296 results about "Fluconazole" patented technology

The present invention refers to a treatment for mixed infectious diseases in the human reproductive system, wherein an association of compounds containing fluconazole and either tinidazole is used, the same being associated in doses lower to those commonly used therapeutically. The combination has proven to be highly efficacious and shown a good degree of tolerance.

The invention relates to a quick diagnostic kit used for testing four or more than four kinds of invasive candidas and an application method thereof. The quick diagnostic kit is characterized in that the kit is internally provided with fluorescent quantitative PCR reaction liquid containing specific primers and fluorescent probes corresponding to the candidas which are at least four kinds as well as positive control materials and negative control materials of the candidas which are at least four kinds; Ct value tested by a fluorescent quantitative PCR tester is used for judging. The kit has the characteristics of good specificity and high sensitivity; due to double control of high specificity amplification of the primers and high specificity hybridization of the fluorescent probes, the false positive is low; therefore, the invention can be used for simultaneously testing four kinds of invasive candidas which have different sensitivities for clinical first-line antifungal drugs such as fluconazole and the like in a simple, convenient, rapid, special and sensitive way.

This invention relates to a method of treating otitis externa using a topical combination medication, including one or more antifungal agent such as, for example fluconazole, voriconazole, itraconazole, clotrimazole, amphotericin B, caspofungin, micafungin, terbinafine, naftifine, butenafine, amorolfine, ravuconazole, posaconazole, flucytosine, econazole, enilaconazole, miconazole, oxiconazole, saperconazole, sulconazole, terconazole, tioconazole, nikkomycin Z, anidulafungin (LY303366), nystatin, pimaricin, griseofulvin, ciclopirox, haloprogin, tolnaftate, and undecylenate and one or more antibacterial agent such as neomycin sulfate, polymyxin B sulfate, colistin sulfate, gentamycin, tobramycin, chloramphenicol, Ciprofloxacin, Ofloxacin, a penicillin compound, a cephalosporin compound, a macrolide compound, a fluoroquinolone compound, streptomycin, or kanamycin.

Antimicrobial and contraceptive compositions and methods which prevent and / or reduce the risk of transmission of sexually transmitted diseases through sexual activity as well as prevent and / or reduce the risk of pregnancy are provided. The compositions contain (1) a matrix-forming agent, (2) a bio-adhesive agent, (3) a buffering agent, (4) optionally a humectant, (5) optionally a preservative, and (6) water; wherein the composition is suitable for application within the vagina; wherein the compositions form a semisolid matrix on contact with ejaculate (thereby trapping ejaculated microbes and spermatozoa); wherein the composition causes hardening of cervical mucus (thereby decreasing the probability of sperm entry); wherein the composition forms a bio-adhesive layer over vaginal surfaces (thereby preventing or reducing the risk of contact of STD-causing microbes with the vaginal surfaces); wherein the composition maintains an acidic vaginal pH of less than about 5 in the presence of semen ejaculated from the male; and wherein the composition does not significantly impair the natural microbiological balance within the vagina. The antimicrobial and contraceptive compositions may also contain additional antimicrobial and / or contraceptive agents (e.g., nonoxynol-9, octoxynol-9, benzalkonium chloride, phosphorylated hesperidins, sulfonated hesperidins, polystyrene sulfonates, substituted benzenesulfonic acid formaldehyde co-polymers, H2SO4-modified mandelic acids, povidone iodine, itraconazole, ketoconazole, metronidazole, clotrimazole, fluconazole, teraconazole, miconazole, tinidazole, iconazole, chloramphenicol, nystatin, cyclopiroxolamine, and the like).

Disclosed is a prescription for liquid status of fluconazole and its preparation, wherein the prescription comprises Fluconazole and medicinal findings, the medicinal findings include diluent (orsolvent), anti-oxidant agent and suspension auxiliary agent, the diluent (orsolvent) includes two types of oil-soluble and water-soluble. The liquid form Fluconazole prepared by the two types of diluent (orsolvent) can be prepared into the dosage forms of capsule, liquid type hard capsule and drop pill.

