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30results about How to "Improve membrane permeability" patented technology

Novel lactam compound

The present invention provides a lactam compound, a sugar transport enhancement agent containing this compound as an active ingredient, an agent for the prevention and / or treatment of diabetes mellitus, diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macrovascular disease, glucose tolerance anomaly, obesity and the like. In addition, the present invention also provides a preparation method for the novel lactam compound, and a preparation intermediate thereof.
Owner:AJINOMOTO CO INC

Curcumin self-microemulsion and preparation method thereof

The invention discloses a self-microemulsion, in particular to a curcumin self-microemulsion and a preparation method thereof. The curcumin self-microemulsion is characterized by the following components by weight percent: 0.05%-10% of curcumin, 1%-35% of oil phase, 20%-80% of surfactant, and 2%-40% of cosurfactant. The curcumin self-microemulsion and the preparation method thereof has the benefits that: a curcumin self-microemulsion release system increases the solubility of drugs, protects the drugs dissolved in oil drops, and improves the stability in a body; and the surfactant can change the flowability of cell membranes, improve membrane permeability of the drugs, enhance the absorption of the drugs in the body and increase the relative bioavailability of oral drugs.
Owner:SHANDONG LUNUO ANIMAL PHARMA

Preparation method of polypeptide supramolecular Bcl-xL antagonist nano-drug with mitochondrial targeting property

The invention discloses a preparation method of a polypeptide supramolecular Bcl-xL antagonist nano-drug with mitochondrial targeting, and relates to the technical field of supramolecular nano-drugs. Based on peptide sequences with mitochondrial targeting and pH-responsive morphologic changes in the tumor microenvironment, a BH3 structural domain derived from pro-apoptotic protein and anti-cancer, anti-inflammatory and antibacterial drugs are connected to polypeptide through covalent bonds, and the supramolecular Bcl-xL antagonist nano-drug is obtained by co-assembling the BH3 structural domain, the anti-cancer, anti-inflammatory and antibacterial drugs and the polypeptide according to different component proportions. The polypeptide supramolecular Bcl-xL antagonist nano-drug disclosed by the invention has the advantages that the polypeptide supramolecular Bcl-xL antagonist nano-drug has excellent mitochondrial targeting property and tumor microenvironment pH responsive morphology transformation, and has good tumor targeting enrichment capacity and excellent anti-tumor treatment effect. The preparation method is simple, easy for industrial production and wide in application field range.
Owner:NANKAI UNIV

Naphthalene-based two-photon fluorescent probes, preparation method and use thereof

ActiveUS20150079625A1Low fluorescence backgroundStrong and specific fluorescent signalMicrobiological testing/measurementNaphthalimide/phthalimide dyesSolubilityTwo-photon absorption
The present invention provides a novel category of naphthalene-based two-photon fluorescent probes having a general formula I, wherein: X is selected from the X1, X2, X3 and X4; The mentioned two-photon fluorescent probes have a low fluorescence background in the non-tumor cells and tissues, and have a strong and specific fluorescent signal in the tumor cells and tissues. These probes have a certain level of water-solubility, while having good membrane permeability. In addition, they have a bigger effective two-photon absorption cross section. The compounds of the present invention also have a lower biotoxicity, phototoxicity and photobleaching. There is sufficient difference between the spectral range thereof and that of a biological sample.
Owner:DALIAN UNIV OF TECH +1

Taxanes Compounds, Preparation Method Therefor, and Uses Thereof

The present invention provides taxanes compounds with a formula (I) or formula (II) structure, a method for preparing the compounds, as well as the use of the compositions containing the compounds, pharmaceutically acceptable salts and solvates thereof as active ingredients in manufacturing oral antitumor medicaments,In formula (I), R1 is —COR6, —COOR6 or —CONR7aR7b; R2 is a C1-C6 alkyl, a C1-C6 alkenyl, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; R3 is —OR6, —OCOOR6, —OCOSR6 or —OCONR7aR7b; R4 is —OR6, —OCOOR6, —OCOSR6, —OCONR7aR7b or H; wherein, R6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; R7a and R7b are respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group. In formula (II), R1 is —COR6 or —COOR6; R2 is an aromatic group; R3 is —OR6; wherein, R6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group.
Owner:JIANGSU TASLY DIYI PHARMA CO LTD

Medicinal application of collagen protein peptide, cucurbitacin oral micelle, and preparation method thereof

