174 results about "Artesunate" patented technology

A pharmaceutical composition comprising a solid unit dosage form comprising: one or more of pharmaceutically active ingredients selected from valacyclovir, olanzapine, voriconazole, topotecan, artesunate, amodiaquine, guggulosterone, ramipril, telmisartan, tibolone, atorvastatin, simvastatin, amlodipine, ezetimibe, fenofibrate, tacrolimus, valgancyclovir, valsartan, clopidrogel, estradiol, trenbolone, efavirenz, metformin, pseudoephedrine, verapamil, felodipine, valproic acid/sodium valproate, mesalamine, hydrochlorothiazide, levosulpiride, nelfinavir, cefixime and cefpodoxime proxetil in combination with a water insoluble polymer and/or a water soluble polymer. Methods for making the pharmaceutical composition are also disclosed.

The invention discloses an artesunate and L-arginine composition for injection. The artesunate and L-arginine composition comprises the following components in parts by weight: 1,000 parts of artesunate as a raw material and 450-900 parts of L-arginine as an auxiliary material. According to the composition, the artesunate which is poor in solubility can be dissolved; the pH value can be adjusted to be neutral to slightly alkaline for injection; the solution is clear, transparent and colorless; the composition has good solubility and mobility, and can be sub-packaged into a practical powder preparation for injection; and more importantly, the stability of the composition is improved beyond thought. The invention also provides a preparation process of the artesunate and L-arginine composition for injection. The preparation method comprises the following steps: directly mixing the raw materials, namely artesunate and L-arginine; sub-packaging, or dissolving and degerming firstly and then preparing powder for injection by adopting a freeze-drying technology. The artesunate and L-arginine composition for injection disclosed by the invention is simple in preparation process and stable and reliable in quality.

The invention discloses an application of an artemisinin derivative in preparation of medicament for treating Crohn disease, and the artemisinin derivative is selected from artesunate or artemether or styrene monomer 905 (SM905). The artemisinin derivative can be used for achieving the purpose of treating the Crohn disease by inhibiting Th1/Th17 immune response and inhibiting nuclear factor-kB activation. Compared with the existing medicaments, the artemisinin derivative has less and light side effects, in one year of following visits for the treatment of rheumatoid arthritis, transient reticulocyte decline and hepatic dysfunction only occur in individual cases, and the health can be restored by liver protection treatment without medicament withdrawal. Therefore, the artemisinin derivative can be taken by patients for a long time, the treatment can be maintained, and the purpose of effective treatment can be achieved.

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.

The invention relates to a preparation method of new preparation of erythrocin, which is characterized in that an endothelin core of erythrocin is prepared, and then an isolating layer, a protective layer, a second isolating layer and an improved enteric-coating material layer are applied one by one. In this way, new preparation of the erythrocin which has certain feature of releasing (dissolving) in acid solution (hydrochloric acid solution 9 to 1000) can be formed. The technology of the new preparation can also be widely applied to drugs which, like erythrocin, when being taken orally by a patient, cause the patient to suffer the side effects of stimulation, sickness and the like after degradation in the stomach of the patient or contact with the stomach of the patient, and drugs which the patient needs to take orally to let the blood concentration to reach the peak value in a short time. Such drugs include macrolides of azithromycin, metronidazole of nitroimidazoles, tinidazole, acyclovir as an antiviral drug, ammonium chloride as a phlegm eliminating drug, bromhexine, chloroquine as an antimalarial, nitroquine, artemisinin, dihydroartemisinin, artesunate, primaquine, pyrimethamine, carbarsone and emetine amebicides and so on.

The present invention discloses a camptothecin and artesunate conjugate represented by a formula (I). The preparation method comprises the steps of dissolving camptothecin represented by a formula (II) and artesunate represented by a formula (III) in an organic solvent, carrying out a stirring reaction at a temperature of 15-50 DEG C under the effects of 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride and 4-dimethylaminopyridine, performing TLC tracking monitoring until the reaction is over, and post-treating the reaction solution to obtain the camptothecin and artesunate conjugate represented by the formula (I). The camptothecin and artesunate conjugate of the present invention can be used for preparing various anti-tumor drugs. The formulas (I), (II) and (III) are shown as follows.

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.

The invention relates to a chlorin and artesunate compound with photosensitive and sound-sensitive activity as well as a preparation method and an application of the compound and belongs to the technical field of chemical medicines. The chlorin and artesunate compound with photosensitive and sound-sensitive activity has different degrees of inhibition effects on human hepatoma cells Hep G2 in in-vitro anti-tumor activity evaluation. The photoactivity and ultrasonic activity are both higher than that of chlorin e6 and artesunate which are used as positive controls. The compound can be used for preparing a photosensitizer and a sound-sensitive agent in photodynamic therapy and sonodynamic therapy methods for tumor therapy.

