39 results about "Itraconazole" patented technology

Disclosed are methods and uses for treating a subject having a condition selected from liver disease, Cushing's syndrome or Cushing's disease, cancer, infection, inflammation, cardiovascular, endocrine or kidney disease, and combinations thereof, or other disease that may thus be administered a drug that may cause hepatotoxicity, the methods and uses having no adverse effects on the liver. The liver diseases comprise fatty liver diseases, high-level liver enzyme can be effectively reduced, and good safety is achieved. The methods and uses include administering to a subject an effective amount of a selective non-steroidal glucocorticoid receptor modulator, such as relacan, including methods and uses for use in combination with other drugs, without adversely affecting liver enzyme levels or liver function. In embodiments, another drug may be a drug that may cause hepatotoxicity, such as a drug that inhibits the CYP3A enzyme, such as itraconazole or ketoconazole.

The invention provides an additive composition for promoting itraconazole absorption, and the additive composition is prepared from the following components in parts by mass: 20 to 40 parts of modified hydroxypropyl methylcellulose acetic acid succinate, 10 to 25 parts of copovidone, 5 to 15 parts of N-capryloyl sodium salicylate, 2 to 8 parts of nano silicon dioxide and 3 to 10 parts of polyoxyethylene-polyoxypropylene segmented copolymer. According to the additive composition disclosed by the invention, the problems of dissolution rate, bioavailability and stability of the itraconazole oral preparation are comprehensively solved through polymer modification, compounding synergy and parameter optimization, and the process cost is remarkably lower than that of the prior art.

Disclosed herein are analogues of itraconazole that are potent hedgehog signaling pathway inhibitors. The compounds are expected to be useful in the treatment of cell proliferation disorders such as cancer, particularly cancers that are dependent upon the hedgehog signaling pathway such as basal cell carcinoma and medulloblastoma.

The present invention provides a combination comprising an amount of itraconazole (ITC) and an amount of a compound, or a pharmaceutically acceptable salt thereof, wherein the compound has the following structure:

The invention provides a synthesis method of itramod, which comprises the following steps: carrying out condensation reaction on a new compound 7 and a compound 8 under the action of alkali to obtain an intermediate compound 9; and finally salifying to obtain a final product compound 10 of istratimod. The istratimod synthesis method is short in synthesis route, simple to operate, high in yield, high in product purity and suitable for industrial production, and the reaction route is # imgabs0 #.

A topical composition for treating fungal skin infections with associated inflammation may include making or administering to the affected skin area an antifungal and steroid, such as a corticosteroid. Certain compositions may include antifungals such as itraconazole or econazole and corticosteroids such as fluticasone, fluocinonide, or clobetasol. The antifungal and steroid may be within a cream. In one example, a commercially available econazole nitrate cream may be used in conjunction with a commercially available fluocinonide cream or commercially available clobetasol cream to treat the affected skin area.

This application relates to the field of biotechnology, and particularly to primer pairs, primer-probe compositions, PCR premixes, kits, and methods for detecting multiple respiratory pathogens. Nucleic acid sequences are shown in primer pairs as indicated by SEQ ID NO: 1-2, 4-5, 7-8, 10-11, 13-14, 16-17, 19-20, 22-23, 25-26, 28-29, 31-32, 34-35, 37-38, and 40-41. For target respiratory pathogens, this application designs specific amplification primer pairs, paired with suitable probes, enabling the simultaneous detection of eight targets. Furthermore, the detection process avoids interference from heme, trimethoprim, sulfamethoxazole, amphotericin B, itraconazole, fluconazole, azithromycin, adrenaline, and lidocaine hydrochloride in the test sample. It exhibits good anti-interference properties and shows no cross-reactivity with *Rhodococcus equi*, *Candida tropicalis*, and *Candida krusei*.

The present invention provides a combination comprising an amount of itraconazole (ITC) and an amount of a compound, or a pharmaceutically acceptable salt thereof, wherein the compound has the following structure:

The present disclosure relates to a method of treating a disease or condition in a subject forbidding oral administration of itraconazole, comprising administering to the respiratory tract of the subject an inhalable dry powder comprising itraconazole. The present disclosure also relates to methods of co-administering itraconazole to a subject in need thereof with a second therapeutic agent wherein the itraconazole is administered to the respiratory tract of the subject in the form of an inhalable dry powder, and wherein the second therapeutic agent is a substrate, inducer and / or inhibitor of an enzyme or receptor that is inhibited by itraconazole or metabolizes itraconazole.

