be determined based on the severity and extent of the infection. Generally, conventional doses can be used, such as 200-400 mg per day for adults. The course of treatment may be adjusted according to the condition and may take several weeks or even months to ensure complete removal of Cryptococcus and prevent recurrence.
3. Application in the study of Cryptococcus infection in experimental animals
In experimental animal research, it is widely used to evaluate its therapeutic effect on Cryptococcus infection. Taking the BALB/c mouse model of Cryptococcus neoformans infection as an example, the relevant experiments divided the mice into different groups and administered different doses of Fluconazole gel 0.5, sertraline (a drug with anti Cryptococcus activity), and the combination of Fluconzole and sertraline.
Observe the inhibitory effect of each group on Cryptococcus neoformans through in vitro drug sensitivity testing and animal experiments.The results of in vitro drug sensitivity tests showed that sertraline can effectively reduce the colony size of Cryptococcus neoformans, and the antibacterial effect is more significant when combined with it.
In animal experiments, in the early stages, both concentrations of sertraline (10 mg/mL and 20 mg/mL) were found to significantly reduce the bacterial count of cryptococcus neoformans in the brain and lung tissues of infected mice. However, in the later stage of the experiment, low concentrations of sertraline lost their antibacterial effect on infected mouse brain tissue.In contrast, its antibacterial effect is superior to that of sertraline in brain and lung tissues, and the combination of fluconzole and sertraline has a stronger antibacterial effect on the lung tissue of mice with cryptococcus neoformans than using sertraline alone or this product.
This indicates that it plays an important role in the treatment of Cryptococcus infection in experimental animals, and its combination with other drugs may have a synergistic effect, enhancing the therapeutic effect.
Application in the prevention of Cryptococcus infection
1. Preventive medication for high-risk populations
(1) AIDS patients
AIDS patients suffer from severe impairment of cellular and humoral immune functions due to the destruction of CD4+T lymphocytes by HIV, which makes them highly susceptible to opportunistic infections, among which cryptococcal infection is a common and potentially life-threatening complication. Cryptococcal infection often involves the central nervous system, lungs and other key organs, and once it develops into cryptococcal meningitis, the mortality rate will increase significantly without timely intervention.
For AIDS patients with CD4+T lymphocyte count below 100 cells/μL-a critical threshold for high infection risk-it recommended as a first-line preventive drug. The recommended dosage is generally 200–400 mg per day, administered orally. The duration of preventive treatment is flexible and adjusted according to the patient's immune status and clinical condition: if the patient receives effective antiretroviral therapy and the CD4+T lymphocyte count rebounds to above 200 cells/μL for a sustained period (usually 3–6 months), the preventive medication can be gradually discontinued under medical supervision; for patients with poor immune recovery, long-term maintenance medication is needed. Clinical data shows that standardized prophylaxis can reduce the incidence of cryptococcal infection in this population by more than 70%.
(2) Organ transplant recipients
Organ transplant recipients need to take long-term immunosuppressive drugs (such as cyclosporine, tacrolimus) to prevent rejection of the transplanted organ. However, these drugs will significantly suppress the body's immune response, leading to a sharp increase in the risk of infection with various pathogens, including Cryptococcus. Cryptococcal infection in transplant recipients has the characteristics of insidious onset, rapid progression and high fatality rate, and it is one of the main causes of post-transplant complications.
For organ transplant recipients, it preventive medication can be implemented according to the type of transplant, the degree of immune suppression and the epidemiological risk of the region. In clinical practice, short-term preventive administration is usually started 1–2 weeks before transplantation to reduce the risk of perioperative infection; after transplantation, the dosage and course of treatment are determined according to the patient's immunosuppressive regimen and immune function monitoring results. For high-risk recipients (such as those with a history of cryptococcal infection, or those receiving intensive immunosuppressive therapy), a low-dose maintenance regimen (usually 100–200 mg/d) can be adopted for 3–6 months after transplantation. This targeted preventive strategy can effectively reduce the incidence of post-transplant cryptococcal infection and improve the long-term survival rate of transplant recipients.
The 2010 IDSA guidelines recommend fluconazole gel 0.5 400-800 mg (6-12 mg/(kg · d)) orally for 8 weeks, which can be used for consolidation therapy after 2 weeks of induction therapy with amphotericin B to prevent the occurrence of cryptococcal infection.
2. Prevention in special environments or after exposure
If animals or humans are in a high-risk environment for Cryptococcus infection, such as exposure to large amounts of pigeon manure, activity in areas heavily contaminated with Cryptococcus, or have a clear history of Cryptococcus exposure, they may consider using it for preventive treatment. The specific dosage and course of treatment should be determined based on individual circumstances and exposure levels. Generally, it can be used shortly after exposure and last for several weeks to prevent the occurrence of Cryptococcus infection.
