39 results about "Cholesterol derivative" patented technology

The invention discloses a fluorescent sensor film preparation method based on a perylene diimide cholesterol derivative. According to the invention, cholesterol-modified perylene diimide is coated on the surface of a glass substrate, such that a fluorescent sensor film is prepared. With the film, sensitive detections upon organic amine gas can be realized. The method provided by the invention is advantaged by simple operation and mild reaction condition. With the method, prepared fluorescent sensor films are advantaged in good stability, long service life, and high sensitivity. The fluorescent sensor films are excellent organic amine gas sensor films. When the films are used in combination with commercial fluorescent devices, sensitive detections upon environmental organic amine can be realized. Also, the sensor films can be prepared into devices, and developed into special organic amine detection devices.

The invention belongs to the technical field of display and relates to frame-sealing glue, a packaging method of a display panel and a display panel. The frame-sealing glue comprises a frame-sealing glue base and also comprises a siloxane side chain-type liquid crystal elastomer. A polymethylhydrosiloxane main chain, a liquid crystal monomer and a cross-linking agent undergo a hydrosilylation reaction to produce the siloxane side chain-type liquid crystal elastomer. The liquid crystal monomer is a cholesterol derivative. The cross-linking agent is a binaphthol derivative. The frame-sealing glue can effectively relieve or prevent the liquid crystal pollution caused by micromolecules in the frame-sealing glue in array substrate and color film substrate closing, reduce the impact produced by liquid crystal on the frame-sealing glue and improve liquid crystal display panel quality.

The invention provides a paclitaxel lipid compound and a micellar compound used in the injection of the paclitaxel lipid compound. The paclitaxel liposome compound is composed of paclitaxel with a therapeutic dose, phospholipid, cholesterol sulfate or / and similar cholesterol derivative, additive and injection water. By means of the lipidization of the paclitaxel, the problem about organic menstruum of an injection and the problem of hypersusceptibility of a surface active agent are solved. A paclitaxel lipid compound injection provided by the invention has the advantages of small side effect, low blood vessel simulation, high drug-loading rate, narrow particle size distribution, capability of filtering and degerming, good pharmaceutical stability, etc.

Provided is a skin irritation suppressant for transdermal preparations, having a sufficient reduction effect of skin irritation due to a drug. Also provided is a transdermal preparation comprising the skin irritation suppressant. One embodiment of the invention is a skin irritation suppressant for suppressing the skin irritation due to a drug and a pharmaceutical ingredient to be used in a transdermal preparation other than the drug, the skin irritation suppressant comprising a sterol compound selected from the group consisting of cholesterol, cholesterol derivatives and cholesterol analogs, and the drug is one or more basic drugs selected from the group consisting of tolterodine, asenapine, bisoprolol, risperidone, nicotine and citalopram, and their pharmaceutically acceptable salts.

The present invention relates to the field of pharmaceutical chemistry, and in particular to methods of preparing cholesterol,and derivatives and analogs thereof. The cholesterol derivatives include, but not limited to, 7-dehydrocholesterol, 25-hydroxycholesterol, 25- hydroxy7dehydrocholesterol and ergosterol. In the invention, phytosterol can be used as a raw material to prepare the compound shown in the formula I through microbial conversion, and then cholesterol and the derivatives and analogues thereof are prepared.

The invention belongs to the technical field of medicine and discloses a preparation method of sub-microemulsion used for the intravenous injection of polyene yew alcohol phospholipid composite. The sub-microemulsion of the polyene yew alcohol phospholipid composite is basically prepared from polyene yew alcohol, phospholipid, liquid oil, a surfactant, cholesterol, a cholesterol derivative, or / and a similar cholesterol derivative, an addition agent and water for injection according to the effective therapeutic dose. The sub-microemulsion of the polyene yew alcohol phospholipid composite provided by the invention has high medicine carrying quantity and good preparation stability; and the preparation method is simple, convenient and easy and is easy for realizing industrialization.

The invention provides a docetaxel lipid compound and a micellar compound used in the injection of the docetaxel lipid compound, belonging to a pharmaceutical preparation. The docetaxel lipid compound is composed of docetaxel with a therapeutic dose, phospholipid, cholesterol sulfate or / and similar cholesterol derivative, additive and injection water. By means of the lipidization of the docetaxel, the problem about organic menstruum of an injection and the problem of hypersusceptibility of a surface active agent are solved. A docetaxel lipid compound injection provided by the invention has the advantages of small side effect, low blood vessel simulation, high drug-loading rate, narrow particle size distribution, capability of filtering and degerming, good pharmaceutical stability, etc.

