321 results about "Ethanolamine synthesis" patented technology

The present invention relates to a method for treprostinil diethanolamine synthesis. The present invention also relates to a novel intermediate used in the method for treprostinil diethanolamine synthesis. The novel intermediate is shown in the following formula (II):

wherein R1 and R2 are described in the description.

The invention discloses paclitaxel nano micelle and an application thereof. The paclitaxel nano micelle is prepared from the following components shown in the following (1), (2) or (3): (1) a carrier and paclitaxel, wherein the carrier is a mixture of polyethylene glycol-distearoyl phosphatidyl ethanolamine (PEG-DSPE), D-alpha-tocopherol polyethylene glycol 1000 succinate (TPGS) and dequalinium chloride; (2) a carrier and the paclitaxel, wherein the carrier is a mixture of the PEG-DSPE and the TPGS; and (3) a carrier and the paclitaxel, wherein the carrier is the PEG-DSPE. After the functionalized paclitaxel nano micelle disclosed by the invention is orally taken, the paclitaxel can penetrate through a barrier of gastrointestinal tract, thus the multi-drug resistance (MDR) of drug-resistant breast cancer is overcome. The oral formulation of the functionalized paclitaxel nano micelle disclosed by the invention can avoid the anaphylactic response, can be applied to numerous cancer patients and is also suitable for MDR tumors at the same time, thereby having great advantage compared with the traditional intravenous injection formulation.

The present invention provides compositions and methods for reducing the immunogenicity and increasing the circulating half-life of therapeutic proteins such as Factor VIII. The compositions comprise lipidic structures such as liposomes, micelles and cochleates comprising a negatively charged lipid and polyethylene glycol derivatized phosphatidyl ethanolamine.

The invention relates to a fluorescence nanometer probe, comprising an inner core formed by polyglycolide lactide, a middle layer formed by phospholipid surrounding on the surface of the inner core and a shell formed by distearoyl phosphatidyl ethanolamine-polyethylene glycol which contains amino or carboxyl and partially penetrates through the middle layer, wherein indocyanine green is dispersed in the inner core. According to the invention, a core-shell structure is formed to ensure that the indocyanine green is wrapped in the polyglycolide lactide, therefore, the indocyanine green is effectively avoided from being aggregated and decomposed and the stability is increased; and the wrapped indocyanine green has a near-infrared fluorescence characteristic to ensure that the background fluorescence penetrating tissues is small and then can be relatively accurately applied to bioluminescence labeling.

The invention provides an Au-ICG (gold-indocyanine green) lipidosome multifunctional nano probe and application thereof. The nano probe consists of a kernel and a shell, wherein the kernel is a nanogold particle of which the surface is wrapped with a poly-dopamine layer and adsorbs indocyanine green; the shell is a DSPE-PEG (distearoyl phosphatidyl ethanolamine-polyethylene glycol) lipidosome film which is coupled with lactobionic acid and is chelated with Gd<3+> ions. The Au-ICG lipidosome multifunctional nano probe disclosed by the invention can be used for various image modes such as MRI (nuclear magnetism imaging), CT (computed tomography) imaging and near infrared fluorescence imaging of the liver cancer; a patient only needs to stand medicine supplying of a contrast agent, and various diagnosis effects can be achieved; furthermore, by virtue of the improvement of the sensitivity, the using amount of the contrast agent can be reduced, so that the toxic and side effect is further relieved; under near infrared illumination at 808 nm, adsorbed ICG molecules can effectively convert light energy into heat energy to produce superhigh heat of 60-70 DEG C, so that liver cancer cells can be killed thermally; therefore, the multifunctional nano probe can be used as a multimodal contrast agent for liver cancer diagnosis and can be used as a photothermal therapy agent for the liver cancer.

Compositions and methods for administering to the diet of humans a composition for inducing rapid weight loss, controlling appetite, managing stress and supporting mental well-being, supporting relaxation, and combating fatigue. A diet supplement comprising Calcium and Potassium double salt of Garcinia Cambogia Extract supplying 60% Hydroxycitric Acid, Gymnema Sylvestre Leaf Extract, Rhodiola Rosea Root Extract, Theanine, Astaxanthin Algae Extract, Chromium Polynicotinate, Hoodia Gordonii, N-olyl-phosphatidyl ethanolamine (NOPE)/EGCG blend, Vinpocetine, Russian Tarragon Extract, N-acetyl tyrosine, and Withania Somnifera Root Extract is provided. Said diet supplement is comprised of at least Hoodia Gordonii wherein the extract does not contain any extract from the root of the plant.

