21 results about "Tenofovir" patented technology

Provided herein are stable formulations containing active ingredients, such as antiviral compositions, or antiretroviral compositions in a powder form for reconstitution for intrarectal delivery to provide pre-exposure prophylaxis (PrEP) against viral infections. The antiviral composition may be tenofovir, for HIV PrEP.

The application relates to the field of biological medicine, in particular to application of TDF in serum cholesterol regulation and a verification method. The application discloses that tenofovir disoproxil fumarate (TDF) can inhibit intestinal cholesterol absorption by specifically down-regulating the expression level of NPC1L1 protein in the intestinal tract, so as to reduce serum cholesterol. The regulation has tissue specificity, and TDF has no significant influence on the expression of key genes of liver cholesterol metabolism. The application also provides a method for verifying the regulation of TDF on serum cholesterol, which is evaluated by detecting blood lipid indexes and the gene and / or protein expression level of NPC1L1 in duodenal tissue. The application provides a treatment scheme with antiviral and cholesterol-lowering effects for patients with chronic hepatitis B combined with hypercholesterolemia, and provides a new idea for developing a lipid-lowering strategy targeting intestinal cholesterol absorption.

The invention relates to the technical field of drug analysis and detection, and particularly discloses a method for detecting related substances in emtricitabine, propiophenol and tenofovir disoproxil fumarate tablets. According to the method, an octadecyl silane bonded silica gel chromatographic column is adopted, a mixed solution of a phosphate buffer solution and a tetrahydrofuran-acetonitrile solution in different volume ratios is taken as a mobile phase A and a mobile phase B respectively, and a gradient elution mode is adopted by a dual-wavelength high-performance liquid chromatography; the method can realize effective separation of a plurality of impurities in the emtricitabine, propofol and tenofovir disoproxil fumarate tablet, and accurately detect the condition of the impurities in the emtricitabine, propofol and tenofovir disoproxil fumarate tablet. The methodology research and verification of specificity, sensitivity and the like of the method provided by the invention find that the method provided by the invention is sensitive, accurate and relatively good in reproducibility, and accurate and quantitative detection of the related substances in the emtricitabine, propofol and tenofovir disoproxil tablet can be realized by using a simple, convenient and rapid method; and a reliable guarantee is provided for improving and better controlling the quality of the emtricitabine, propofol and tenofovir disoproxil fumarate tablet product.

The present invention relates to a dolutegravir-tenofovir-lamivudine combination tablet. Specifically, the present invention provides a dolutegravir-tenofovir-lamivudine combination bilayer tablet, comprising a first immediate-release tablet and a second immediate-release tablet; the first immediate-release tablet comprising dolutegravir, lamivudine, a diluent, optionally a binder, and optionally a disintegrant; and the second immediate-release tablet comprising tenofovir disoproxil, a diluent, optionally a binder, and optionally a disintegrant. The dolutegravir-tenofovir-lamivudine combination tablet of the present invention has a fast dissolution rate and high stability, thereby having excellent bioequivalence and shelf life.

The invention provides a solid oral dosage form comprising tenofovir alafenamide or a pharmaceutically acceptable salt thereof, and emtricitabine or a pharmaceutically acceptable salt thereof.

A pharmaceutical composition including an active ingredient, wherein the active ingredient includes at least a first drug conjugate having a structure shown by the following formula: Z-(linker-[R]m)n. In the formula, Z is a drug compound, R is a sugar, and m and n are independently an integer from 1 to 6. The drug compound Z is a first drug compound X selected from the group consisting of Tenofovir, Tenofovir diisoproxil, Tenofovir alafenamide, Entecavir, Telbivudine, Adefovir, Adefovir dipivoxil, Lamivudine, Interferon-α-2A, Interferon-α-2B, Selgantolimod, BI-82 and Zosuquidar, and the sugar R is selected from the group consisting of a monosaccharide, a disaccharide, a trisaccharide, a tetrasaccharide, an oligosaccharide, and a polysaccharide.

Provided herein are stable formulations containing active ingredients, such as antiviral compositions, or antiretroviral compositions in a powder form for reconstitution for intrarectal delivery to provide pre-exposure prophylaxis (PrEP) against viral infections. The antiviral composition may be tenofovir, for HIV PrEP.

The invention discloses an application of tenofovir disoproxil fumarate in preparation of a medicine for preventing or / and treating alpha-synucleinopathy, and also discloses a related combined application of the tenofovir disoproxil fumarate. Specifically, the tenofovir disoproxil fumarate protects neurons by reducing the level of alpha-synuclein in nerve cells and relieving behavior defects induced by alpha-synuclein, realizes effective prevention and treatment of alpha-synucleinopathy, and improves the insufficiency of the efficacy of existing drugs.

1. Name of the design product: packaging box (metformin hydrochloride and pioglitazone hydrochloride tablet). 2. Use of the design product: the design product is used for the packaging of medicines. 3. Design points of the design product: the combination of shape and pattern. 4. Picture or photo best indicating the design points: perspective view.

The invention provides a high performance liquid chromatography detection method of an inomitib tablet related substance. Specifically, the invention provides a method for detecting the related substances of the inomitetib tablets, which comprises a detection method for separating and detecting a related substance A from tenofovir disoproxil fumarate-inovirine and a detection method for separating and detecting a related substance B from lamivudine. The detection method disclosed by the invention can be used for rapidly and effectively separating and detecting all the related substances in the inomitib tablets, and an effective method is provided for controlling the related substances in the inomitib tablets.

