80 results about "Disulfiram" patented technology

The invention relates to a medicament in combination of a disulfiram preparation and copper, having an anti-tumor function. The combination of disulfiram and copper in the invention plays a role in treating tumor cells, belonging to the technical field of medicaments. The anti-tumor combination medicament comprises disulfiram or derivatives thereof and copper and any one or more optional medicinal vectors, which are used simultaneously, respectively or sequentially; the dosage of the disulfiram in each single medicament ranges from 2 to 200 mg / kg or equals to the equivalent dosage of disulfiram derivatives; and the copper comprises micro copper ions contained in the human body and other absorbable forms of copper irons, wherein the dosage of the copper in each single medicament is 0.1-5 mg per day. The combination medicament disclosed by the invention has remarkable effect in treating tumors and reduced toxic and side effects.

A novel pharmaceutical composition is provided for the control of stimulant effects, in particular treatment of cocaine addiction, or further to treatment of both cocaine and alcohol dependency, including simultaneous therapeutic dose application or a single dose of a combined therapeutically effective composition of disulfiram and selegiline compounds or pharmaceutically acceptable non-toxic salt thereof.

A disulfiram formulation comprising disulfiram or a derivative thereof together with a component that increases the in vivo half life of the disulfiram or the derivative thereof, and methods and uses thereof. In particular, the disulfiram formulation is used with or without a separate copper formulation for the treatment of cancer.

There is described a composition comprising a therapeutically active imidazole, or a derivative thereof, and disulfiram, or a derivative thereof, for treating an infection contributed to or caused by multi-drug resistant bacterial species.

Methods, compositions of matter, and kits for treatment of breast cancer, and in particular for inflammatory breast cancer, in a patient are disclosed. The methods can include administering a redox modulating agent to the patient. The redox modulating agent can be disulfiram.

The present invention provides an implantable composition which contains disulfiram, an anti-inflammatory agent, and optionally a pharmaceutically acceptable carrier. Methods of making the implants, and methods of using the implants to treat alcoholism and opioid dependency are also disclosed.

Provided are a synthesis and preparation method of disulfiram entrapped polylactic acid microspheres having pH responsiveness and application thereof. A pH sensitive polylactic acid material containing acetal bonds and disulfiram are prepared as model drugs by preparing lactide, polylactic acid macromolecules containing acetal bonds serve as a carrier material, the polylactic acid microspheres having pH responsiveness can be obtained by preparing polylactic acid drug carrying microspheres through a W1 / O / W2 double-emulsification solvent evaporation method, the synthesized and prepared disulfiram entrapped polylactic acid microspheres having pH responsiveness are applied to inhibition of tumor activity, biodegradable macromolecular drug carrying microspheres can be prepared by injecting thepolylactic acid material containing acetal bonds and coat disulfiram and Cu<2+>, the specificity is improved, and the success rate of tumor treatment is greatly improved.

The invention relates to an application of disulfiram in preparing pharmaceuticals for relieving hepatic injury and further relates to an application of the disulfiram in preparing anti-liver fibrosis, anti-liver cirrhosis or liver fat reducing pharmaceuticals. The invention also discloses a heptatic stellate cell external proliferation inhabitation function of the disulfiram. A specific brand-new pharmaceutical is provided for treating anti-liver fibrosis and anti-liver cirrhosis.

The invention relates to mesoporous silica nanoparticles having a disulfiram monomer and a preparation method and application thereof. The method includes (1) preparing mesoporous silica nanoparticles; and (2) by utilizing disulfide bonds of disulfiram, preparing mesoporous silica nanoparticles having a disulfide-bond-containing disulfiram monomer (diethyldithiocarbamate), with the average particle size of the nanoparticles being 50-300 nm. The prepared nanoparticles having the disulfiram monomer are uniform in distribution and good in dispersibility, facilitate improvement on medicine targeting properties, increase medicine bioavailability, make drug preparation costs low, greatly reduce the treatment cost of patients and have potential market value and far-reaching social significance.

The invention relates to an anti-cancer transdermic absorption preparation. The preparation formula is prepared from the following forming components in parts by weight: 0.1 to 10 parts of a primary medicine, 0.1 to 23 parts of a substrate, 0.1 to 15 parts of a humectants, 0.5 to 15 parts of a thickening agent, 0.1 to 10 parts of an emulsifier, 0.1 to 10 parts of a transdermal enhancer, 1 to 10 parts of an inclusion agent, 0 to 2 parts of a preservative, and 45 to 85 parts of a wetting agent, wherein the primary medicine is one or a mixture of two or more components of DDC (diethyldithiocarbamic acid)-Zn, DDC-Cu and DS (disulfiram). The anti-cancer transdermic absorption preparation has the advantages of stable physical property and chemical property, high absorption performance, high medicine controllability, easiness in use and favorability for acceptance by patients, and can be widely applied to anti-cancer treatment of in-patients and out-patients suffering from malignant tumors.

