121 results about "Artemether" patented technology

The present invention relates to use alpha -arteether as a antibacterial agent, preferably for gyr mutant bacteria which are resistant to quinolone drugs and can be used as therapeutic agents for treating drug resistant bacterial infections, and also as a antifungal agent.

An artemether microemulsion as novel antimalaria contains artemether, arteether or artesunate, emulsifier, emulsifying aid and plant oil. It can be applied by intravenous injection, oral taking, percutaneous absorption, and spray. Its preparing process is also disclosed.

The invention discloses stereospecific synthesis of beta-artemether by using artemisinin as a raw material through a one-pot method, which comprises the following steps of: in a system of alkaline solution of dichloromethane, taking sodium borohydride as a reducing agent and aluminium tert-butoxide as a catalyst, and reducing to obtain dihydroartemisinin; and separating out a water phase, adding methanol, sodium acid sulfate, aluminum perchlorate nonahydrate, nickelousperchlorate and the like serving as catalysts for methyl etherification, and reacting at room temperature for 2 hours to obtain the beta-artemether, wherein the maximum yield rate of the beta-artemether is 85 percent and the maximum total yield rate of artemether is 93.5 percent. The method has the characteristics of low cost, high yield, short time and simple and safe operation, and is completely suitable for industrial production.

A composite medicine for treating the umatoid arthritis and autoimmune disease contains the sweet worm wood herb's extract (dihydroarteannuin, artesumate, artemether, etc).

The present invention relates to an improved method for the preparation of Artemether. Artemether prepared from the process is useful for the treatment of uncomplicated, severe complicated and multi drug resistant malaria.

The present invention relates to a synergistic formulation comprising pharmaceutically effective amount of alpha / beta arteether and a neutralized refined vegetable oil suitable for administration by rectal route, method for the treatment of cerebral and comatose malaria and process for the preparation of the said formulation.

The invention discloses a medicinal composition for resisting non-small cell lung cancer. The active components of the medicinal composition comprise an artemisinin derivative and EGFR-TKI (epidermal growth factor receptor-tyrosine kinase inhibitor), wherein the artemisinin derivative is selected from one of dihydroartemisinin, artesunate, artemether and arteether; and the EGFR-TKI is selected from one of gefitinib, erlotinib, afatinib and osimertinib. The invention also discloses application of the medicinal composition to preparation of medicines for treating and resisting the non-small cell lung cancer. When the medicinal composition provided by the invention is used for treating the non-small cell lung cancer, the medicinal effect which is more excellent than that of the singly used EGFR-TKI can be achieved, the sensitizing effect is achieved, the problem of partial medicine resistance of the non-small cell lung cancer EGFR-TKI is solved, and a scientific basis is provided for the development of new medicines.

The present invention describes a method of treating individuals suffering from microbial infections, including a parasitic disease such as malaria, by using an improved Artemisinin Combination Therapy, known as Tri-ACT. The improved ACT therapy includes administering a combination of three drugs. In one embodiment of the present invention, the method includes administering to an individual a first composition comprising a therapeutically effective amount of an artemether spray sublingually. The individual is then administered a second composition, a therapeutically effective amount of artesunate. A third composition, an effective amount of berberine, or its pharmaceutically acceptable derivatives or salts is administered to the individual.

A method for treating cancer in a mammal includes administering to the mammal in need thereof a therapeutically effective amount of artemisinin (ART) or its derivative, such as dihydroartemisinin (DHA), artemether (ARM), or artesunate (ARS) alone or in combination with a chemotherapeutic agent, such as gemcitabine and carboplatin. A method for inhibiting tumor cell proliferation includes contacting a tumor cell with ART or its derivative, such as DHA, ARM, and ARS, in an amount effective to inhibit tumor cell proliferation or in combination with a chemotherapeutic agent, such as gemcitabine and carboplatin.