The invention discloses an ethylene glycol bi-sulpho succinic acid bi(2-methyl amyl) artesunate and a production method thereof. The product is prepared by reacting maleic anhydride with 2-methyl-1-amyl alcohol to form a monoesterfication product, reacting the monoesterfication output with sodium sulfite to form a sulphonated product, and then reacting the sulphonated product with ethylene glycol. The product has good performance and is simple to synthesize.

The invention relates to a method for co-transforming hmgr and fps in the field of biotechnology to increase the content of artemisinin in artemisia annua. The present invention clones hmgr and fps genes from Artemisia annua, constructs a plant expression vector containing said DNA molecules, uses Agrobacterium tumefaciens to mediate, simultaneously introduces hmgr and fps genes into Artemisia annua and regenerates plants, and detects exogenous objects by PCR The integration of genes hmgr and fps was determined, and the content of artemisinin in Artemisia annua was determined by high performance liquid chromatography-evaporative light scattering detector, and the transgenic plants of Artemisia annua with increased artemisinin content were screened. The content of artemisinin in the transgenic Artemisia annua obtained by the present invention is significantly increased, up to 2.32 times that of the non-transformed control plants.

The invention discloses an Artesunate nanoemulsion drug that is an O/W (oil-in-water type) nanoemulsion system consisting of ethyl oleate, Tween-80, normal butanol, ultrapure water and Artesunate. The nanoemulsion drug effectively overcomes the first-pass effect of traditional tablets in liver, causes no sense of pain in injection and greatly improves the insecticidal and helminthic effect of original Artesunate. Meanwhile, the nanoemulsion system has high drug-loading rate, is stable when stored, has certain slow release function compared with merchant Artesunate injection, and further is convenient for administration, thus greatly improving the bioavailability. Besides, shown by acute toxicity tests and clinical drug effect tests on mice, the nanoemulsion has no obvious toxic or side effect and is a safe, reliable and high-efficiency nano level antiparasitic drug.

The invention relates to application of artesunate as a drug for treating systemic lupus erythematosus, adopting the artesunate with a molecular formula of C19H2808 for treating the systemic lupus erythematosus. The invention overcomes the defects that the prior common drug for treating SLE, such as cyclophosphamide, glucocorticoid, mycophenolate mofetil, hydroxychloroquine sulfate, leflunomide, azathioprine and the like has multiple side effects, is expensive, influences the life quality of a patient and even causes the patient to die because of some side effects, and the like. The invention has the advantages of cheap raw materials, easy availability, non or low toxicity, no pollution, mature production technology of a artesunate finished product, stable and reliable quality and little toxic side effects. Through comparison and study on a lupus mouse show that the efficacy of the artesunate is superior to a contrast group with little side effect. Therefore, the artesunate has a favorable prospect to treat the systemic lupus erythematosus.

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.

The invention relates to a nano-Artesunate capsule and a preparation process thereof. A capsule heart is Artesunate, a capsule film is gelatin, a capsule shape is in a ball shape or an ellipsoid shape, and the diameter of the capsule is 30 nm. The invention adopts the following preparation process: swelling the gelatin by distilled water to form colloid, dissolving powdered Artesunate in ethanol at the room temperature, dissolving glacial acetic acid in the distilled water, taking gelatin solution, slowly dropping the Artesunate ethanol solution under the stirring in a water bath with the constant temperature of 40 DEG C, adjusting pH value with glacial acetic acid solution, slowly dropping formaldehyde under the condition of ice bath, solidifying to form the capsule, and freezing and drying to obtain powder of the nano-Artesunate capsule. The capsule prepared by the invention can be taken orally as well as injected by injection, the dosage is small, and no toxic or side effect occursby taking orally; and the injection cannot cause thrombus, and the like in blood vessels, can support sustained release of medicine delivery, and the injection has high efficiency and long effective period. The grain size of the capsule is uniform, the covering state is good, and the covering rate is 50%; the addition of emulsifier and coagulant aid is not needed during preparation, the process issimple, and the operation is convenient.

An application of artesunate in preparing the medicines for preventing and treating the hepatic fibrosis and preventing heptocirrhosis and liver cancer is disclosed.