The invention relates to application of an effective part of a cockroach extract in preparing a drug for inhibiting fungus growth, and particularly relates to application of an effective part obtained by refining a crude cockroach extract through macroporous adsorption resin in the aspect of preparing a drug capable of resisting fungal infection. The effective part is refined from a fresh or dried Periplaneta americana L. polypide product through alcohol and water extraction, macroporous adsorption resin column chromatography and alcohol solvent elution, and has an obvious inhibition effect on the growth activity of candida albicans and a fungus growth inhibition capacity 80 times higher than that of fluconazole and 5-fluorocytosine and 800 times higher than that of amphotericin. The effective part of the cockroach extract can be prepared into forms, such as a hydrogel, a frothy gel, a cataplasm, freeze-dried powder, a water aqua, an aerosol, a suppository, a film, an external liniment, an ointment and the like, and is used for preparing pharmaceutical preparations for preventing and curing fungal infection, medical appliances and daily-use chemical products.

The invention relates to the technical field of medicaments, in particular to novel application of kaempferol as a synergist of anti-fungal medicaments. The anti-fungal medicaments are azole-type or polyene-type anti-fungal medicaments and based on the effective concentration of the anti-fungal medicaments, the adding ratio of the kaempferol is 0.5 to 16 mu g / ml. Tests show that when the kaempferol and the anti-fungal medicaments such as fluconazole, ketoconazole, miconazole and amphotericin B are used together, not only the anti-fungal effect is guaranteed on the premise of lowering the consumption of the anti-fungal medicaments, but also the anti-fungal medicaments can restore the function of killing the drug-resistant fungi, so that the kaempferol can be used as a synergist of the anti-fungal medicaments. The kaempferol used as the synergist of the anti-fungal medicaments can lower the consumption of the azole-type or polyene-type anti-fungal medicaments so as to reduce the toxic and side effects of the medicaments; and the kaempferol can make the anti-fungal medicaments restore the function of killing the drug-resistant fungi, so that the kaempferol can effectively treat mycotic infection, particularly drug-resistant t mycotic infection, and has quite important clinical application values.

The invention relates to a novel broad-spectrum antifungal medicine compound, a broad-spectrum antifungal medicine composition, an application of the compound or the composition in the preparation of a broad-spectrum antifungal medicine, and an application of the compound or the composition in the preparation of a medicine used for treating severe invasive infection (comprising Candida krusei) caused by invasive aspergillosis and / or Fluconazole-resistant Monilia and / or severe infection caused by Scedosporium and fusarium. The novel broad-spectrum antifungal medicine compound and the broad-spectrum antifungal medicine composition have extensive and strong antifungal activity and better dynamic property and safety. For deep mycotic infection, the novel broad-spectrum antifungal medicine compound and the broad-spectrum antifungal medicine composition are better than the original voriconazole in the aspects of the antibiotic activity and the medicine resistance and is better than amphotericin B in the aspects of safety and effectiveness; and compared with the formerly applied voriconazole, Fluconazole, itraconazole and amphotericin B, the novel broad-spectrum antifungal medicine compound and the broad-spectrum antifungal medicine composition have reinforced medicine effect, less adverse reaction and good safety.

The invention discloses a berberine azole compound shown in general formulas such as I-IV, and a pharmaceutically acceptable salt thereof, and also discloses a preparation method of the compound, which comprises the following steps that: a compound VI and an azole compound HIm or 1H-2-mercaptobenzimidazole are reacted to obtain an intermediate VII or VIII, and then the obtained intermediate is reacted with a compound V to obtain the berberine azole compound shown in general formulas such as I or II; and the compound V and a compound IX or XI are reacted to obtain an intermediate X or XII, and then the obtained intermediate is reacted with the azole compound Him to obtain the berberine azole compound shown in general formulas such as III or IV. The berberine azole compound has a certain inhibitory activity on Gram-positive bacteria, Gram-negative bacteria and fungi, the anti-bacterial activity of part of the compounds is equal to or even stronger than that of chloramphenicol or norfloxacin, the antifungal activity of part of the compounds is equal to or even stronger than that of fluconazole, and the berberine azole compound can be used for preparing anti-microbial drugs.

The invention discloses antifungal application of fraxetin, belonging to the technical field of medicines. In-vitro experiments show that fraxetin has relatively good inhibition effect to the fungi, is capable of restoring the effect of an antifungal drug, namely fluconazole to drug-resistant fungi and therefore can be taken as the antifungal drug and a synergist for the antifungal drug. Accordingto the antifungal application, the new use of fraxetin is opened up, fraxetin is used as the antifungal drug and the synergist for the antifungal drug, a new candidate drug is provided for the fungustreatment, and the antifungal effects of existing drugs are improved. Under the conditions that clinical fungus drug resistance becomes common increasingly and the drug resistance level becomes serious increasingly, the effect of an antifungal drug to the drug-resistant fungi is restored, and the use dosage of the antifungal drug is reduced, so that the medical expense of a patient is saved, andthe toxic and side effects of the drugs are reduced.