The present invention describes a method of treating individuals suffering from microbial infections, including a viral infection such as Dengue Fever, using an improved Artemisinin Combination Therapy (ACT), known as Tri-ACT. The improved ACT therapy includes administering a combination of three drugs. In one embodiment of the present invention, the method includes administering to an individual a first composition comprising a therapeutically effective amount of an artemether spray sublingually. The individual is then administered a second composition, a therapeutically effective amount of artesunate. A third composition, an effective amount of berberine, or its pharmaceutically acceptable derivatives or salts is then administered to the individual.

A self-emulsifying compound artemether in the form of capsule able to be automatically emulsified in the body fluid of stomach and intestine is proportionally prepared from artemether, benflumetol, oil, non-ionic surfactant and assistant.

The invention discloses an artemether nanoliposome, and a preparation method and an application thereof. The artemether nanoliposome is prepared from the following raw materials in parts by weight: 1 part of artemether, 2 parts of cholesterol and 8-10 parts of egg yolk lecithin. The preparation method comprises a film dispersion-sonication-film filtering method and an ethanol injection-sonication method. The artemether nanoliposome is applied to the preparation of artemether targeting preparation drugs. The encapsulation rate of the artemether nanoliposome is 61.33-63.86%, the average particle size is 161.65-162.73nm, and the poly dispersition index (PDI) is 0.2678-0.4463. The artemether nanoliposome has good stability when being stored at 4 DEG C.

The present invention relates to an artemether cataplasma and the application. The cataplasma is prepared by artemether and proper excipients. The artemether cataplasma of the present invention is composed of three parts of a back lining layer, a paste body containing drug and a cover lining layer. The major part is the paste body containing drug which is prepared by artemether, adhesives, fillers, transdermal enhancers, moisturizing agents and other excipients according to a certain mixing ratio, each paste contain 20mg to 300mg of artemether. The cataplasma has the anti-fever effect and is characterized by fast acting, good moisture retention performance, good air permeability and comfortable usage, the product of the present invention has easy usage, small irritation on the skin and high compliance of the patients.

The invention discloses an application of artemisinin and derivatives thereof in preparation of medicaments for treating hepatitis C viruses (HCV). The medicaments which almost do not have toxic concentration are used for anti-virus test; and by detecting the influence of the artemisinin and the derivatives thereof such as dicyanogen artemisinin, artemether and artesunate on HCV replication, the artemisinin and the derivatives thereof serving as small molecular compounds have remarkable viral activity resistance and are dose-dependent. The artemisinin and the derivatives thereof which have already been used for clinical antimalarials have low toxic or side effect on a human body. The artemisinin and the derivatives thereof which almost do not have toxicity can inhibit about 90 percent of HCV replication, and are efficient and low-toxic anti-HCV compounds. The compounds have a broad prospect for developing anti-HCV medicaments.

An application of arteannuin and its derivatives (dihydroarteannuin, artemether, arteether and artesunate) in preparing the medicines for preventing and treating the sepsis caused by CpG-ODN and bacteria is disclosed.

The present invention describes a method of treating individuals suffering from microbial infections, including a parasitic disease such as malaria, by using an improved Artemisinin Combination Therapy (ACT), known as ActRx Tri-ACT Plus. The improved ACT therapy includes administering a combination of four drugs. In one embodiment of the present invention, the method includes administering to an individual a first composition comprising a therapeutically effective amount of an artemether spray sublingually. The individual is then administered a second composition, a therapeutically effective amount of artesunate. A third composition, an effective amount of berberine, or its pharmaceutically acceptable derivatives or salts is administered to the individual. A fourth composition, an effective amount of primaquine, or its pharmaceutically acceptable derivatives or salts is administered to the individual.

