36 results about "Lopinavir" patented technology

The invention includes methods, compositions, and kits useful for treating a viral infection by coadministering 6-(3-chloro-2-fluorobenzyl)-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof, with lopinavir or a pharmaceutically acceptable salt thereof.

The invention relates to a lopinavir preparation and purification process, and belongs to the field of drug synthesis. The purification process comprises: dissolving a lopinavir crude product in methanol, cooling to a temperature of 0-5 DEG C, adding water firstly, continuously cooling to a temperature of 5-15 DEG C, carrying out first thermal insulation stirring, standing, separating to obtain a supernatant, adding water secondly to the supernatant in a dropwise manner, stirring until the solid is precipitated, adding water thirdly, carrying out second thermal insulation stirring at a temperature of 10-15 DEG C after completing the water adding, and separating to obtain the lopinavir, wherein the concrete step of the third water adding is that the water is added in a dropwise manner in a plurality of batches within an interval time. According to the present invention, in the purification process, a small amount of the methanol and a large amount of the water are adopted as the purification solvent, such that the toxicity is low, and the cost is low; and with the purification process, the lopinavir crude product with the HPLC purity (peak area%) of less than 99.5%, preferably less than 99.1% and containing more than two single impurities with the content of more than 0.1% can be purified into the lopinavir with the single impurity content of less than 0.1% and the HPLC purity of more than 99.5%, wherein the loss during the purification process is less than 10%.

An extrusion process for preparation of solid dispersion of lopinavir and ritonavir carried out in twin screw extruder.

The invention belongs to the technical field of medicines, and discloses a lopinavir inhalation aerosol and a preparation method thereof. The lopinavir inhalation aerosol is composed of lopinavir serving as an active ingredient, a propellant, a cosolvent, a surfactant and the like according to a certain ratio . The aerosol inhalant is administrated through the oral cavity and directly acts on thelung to achieve targeted administration. The inhalation preparation disclosed by the invention can target a focus, is accurate in dosage, takes effect rapidly, can quickly improve the pulmonary infection condition, is beneficial to improve the adaptability of an infected person, and avoids gastrointestinal tract absorption so as to reduce side effects on the gastrointestinal tracts.

The invention relates to preparation of lopinavir as shown in formula (I) by a one-pot method. 2, 6-dimethylphenoxyacetic acid, a carboxyl activator and a compound as shown in a formula (III) are subjected to a condensation reaction in an organic solvent under a mild condensation reaction condition, the reaction can be carried out at room temperature without heating or cooling. The preparation method does not need special chemical reagents, and the solvent and the reagents used in the method are commonly used in laboratories. The total yield is higher than 85%, preferably higher than 90%, andthe yield reaches 96% in some embodiments. The preparation method is especially suitable for industrial production.

The invention relates to the new application of medicine and particularly relates to lopinavir which can be used for guarding against or treating ischemic cardiovascular and cerebrovascular diseases through restraining the expression of HMG (High Mobility Group Protein) B1. According to the invention, the dosage range is 120 mg-6000 mg and 120-3000 mg of lopinavir is particularly preferred.

The invention relates to a lopinavir and ritonavir compound tablet. The tablet comprises lopinavir, ritonavir, a dispersion carrier material, a flow aid, a surfactant and other additional auxiliary materials. A hot-melt extrusion mode is adopted for preparation. A preparation method comprises the following steps of uniformly mixing the bulk drugs lopinavir and ritonavir, the dispersion carrier material and the flow aid according to the prescription dosage to prepare a mixed material, crushing or grinding the mixed material until D90 is 100-150 [mu]m, performing extrusion through a hot melt extruder, and adding the auxiliary materials to prepare the tablet. The hot melt extrusion temperature is 90-110 DEG C. The prepared compound tablet is good in dissolution rate and uniform in content, and the components of the two effective medicines can be synchronously released.

The present invention relates to the use of a dioxolane thymine compound according to the chemical structure of Formula (I): where R¹ is H, an acyl group, a C₁-C₂₀ alkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group, for use in the treatment of HIV infections which exhibit resistance to 3TC and/or AZT. Preferably, compounds according to the present invention are combined with at least one anti-HIV agent which inhibits HIV by a mechanism other than through the inhibition of thymidine kinase (TK). These agents include those selected from among nucleoside reverse transcriptase inhibitors (NRTI), non-nucloeoside reverse transcriptase inhibitors, protease inhibitors, fusion inhibitors, among others. These agents are generally selected from the group consisting of 3TC (Lamivudine), AZT (Zidovudine), (−)-FTC, ddI (Didanosine), ddC (zalcitabine), abacavir (ABC), tenofovir (PMPA), D-D4FC (Reverset), D4T (Stavudine), Racivir, L-D4FC, NVP (Nevirapine), DLV (Delavirdine), EFV (Efavirenz), SQVM (Saquinavir mesylate), RTV (Ritonavir), IDV (Indinavir), SQV (Saquinavir), NFV (Nelfinavir), APV (Amprenavir), LPV (Lopinavir), fuseon and mixtures thereof. The TK dependent agents, such as AZT and D4T, may be used in combination with one of the dioloxane thymine compounds according to the present invention, but the use of such agents may be less preferred. In preferred compositions according to the present invention, R¹ is preferably H or a C₂-C₁₈ acyl group or a monophosphate group. Pharmaceutical compositions and methods of reducing the likelihood that a patient at risk for contract an HIV infection will contract the infection are other aspects of the present invention.

The present invention concerns pharmaceutical compositions formulated for topical application that are useful in the treatment of HPV-related pathologies and in particular the treatment of premalignant and malignant conditions of the cervix. The compositions comprise a therapeutically effective amount of lopinavir and ritonavir in a pharmaceutically acceptable vehicle and wherein the weight ratio(w/w) of lopinavir: ritonavir is between 9:1 and 18:1.

The present invention relates to a novel tenofovir disoproxil salt and the preparation method thereof. The crystalline form of tenofovir disoproxil orotate according to the present invention is an anhydride and it has superior physicochemical properties that are useful in pharmaceutical preparation as it resolves problems caused by physicochemical properties of tenofovir disoproxil fumarate. Namely, the crystalline form of tenofovir disoproxil orotate according to the present invention has a better than equal light stability compared to tenofovir disoproxil fumarate and has a superior stability especially under extreme stress conditions. Additionally, it is neither corrosive nor harmful to human body, thus making it safe for preparation and easy to manage. All of these characteristics make this invention useful for mass production. The present invention also provides a preparation method with and without using organic solvent, thus providing an industrially applicable and environment-friendly preparation method. Furthermore, tenofovir disoproxil orotate prepared according to the present invention can be used as an antiviral treating agent and can also be made into an anti-HIV treating composition if mixed with other drugs that have anti-HIV activity. The composition can be made into mixtures with one to six of the following other anti-HIV active ingredient medications that include Emtricitabine, Efavirenz, Rilpivirenz, Cobicistat, Elvitegravir, Raltegravir, Ritonavir, Lopinavir, Darunavir, Atazanavir and salts thereof for the treatment of HIV infection.

Provided are therapeutic agents, combination therapies, and methods for the treatment of coronavirus infections and related diseases, particularly COVID-19. The therapeutic agents provided include oseltamivir, lopinavir, ritonavir, chloroquine or hydroxychloroquine, azithromycin, clarithromycin, doxycycline, ivermectin, and combinations thereof.