The present invention refers to a treatment for mixed infectious diseases in the human reproductive system, wherein an association of compounds containing fluconazole and either tinidazole or secnidazole is used, the same being associated in doses lower to those commonly used therapeutically. The combination has proven to be highly efficacious and shown a good degree of tolerance.

The invention relates to a freeze-drying composition of a posaconazole prodrug and a preparation method and application of the freeze-drying composition of the posaconazole prodrug. The freeze-drying composition has the advantages that the freeze-drying composition is high in water solubility, and safety of the freeze-drying composition is guaranteed due to the fact that cyclodextrins auxiliary materials need not to be added during the preparation of the freeze-drying composition; the freeze-drying composition is suitable for being used for treating various amphotericin-intolerant or refractory adult invasive fungal infections; the freeze-drying composition is used as a preventive drug for high-risk patients, the freeze-drying composition is applicable to patients above 13 years old and with impaired immunity and especially applicable to patients who have graft versus host disease (GVHD) after hematopoietic stem cell transplant, patients with leukemia and patients with long-term leukopenia due to chemotherapy; compared with control drugs such as fluconazole and itraconazole, the freeze-drying composition can effectively prevent invasive aspergillosis and can lower the mortality related to the invasive fungal infections.

The invention discloses a novel application of honokiol and fluconazole in antifungal cooperation. According to the invention, the fungi are candida albicans. According to the invention, a standard macrodilution drug sensitivity experiment recommended by CLSI is adopted, in vitro sensitivity of honokiol towards clinically separated drug resistant candida albicans is evaluated with systematic methods such as a checkerboard macrodilution method and a time-kill curve method. Also, an in vitro synergistic effect of honokiol and fluconazole in clinic drug resistant fungi resistance is evaluated. Further, with a mice infection and treatment experiment, an in vivo synergistic effect of honokiol and fluconazole in clinic drug resistant fungi resistance is evaluated.

A method of treating or preventing fungal infection, which includes identifying a plant or animal having a fungal infection and administering an effective amount of an anti-fungal composition to the plant or animal to reduce the fungal infection. In a preferred form of the present invention, the antifungal composition is compound 13 or 33 and is combined with an azole compound, such as fluconazole.

The invention discloses an application of a combination of a tetracycline medicine and fluconazole (FLC) in the preparation of an antifungal product, and the product thereof, and concretely discloses a synergistic effect of three cell calcium regulators of a non-selective calcium channel retarding agent benidipine (BEN), a selective L-type calcium channel retarding agent nifedipine (NIF) and a calcium ion chelating agent ethylene diamine tetraacetic acid (EDTA) to the FLC and tetracycline antifungal medicines of doxycycline (DOX) and minocycline (MINO), and an application of the three cell calcium regulators in Candida albicans resisting, wherein a synergistic antifungal effect can be generated by the combined application of the FLC, the DOX and the MINO. Results confirm that the combined application of the FLC and the DOX / MINO can generate the synergistic antifungal effect, and has a substantial killing effect on drug-resistant Candida albicans; the BEN, the NIF and the EDTA can obviously enhance the combined antifungal effect of the FLC and the DOX / MINO to the Candida albicans, and can obviously reduce the lowest effective concentration during the combined application of the FLC, the MINO and the DOX; and the combined application of the three calcium regulators and the FLC can enhance the antifungal effect.

The invention discloses a triazole compound. The triazole compound has excellent water solubility. The triazole compound is obtained by introduction of a novel functional group to high efficiency and wide spectrum antifungal compound voriconazole and fluconazole drugs found in the existing clinical application and novel drug development so that the triazole compound greatly improves voriconazole and fluconazole water solubility and reduces drug toxicity.

The invention relates to a compound ear drop for treating otitis externa mycotica, in particular to an ear drop for treating otitis externa mycotica. The drop is prepared by the the following ingredients: 3-30g of fluconazol, 5-50g of tinidazole, 3-30g of menthol, 100-800g of glycerine, 30-200ml of alcohol, 5-100ml of 1mol / L sodium hydroxide solution, and 1000ml of distilled water. The drop contains both antifungal drug and antianaerobic drug which enable the ear drop to have both antifungal activity and antianaerobic activity. In the process of preparation allocation, the tinidazole being slightly soluble into water need be heated by aqueous bath to be dissolved, the fluconazol and the menthol are easily dissolved into the alcohol. The alcohol is used for not only dissovling both the fluconazol and the menthol, but also being taken a transdermal accelerant of the ear drop, as well as drying the external acoustic meatus. The menthol can dispel wind to make the skin and the membrana mucosa cool and relieve the complaint and pain. A fixed amount of glycerine can protect the ear mucosa and keep the preparation tensile and adhesive.