The invention relates to the preparation of a chemical medicine preparation, which is a compound artemether methyl ether droping pill used for curing malaria. The present invention has the advantages that: 1. Serving as main ingredients, antimalarial lumefantrine and artemether are sufficiently dispersed by water-soluble auxiliary-ingredient polyethylene glycol or poloxamer, thus being favorable for absorbing the main ingredients. 2. The dropping pill preparation can be taken under tongue and also can be swallowed with very short disintegration (dissolve) time limit. And the invitro dissolve quantities are greatly improved and the peak value of the blood concentration can be reached rapidly, thus being beneficial to the improvement of the curative effect; 3. The main ingredients and the auxiliary ingredients are equably mixed at the temperature of 80 to 90 DEG C and insulated for some time, and then are dropped into methylsilicone oil or liquid paraffin at the temperature ranging from 5 to10 DEG C; 4. The method is simple in production process and short in production cycle. The cost can be decreased; 5. As the medicine is left in stomach for a short time or maybe the first-pass effect of the stomach can be avoided, so the generation of drug resistance and other side effects decreases.

The invention discloses a method for preparing artemether from artemether synthetic mother liquor. The method includes: using organic solvent to dissolve solid obtained by concentrating and drying artemether synthetic mother liquor, sampling on a macroporous resin column, using acetone with the volume concentration of 20-70% for eluting, performing thin layer chromatographic detection, and fractionally collecting eluant containing alpha-artemether and eluant containing beta-artemether; and respectively recovering solvents in the eluant containing alpha-artemether and the eluant containing beta-artemether, filtering to obtain crude alpha-artemether and crude beta-artemether, using ethanol to dissolve the crude alpha-artemether and the crude beta-artemether, and adding water for crystallization to obtain alpha-artemether and beta-artemether. Compared with the prior art, the method has the advantages that the alpha-artemether and the beta-artemether are successively separated from the artemether synthetic mother liquor, filler for chromatography is cheap and simple in regeneration, and elution solvent is simple and easy to recovery; and the whole process is simple and easy to control, the production cost is low, and industrial production is easier to implement.

The invention provides application of artemether as an algae inhibiting agent. Artemisinin simple ether derivatives have a good inhibition effect on copper aluminum microcystis, scenedesmus obliqnus and the like. The artemisinin simple ether derivatives can be prepared into missible oil, clathrate, slow release microcapsules and the like as algae inhibiting agents applied in nature water bodies like ponds, reservoirs and lakes for inhibiting algae booms.

The invention relates to an application of an artemisinin compound in treatment of coronavirus infection. Specifically, the invention provides application of the compound, and a stereoisomer, a pharmaceutically acceptable salt, a solvate or a hydrate thereof in preparation of medicines. The medicines are used for treating diseases or infection caused by coronavirus (preferably SARS-CoV-2), and thecompound is selected from one or more of artemisinin, arteether, artemether, artemisinin, dihydroartemisinin, artesunate, artemisinin B and arteannuic acid.

The invention belongs to the field of bioactive substances (comprising drugs) and healthy substances, and researches and development of products of the bioactive substances and the healthy substances, relates to a bioactive substance (comprising a drug) and healthy substance, and especially relates to a bioactive substance (comprising a drug) with mite killing and dispelling effects, and an application of the bioactive substance (comprising a drug) with mite killing and dispelling effects. All effective components are separated, extracted and purified from Artemisia carvifolia and sweet wormwood herb through adopting a solvent extraction method, chromatography, a crystallization method, an extraction method and other appropriate chemical methods, and artemisinin, derivatives and artemisinin related substances (dihydroartemisinin, artesunate, artemether, arteether, artemisinin C12 derivatives, artemisinin C4 derivatives, steroid artemisinin, ring-opened artemisinin and artemisinin structure simplifiers) are pharmacodynamically verified in monomer compound or composition forms in order to obtain the bioactive substance and healthy substance with mite killing and dispelling effects. The bioactive substance and healthy substance with mite killing and dispelling effects can be applied to drugs, health products, healthy products, personnel nursing products (infant nursing products), household cleaning products, pet cleaning products, agriculture and gardening products and other commercial products.