This invention discloses an ultrasonic microbubble contrast agent of carrier gene, it includes microbubble, fluorocarbon gas, gene or medicine. Microbubble wall is made up by lipid bielement, fluorocarbon gas is encapsulated in it, gene or medicine entrapped in microbubble envelope. This invention also discloses its preparation method, two stearyl phosphatidylcholine, two palmitoyl phosphatidyl ethanolamine, sapn-60, glycerol, phosphate buffer solution and gene or medicine is mixed as proper proportion for mechanical oscillations. The property of carry gene or medicine microbubble is stable, particle diameter disperses equally, local tissue medicine concentration can be obviously advanced though effect of transonic breaking microbubble, and curative effect is advanced and side effect can be reduced. Flushing and dilution of blood to gene and medicine can be prevented when used in body, and also prevent gene or medicine from degrading by nuclease in cycle to ensure that lot of gene and medicine can be transported to target tissue. And it is linear increase follow gene or medicine input amount in certain range.

The invention relates to a DSPE-PEG2000-FA-modified nanometer paclitaxel liposome. A molar ratio of the DSPE-PEG2000-FA to egg yolk lecithin is 0.05% to 0.15%, and a particle size of the liposome is less than 150 nm. A preparation method of the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome comprises the following steps: first, preparing a DSPE-PEG2000-FA into a DSPE-PEG2000-FA micelle; second, performing incubation on the phosphatidyl ethanolamine-polyethylene glycol2000-folic acid micelle and a paclitaxel liposome together to obtain a DSPE-PEG2000-FA-modified nanometer paclitaxel liposome. Materials, which are forbidden to be used in clinical practice, are not used as crude materials in the present invention. According to the invention, the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome has a small particle size, and the content of the DSPE-PEG2000-FA is low; besides, the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome has good drug entrapment efficiency and good colloid stability. Moreover, the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome can be absorbed effectively by an ovarian cancer cell having properties of sensitiveness to folic acid (+) and drug resistance, and the cytotoxicity of folic acid dependence is displayed; therefore, the efficacy of the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome is stronger than that of a paclitaxel injection.

The invention relates to a method for increasing medicament carrying amount and entrapment rate of polymer micelles on an anti-tumor medicament by using hydrophobic molecules. The polymer micelles are prepared from amphipathilic polymer such as polyethylene glycol-phosphatidyl ethanolamine (PEG-DSPE) by a membrane hydration method, and the micelles can be used for wrapping insoluble or low water-soluble anti-tumor medicaments for chemotherapy of tumor. Compared with the polymer micelles prepared without adding hydrophobic molecules, the polymer micelles obtained by adding the hydrophobic molecules such as phospholipid molecules with longer aliphatic chains (10 to 20 carbon atoms) in a certain proportion during preparing the polymer micelles by using the membrane hydration method obviously increase the entrapment rate and the medicament carrying amount on the raw material medicaments of the anti-tumor medicaments. The entrapment rate increment of the polymer micelles on the raw material medicaments improves the utilization rate of the raw material medicaments, and the medicament carrying amount of the polymer micelles improves the efficiency of medicament transmission during treating the tumor so as to lay a foundation for further increasing the curative effect of the anti-tumor medicament.

The invention discloses a tetravinyl-based Gemini type amphiphilic compound as well as a preparation method and application thereof. The compound disclosed by the invention is mainly prepared through McMurry coupling reaction, nucleophilic substitution reaction and Click reaction; the structure of the compound is also confirmed through infrared, nuclear magnetic and mass-spectrum ways; in an aqueous solution, molecules of a derivative of the compound disclosed by the invention self-assemble to form aggregation-induced fluorescence-enhanced micelles (AIE micelles); the compound acts with a nucleic acid, and then can co-aggregate to form nano particles easy for cellular uptake; green fluorescent protein (GFP) and luciferase (Luciferase) expression assays prove that the compound self and a liposome formed with dioleoyl phosphatidyl ethanolamine (DOPE) can be used as non-viral gene vectors; meanwhile, the derivative is successfully used for tracing the cellular uptake and release processes of pGL-3 and FAM-DNA by utilizing the reversible transformation between the self-assembly of the compound and the co-assembly with DNA (Deoxyribonucleic Acid).