The invention provides application of magnolol and azole medicines to preparation of antifungal combined medicines. The application indicates that azole medicines such as fluconazole, ketoconazole, itraconazole, miconazole and voriconazole are used together with magnolol to generate a synergetic antifungal effect; the magnolol serving as an efflux pump Cdrlp substrate is utilized to compete with the azole medicines for an efflux system, so that the concentration of efflux medicines can be reduced, and the curative effect of medicines can be improved. Furthermore, magnolol acts on the synthetic pathway of ergosterol and is combined with azole medicines to form a double-edged sword to inhibit synthesis of ergosterol together.

The present invention provides oral pharmaceutical formulation for azole antimicrobial drugs such as itraconazole, saperconazole, ketoconazole, and fluconazole. The oral pharmaceutical formulation contains a core and a drug coating layer. The drug coating layer contains the azole antimicrobial drug and a binder, but not containing an emulsion (such as polyoxypropylene-polyoxyethylene block copolymers, polyoxyethylene-sorbitan-fatty acid esters, sodium lauryl sulfate, or vitamin E polyethylene glycol succinate) and / or an absorbent aid (such as DL-malic acid, citric acid, ascorbic acid, and alginic acid). The oral pharmaceutical formulation can optionally contain a protective layer, such as polyethylene glycol 20,000. The present invention also provides a method for preparing and using the formulation.

The present invention relates to pharmaceutical dosage forms which include an antifungal having poor solubility. The pharmaceutical dosage forms of the present invention further comprise non-spherical granules, which do not contain a coated core region and may be formed into pharmaceutically acceptable dosage forms. The antifungal active pharmaceutical ingredients include itraconazole, saperconazole, ketoconazole, voriconazole and fluconazole.

The invention discloses 3,5-diaryl pyrazole or 3,4-diaryl pyrazole derivative and application thereof. The 3,5-diaryl pyrazole or 3,4-diaryl pyrazole derivative is prepared from compound which is shown in a formula (I), a formula (II), a formula (III) or a formula (IV) or pharmaceutical-acceptable salt of the compound. A formula of the 3,5-diaryl pyrazole or 3,4-diaryl pyrazole derivative is shownin a following image, wherein R1, R2, R3, R4 and R5 are respectively and independently chosen from hydrogen atom, hydroxy, nitro, amino, alkoxy or ester group with a C1 to C10 alkyl substituent group; alkyl in the alkoxy is a C1 to C10 alkyl; R is independently chosen from hydrogen atom, 2-ethoxy, acetyl, phenyl, benzoyl, p-methoxyphenyl, 4-trifluoromethoxy, 2-cyanoethyl or C1 to C10 alkyl. The 3,5-diaryl pyrazole derivative or the 3,4-diaryl pyrazole derivative can be applied to preventing and treating fungal infection; especially, application in treating candida albicans infection and reversing fluconazole drug resistance has good development value.

The invention discloses a pesticide composition containing fluconazole hydroxylamine and prochloraz and application thereof. The pesticide composition comprises effective components; the effective components are fluconazole hydroxylamine and prochloraz; the mass ratio of fluconazole hydroxylamine to prochloraz is 20:1 to 1:20. The invention further discloses the application of the pesticide composition containing fluconazole hydroxylamine and prochloraz to the treatment of fusarium head blight. The pesticide composition disclosed by the invention has the benefits that the respective potential drug resistance risk of gibberella zeae to fluconazole hydroxylamine and prochloraz is reduced; after fluconazole hydroxylamine and prochloraz are combined, an obvious synergistic effect exists between fluconazole hydroxylamine and prochloraz; the effect on prevention and treatment of the fusarium head blight is significant.

The invention discloses an anti-CA (candida albicans) product combining harmine hydrochloride and fluconazole and an application of the product and belongs to the technical field of medicines. The combined antifungal function of fluconazole and harmine hydrochloride on drug-resistant CA are researched with multiple methods. The effective concentration of fluconazole to harmine hydrochloride is 1:32 (mu g / mL, for CA3) or 1:16 (mu g / mL, for CA2) when fluconazole and harmine hydrochloride are combined to be applied, the minimum inhibitory concentration is 8 mu g / mL and 0.25 mu g / mL (for CA3) or 0.5 mu g / mL (for CA4). When harmine hydrochloride and fluconazole are combined, the antibacterial activity of fluconazole for drug-resistant CA can be enhanced, the coordinated antifungal action can be generated, the drug resistance of drug-resistant CA to fluconazole can be reversed, and a research direction is provided for development of new drugs and new application of old drugs.