Advantages of in treating Cryptococcus infection
Cryptococcosis is a deep-seated mycosis caused by pathogenic Cryptococcus species such as Cryptococcus neoformansMedlinePlus. It can involve multiple sites including the skin, mucous membranes, and central nervous system. Among these, cutaneous and mucosal cryptococcosis is a common clinical type, predominantly occurring in immunocompromised individuals, such as those with AIDS, organ transplant recipients, and long-term users of glucocorticoidsMedlinePlus. As a topical antifungal preparation, it exhibits unique and significant advantages in the treatment of cutaneous and mucosal cryptococcal infections. Compared with oral or intravenous antifungal agents, it is more suitable for targeted intervention of local lesions, with the following specific advantages:
High Local Drug Concentration, Strong Targeting, and Significant Fungicidal Efficiency
Cutaneous and mucosal lesions of cryptococcosis are mostly manifested as papules, nodules, ulcers, or plaques, with relatively localized lesions. By directly applying it to the affected area, a protective drug film can be formed on the surface of the skin and mucous membranes. The active ingredients can quickly penetrate into the stratum corneum and superficial dermis, achieving a much higher local drug concentration at the lesion site than that of oral preparations.
The mechanism of action of it is to inhibit the synthesis of ergosterol in the fungal cell membrane, destroy the integrity of the Cryptococcus cell membrane, and thereby inhibit its growth and reproduction. The high-concentration local drug action can directly target Cryptococcus within the lesion, avoiding the problem of reduced local concentration of oral drugs after systemic metabolism, and greatly improving the efficiency of killing and inhibiting local Cryptococcus. Clinical data show that for localized cutaneous cryptococcal nodules or plaques, regular use of it can lead to gradual shrinkage and resolution of most lesions within 2 to 4 weeks, with a significantly faster symptom relief rate than adjuvant treatment with oral drugs alone.
Minimal Systemic Absorption, High Safety, and Low Incidence of Adverse Reactions
Unlike oral or intravenous it, the product is a topical preparation, with minimal absorption of the drug into the bloodstream through the skin and mucous membranes, resulting in negligible impact on systemic organs.
On one hand, for patients with cryptococcal infection complicated by liver dysfunction, oral it may increase the metabolic burden on the liver and even cause elevated liver enzymes, while the topical gel completely avoids this risk. On the other hand, for organ transplant recipients or AIDS patients taking multiple medications for a long time, the topical gel does not cause systemic drug interactions with other drugs, preventing reduced efficacy or superimposed adverse reactions due to drug interactions. In addition, local adverse reactions of the gel are mainly mild skin irritation, such as transient burning sensation and erythema, with an incidence of less than 3%, and these symptoms are mostly self-limiting. Compared with systemic adverse reactions such as gastrointestinal reactions and headaches that may occur with oral preparations, the safety advantage is very prominent.
Wide Range of Applications, Can Cooperate with Systemic Treatment to Improve Overall Efficacy
The product can not only be used alone for mild, localized cutaneous and mucosal cryptococcal infections but also serve as an adjuvant to systemic antifungal therapy for the management of local lesions in moderate to severe cryptococcosis.
In clinical practice, patients with cryptococcal meningitis often require long-term intravenous infusion of it or itraconazole for systemic treatment, but local cutaneous and mucosal lesions heal slowly and are prone to becoming a source of recurrent Cryptococcus dissemination. At this time, combined use of it to apply to cutaneous and mucosal lesions can accelerate the healing of local lesions, reduce the colonization of Cryptococcus in the local area, and lower the risk of disease recurrence during systemic treatment.
Meanwhile, for special populations such as infants and the elderly, dose adjustment of oral drugs is difficult. The topical gel can effectively control local infections through local administration without increasing the systemic dosage, expanding the applicable population for cryptococcosis treatment.
Limitations and coping strategies for treating cryptococcal infections
With the widespread application in the treatment of cryptococcal infections, the issue of drug resistance has gradually become prominent. Cryptococcus may develop resistance to it through various mechanisms, such as mutations in the ERG11 gene leading to structural changes in the target enzyme 14 α - demethylase, reducing its affinity for the target enzyme; Overexpression of efflux pumps increases drug efflux, leading to a decrease in intracellular drug concentration; Biofilm formation can significantly reduce the sensitivity of Cryptococcus to Fluconzole.
To address the issue of drug resistance, the following strategies can be adopted:
One is to use drugs reasonably, avoid indiscriminate prophylactic medication and excessive use, strictly follow the indications and treatment courses of the drugs, and reduce the selection pressure of drug-resistant strains.
The second is to conduct drug sensitivity tests and select appropriate antifungal drugs based on the drug sensitivity results. For Fluconzole resistant Cryptococcus infections, other categories of antifungal drugs such as echinocandins (such as caspofungin) or amphotericin B can be considered.
The third is combination therapy, which can be used in combination with other antifungal drugs with different mechanisms of action to produce synergistic effects, improve treatment efficacy, and overcome drug resistance. For example, its combination therapy with sertraline has shown a synergistic effect against Cryptococcus in experimental animal studies, providing some reference for clinical treatment.
FAQ
What happens if I take it without a yeast infection?
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If you don't have a yeast infection, antifungals won't help you get better. They can actually prolong the problem because the real cause will continue to get worse.
Is it safe in pregnancy?
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The product label for it recommends women who are pregnant not use this medication except in cases of severe or potentially life-threatening fungal infections. However, the benefit of using it might outweigh possible risks.
Is it good for skin fungus?
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It is also sometimes used to treat serious fungal infections that begin in the lungs and can spread through the body and fungal infections of the eye, skin and nails.
How effective is it?
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The clinical response rate showed 97% cure after 14 days in the treated with in situ gel. In comparison, the control group treated with it tablets showed 85% improvement in symptoms of oral candidiasis.
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