The invention relates to an antitumor drug combination and a preparation and application thereof. The drug combination comprises a tumor angiogenesis inhibitor compound and disulfiram. Weight ratio ofthe angiogenesis inhibitor compound to disulfiram is (1-15): (1-20). By combination of the tumor angiogenesis inhibitor compound and disulfiram for medication, the antitumor drug combination has thefunction of remarkably raising anticancer effect in comparison with any single ingredient. In addition, tumor inhibiting rate is raised by 20% and above. The data is a great progress in the research on cancer treatment. In the inventor's first research, it is found that the combination of the angiogenesis inhibitor and disulfiram at a specific ratio has a remarkable synergistic effect and the drugcombination has a good clinical application prospect.

The invention relates to application of disulfiram in preparing drugs for preventing and treating diseases related to NLRP3 inflammasome. During research, phenomena are found that the disulfiram can effectively inhibit activation of the NLRP3 inflammasome and inhibit maturation and secretion of an inflammatory activation signal molecule Caspase-1P20 and an inflammatory cytokine IL-1[beta], accordingly has good prevention and treatment effects on the diseases related to the NLRP3 inflammasome, and especially has significant prevention and treatment effects on peritonitis and gouty arthritis.

The invention belongs to the technical field of biological pharmacy and particularly relates to preparation of a nano-drug delivery system loaded with classical ''abstinence drug'' disulfiram and photosensitizer indocyanine green based on a low-generation PAMAM (polyamide-amine) dendrimer and application of the nano-drug delivery system in the anti-tumor field. According to the invention, disulfiram DSF and indocyanine ICG are entrapped into low-generation dendrimer PAMAM-G0 by virtue of a solvent cross-linking method, so as to obtain the nano-drug delivery system. The prepared nano-drug delivery system is gathered at a tumor site through an EPR effect and can simultaneously play roles of chemotherapy and photodynamics therapy, so that the tissue toxicity of chemotherapeutic drugs and thephototoxicity of the photodynamics therapy are reduced, and a new research direction is provided for the anticancer treatment of disulfiram.

The invention provides a polyester material supported disulfiram nanoparticle, which is prepared from the following components: 1-20 parts by weight of disulfiram or derivatives thereof, 20-95 parts by weight of a polyethylene glycol-polyester segmented copolymer and 5-80 parts by weight of polycaprolactone. According to the disulfiram nanoparticle designed by the invention, a hydrophobic core, provided by polycaprolactone, is stably encapsulated inside the disulfiram, and the polyethylene glycol-polyester segmented copolymer is modified on the surface, so as to guarantee the solubility and the long-circulation capacity of the disulfiram nanoparticle. The application also provides application of the disulfiram nanoparticle on treating tumors.

There is provided a method for inhibiting ATF / CREB and cancer cell growth using disulfiram, administered in combination with heavy metals. It was found that disulfiram disrupts transcription factor DNA binding by forming mixed disulfides with thiols within the DNA-binding region, and that this process is facilitated by metal ions. Disulfiram administered to melanoma cells in combination with copper (II) or zinc(II) decreased expression of cyclin A, reduced proliferation in vitro, and inhibited growth of melanoma cells. The combination of oral zinc gluconate and disulfiram at currently approved doses for alcoholism stabilized tumor growth in two of three patients with Stage IV metastatic melanoma, with 12 and 17 month survivals, respectively, to date, and produced a >50% reduction in hepatic metastases in one individual.

The present invention provides a method for treating pleuroperitoneal membrane cancers, and comprises: delivering disulfiram or a derivative thereof that is effective in amount in the treatment, into the pleura and / or the peritoneum of a test person that needs to be treated. The present invention also provides a pharmaceutical component comprising the disulfiram or the derivative thereof, and a reagent kit.

The invention relates to a disulfiram implant and a preparation method thereof. The disulfiram medicinal composition can be slowly and stably released in a human body, and the disulfiram implant comprises 60-80 parts of disulfiram and 20-40 parts of a biodegradable high polymer material. The disulfiram implant can be injected and implanted into the human body, and patients suffering from alcohol dependence can be treated so as to avoid repeated drinking. The therapeutic concentration can be maintained for a long time after administration, a first-pass effect is avoided, the bioavailability is improved, the compliance of the patients is improved, and the clinical requirements of the patients can be met.