Xanthochymol and garcinol, isoprenylated benzophenones purified from Garcinia xanthochymus fruits, showed multiple activities against fungal biofilms. Both compounds effectively prevented emergence of fungal germ tubes and were also cytostatic, with MICs of 1 to 3 ΞM. The compounds therefore inhibited development of hyphae and subsequent biofilm maturation. Xanthochymol treatment of developing and mature biofilms induced cell death. In early biofilm development, killing had the characteristics of apoptosis. These activities resulted in failure of biofilm maturation and hyphal death in mature biofilms. In mature biofilms, xanthochymol and garcinol caused the death of biofilm hyphae, with 50% effective concentrations (EC50s) of 30 to 50 μM. Additionally, xanthochymol-mediated killing was complementary with fluconazole against mature biofilms, reducing the fluconazole EC50 from greater than 1,024 μg per ml to 13 μg per ml.

The invention belongs to the technical field of medicine preparations and particularly relates to fluconazole tablets and a preparation method thereof. The fluconazole tablets comprise the following raw materials in parts by weight: 40 to 50 parts of fluconazole, 15 to 40 parts of a filling agent, 2 to 15 parts of a disintegrating agent, 5 to 10 parts of an adhesive and 0.2 to 2 parts of a lubricant, wherein the filling agent comprises sodium alginate, microcrystalline cellulose and anhydrous calcium hydrogen phosphate; the disintegrating agent comprises croscarmellose sodium; the adhesive ispovidone K30; and the lubricant is magnesium stearate. The fluconazole tablets have the advantages of high compressibility, controllable friability and dissolubility, rapidness in disintegration, excellent stability and dissolution performance, high bioequivalence and high bioavailability.

The invention provides a solid preparation of fluconazole liposome and a new application thereof. Specifically, the solid preparation of the fluconazole liposome is prepared by the fluconazole liposome and auxiliary materials. The invention discovers unexpectedly that when fluconazole and specific phospholipid and cholesterol are mixed in a certain matching ratio and combined with an antioxidant to prepare the liposome, and the problems about stability and dissolution rate of the solid preparation of the fluconazole liposome and the like are resolved. The liposome technique has high entrapment rate and good product quality and can be used for treating mucormycosis.

The invention discloses an antifungal product combining ambroxol hydrochloride with fluconazole and application thereof and belongs to the technical field of medicine. Static and dynamic combined antifungal effect, on medicine-resistant Candida albicans, of combined use of fluconazole and ambroxol hydrochloride is studied through various methods. An effective concentration proportion of fluconazole to ambroxol hydrochloride when ambroxol hydrochloride and fluconazole are combined for application is 1:64 (ug / mL), and lowest antibacterial concentrations are 128 ug / mL and 2 ug / mL respectively. When ambroxol hydrochloride is combined with fluconazole, antibacterial activity, to medicine-resistant Candida albicans, of fluconazole can be improved, synergistic antifungal effect can be generated, medicine resistance, to fluconazole, of medicine-resistant Candida albicans can be reversed, and a studying direction is provided for development of new drugs and new application of old drugs.

The invention relates to the technical field of medicines, in particular to new application of theaflavin as a synergist of antifungal drugs. Through in vitro experiments, when used together with fluconazole, itraconazole, miconazole, ketoconazole and other antifungal drugs, theaflavin can increase therapeutic effect on slight surface and deep fungus infection to some extent and can restore the effect of the antifungal drugs on drug-resisting fungi. Therefore, the theaflavin can be used as the synergist of the antifungal drugs. The invention provides new application for the theaflavin; when used as the synergist of the antifungal drugs, the theaflavin not only can increase the antifungal effect of the drugs, but also can restore the effect of the antifungal drugs on the drug-resisting fungi in the condition that clinic fungal drug resistance is more and more common and drug resistance degree is more and more serious. The application dosage of the antifungal drugs can be reduced, so that medical expenses can be saved for patients, and the toxic and side effects of the drugs are reduced.

An application of the berberine as the synergist of antifungus medicine (fluconazole, ketoconazole, etc) is disclosed.