58 results about "Efavirenz" patented technology

This invention relates to a 50% drug loaded compressed tablet formulation for efavirenz. Efavirenz is a non-nucleoside reverse trancriptase inhibitor being studied clinically for use in the treatment of HIV infections and AIDS.

The present invention relates to a combination therapy for treating an HIV infection or inhibiting integrase comprising (S)-6-(3-Chloro-2-fluorobenzyl)-1-(1-hydroxymethyl-2-methylpropyl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (“Compound A”) or a pharmaceutically acceptable solvate or salt thereof in combination with at least one other anti-HIV agent. In some embodiments of the present invention, the other anti-HIV agents are chosen from reverse transcriptase inhibitors and protease inhibitors. In certain embodiments of the present invention, the other anti-HIV agents are chosen from AZT, 3TC, PMPA, efavirenz, indinavir, nelfinavir, a combination of AZT/3TC, and a combination of PMPA/3TC. Since Compound A has a high inhibitory activity specific for integrases, when used in combinations with other anti-HIV agents it can provide a combination therapy with fewer side effects for humans.

The present invention provides a novel crystalline form of Tenofovir disoproxil fumarate (Tenofovir DF), designated Co-crystal TDFA 2:1, methods for the preparation thereof and its use in pharmaceutical applications, in particular in anti-HIV medicaments. The crystalline form TDFA 2:1 can be used in combination with other anti-HIV medicaments such as Efavirenz, Emtricitabine, Ritonavir and/or TMC114.

The invention discloses a tri-combination compound mini-pill tablet co-prepared by disoproxil fumarate DF coated mini-pills, lamivudine coated mini-pills and efavirenz mini-pills and a preparation method thereof. The invention solves the problems that effective component degradation and dissolution delaying phenomena are generated due to interaction among the tri-combination compound components, tabletting is not facilitated during preparation and patient swallowing is not facilitated; and the single-layer tablet having the three component drugs without mutual contact is prepared by a mini-pill tabletting method, so as to obtain good stability and fast dissolving rate.

The invention discloses a synthetic method of intermediate cyclopropyl acetylene of an anti-aids drug efavirenz, and relates to the technical field of synthesis of cyclopropyl acetylene. The synthetic method comprises the following steps: reacting in an organic solvent to produce alpha, alpha-ethyl dichloride cyclopropane by taking cyclopropyl methyl ketone as a raw material and taking phosphorus pentachloride as a chlorinating agent; and obtaining the cyclopropyl acetylene by adding the alpha, alpha-ethyl dichloride cyclopropane into strong base aqueous liquor through a phase transfer catalyst. The synthetic method has the beneficial effects that the organic solvent and inorganic strong base are not needed to be adopted, expensive reagents such as the organic solvent and potassium tert-butoxide are avoided; moreover, process raw materials are easily available, process is simple, operation is convenient, cost is lowered and the three wastes are reduced, and therefore, the synthetic method is suitable for industrial production.

The present disclosure relates to a pharmaceutical composition, a health functional food composition, and a method for preventing or treating a brain disease or diabetes. The pharmaceutical composition, health functional food composition, and method includes at least one active ingredient that is chlorhexidine, thioguanosine, mebendazole, fenbendazole, colchicine, farnesol, trimethobenzamide hydrochloride, disulfuram, azathioprine, mebeverine hydrochloride, zaprinast, tosufloxacin hydrochloride, efavirenz, thiostrepton, probenecid, entacapone, harmine hydrochloride, flunisolide, thimerosal, hexestrol, sulfaquinoxaline sodium salt, monensin sodium salt, raloxifene hydrochloride, 2-chloropyrazine, or topotecan.

The invention discloses a method of synthesizing efavirenz which is an anti-AIDS medicine. The synthesizing steps are that: 4-chloro-2-trifluoroethylanilid is taken as raw material, after an h (hydrogen) on N being protected by protective group and the function of a ligand, the raw material is reacted with the substitute of cyclopropyl acetylene, thereby acquiring a chiral intermediate which is ring-closured and deprotected to obtain efavirenz product. The synthesizing method has the advantages that the cost is low, the reaction route is safe and environment protective and the chiral ee value of the product is high, etc.

The invention relates to a simple, convenient and high-efficiency synthesis method of 4-chloro-2-trifluoroacetylaniline and analogs thereof. The 4-chloro-2-trifluoroacetylaniline can be used as a key midbody for synthesizing the anti-AIDS (Acquired Immune Deficiency Syndrome) drug efavirenz.

The present invention describes a method and composition for a pharmaceutical product based on Tenofovir disoproxil hemifumarate, Emtricitabine and Efavirenz. The composition can be prepared by a process comprising a wet granulation step to produce a stable dosage form suitable for the treatment of HIV in essential absence of known degradation products.

The invention discloses an efavirenz preparation adopting a micronization technology. The invention provides a modified efavirenz orally-taken preparation which is used for inhibiting human immunodeficiency virus (HIV), preventing or treating HIV infection, and treating acquired immunodeficiency syndrome (AIDS) caused by the HIV infection, and in particular relates to tablets or a capsule which comprises efavirenz, wherein a micronization technology which can promote the dissolution velocity of the efavirenz in gastrointestinal tract, so that the absorption velocity and the absorption extent of the efavirenz in bodies is involved.

The invention is based on the finding that an increased daily dose of Efavirenz should be used for the treatment of cancer compared to the daily dose used in the treatment of AIDS. The invention thus relates to the use of Efavirenz for preparing a medicament intended for the treatment of cancer, wherein Efavirenz is administered at a dose generating an Efavirenz plasma concentration in said patient superior to 3000 ng/ml. It further relates to the use of Efavirenz for preparing a medicament intended for the treatment of cancer, wherein Efavirenz is administered at a daily dose of at least 1800 mg, in particular between 1800 and 2200 mg. It also relates to the use of Efavirenz for preparing a medicament intended for the treatment of cancer, in which the daily dose of Efavirenz is optimized after administration of a preliminary daily dose and measure or Efavirenz plasma concentration. It also relates to a unique dosage form of Efavirenz, comprising Efavirenz in an amount generating an Efavirenz plasma concentration in said patient superior to 3000 ng/ml, and a pharmaceutically acceptable carrier.

The present invention relates to a process for the preparation of Efavirenz (Formula I), wherein triphosgene is used as a cyclizing agent.

The present invention provides improved oral dosage form formulations of efavirenz that are useful in the inhibition of human immunodeficiency virus (HIV), the prevention or treatment of infection by HIV, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS). In particular, the present invention relates to compressed tablets or capsules comprising efavirenz that contain one or more disintegrants that enhance the dissolution rate of the efavirenz in the gastrointestinal tract thereby improving the rate and extent of absorption of efavirenz in the body. The present invention also relates to the process of making such tablets or capsules.

The invention relates to the field of medicine preparations, and provides a tenofovir disoproxil fumarate, efavirenz and lamivudine triplex compound tablet in tablet and a preparation method thereof. The tablet in tablet comprises a tenofovir disoproxil fumarate coating tablet core, and the tablet core is coated by the efavirenz, the lamivudine and auxiliary materials. The preparation method of the tablet in tablet has the advantages that the problem of degrading and slow dissolving caused by contact with the tenofovir disoproxil fumarate and other two crude drugs is solved; the degrading of the tenofovir disoproxil fumarate caused by contact of the tenofovir disoproxil fumarate with the efavirenz and the lamivudine is effectively avoided, and the good product stability is obtained.