The invention discloses an anti-aging flame-retardant plastic and a preparation method thereof. The anti-aging flame-retardant plastic is prepared from the following raw materials in parts by weight: 110-130 parts of HDPE (high-density polyethylene), 40-55 parts of PA66, 30-40 parts of ABS (acrylonitrile-butadiene-styrene), 10-15 parts of coupling agent, 5-8 parts of disulfiram, 10-15 parts of toughener, 5-10 parts of antioxidant, 10-20 parts of stabilizer, 10-20 parts of nano antimony trioxide, 10-15 parts of ultraviolet absorbent, 10-15 parts of auxiliary antioxidant, 5-10 parts of epoxy octyl stearate and 1-5 parts of zinc borate. The preparation method comprises the following steps: uniformly mixing the components, adding the mixture into a double screw extruder, and granulating by melting and plastifying, and carrying out injection molding on the granules. The plastic disclosed by the invention has the characteristics of high notch impact strength, high bending strength, high hardness, favorable flame retardancy, favorable aging resistance and the like; and the method disclosed by the invention is simple in technique and convenient for large-scale production.

The invention discloses a drug for treating and / or preventing tumor. The drug comprises active components, namely a component A and a component B, wherein the component A is ascorbic acid soluble salt or ascorbic acid, and the component B is disulfiram. The compound drug which comprises sodium ascorbate and the disulfiram can effectively inhibit the growth of in-vivo in-vitro cancer cells, achieves the synergistic effect, achieves the selective killing effect on tumor cells and can be used as a low-toxicity effective compound drug for treating and / or preventing the tumor.

The invention discloses a disulfiram nano-particle, and a preparation method and application thereof. The nano-particle consists of disulfiram, nanometer metallic oxides and silk fibroins, and belongsto the technical field of nanometer drug carriers. The invention also discloses a preparation method for the nano-particle. The preparation method comprises the following steps of: firstly, slowly dripping disulfiram solutions into a nanometer metallic oxide dispersion liquid; continuously stirring, then, adding a silk fibroin solution to be continuously stirred, and finally, adding three times of acetonitrile for crosslinking solidification; and carrying out rotary evaporation to remove organic solvents, and carrying out freeze-drying to obtain the disulfiram nano-particle. The disulfiram nano-particle prepared by the preparation method is simple in preparation, is high in drug carrying amounts, is high in stability, can effectively inhibit the proliferation of tumor cells under a low dosage, and has a wide clinic application prospect, and the anti-tumor effect of the disulfiram nano-particle is obviously superior to a disulfiram drug.

The invention discloses a disulfiram-based glucan nanometer prodrug, and a preparation method and applications thereof. The disulfiram-based glucan nanometer prodrug is a disulfiram-based glucan nanometer prodrug with oxidation-reduction response characteristics, glucan is selected as a skeleton, and a drug is connected with a polymer skeleton through a disulfide bond. The invention provides a polymer drug delivery system with oxidation-reduction response. According to the nanometer prodrug, the disulfide bond can be reduced into sulfydryl by reduced glutathione in cancer cells, and a responsemechanism is provided, so that the structure of a carrier is changed, and the drug is quickly released. The nanometer prodrug shows good biological safety and a good cancer cell killing effect, and an intelligent drug delivery system is provided for tumor treatment.

Provided herein are pharmaceutical products comprising therapeutically effective combinations of ALDH inhibitors (e.g., disulfiram and / or derivatives thereof) and targeted therapeutics, as well as methods of using said combinations for the treatment of cancer.

The invention discloses an application of disulfiram to preparation of a drug for treating systemic lupus erythematosus. For the systemic lupus erythematosus, a lupus mouse model induced by pristane is taken as an experiment object. According to the application, the disulfiram can effectively improve the disease condition of a lupus mouse, and specific performances are as follows: (1) the urine protein level of the lupus mouse after being treated with the disulfiram is significantly reduced; (2) the disulfiram can reduce the level of a peripheral blood anti-dsDNA and the level of an inflammatory factor IL-1beta of the lupus mouse; and (3) after intervention is carried out by using the disulfiram, pathological damage to kidney of the lupus mouse is significantly reduced, and immune complexIgG and C3 deposits are also reduced.

The invention relates to the technical field of medicines, and especially relates to a preparation method and application of a disulfiram-loaded nano-emulsion in-situ gel. The preparation method comprises the following steps: (1) mixing an oil phase, an emulsifier and a co-emulsifier, adding polyethylene glycol-modified phospholipid, and uniformly mixing to obtain a first mixed solution; (2) adding disulfiram into the first mixed solution, and obtaining a second mixed solution after the disulfiram is completely dissolved; and (3) adding ultrapure water containing an in-situ gel agent into thenano-emulsion, and carrying out self-assembly to obtain the disulfiram-loaded nano-emulsion in-situ gel. According to the disulfiram-loaded nanoemulsion in-situ gel, the solubility of disulfiram is remarkably improved, an ideal slow release effect is achieved, the in-vivo stability of disulfiram is improved, high safety is achieved, and the characteristic of remarkable brain enrichment during nasal administration is achieved.