The invention discloses a propranolol hydrochloride lipidosome gel, which is prepared by the following bulk drugs and auxiliary materials by weight percent: 0.012-0.075% of propranolol hydrochloride, 0.037-0.150% of phosphatidyl ethanolamine, 0.012-0.075% of cholesterol, 2.5-5% of triethanolamine, 1-2% of carbopol, and the balance of water. According to the propranolol hydrochloride lipidosome gel, during the preparation, the lipidosome is uniformly dispersed in the gel, so that the stability of the lipidosome is improved; the water-soluble gel carbopol has excellent biocompatibility, can be well adhered to skin and cannot stimulate skin; drug administration time is prolonged, the toxic and side effects on the whole body are reduced, the adaptability of patients is improved, and the propranolol hydrochloride lipidosome gel has excellent application prospect.

The invention discloses a hollow lipid microfoam composition with fluorocarbon/nitrogen and preparing method, wherein the microfoam filming material is composed of phosphatide, protective and polymer; the phosphatide is selected from phosphatidyl Choline and phosphatidyl ethanolamine; the protective can be middle and macromolecular hydroxyethyl amidon; the polymer is selected from boluoshamu 188 or medically acceptable surface activator for vein injection; the lipid filming material covers the fluorocarbon liquid to form emulsion particle, which forms hollow lipid microball under high temperature instantaneously through gasifying the liquid fluorocarbon; the fluorocarbon/ nitrogen is guided to produce the lipid microball for ultrasonic imaging with effectively reinforcing time over 60 min. The invention has high yield rate and fast manufacturing speed, which improves the microball dispersity and microball density effectively.

The invention discloses a method for detecting lipid molecules in salmon. The method includes the following steps that firstly, a sample is processed in advance, wherein salmon meat is cleaned and ground into meal, an organic solvent I is added into the salmon meal to be shaken and evenly mixed, ultrasonic ice bath extraction is conducted, pure water is added after extraction to be shaken and evenly mixed, the obtained mixture is centrifuged by a freezing centrifugal machine, a bottom-phase solution is obtained, dried at low temperature and dissolved again by means of an organic solvent II, and a lipid crude extract is obtained; secondly, enrichment and purification are conducted, wherein a solid-phase extraction column is activated, then the lipid crude extract is subjected to sample loading, spraying and elution, and the collected elution solution is a lipid extraction solution; thirdly, the lipid extraction solution is subjected to mass spectrometric detection and analysis. By means of the method, structure verification and quantitative analysis of phosphatidylcholine (PC) and phosphatidyl ethanolamine (PE) in salmon can be achieved.

The invention discloses a DQA-PEG 2000-DSPE (Dequalinium Chloride-Polyethylene Glycol-Distearoyl Phosphatidyl Ethanolamine) conjugated compound and resveratrol liposome modified thereby. The structural formula of the compound is shown by a formula I. In terms of composition, the resveratrol liposome comprises resveratrol and a fat material, wherein the mass ratio of the resveratrol to the fat material is (1:20)-(1:40); and the fat material consists of egg yolk lecithin, cholesterol and the compound shown by the formula I in the molar ratio of (63-67):(18-22):(2-4.35) in sequence. Pharmacodynamic tests prove that mitochondrial targeted resveratrol liposome has an extremely strong cell toxic effect in in-vitro cell experiments of human lung adenocarcinoma A549 cells and drug-resistant A549/cDDP cells thereof, a tumor sphere model and an in-vivo transplantation tumor model and can penetrate through the core of the tumor sphere. The anti-tumor effect of vinorelbine liposome on the drug-resistant A549/cDDP cells can be obviously improved by combining the resveratrol liposome with the vinorelbine liposome for use (formula I).

The invention discloses a T7 peptide-modified ZL006 long-circulating liposome which comprises phospholipid, cholesterol, methoxy-polyethylene glycol-phosphatidyl ethanolamine, T7 peptide-polyethylene glycol-phosphatidyl ethanolamine and therapeutically effective amount of ZL006. The invention also discloses a preparation method of the T7-modified ZL006 long-circulating liposome. According to the T7-modified ZL006 long-circulating liposome, the medicine ZL006 is encapsulated in a lipid bilayer, so that the circulating time of the medicine in the body is greatly prolonged; by means of T7 peptide modification, the blood brain barrier penetration capability of the medicine is improved, the medicine for treating cerebral apoplexy is effectively and concentratedly transferred to the cerebral apoplexy part, the treatment effect of the medicine is furthest exerted, and meanwhile, the toxic and side effects of the whole body are reduced.

