30 results about "Itraconazole" patented technology

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 #.

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 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 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.

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 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.

The invention relates to the technical field of biology, in particular to a primer pair, a primer probe composition, a PCR premix, a kit and a method for detecting multiple respiratory pathogens. The invention discloses a primer pair with nucleic acid sequences as shown in 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. Aiming at a target respiratory pathogen, a specific amplification primer pair is designed and is matched with a proper probe, so that eight-target joint detection can be realized, and the influence of heme, trimethoprim, sulfamethoxazole, amphotericin B, itraconazole, fluconazole, azithromycin, epinephrine and lidocaine hydrochloride in a detection sample can be avoided in the detection process; the anti-interference performance is good, and cross reaction with rhodococcus equi, candida tropicalis and candida krusei does not exist.

The invention belongs to the technical field of medicines, and particularly relates to a drug-loaded polymer-based itraconazole solution and application thereof. The preparation method of the drug-loaded polymer-based itraconazole solution comprises the following steps: (1) mixing itraconazole and a polymer according to a mass ratio of 1: 10-1: 20, and adding the mixture into an organic solvent; (2) stirring at 25-60 DEG C for 4-6 hours until a uniform and transparent drug-loaded polymer solution is formed; and (3) removing the organic solvent through reduced pressure distillation or freeze drying to obtain the drug-loaded polymer-based itraconazole solution. According to the polymer-based itraconazole solution preparation provided by the invention, itraconazole is loaded into a specific polymer matrix to form a uniform and stable solution system, so that the solubility of itraconazole can be remarkably improved. And the used polymer material has excellent biocompatibility and safety.

Provided is a pharmaceutical composition comprising an effective amount of itraconazole, and a pharmaceutically acceptable excipient. The use of the pharmaceutical composition for treatment of idiopathic pulmonary fibrosis is also provided.

The invention provides a preparation method of itramod, and relates to the technical field of pharmaceutical chemicals. The method comprises a coupling-oxidative hydroxylation reaction, a mitsunobo reaction, a hydrolysis reaction and a salt forming process. According to the preparation method of the itramod, provided by the invention, the itramod arginine salt is prepared, the process route is novel, the total molar yield is high, and the preparation method has the characteristics of more controllable quality, high chiral purity, high atom economy and stable process.

Itraconazole, a widely used antifungal drug, has been found to possess potent antiangiogenic and anti-hedgehog activities and has shown promising antitumor activity in several human clinical studies. However, its widespread use in cancer treatment has been limited by its potent inhibition of the drug-metabolizing enzyme CYP3A4, which can cause drug-drug interactions. In an effort to eliminate itraconazole's CYP3A4 inhibition while retaining its antiangiogenic activity, we synthesized a series of itraconazole derivatives. The newly synthesized itraconazole analogs were evaluated for their cytotoxicity and CYP3A4 inhibitory activity against human umbilical vein endothelial cells (HUVECs).

The invention provides an oral solution capable of obviously improving the palatability of cats and good in stability and a preparation method of the oral solution. The oral solution comprises the following raw materials: 1%-2% of itraconazole, 35%-45% of hydroxypropyl beta-cyclodextrin, 10%-15% of propylene glycol, 20%-30% of an amorphous sorbitol solution, 1%-1.5% of vitamin C, 0.1%-1% of essence, 0.01%-0.025% of sucralose, a proper amount of a pH regulator and the balance of purified water; the traditional cognition that cats do not have sweetness perception, so that sweeteners are invalid is broken through, the bitterness of itraconazole and the acerbity of a solution are remarkably covered through compounding of specific components, the adverse reaction rate after the cats take the itraconazole is reduced, and the medication compliance is improved to 90% or above; components with dual functions are introduced, so that the flavoring is assisted, the hydrolysis and oxidative degradation of itraconazole can be inhibited, the solution is ensured to keep high quality under the conditions of high temperature and accelerated storage, and the validity period is prolonged.