This invention discloses a screening method for inhibitors of the interaction between ATF3 and Importin α and its application. By constructing a target model based on the interaction interface between Importin α and ATF3, this target model is used to perform virtual screening of a small molecule compound library based on molecular docking, and the binding free energy is calculated to screen for candidate compounds that can bind to Importin α and effectively block its interaction with ATF3. The effects of the candidate compounds on the interaction between Importin α and ATF3 are verified through in vivo and / or in vitro experiments. This invention has screened and obtained several small molecule candidate drugs, with itraconazole as a representative small molecule compound, capable of inhibiting the interaction between Importin α and ATF3.

The present invention discloses a preparation method of an itraconazole intermediate, which relates to the technical field of compound preparation; the synthesis method of the itraconazole intermediate includes: providing compound A, using compound B to replace the hydrogen in the N-H group of compound A, and then reacting with compound C containing a halogen substituent to generate compound D, and the compound D is subjected to hydrolysis, decarboxylation, demethylation, and esterification reactions to obtain the itraconazole intermediate. The preparation method of the itraconazole intermediate provided by the present invention has a high yield, high purity of the obtained itraconazole intermediate, low cost, and is easy to promote and use.

The invention relates to the technical field of gene engineering, in particular to preparation of a gene-deleted target SOD6 and application of the gene-deleted target SOD6 in fungi. On the basis of an instantaneous CRISPR / Cas9 technology, sgRNA and repair DNA are designed, NAT is used as a selection marker, NAT is inserted into a fungal genome through a homologous recombination method, fixed-point knockout of a target gene SOD6 is achieved, and a candida albicans attenuated strain without the SOD6 gene is obtained; candida albicans SOD6 is found to regulate pathogenicity, itraconazole sensitivity, DNA damage, oxidative stress and ROS accumulation, a novel pathogenic target SOD6 of Candida albicans is found, the novel pathogenic target SOD6 is a potential ideal therapeutic target, and inhibitors or vaccines can be researched and developed in a targeted manner in the later stage.

The present disclosure relates to methods of treating cancer, such as lung cancer (e.g., non-small cell lung cancer) by administering a dry powder to the respiratory tract of a subject in need thereof (e.g., by oral inhalation), the dry powder comprising respirable dry particles that comprise an angiogenesis inhibitor (e.g., itraconazole), and optionally a stabilizer (e.g., polysorbate 80) and / or one or more excipients (e.g., leucine and a sodium salt, such as sodium sulfate).

The invention belongs to the technical field of medicines, and particularly relates to itraconazole transdermal cream and a preparation method thereof. According to the itraconazole transdermal cream provided by the invention, the itraconazole and the clove essential oil are jointly applied by adopting an emulsification method, the limitation of single use of the itraconazole and the clove essential oil is broken through, the bioavailability of the itraconazole and the clove essential oil is improved, and the itraconazole transdermal cream acts on an infected part after being subjected to transdermal absorption through local administration, so that the itraconazole is absorbed into blood and reaches the skin of the whole body to play a role; the traditional Chinese medicine composition can achieve the same blood concentration and effect of oral administration, is convenient to use, reduces liver toxicity and gastrointestinal tract adverse reactions, and reduces the risk of adverse reactions and drug interaction at the same time.

The invention belongs to the field of medicine powder preparations, and relates to itraconazole inhalation type dry powder as well as a preparation method and application thereof. The preparation method comprises the following steps: preparing an itraconazole eutectic through a solvent evaporation method, forming an eutectic nano suspension from the itraconazole eutectic through a medium grinding method, mixing the nano suspension with an excipient, and preparing dry powder through spray drying. The particles of the dry powder composition are spherical, and the aerodynamic diameter is smaller than 4 microns. The emptying rate is greater than 90%, the fraction of fine particles is greater than 40%, and the aerosol can be quickly dispersed after in-vitro atomization and has a good in-vivo lung positioning effect.

The application discloses a kind of containing it is the preparation method of spray and preparation method of eucalyptol for external use, and each 1000ml external use spray material composition: it is 8~10g, eucalyptol 10~20g, hydroxypropyl-β-cyclodextrin 250~300g, propylene glycol 100~140g, 9.5~12g of hydrochloric acid, diethylene glycol monoethyl ether 140~160g, caprylic acid capric acid polyethylene glycol glyceride 40~60g, 1.9~2.1g of sodium hydroxide, the rest is pure water, and preparation is obtained external use spray, mass is stable, antifungal effect is remarkable, clinical use is convenient.

The presently disclosed subject matter provides a method and pharmaceutical composition for long-term use in treating or preventing disease conditions caused by the parasite Trypanosoma cruzi known as Chagas disease. The pharmaceutical composition is a long-term injectable composition that can include a dose of Itraconazole and a dose of Amiodarone in an amount effective to treat Chagas disease, or in an amount effective to prevent Chagas disease in a human or animal patient such as a mammal. The pharmaceutical composition may also include a pharmaceutically acceptable vehicle, carrier, or excipient. The form of itraconazole used in the pharmaceutical composition may be prepared by any suitable process wherein the active ingredients to have sufficient bioavailability when injected into a human or animal subject. The long-term method for treating or preventing Chagas disease is carried out by a single injection of Itraconazole and Amiodarone in an amount effective to treat a subject in need thereof, and / or in an amount effective to prevent the subject from contracting the disease so that repeated dosages are not required again for a long-term period such as 6 or 12 months. The present compositions, methods, and uses are safer and longer lasting, more patient friendly, and provide a safer and more effective way of treating or preventing Chagas disease than previously possible.