Artesunate is a derivative of artemisinin isolated from a Chinese herb Artemisia annua L. It is used clinically for the treatment of malaria. We investigated potential anti-inflammatory actions of artemisinin derivatives. artemisinin derivatives significantly inhibited OVA-induced signs, symptoms and parameter of airway disorders Taken together, our results clearly demonstrate anti-inflammatory effects of artemisinin derivatives. Artemisinin derivatives can be used to complement or to replace oral steroids during asthma exacerbation treatment. Further artemisinin derivatives can be used as an anti-inflammatory agent for controlling airway disorders.

The invention relates to the technical field of daily chemical products, and in particular relates to artemisia apiacea toothpaste and a preparation method thereof. The artemisia apiacea toothpaste is prepared from the following raw materials in percentage by weight: 18 to 25 percent of friction agent, 0.3 to 0.6 percent of adhesive, 54 to 64 percent of humectant, 2 to 7 percent of foaming agent, 0.05 to 0.2 percent of sweetening agent, 0.1 to 0.4 percent of preservative, 0.3 to 0.6 percent of sodium pyrophosphate, 1 to 2 percent of essence, 0.1 to 0.3 percent of artemisinin or artesunate and the balance of artemisia apiacea grass extract aqueous solution. By matching the fresh artemisia apiacea grass extract aqueous solution with the artemisinin or the artesunate, the artemisia apiacea toothpaste disclosed by the invention has the functions of killing bacteria, resisting bacteria and inhibiting bacteria and can be used for preventing gingival bleeding; in addition, by adding the sodium pyrophosphate, the artemisia apiacea toothpaste has good effects of preventing and treating dental calculus and dental plaque.

The invention relates to an artesunate purification process, and aims to provide an artesunate purification process with simple process, high yield and short crystallization time, and a preparation method. The artesunate purification process comprises six steps including esterification, extraction, concentration, crystallization, purification and drying. The process provided by the invention simplifies the purification and separation of artesunate, has advantages of short reaction time, especially greatly shortened crystallization time of only 4-6 min, product yield above 93%, product purity higher than 99%, recyclable solvents, low energy consumption and environmental protection, so as to greatly reduce costs of artesunate anti-malaria drugs and contribute to the public welfare of the global against malaria resistance.

The invention provides novel application of artesunate. The artesunate is used for reversing erlotinib drug resistance of lung adenocarcinoma, or the artesunate is used together with erlotinib. The problem that clinical application of a conventional molecular targeted drug is limited as drug resistance can be resulted ultimately can be solved. The invention belongs to the field of lung cancer treatment.

The invention discloses an artesunate fat emulsion injection preparation which contains 0.01 to 30 wt% of artesunate, 10.0 to 30.0 wt% of oil for injection, 0.6 to 30.0 wt% of an emulsifier, 0 to 10 wt% of a solubilizer, 0 to 5 wt% of a co-emulsifier, 2.25 to 7 wt% of an isotonic agent and 0.002 to 0.075 wt% of an anti-oxidant, with the balance being injection water. The invention also discloses a preparation method and pharmacodynamic and safety evaluation for the artesunate fat emulsion injection preparation. The artesunate fat emulsion provided by the invention has the characteristics of good biocompatibility, high physical stability, convenient preparation, good security, high drug loading capacity and the like, has a particle size of less than 200 mu m and is suitable for injection, e.g, intravenous injection and intramuscular injection. According to the invention, the characteristic that a soybean oil fat emulsion inhibits growth of plasmodium falciparum is utilized to enhance anti-malarial effects of drugs, to improve bioavailability of the drugs and to reduce toxic and side effects of the drugs; nutrients needed by the body of a patient with malaria can be provided, the activity of lymphocytes of the patient is improved, which assists the patient in resisting malaria and recovering.

The invention relates to a compound antimalarial composition. Particularly, the invention relates to a compound antimalarial composition containing artesunate and febrifugine and in particular relates to a compound antimalarial ethosome composition containing artesunate ethosomes and febrifugine ethosomes, a compound antimalarial ethosome gel paste as well as a preparation method and an application of the compound antimalarial ethosome gel paste. The compound antimalarial ethosome gel paste is prepared from the following components including a gel paste matrix, the artesunate ethosomes, the febrifugine ethosomes, a backing and an antisticking layer. According to the compound antimalarial ethosome gel paste disclosed by the invention, by utilizing the carrier permeation enhancing property of the ethosomes, the percutaneous permeability of an antimalarial medicament and the antimalarial effect of the medicament are improved; in addition, with the adoption of the compound antimalarial ethosome gel paste, the preparation technology is simple, high-temperature heating is not needed in the preparation process, and a harmful organic solvent is avoided.