The present application provides a combination of an siRNA agent and a reverse transcriptase inhibitor and a use thereof in treating hepatitis B. The present application specifically relates to a drug combination of an siRNA agent and tenofovir or a pharmaceutically acceptable prodrug thereof or a pharmaceutically acceptable salt thereof, a drug combination of an siRNA agent and entecavir or a pharmaceutically acceptable salt thereof or a solvate thereof, and a pharmaceutical use thereof.

The present invention provides oral pharmaceutical compositions of tenofovir alafenamide succinate, polymorph, cocrystal thereof, alone or in combination with one or more anti-viral drug and one or more pharmaceutically acceptable excipients. The present invention provides oral pharmaceutical compositions of tenofovir alafenamide succinate in combination with one or more anti-viral drug and one or more pharmaceutically acceptable excipients.

The present invention relates to a method for preparing 9-[(R)-2-[[(S)-[[[1-(isopropoxycarbonyl)-1-methyl]ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine fumarate of a compound of formula (I). The method comprises taking (R)-9-(2-methoxypropyl phosphate)-adenine as a starting material, first reacting it with phenol in the presence of a condensing agent to obtain compound (II); further chlorinating compound (II) to obtain compound (III-1), which is then condensed with compound (IV) to obtain compound (V); salifying compound (V) with D-(+)-dibenzoyltartaric acid anhydrate, followed by separation in an acetone / water mixed solvent to obtain compound (VI); dissociating compound (VI) through crystallization to obtain compound (VII); and finally salifying compound (VII) with fumaric acid to obtain a finished compound of formula (I). This synthetic method has high yield, good stability, simple operation, and is suitable for industrial production of pharmaceuticals. #imgabs0#

The invention relates to a preparation method of a compound 9-[(R)-2-[[(S)-[[[1-(isopropoxycarbonyl)-1-methyl] ethyl] amino] phenoxyphosphinyl] methoxyl] propyl] adenine fumarate as shown in a formula (I), which comprises the following steps: taking (R)-9-(2-phosphate methoxyl propyl)-adenine as a starting material, and firstly reacting with phenol under a condensing agent to obtain a compound (II); further chlorinating the compound (II) to obtain a compound (III-1), condensing the compound (III-1) with a compound (IV) to obtain a compound (V), salifying the compound (V) with D-(+)-dibenzoyl tartaric acid anhydride, splitting in an acetone / water mixed solvent to obtain a compound (VI), and performing free crystallization on the compound (VI) to obtain a compound (VII), and finally, salifying the compound (VII) and fumaric acid to obtain a compound finished product shown in the formula (I). The synthesis method is high in yield, good in stability, simple to operate and suitable for industrial production of medicines. # imgabs0 #

The invention belongs to the technical field of chemical pharmacy, and relates to a preparation method of a tenofovir intermediate R-(+)-9-(2-hydroxypropyl) adenine, adenine and R-propylene oxide are used as raw materials, tetraethylammonium bromide is used as a catalyst, under the action of sodium hydroxide, a ring-opening condensation reaction is carried out, and the tenofovir intermediate R-(+)-9-(2-hydroxypropyl) adenine is obtained. And the tenofovir intermediate R-(+)-9-(2-hydroxypropyl) adenine is generated. According to the preparation method of the tenofovir intermediate R-(+)-9-(2-hydroxypropyl) adenine, provided by the invention, the content of isomer impurities is greatly reduced, and the yield of a finished product is improved.

The present invention belongs to the field of medicinal chemistry, and relates to a pharmaceutical combination containing a capsid protein inhibitor or a pharmaceutically acceptable salt thereof and a reverse transcriptase inhibitor or a pharmaceutically acceptable prodrug thereof, or a pharmaceutically acceptable salt or a solvate thereof. Specifically, the present invention relates to a pharmaceutical combination of a capsid protein inhibitor or a pharmaceutically acceptable salt thereof and entecavir or tenofovir, or a pharmaceutically acceptable prodrug thereof, or a pharmaceutically acceptable salt or a solvate thereof, or the use thereof in the treatment of hepatitis B virus infection. The pharmaceutical combination has a good anti-hepatitis B virus infection effect.

The application discloses a kind of acyclic nucleoside phosphonate compounds and preparation method, analysis method and application thereof.The detection method of the acyclic nucleoside phosphonate compounds I-R of the application includes the following steps, using high performance liquid chromatography, elution is carried out to the analyte on chiral chromatographic column using mobile phase;The analyte includes acyclic nucleoside phosphonate compounds I-R.The detection method of the acyclic nucleoside phosphonate compounds of the application can directly detect the chiral purity of acyclic nucleoside phosphonate compound, and on the basis of the detection method, the chiral purity of tenofovir disoproxil (1) can also be known after derivatization;The method has good separation effect and high sensitivity.

The invention discloses a synthesis technique for a tenofovir intermediate, 9-propylene adenine is synthesized by the imino group of an acetyl-protected adenine and propionaldehyde selective enamination reaction, and then the acetyl-protected tenofovir intermediate (R)-9-(2-hydroxypropyl) adenine is synthesized by the method for synthesizing a chiral group through S-(-)-1,1'-binaphthyl-2,2'-bisdiphenylphosphine-induced oxidation. The invention has the beneficial effects of: the synthetic route of the present invention is simple to operate, process step is few, raw materials are easy to obtain, and reaction product is easy to process, and is suitable for industrial expansion production. The technical scheme of the present invention does not need to use expensive chiral reagents, and the reaction selectivity of the synthetic chiral group is high, so the yield yield and purity are higher, and the generation of by-products can be effectively reduced and the difficulty of by-product treatment can be reduced.