192 results about "Itraconazole" patented technology

The present invention relates to compositions containing itraconazole with a greatly increased bioavailability and their preparation methods. More specifically, the present invention relates to compositions containing itraconazole which is a sparingly-soluble drug, fatty acid or fatty alcohol and surfactant and their preparation methods. Compositions according to the present invention act as Self-MicroEmulsifying Drug Delivery System(SMEDDS) wherein itraconazole which is a sparingly-soluble drug is dissolved and dispersed to form a mocoidal phase, and the mocoidal phase is dissolved in water to form microemulsion. And because of increased dissolution property and increased bioavailability, compositions according to the present invention show equal efficacy using less amount than commercial pharmaceutical preparations such as sporanox capsule and are cheaper rather than the commercial pharmaceutical preparations such as sporanox capsule.

The invention disclsoes an optically pure itraconazole key intermediate and synthetic method thereof, and a method for synthesizing the optically pure itraconazole from the intermediate. The method of the invention uses 1-(2,4-dichlorobenzene)-2-(1-methylene-1,2,4-triazole)-1-ketone for preparing the optically pure itraconazole key intermediate, and the optically pure itraconazole key intermediate is used for the preparation of optically pure itraconazole. The method uses easily available raw materials, not only reduces the production cost, but also obtains the product with high purity; through the control of the optical purity of the key intermediate compound VII, the optical purity of the target product itraconazole can be effectively controlled; therefore, the invention has with industrial value.

The invention provides a novel itraconazole isomer composition and a method for increasing the therapeutic index of the novel itraconazole isomer composition. The itraconazole isomer composition can be used for improving the selectivity to fungi and endothelial cells and also lowering the toxicity of liver cells. The itraconazole isomer composition provided by the invention is a drug with potential for treating fungi and angiogenesis related diseases, and meanwhile, the side effects caused by taking itraconazole are avoided.

A softcapsule of itracnoazole is prepared through dissolving gelatin in water, adding glycerineand antiseptic, vacuum degrassing, adding the suspending aid to vegetable oil, mixing with itraconazole, adding antioxidizing agent, and die pressing.

The present invention relates to agent containing itraconazole with both improved bioavailability, due to higher water-solubility and impressively reduced difference of pH-dependent solubility, and narrow intra- and inter-individual variation of its absorption- and a manufacturing method thereof. Agent containing itraconazole of the present invention consists of itraconazole, water-soluble macromolecule of 10-100 % w/w to itracotazole, solubilizing agent of 0.1-100 % w/w to itraconazole and pharmaceutically allowed additives. Agent containing itraconazole of the present invention minimizes absorption variation by dozing time after food intake as well as is available for adults with hypoacidity, AIDS patients and normal people. In addition, the manufacturing method introduces the elementary process, the spray drying, thereby control of physical properties of particles containing drug is easier and economy/production is improved.

The invention discloses a freeze-drying combination of itraconazole nanosuspension for injection and preparation and using methods of the nanosuspension. The invention selects serum albumin of the human as main adjunct; itraconazole nano-sized granulation can be successfully realized by adopting the drying technology and freeze drying technology in combined liquid of high pressure homogenization nanometer emulsification technology; and the invention can be filtered to sterilize and can be stored in the form of freeze-dried powder. The itraconazole nanosuspension is prepared in acceptable waterborne diluent in pharmacy, and then the average particle size of the itraconazole nanosuspension is less than 0.3 microns after reconstruction, so the itraconazole nanosuspension can be made into nanosuspension for intravenous injection. The nanosuspension is composed of the following components : the ratio between the itraconazole and albumin is 1 : 200 to 10 : 1; and the nanosuspension also comprises surfactant, stent agent, osmo-regulator and other injection additives, etc. The nanosuspension has the advantages of drug loading, safety, low toxicity, high stability and good warming promotion without hemolysis or stimulation on vein vascular. And the preparation method is simple and easy, and thus the product forming can be realized easily.