The invention relates to medicated bath granules of artemisinin or derivatives of the artemisinin and application of the medicated bath granules. The medicated bath granules take the artemisinin or the derivatives of the artemisinin as main active pharmaceutical ingredients, and comprise the following components in weight proportion: 0.1 to 20g of artemisinin or the derivatives of the artemisinin, 1 to 40g of sodium bicarbonate and 1 to 40g of sodium sulfate; the derivatives of the artemisinin are selected from dihydroartemisinin, artesunate and artemether.

The invention relates to a pharmaceutical composition for treating brain glioma and belongs to the field of medicines. The pharmaceutical composition which takes artemether and temozolomide as active components comprises the active components in parts by weight: 40-70 parts of artemether and 0.5-4.0 parts of temozolomide, further preferably 65-67 parts of artemether and 0.5-2.0 parts of temozolomide. The pharmaceutical composition provided by the invention has a remarkable inhibiting effect to the C6 cell line of brain glioma of a SD rat cultured in vitro. The effect of using artemether and temozolomide in a combined or independent manner is in time and concentration dependency, and the artemether and temozolomide which are combined in use are in synergic relationship. When the artemether and temozolomide which are combined in use, IC50 value is lower than that when the artemether and temozolomide are independently used. Animal experiments sufficiently prove that when the artemether and temozolomide are combined in use, a good antitumor effect is achieved, and is stronger than that when the artemether and temozolomide are independently used; pathological section results show that when the artemether and temozolomide are combined in use, the quantity of microvessels of brain glioma is remarkably reduced, and the anti-angiogenic effect is stronger than that when the artemether and temozolomide are independently used. The pharmaceutical composition has the advantages of low price, remarkable curative effect and low toxic and side effect.

The invention relates to an application of an artemisinin derivative to preparation of a medicine for preventing and treating 2-type diabetes mellitus and complications of the 2-type diabetes mellitusand a medicine composition containing the artemisinin derivative. According to the application, experiments confirm that the artemisinin derivative such as artemether can increase the respiration quotient of the 2-type diabetes mellitus, oxidation of metabolic substrate glucose is facilitated, blood glucose of the 2-type diabetes mellitus is reduced, polydipsia and polyuria symptoms are improved,and urinary albumin excretion is decreased. The artemisinin derivative has an obvious protection effect on the 2-type diabetes mellitus and the complications thereof.

The invention relates to a medicine for curing and radically curing malaria. The weight parts of the components are: 1 to 5 parts of arteannuin ramification and 5 to 100 parts of large ring lactone antibiotic. The arteannuin ramification can be any artesunate medicine, such as arteannuin, artesunate, artemether or dihydro-arteannuin. The large ring lactone antibiotic can be first, second or third generation large ring lactone antibiotic, such as erythrocin, azithromycin, telithromycin and kui erythrocin. The medicine of the invention is low in poison, safe, rapid in effect, high sufficient and can radically cure malaria, which solves the problem that the after-combustion rate and the recurerence rate of the arteannuin ramification medicine is high after curing malaria; furthermore, the invention is high in medicine safety and has the functions of preventing, curing and blocking spreading of malaria, which is not only suitable for the common malaria infected area, but also more suitable for the infected area with multiple drug fastness malaria, thereby being very safe and effective to the children and pregnant women patients.

The invention discloses application of artemether to prevention and treatment of Alzheimer disease. The artemether is a safe and effective compound in anti-malaria treatment and activates an AMPK signal channel in the brain of an Alzheimer disease transgenic model mouse, the learning and memory ability of the Alzheimer disease transgenic model mouse is improved, apoptosis of nerve cells in the brain is reduced, the function of a choline acetyl transferase is improved, the activity of spongiocyte is inhibited, deposition of amyloid plaques, tangling of nerve fiber and the loss of nerve cells are reduced, and the experimental basis is provided for the clinical study for treating Alzheimer disease.