The invention discloses a folate-targeted hydrophobic medicine-loaded polymeric vesicle and a preparation method and use thereof. The polymeric vesicle is prepared by the following steps of: (1) dissolving amphiphilic triblock copolymer and a hydrophobic medicine in an organic solvent, adding distearamide phosphatidyl ethanolamine-polyethylene glycol (2000) folate, evaporating to remove the organic solvent to prepare a uniform thin film, blowing and drying; and (2) adding double distilled water and products in the step (1) into a container, hydrating, shaking and uniformly mixing to ultrasonically form stable emulsion, performing film filtering, collecting filter liquor and performing freeze drying, The polymeric vesicle has main advantages of liposome, nanoparticles and other particle medicine-loaded systems, stability in vivo and in vitro obviously superior to the liposome, thicker film layer, contribution to encapsulating the hydrophobic medicine, dual-targeting function of EPR passive targeting and folate active targeting, and capacity of making the medicine-loaded vesicle effectively targeted and gathered on a tumor part and fulfilling the aim of targeted therapy.

The invention relates to a quercetin hydroxypropyl Beta-cyclodextrin inclusion liposome, a preparation method and application thereof, belonging to the field of pharmaceutical preparation. The invention provides a medicine capable of improving the bioavailability of quercetin and a preparation method of the medicine. The medicine capable of improving the bioavailability of the quercetin is the quercetin hydroxypropyl Beta-cyclodextrin inclusion liposome which is prepared from the following components in parts by weight and a pharmaceutically-acceptable solvent: 1 part of quercetin, 1-100 parts of hydroxypropyl Beta-cyclodextrin, 5-50 parts of granulesten, 1-10 parts of cholesterol and 0.1-5 parts of polyethylene glycol-distearin phosphatidyl ethanolamine.

The invention discloses a metabolic marker for diagnosing a coronary heart disease. The metabolic marker comprises one or more of 1-palmitoyl-sn-glycerinum-3-phosphatidylcholine, 1-octadecatetraenoicenoyl-sn-glycerinum-3-phosphatidylcholine, 1-linoleoyl-sn-glycerinum-3-phosphatidylcholine, 1-stearoyl-sn-glycerinum-3-phosphatidylcholine, 1-linoleoyl-2-hydroxy-sn-glycerinum-3-phosphatidyl ethanolamine, 1-linoleoyl-sn-glycerinum-3-phosphatidylcholine, 1-oleoyl-sn-glycerinum-3-phosphatidylcholine, 1-hexadecene acyl-sn-glycerinum-3-phosphatidylcholine, phytosphingosine and hexadecanamide. The metabolic marker provided by the invention can accurately diagnose the coronary heart disease, accurately distinguish patients with the coronary heart disease and healthy persons, can also accurately distinguish the patients with the coronary heart disease from patients with atherosclerosis of coronary artery, and has high accuracy, sensitivity and specificity.

The invention relates to oligoarginine modified phospholipid, nanoparticles assembled by the oligoarginine modified phospholipid, a preparation method of the oligoarginine modified phospholipid and an application of the nanoparticles. After oligoarginine peptide chains are activated by DCC (dicyclohexylcarbodiimide)/NHS (N-hydroxysuccinimide), the oligoarginine peptide chains react with phosphatidyl ethanolamine, purification is performed, and oligoarginine modified phosphatidyl ethanolamine is obtained; or the oligoarginine peptide chains react with DCC/NHS activated phosphatidic acid, and oligoarginine modified phosphatidic acid is obtained through purification; or the oligoarginine peptide chains react with nitrophenyl chloroformate activated phosphatidylcholine, and oligoarginine modified phosphatidylcholine is obtained through purification. The nanoparticles assembled by the oligoarginine modified phospholipid is used for supporting genes, small-interfering RNA, polypeptides or proteinic drugs, antibodies and chemical drugs, and the formed aqueous dispersion of the drug-carrying nanoparticles is used for delivering drugs for in-vitro cells or in-vivo local intravenous injection. The nanoparticles are effectively promoted to enter the cells, and the intracellular drug delivery efficiency is improved.