The invention discloses an itraconazole inhalation powder aerosol and its preparation method. The inhalation powder aerosol is prepared by using itraconazole and 20-80mass% of a carrier, and the carrier is at least one of lactose, mannitol, inulin and amino acids. The method comprises the following steps: mixing itraconazole with the carrier, adding the obtained mixture into a double screw hot melt extruder, setting the extrusion temperature at 150-170DEG C, starting screws after the preset temperature is reached, and carrying out strip extrusion under a screw rotating speed of 150-200r/min, cooling obtained strips in a dryer to room temperature, crushing by using a micro pulverization machine, and micronizing by using an airflow crusher to obtain the above powder. The inhalation powder aerosol has the advantages of good physical stability, good powder fluidity, high deposition amount at effective positions, high dissolution rate, fast dissolution speed, small drug dose, and low incidence rate of toxic side effects; and the method has the advantages of simple technology, no organic solvents, antiseptics or other impurities in the process, good reappearance and easy industrial production.

The present invention provides a method of preparing particles with polymorph and size control of a pharmaceutical compound, the method including the steps of: (1) providing pharmaceutical compound in a first phase; (2) seeding the compound; (3) causing a phase change in the pharmaceutical compound to a second phase of a desired polymorphic form; and (4) wherein the mean particle size of the particles is less than 7 mum. The present invention further provides a polymorphic form of itraconazole.

The invention provides a micromolecule compound inhibitor for enterovirus and an application of the inhibitor. Specifically, the invention provides an application of itraconazole, an itraconazole analogue, or pharmaceutically acceptable salt of itraconazole or the itraconazole analogue to preparation of a reagent, which is used for inhibiting growth or reproduction of enterovirus and/or for inhibiting synthesis of enterovirus RNA. The invention also provides an inhibitor and medicine composition containing itraconazole or the itraconazole analogue for enterovirus, and provides a method for in-vitro non-therapeutically inhibiting growth of enterovirus or killing enterovirus. Experimental results show that itraconazole and the itraconazole analogue has an excellent inhibition effect on multiple kinds of enterovirus.

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 relates to itraconazole injection for dogs and a preparation method thereof and belongs to an animal medicament. The injection consists of itraconazole, hydroxypropyl-beta-cyclodextrin, propylene glycol, 12 mol.L<-1> of concentrated hydrochloric acid and double distilled water. The preparation method comprises the following steps of: preparing itraconazole inclusion liquid by using hydroxypropyl-beta-cyclodextrin inclusion technology; adding sodium hydroxide solution into the inclusion liquid; adjusting the pH value; filtering the mixture; and circulating vapor for sterilization to obtain the itraconazole injection for the dogs. The injection finished product prepared by the method is yellow and transparent liquid and has the characteristics of high stability, sustained-release property and long-term effectiveness; the inclusion rate of the itraconazole can reach 80 percent; pharmacokinetic characteristic and pharmacodynamics are superior to those of the conventional formulations.

The invention relates to a method for solving a problem of bacterial variation degradation of liquid-strain nutrition liquid, in particular to a method for mushroom-liquid liquid strains. The method comprises a step of using an efficient mutagenic agent, wherein the efficient mutagenic agent comprises itraconazole and rapamycin, and the weight percentage of the itraconazole and the rapamycin in the nutrition liquid is respectively 0.5-5 percent and 1-7 percent. The method also comprises a step of low-temperature preservation strain, a step of adjusting culture conditions and a step of separation and purification. The method taking the itraconazole and the rapamycin as the efficient mutagenic agent as the core method, the mutagenesis is mild, and meanwhile, the strain preservation condition, the nutritional condition of the nutrition liquid, the passage number condition, the purification condition and the like are optimized. Experiments prove that the problem of bacterial variation degradation of various kinds of mushroom liquid-strain nutrition liquid can be basically solved, the method has an obvious economic value, and high-producing strain is obtained.