76 results about "Emtricitabine" patented technology

In accordance with this invention a novel pharmaceutical product containing efavirenz, emtricitabine and tenofovir DF are provided as a multicomponent unitary oral dosage form, component 1 comprising tenofovir DF (and, optionally, emtricitabine) and component 2 comprising efavirenz, wherein components 1 and 2 are in a stabilizing configuration. In preferred embodiments component 1 is made by dry granulation.

This invention prepn. method consists procedures (as shown in route chart) of: (1). hydrated glyoxalic acid is reacted with menthol in solvent and catalyst to produce stable intermediate-glyoxalic (1,R,2,5,5,R) menthol ester (V); then, reacting with 2,4-dihydroxy-1,4-dithiothiane to produce menthol ester (IV); (2). said product being proceeded acidylation by hydroxy to produce menthol ester (III); (3) being condensed with 5-fluorocytosine under the protection of silanized reagent, after purification to obtain menthol ester (II); (4). above-said product is reduce by reducing agent to obtain final invention product enqutabin (I) This invention has advantages of: available raw material, high yield, safety and commercialization prodn.

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 slow released anticancer injection consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is special solvent containing suspending agent. The effective anticancer component is antimetabolite Zalcitabine, Emtricitabine, etc and/or antimetabolite synergist selected from hormone anticarcinogen and/or platinum compound. The slow releasing supplementary material is selected from difatty acid-sebacic acid copolymer, poly (erucic acid dipolymer-sebacic acid), poly(fumaric acid-sebacic acid), etc or their composition. The suspending agent is carboxymethyl cellulose, etc. and has viscosity of 80-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent for use alone or together with chemotherapeutic medicine, radiotherapeutic medicine, etc.

The invention discloses a method for preparing emtricitabine. The method comprises the following steps: refining so as to obtain 5S-(5'-flucytosine-1')-1,3-oxythiacyclopentane-2-carbethoxy-(1'R,2'S,3'R)-menthyl lactate; under a weak alkali and solvent condition, removing a chiral aid L-menthol, thereby obtaining a product of emtricitabine. The initial raw material used in the method is low in price, easy to obtain, mild in reaction condition, high in atom utilization rate and simple and convenient in operation process, the reagent is environmentally friendly, the obtained product is high in chemical purity, meets medicine standards, and is applicable to industrial production of emtricitabine.

The invention discloses a method for purifying and refining lamivudine and emtricitabine. In the method, the lamivudine or the emtricitabine in a material system after reduction reaction is purified and refined by a physical method. The method comprises the following basic steps: flocculation, filtration, adsorption, desorption, decoloration, crystallization and the like, and finally the high-purity lamivudine or emtricitabine product is obtained. The method disclosed by the invention is safe and reliable to operate, is simple and feasible and is applicable to large-scale production. By using the method, the product quality is improved and environmental pollution is reduced.

The present invention relates to an oral unit dosage form comprising Emtricitabine, Tenofovir, Darunavir and Ritonavir and a monolithic tablet comprising Darunavir and Ritonavir and their use to treat HIV infection.

The invention relates to an anti-cancer drug slow release injection containing gemcitabine, which comprises slow release microspheres and a menstruum, wherein the microsphere comprises anti-cancer active ingredients and slow release auxiliary materials, and the menstruum is a special menstruum containing a suspending agent; the anti-cancer active ingredients are gemcitabine, or antimetabolites selected from zalcitabine, emtricitabine, galocitabine, ibacitabine, ancitabine, decitabine, flurocitabine, enocitabine, imidazole gemcitabine, capecitabine, gemcitabine, fludarabine or cladribine, and/or antimetabolite potentiating agents selected from phosphoinositide 3-kinase inhibitor, pyrimidine analogue and/or DNA repair enzyme inhibitor; the slow release auxiliary materials are polifeprosan, dienoic fatty acid, decanedioic acid copolymer, polylactic acid copolymer, EVAc and the like; the suspending agent has a viscosity of 100cp-3000cp (20-30 DEG C), and is selected from sodium carboxymethylcellulose and the like. The slow release microspheres can be prepared into slow release implants. When injected or placed into tumors or at peripheries of tumors, the slow release microspheres can enhance the treatment effect of non-operative treatment methods, such as radiotherapy, chemotherapy, etc.

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.

A solid oral dosage form is provided, comprising a compound of Formula I or a pharmaceutically acceptable salt thereof, tenofovir alafenamide or a pharmaceutically acceptable salt thereof, and emtricitabine or a pharmaceutically acceptable salt thereof.