The invention discloses a preparation method of a cholesterol derivative-based organic-inorganic composite nano vesicle. The preparation method is characterized in that: the structure of an organic-inorganic composite cholesterol derivative is Si-L-Ch, wherein the Si is a silicane head group; the L is an aliphatic chain linking group; carbon number in the L is between 2 and 18; and the Ch is a cholesterol group or a cholesterol derivative group. The method comprises the following steps of: performing derivation on a hydroxy group of a cholesterol molecule to form a carboxyl; reacting the carboxyl and an amino of garma-aminopropyltriethoxysilane (APTES) under the condition of dehydration by using EDC as a dehydrating agent; and synthesizing the novel silicane head group-containing cholesterol derivative through covalent connection of an amido bond or by directly reacting the carboxyl on the cholesterol molecule and isocyanatopropyltriethoxysilane (IPTES). The cholesterol derivative-based organic-inorganic composite nano vesicle has excellent biocompatibility. The organic-inorganic composite cholesterol derivative can perform self assembly to form a highly dispersed system similar to a liposome and is applied to embedding, transferring and sustained release of various medicaments, such as hydrophilic medicaments, oleophylic medicaments, amphiphilic medicaments and the like. The method has a simple operation process and high repeatability, can be relatively widely applied to the synthesis of a plurality of organic-inorganic composite cholesterol derivatives and has a wide application prospect.

The invention relates to a cholesterol ramification containing azobenzene group and the compounding method, and the application as light controlling releasing material. It has simple method, and is suitable for industrializing manufacturing.

The invention discloses a cholesterol derivative, an O / W / O multi-phase gel emulsion prepared from the cholesterol derivative, and a method for preparing a porous silicon dioxide bulk material from the emulsion. The structural formula of the cholesterol derivative is as shown in the description, wherein n is an integer of 6 to 12, and R represents a C1-C4 alkyl group. The O / W / O multi-phase gel emulsion is prepared according to a one-step method by taking the cholesterol derivative as a sing surfactant and taking a silanization reagent as an oil-phase material, and is high in stability, stable to acid and alkali, uniform in droplet distribution, and high in water-phase content which is 80 to 97 percent of the total volume. The porous silicon dioxide bulk material is prepared by taking the O / W / O multi-phase gel emulsion as a template at an ammonia gas atmosphere. The method is simple and low in cost; the prepared silicon dioxide bulk material is low in density, and has rich hierarchical porous structures which are regular and high in permeability; moreover, the porous silicon dioxide bulk material is large in surface area, high in heat stability, adjustable in hydrophilicity and hydrophobicity, and excellent in water or oil adsorption property.

A transdermal absorption preparation containing at least one drug selected from oxybutynin and pharmaceutically acceptable salts thereof and 0.05% by mass or more of a sterol selected from cholesterols, cholesterol derivatives and cholesterol analogs, relative to a total amount of the transdermal absorption preparation.

The invention provides a cell membrane fluorescent probe with high brightness, high stability and insensitivity to environment, particularly a naphthalimide probe which can be used for cell membrane fluorescence imaging. The fluorescent probe has the advantages of being low in synthetic raw material cost, simple in method, easy to derive and the like. Research finds that azetidine, azolidine and other high-rigidity structures are introduced to the 4-position and the 5-position of a naphthalimide parent of the dye, and the rigidity and lipophilicity of the dye are improved. The molar extinctioncoefficient of the dye in ethanol is 35000 M<-1>cm<-1> or above, the highest quantum yield can reach 0.72, and the dye has very high brightness and light stability; the dye also has environmental insensitivity, extremely small spectral property difference in different environments and good imaging accuracy; the dye structurally contains structures such as long aliphatic hydrocarbon chains or cholesterol derivatives or quaternary ammonium salts and can interact with cell membranes, so that the cell membranes can be quickly and accurately positioned, can be quickly labeled and can be applied tothe fields of cell membrane fluorescence imaging and the like.

Docetaxel and doxorubicin can be formulated in liposomal pharmaceutical compositions. In various embodiments, the pharmaceutical compositions include (i) a first liposome type comprising a first lipid layer comprising an unsaturated phospholipid, cholesterol or a cholesterol derivative, DC-cholesterol, a cationic lipid, and preferably a pegylated phospholipid, and a first active pharmaceutical ingredient (API) comprising docetaxel in the first lipid layer; and (ii) a second liposome type comprising a second lipid layer, an aqueous interior, and a second API comprising doxorubicin crystallized in the aqueous interior, (iii) where the first liposome type does not comprise doxorubicin and the second liposome type does not comprise docetaxel. The pharmaceutical composition can be used to treat a subject, for example, a human subject having cancer. The cancer can be, for example, a lung cancer, preferably non-small cell lung cancer (NSCLC), colon cancer, breast cancer, or liver cancer, preferably hepatocellular carcinoma (HCC).