The presently disclosed subject matter provides a method and pharmaceutical composition for long-term use in treating or preventing disease conditions caused by Leishmania species parasites such as Leishmaniasis. The pharmaceutical composition is a long-term injectable composition that can include a dose of Itraconazole and a dose of Amiodarone in an amount effective to treat Leishmaniasis, or in an amount effective to prevent Leishmaniasis in a human or animal patient such as a mammal. The pharmaceutical composition may also include a pharmaceutically acceptable vehicle, carrier, or excipient. The long-term method for treating or preventing Leishmania disease is carried out by a single injection of Itraconazole and Amiodarone in an amount effective to treat a subject in need thereof, and / or in an amount effective to prevent the subject from contracting the disease so that repeated dosages are not required again for a long-term period such as 6 or 12 months. The present compositions, methods, and uses are safer and longer lasting, more patient friendly, and provide a safer and more effective way of treating or preventing Leishmaniasis than previously possible.

Compositions and methods for the treatment of onychomycosis. The compositions include a pharmaceutically effective amount of one or more anti-fungal agents in a petrolatum carrier. The one or more anti-fungal agents may include, for example, terbinafine HCl, ciclopirox, ciclopirox olamine, fluconazole, itraconazole, ketoconazole, amorolfine, efinaconazole, clotrimazole, miconazole (miconazole nitrate), and any combination thereof.

The invention discloses a biocompatible antibacterial composite material and a preparation method thereof. The biocompatible antibacterial composite material is prepared from N-isopropylacrylamide and a vinyl proline choline ionic liquid monomer, or the N-isopropylacrylamide, acrylic acid and the vinyl proline choline ionic liquid monomer through free radical polymerization. According to the invention, the obtained aerogel is immersed in an itraconazole (ITR)-loaded solution or an ibuprofen-loaded solution, the obtained drug-loaded gel is freeze-dried again, the drug-loaded effect is observed, and a drug dissolution experiment is carried out. The crystallinity of the medicine in the medicine-loaded composite material is observed through an XRD technology, and the result clearly shows that the medicine is kept in an amorphous state. The preparation method is simple and easy to implement, and the prepared composite material has a wide application prospect in the field of biomedicine.

An additive compound for dyeing an aluminum or aluminum alloy substrate after anodic oxidation to provide better uniformity in dyeing and hence a better finished appearance includes a main agent, an auxiliary agent, a pH stabilizer, an antibacterial agent, and a moderating agent. The antibacterial agent includes at least one of sorbic acid, fluconazole, itraconazole, artemisia argyi, benzyl alcohol, benzoic acid, salicylic acid, and boric acid. The moderating agent includes at least one of amino acid, amino salt, sulfate, nitrate, and chloride. An additive solution and a dyeing method are also provided, the use of the compound also allows for a more rapid dyeing process.

The invention belongs to the technical field of medicines, and particularly relates to application of rutin in preparation of a preparation for preventing and / or treating talaromyces marneffei infection. The invention provides application of rutin in preparation of a preparation for preventing and / or treating talaromyces marneffei infection. It is found for the first time that the natural flavonoid compound rutin has a remarkable inhibiting effect on talaromyces marneffei infection, and compared with the liver and kidney toxicity and drug resistance problems possibly caused by conventional antifungal drugs such as amphotericin B and itraconazole, the rutin can effectively reduce side effects when applied to resisting talaromyces marneffei infection, and has a good application prospect. The drug-resistant strain generation risk is reduced, and the treatment safety is improved.

The invention belongs to the technical field of new application of medicines, and particularly relates to application of itraconazole in preparation of a product for amplifying an induced T cell into a central memory T cell in vitro. It is found through experiments that itraconazole is additionally added into a CAR-T cell culture medium, CAR-T cells can be rapidly induced, differentiated and amplified into central memory CAR-T cells in vitro, and the proportion of the central memory CAR-T cells in the CAR-T cells is obviously increased. Itraconazole is a clinical medicine, pharmacokinetic and toxicological studies are clear, the safety is high, good technical support is provided for tumor cell treatment, and the itraconazole has important significance.