The invention discloses an auxiliary nutritive oral liquid for treating cancer and a preparation method thereof, wherein the oral liquid is mainly prepared from the following materials in parts by weight: 6-11 parts of disulfiram, 5-7 parts of pearl powder, 8-10 parts of bletilla striata, 20-25 parts of turnip sprouts, 10-15 parts of dendrobium officinale and 15-20 parts of wheat germ. According to the invention, by reasonable formula, the amount of disulfiram decomposed by gastric acid is reduced, the generation of cancer cell targeted substance is promoted, the amount of disulfiram initiatoris reduced, and the anti-cancer effect is optimized.

The invention belongs to the technical field of medicine, and specifically relates to mycobacterium tuberculosis resisting compounds, and applications thereof. The compounds comprise pyrrolidine dithiocarbamate (PDTC), diethyl dithiocarbamate (DETC) and disulfiram. The compounds have effective in vitro effects in inhibiting and killing mycobacterium tuberculosis. The compounds can be combined with first-line antituberculosis drugs pyrazinamide and rifampicin, and assist in improving the in vitro antibacterial activities of pyrazinamide, and pyrazinamide plus rifampicin. The compounds provided by the invention can effectively acts upon tuberculosis mycobacterium in growing phases and stationary phases. Mycobacterium tuberculosis resisting activities of the compounds can be presented. The compounds can be used in the treatment of drug-sensitive tuberculosis and multi-drug-resistant tuberculosis, and further can be applied in preparations of novel mycobacterium tuberculosis resisting medicines.

The invention belongs to the technical field of medicines, relates to disulfiram in-situ-forming gel eye drops as well as preparation and application thereof, in particular to in-situ-forming gel eyedrops which are treated based on a solid dispersion technology and prepared from disulfiram. The disulfiram in-situ-forming gel eye drops are prepared from a main drug, a solid dispersion matrix, an in-situ-forming gel matrix, a bacteriostatic agent, a pH value regulator, a gelation temperature regulator, an osmotic pressure regulator and injection water, wherein the main drug is the disulfiram; the solid dispersion matrix is one or more of HPMC, P407, P188 and PVP; the pH value regulator is borate and has the concentration of 0.001-0.05 percent; and the gel matrix is one or more of the P188 and the P407. The disulfiram in-situ-forming gel eye drops provided by the invention have the efficacy of preventing and treating cataract. According to the preparation, the solid dispersion technologyimproves the solubility and the permeability of indissolvable drugs, and an in-situ-forming gel technology prolongs the corneal retension time of the drugs. The eye drops improve the efficacy of thedisulfiram and have wide development prospect.

The invention belongs to the field of nano medicines and new materials, and discloses a disulfiram prodrug monomer, an amphiphilic block copolymer prodrug synthesized on the basis of the disulfiram prodrug monomer, and a preparation method and application of the amphiphilic block copolymer prodrug. The preparation method comprises the following steps: firstly synthesizing the disulfiram prodrug monomer, then copolymerizing a hydrophilic polyethylene glycol methyl acrylate monomer (PEGA) and a hydrophobic disulfiram prodrug monomer (DTCM) through a reversible addition fragmentation transfer (RAFT) method to obtain an amphiphilic block copolymer prodrug (PPEGA-PDTCM), and further constructing a self-assembled polymer vesicle. The prepared polymer vesicle can improve the solubility and stability of disulfiram, premature release of disulfiram in vivo is avoided, the limitation of clinical treatment of disulfiram is overcome, the polymer vesicle can load another medicine at the same time, and combined treatment of the two medicines is achieved. The polymer vesicle has better reduction response drug release property and has the activity of inhibiting the growth of tumor cells.

The invention belongs to the field of medicine, and particularly relates to an oral drug composition for treating ventricular remodeling after myocardial infarction. The oral drug composition for treating ventricular remodeling after myocardial infarction is prepared from pharmaceutically acceptable adjuvants in medical science and the following components in parts by weight: 53-97 parts of atorvastatin, 8-14 parts of disulfiram, 5-11 parts of neoquipenyl, and 3-7 parts of rolapitant. In the composition, rolapitant can inhibit the cardiovascular toxic effect of disulfiram and neoquipenyl, andcan eliminate the phenomenon that the efficacies of disulfiram and neoquipenyl counteract when being combined in use. The formula of atorvastatin, disulfiram, neoquipenyl and rolapitant has good effects and safety for resisting ventricular remodeling after myocardial infarction.