The invention relates to an emtricitabine-containing tablet, which is composed of emtricitabine accounting for 30-80% of the total weight of the tablet and pharmaceutical adjuvants accounting for 20-70% of the total weight of the tablet. The pharmaceutical adjuvants contain a diluents accounting for 10-30% of the total weight of the tablet and a disintegrating agent accounting for 3-10% of the total weight of the tablet. The tablet provided by the invention has the characteristics of good stability, high l dissolution rate, appropriate tablet weight, and convenient drinking. Due to adoption of the single active component emtricitabine, the dosage is accurate. During use, the dosage can be adjusted according to the actual situation, thus facilitating combined use with other antiviral drugs. The preparation method provided by the invention has the advantages of simple process, cheap and easily available adjuvants, and easy industrial production.

The invention discloses a preparation method for an embritabine isomer. The preparation method comprises the following steps: with Solketal as a starting material, allowing the Solketal to undergo a six-step reaction of esterification, hydrolysis, oxidation, condensation cyclization, acetylation and glycosylation condensation so as to synthesize four mixture intermediates of emtricitabine; and splitting the four isomer intermediates into a cis-isomer mixture and a trans-isomer mixture through a chiral reagent. According to the invention, by adoption of a simple starting material, a mixture forsplitting key intermediates of four optical isomers of the emtricitabine is synthesized through the six-step reaction, and chiral acid is utilized to split the four isomers into a mixture of cis andtrans isomers, so the preparation method provided by the invention has the advantages of simple and convenient operation, high yield and high isomer chiral purity.

The present invention relates to a pharmaceutical composition for treating the human immunodeficiency virus (HIV) in a human being, comprising four active principles selected as being: one nucleoside inhibitor of reverse transcriptase (NRTI) selected from lamivudine and emtricitabine; two nucleoside or nucleotide inhibitor of reverse transcriptase (NRTI) selected from didanosine, abacavir and tenofovir; and the fourth active principle is selected from (i) a non-nucleoside inhibitor of reverse transcriptase (NNRTI) selected from nevirapine, efavirenz and etravirine; or (ii) a protease inhibitor selected from atazanavir, lopinavir, saquinavir, ritonavir, indinavir, amprenavir, nelfinavir, fosamprenavir, tipranavir and darunavir.

The present invention also relates to an electronic portable pillbox comprising a multidrug therapy for treating the immunodeficiency virus (HIV) in human beings allowing improving the observance of medication intake.

The invention discloses a method of reducing impurities in a synthesis process of an emtricitabine intermediate MGH. The method comprises the following steps: taking L-menthol and glyoxylic acid as raw materials; carrying out an esterification reaction under acid catalysis; carrying out an addition reaction under the action of sodium hydrogen sulfite; carrying out a hydroxylation reaction under the action of formaldehyde; carrying out post-treatment to obtain L-menthyl dyhydroxy acetate, wherein in the process of the addition reaction, the pH value is 4-6, and the reaction temperature is 40-80 DEG C and the reaction time is 4-10 hours. With the adoption of the method, the reaction time is greatly shortened and a reaction period is shortened; meanwhile, in a reaction process, cyclohexane is only used as an organic solvent, so that the operation is simple and the post-treatment is convenient; by controlling process conditions and post-treatment conditions, the content of impurities is greatly reduced and the yield is improved. Meanwhile, certain helps are provided for registration and application, and production and center control of emtricitabine, and improvement of quality standards of the emtricitabine intermediate.

The invention provides a stable emtricitabine and tenofovir medicine composition. The prepared medicine composition can effectively control degradation of effective components in the preparation and storage process, and the physical and chemical stability of medicines is improved. The invention further relates to a preparation method and an application of the medicine composition.

Polymer-of-prodrug (POP) materials enable new nucleoside reverse transcriptase inhibitor (NRTI) therapy strategies. The materials are prodrugs of NRTIs in the form of polymers. Suitable materials include products which are polymeric NRTI delivery systems comprising polymeric materials which are capable of degradation after administration to release NRTIs or NRTI prodrugs which themselves are capable of metabolism to the parent NRTIs. The NRTIs may optionally be selected from tenofovir (TFV), emtricitabine (FTC), lamivudine (3TC) and MK-8591 (EFdA). The invention facilitates long-acting (LA) regimens. Constructs of the materials may be in the form of injectable compositions or implants.