The invention discloses an itraconazole solid dispersion with high drug loading capacity. The itraconazole solid dispersion is prepared from the following components in percentage by weight: 40-55% of itraconazole, 40-55% of a polymer carrier and 2-6% of a crystallization inhibitor, the polymer carrier is selected from one or a combination of at least two of hydroxypropyl methylcellulose, copovidone and a polyethylene caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer; the crystallization inhibitor is selected from one or a combination of at least two of lauryl sodium sulfate, poloxamer and polysorbate. According to the itraconazole solid dispersion, itraconazole is highly dispersed in the polymer carrier, so that the dissolution rate of itraconazole in the solid dispersion is further improved on the basis of ensuring that the raw materials are stable and are not degraded; the crystallization inhibitor such as lauryl sodium sulfate is used for effectively inhibiting the recrystallization and easy aging and dissolution rate reduction behaviors of itraconazole in the storage process of the high-drug-loading-capacity solid dispersion.

This invention belongs to the field of pharmaceutical powder formulations, and relates to an itraconazole inhalation dry powder, its preparation method, and its application. The preparation involves preparing itraconazole cocrystals via solvent evaporation, then forming a cocrystal nano-suspension through media milling. The nano-suspension is mixed with an excipient and then spray-dried to prepare the dry powder. The dry powder composition of this invention has spherical particles with an aerodynamic diameter of less than 4 μm. It exhibits an air displacement rate greater than 90%, a fine particle fraction greater than 40%, rapid dispersion after in vitro atomization, and good localization effect in the lungs in vivo.

The invention relates to the technical field of western medicine preparations, and discloses an itraconazole solid dispersion as well as a preparation method and application thereof, and the solid dispersion is prepared from itraconazole, a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol grafted copolymer and copovidone in a mass ratio of (0.5-2): (0.1-5): (0.01-5). The preparation method comprises the following steps: mixing the itraconazole, the polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol grafted copolymer and the copovidone according to the formula ratio, and adding into a hot melt extruder; the temperature of an extruder is set to be 145-175 DEG C, the rotating speed of a screw of equipment used for hot melt extrusion is 100-250 rpm, and crushing is performed after extrusion to obtain the itraconazole dispersion. The itraconazole solid dispersion prepared by the invention has better dissolution rate in cat gastrointestinal tracts and is easy to disperse, the dissolution rate of the itraconazole solid dispersion is 85-95%, and the complete dispersion time is 1-3 minutes.

The application belongs to the technical field of new use of medicines, and particularly relates to application of itraconazole in preparation of a product for inducing T cells to be central memory T cells in vitro. It is found through experiments that, by additionally adding itraconazole in a CAR-T cell culture medium, CAR-T cells can be rapidly induced and differentiated to be central memory CAR-T cells in vitro, and the proportion of the central memory CAR-T cells in the CAR-T cells is obviously increased. Itraconazole is a clinical drug, and pharmacokinetics and toxicology research is clear, and the safety is high. The application provides good technical support for tumor cell treatment, and has important significance.

The invention belongs to the technical field of biological medicines, and relates to itraconazole-loaded chitosan gel as well as a preparation method and application thereof. Comprising itraconazole and chitosan gel, the content of the itraconazole loaded on the chitosan gel is not lower than 0.300 mg / mL, and the chitosan gel is chemically crosslinked hydrogel which is formed by reacting chitosan with four-arm polyethylene glycol active ester through amino in the chitosan and NHS groups in the four-arm polyethylene glycol active ester to generate amido bonds. The aperture of the cross section of the hydrogel in the gel forming direction is 15-30 microns, and the cross section of the hydrogel in the direction perpendicular to the gel forming direction is of a lamellar structure. The itraconazole-loaded chitosan gel provided by the invention has an exact fibrosis inhibition effect, can stay in a uterine cavity for a long time, and has a certain mechanical support effect on the uterine cavity.

The present invention relates to a triazole drug suspension, a preparation method therefor, and use thereof. The triazole drug suspension of the present invention comprises a therapeutically effective amount of itraconazole, a surfactant, solvent water, an osmotic pressure regulator, a metal complexing agent, and a pH regulator, wherein the mass ratio of itraconazole to the surfactant is 5:1-15:1. Itraconazole has a D10 particle size of greater than or equal to 0.5 μm, a D50 particle size of 1.5-3.5 μm, and a D90 particle size of less than or equal to 6.0 μm. The concentration of free itraconazole in the suspension is not less than 0.04 μg / ml. The suspension of the present invention has a suitable free-state drug content and a suitable granular drug particle size distribution, enabling, after the suspension of the present invention is administered by means of inhalation, the drug to be rapidly absorbed by a target part and to act, and maintaining sustained and slow release. While a therapeutic dose is maintained, the frequency of administration is reduced, thereby improving the safety of drug administration.

Provided herein are Itraconazole analogs. Also provided herein are methods of inhibition of Hedgehog pathway, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, angiogenesis and treatment of disease with Itraconazole analogs.