Polyethylene glycol-phospholipid choline polymeride or its medicinal acid salt and application in pharmacy belong to technology field of nanometer medicine preparation. Polyethylene glycol-phospholipid choline polymeride or its medicinal acid salt is indicated as the following general formula (I), namely methoxypolyethylene glycol and phospholipid choline is associative through link which is substituted methylene or ether substituted benzene methylene or oxalyl. The polymeride can be used as medicine carrier, especially in preparing antitumor liposome preparation, can thicken antitumor drug at tumour position. The invention provides the application of polymeride with general formula (I) or its medicinal acid salt in preparing medicine for treating tumour, cardio-cerebrovascular diseases, inflammation infection, and asthma.

The invention provides an emulsion composition containing lecithin, other liposoluble substances and water. The water content of the emulsion composition in percent by weight is larger than 70%; the other liposoluble substances comprise one or more of arachidonic acid, linolenic acid, linoleic acid, conjugated linoleic acid, conjugated linoleic acid glyceride, phosphatidylserine, polyene phosphatidyl choline, phosphatidyl ethanolamine, phosphatidylinositol, phosphatidyl glycerol, phytosterol, phytosterol ester, plant stanol ester and medium-long-chain fatty acid. The preparation method of the emulsion composition comprises the steps of mixing and emulsifying the lecithin and the other liposoluble substances with the water to obtain the emulsion composition, wherein the water content of the emulsion composition in percent by weight is larger than 70%, and the particle sizes of fat globules in the emulsion are smaller than 5 micrometers. Furthermore, the invention provides a preparation method of the emulsion composition and the application of the emulsion composition in oral phosphatide and unsaturated fatty acid replenishers and protection of heart and cerebral vessels.

The invention discloses a metabonomics-based application of endogenous small-molecular substances in rapid detection of hepatotoxicity. The endogenous small-molecular substances are 12 hepatotoxicity biomarkers, i.e., L-alanine, L-phenylalanine, L-carnitine, L-carnitine palmitoyl, tryptophan, arachidonate, cholic acid, lysophosphatidylcholine (14:0), lysophosphatidylcholine (16:1), lysophosphatidylcholine (18:2), lysophosphatidylcholine (20: 3) and hemolysis phosphatidyl ethanolamine (18:2); and the endogenous small-molecular substances also refers to 3 special hepatotoxicity biomarkers, i.e. L-carnitine, cholic acid and lysophosphatidylcholine (14:0). By adopting the hepatotoxicity biomarkers, the discovery and diagnosis of the liver injury can be earlier than those of the existing biochemical detection indexes, the hepatotoxicity biomarkers can be well used for preventing, discovering and treating the hepatotoxicity, the limitation of the existing indexes can be overcome, and accurate detection information can be provided in time.

The invention provides an emulsion composition containing lecithin, DHA, other fat-soluble substances and purified water. The content of the purified water in the emulsion composition is more than 70% by weight, the weight ratio of the lecithin to the DHA is 1: (0.005-1), the particle size of fat balls in the emulsion is less than 5 mu m, and the other fat-soluble substances comprise one or more of the following components: arachidonic acid, linolenic acid, alpha-linolenic acid, gamma-linolenic acid, linoleic acid, conjugated linoleic acid, conjugated linoleic acid glyceride, phosphatidylserine, polyene phosphatidyl choline, phosphatidyl ethanolamine, phosphatidyl inositol, phosphatidyl glycerol, phytosterol, plant sterol ester, plant stanol ester and medium and long-chain fatty acid. The invention further provides a preparation method of the emulsion composition and application of the emulsion composition in the functional aspects of supplementing phospholipids and unsaturated fatty acids by oral administration, protecting heart and brain blood vessels, reducing blood lipids, reducing blood pressure, treating fatty liver and the like.

The invention discloses a manufacturing method of a composite membrane containing aquaporin. The manufacturing method comprises the steps that dopamine is auto-polymerized on the surface of a base membrane, and the base membrane with polymerized dopamine attached to the surface and amidogen of a phosphatidyl ethanolamine membrane containing aquaporin are made to react, and therefore the composite membrane is manufactured. According to the manufactured composite membrane, covalent bonds exist between a functional layer and the base membrane, composite strength is high, etching resistance and hydrolysis resistance are strong, service life is long, surface hydrophilicity is good water permeability is high, the manufacturing condition is mild, and the composite membrane has wide application prospects in the field of water treatment and membrane separation.