The invention belongs to the technical field of medicines and especially relates to a medicinal application of collagen protein peptide, a cucurbitacin oral micelle, and a preparation method thereof.The application is that the collagen protein peptide is used as a medicine transmembrane tool in preparation of the oral medicine preparation, wherein the collagen protein peptide carries positive charges. The invention provides the cucurbitacin oral micelle containing the collagen protein peptide, which comprises, by weight, 8-15 parts of cucurbitacin, 30-70 parts of lecithin, 50-75 parts of octanoic decanoic polyethylene glycol glyceride, 25-50 parts of polyethylene glycol 15-hydroxystearate and 80-100 parts of the collagen protein peptide carrying the positive charges. The collagen proteinpeptide, cooperated with other carrier materials, can improve membrane-permeability of the medicine and reduce excretion of the medicine, so that the collagen protein peptide can be used as the medicine transmembrane tool. For solving problems about oral bioavailability of the cucurbitacin, the invention provides the technology of collagen protein peptide coating nano-micelle, wherein by means ofthe characters of the collagen protein peptide, the problem of low bioavailability of medicines, such as the cucurbitacin, is solved.
Owner:ZHEJIANG UNIV OF TECH

(Z)-beta-trifluoromethyl dehydrotryptophan compound and synthesis method and application thereof

The invention belongs to the field of organic synthesis, and relates to a (Z)-beta-trifluoromethyl dehydrotryptophan compound, in particular to a (Z)-beta-trifluoromethyl dehydrotryptophan compound and a synthesis method and application thereof. The synthesis method comprises the following steps of: weighing a 3-trifluoroacetyl indole compound, an isocyanate compound, a catalyst and a solvent according to a certain ratio, stirring and reacting for 15-60 h at a temperature of 20-40 DEG C, and after the reaction is finished, carrying out pressure reduction and separation to obtain the (Z)-beta-trifluoromethyl dehydrotryptophan compound. According to the synthesis method disclosed by the invention, the (Z)-beta-trifluoromethyl dehydrotryptophan compound is simply, conveniently and efficientlyconstructed by taking 3-trifluoroacetyl indole as a trifluoromethyl source and carrying out a reaction between the trifluoromethyl source and isocyanate. Due to the introduction of trifluoromethyl, the membrane permeation function of the dehydrotryptophan-containing cyclic active peptide is effectively improved, the oil-water separation coefficient is increased, the lipophilicity and metabolic stability are enhanced, and the biological activity of the dehydrotryptophan-containing cyclic active peptide is improved.
Owner:SHANGQIU NORMAL UNIVERSITY

Pharmaceutical application of collagen peptide, cucurbitacin oral micelles and preparation method thereof

The invention belongs to the technical field of medicines and especially relates to a medicinal application of collagen protein peptide, a cucurbitacin oral micelle, and a preparation method thereof.The application is that the collagen protein peptide is used as a medicine transmembrane tool in preparation of the oral medicine preparation, wherein the collagen protein peptide carries positive charges. The invention provides the cucurbitacin oral micelle containing the collagen protein peptide, which comprises, by weight, 8-15 parts of cucurbitacin, 30-70 parts of lecithin, 50-75 parts of octanoic decanoic polyethylene glycol glyceride, 25-50 parts of polyethylene glycol 15-hydroxystearate and 80-100 parts of the collagen protein peptide carrying the positive charges. The collagen proteinpeptide, cooperated with other carrier materials, can improve membrane-permeability of the medicine and reduce excretion of the medicine, so that the collagen protein peptide can be used as the medicine transmembrane tool. For solving problems about oral bioavailability of the cucurbitacin, the invention provides the technology of collagen protein peptide coating nano-micelle, wherein by means ofthe characters of the collagen protein peptide, the problem of low bioavailability of medicines, such as the cucurbitacin, is solved.
Owner:ZHEJIANG UNIV OF TECH

Process for preparing low-free-alkali sodium methoxide methanol solution based on alkaline method

The invention discloses a process for preparing a low-free-alkali sodium methoxide methanol solution based on an alkali method, and relates to the technical field of chemical synthesis; the process comprises the following steps: S1, adding solid sodium hydroxide into an alkali dissolving tank containing methanol in proportion, performing standing precipitation, then conveying clear liquor to an alkali liquor inlet at the upper part of a reaction stripping tower through a pump to enter a reaction tower, and after the reaction, discharging mixed steam from the top of the tower, and forming a product at the bottom of the tower; s2, heating the mixed steam discharged in the step S1 and feeding the steam into a rectification section to separate the methanol and water in the mixed steam through a steam permeable membrane; s3, obtaining a sodium methoxide-methanol solution at the tower bottom. According to the process method provided by the invention, the content of free alkali in the prepared sodium methoxide methanol solution is low; water generated in the reaction is separated and removed through an evaporation permeable membrane, so that the production efficiency of sodium methoxide is improved; methanol separated and recycled from mixed steam can continue to react, so that the utilization rate of raw materials is increased, and the cost is reduced.
Owner:NINGBO ZHETIE JIANGNING CHEM
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