The present invention relates to a 25-hydroxy-7-dehydrocholesterol synthetic method, a 25-hydroxy-7-keto-cholesterol derivative is used as a raw material for mechanical milling reaction in a ball mill pot under the effect of sulfonyl hydrazide and a base in the absence of an organic solvent, and then hydrolysis reaction is performed to obtain 25-hydroxy-7-dehydrocholesterol synthetic method. According to the method, in the absence of a solvent, mechanical milling reaction is performed, no dust is spilled over in the grinding process, reaction controllability is good, reaction efficiency is high, the solvent recovery operation in the post-processing process can be avoided, operation is simplified, environmental pollution is reduced, the reaction selectivity is good, yield is high, operation is simple, cost is low, post-treatment is simple, three-waste is less, product is easy to separate, purity is high, the yield is up to 89%, the melting process is short, and the product purity is high.

The invention relates to methacrylate slurry which is characterized in that the methacrylate slurry comprises the following components in part by weight: 10-30 parts of modified starch, 1-10 parts of urea starch, 1-15 parts of phospholipid and 10-25 parts of methacrylate. The positive-charge phospholipid contains stearamide (SA), cholesterol derivatives and the like, simultaneously has hydrophilic and hydrophobic groups and can improve the hydrophilcity of surface groups of the methacrylate slurry, effectively improve the moisture absorption and the viscosity of the methacrylate slurry and reduce the use quantity of PVA (Poly Vinyl Alcohol) after being combined with the methacrylate.

Provided is a compound represented by the general formula (1) (where: G represents a hexose-6-phosphate residue; and L represents a divalent linker group).

The present invention describes compositions containing cholesterol-linker-glutathione conjugates for targeting the brain by overcoming barrier entry to the CNS through the blood brain barrier (BBB), including micelle and liposome forms of such compositions. In addition, methods for treating subjects by administering such compositions are also disclosed.

The invention provides a cationic cholesterol derivative, a nano-composite as well as a preparation method and application of the nano-composite, and particularly relates to a cationic lipid gene transfection reagent. The invention relates to a preparation method of a cationic cholesterol derivative containing a natural cholesterol skeleton and a lysine head group, in particular to a synthesis method of a cationic cholesterol derivative containing a natural cholesterol skeleton and a lysine head group, a preparation method of a nano-composite and an application of the nano-composite serving as an efficient gene vector to a small interfering RNA (siRNA) and microRNA transfection reagent. According to the cationic cholesterol derivative containing the natural cholesterol skeleton and the lysine head group provided by the invention, the Linker chain length most suitable for siRNA combination is selected, and the nano-composite provided by the invention preferably adopts a micro-fluidic technology to systematically optimize various parameters (including total flow velocity, flow velocity ratio, buffer system, chip structure and the like), so that the stability of the nano-composite is improved, and the stability of the nano-composite is improved. A stable nano compound is formed, and efficient gene delivery capability can be realized without auxiliary lipid.

Docetaxel and doxorubicin can be formulated in liposomal pharmaceutical compositions. In various embodiments, the pharmaceutical compositions include (i) a first liposome type comprising a first lipid layer comprising an unsaturated phospholipid, cholesterol or a cholesterol derivative, DC-cholesterol, a cationic lipid, and preferably a pegylated phospholipid, and a first active pharmaceutical ingredient (API) comprising docetaxel in the first lipid layer; and (ii) a second liposome type comprising a second lipid layer, an aqueous interior, and a second API comprising doxorubicin crystallized in the aqueous interior, (iii) where the first liposome type does not comprise doxorubicin and the second liposome type does not comprise docetaxel. The pharmaceutical composition can be used to treat a subject, for example, a human subject having cancer. The cancer can be, for example, a lung cancer, preferably non-small cell lung cancer (NSCLC), colon cancer, breast cancer, or liver cancer, preferably hepatocellular carcinoma (HCC).

The invention discloses a drug-loaded nano-micelle with multiple drug release functions and a preparation method of the drug-loaded nano-micelle. The preparation method comprises the following steps that: firstly, carboxylation modified beta-CD is chemically grafted onto a PEG molecular chain to prepare a CD-PEG monomer; then, a cholesterol derivative is grafted to a molecular chain of the CD-PEG, and a Chol-PEG-CD ternary monomer is prepared; an ultrasonic emulsification-solvent evaporation method is adopted, and an anti-cancer drug is entrapped in the Chol-PEG-CD molecule self-assembly process, so that a drug-loaded nano-micelle is prepared. The drug-loaded micelle prepared by the invention has a multi-stage drug release function which is characterized in that the drug-loaded micelle is firstly suddenly released for rapid drug delivery and then slowly released for continuous drug delivery. The drug-loaded nano-micelle can deliver a drug to a focus site in a targeted manner through an EPR effect, so that the toxic and side effects of the drug are reduced. The drug-loaded nano-micelle with multiple drug release functions prepared by the invention has application advantages in the aspects of targeted delivery of anti-cancer drugs and tumor treatment.

The invention specifically relates to a chloroquine cholesterol derivative, and a preparation method and application thereof, belonging to the field of the chemical pharmaceutical industry. The chloroquine cholesterol derivative provided by invention has a structure as shown in a formula I which is described in the specification. The invention also provides the preparation method and application of the chloroquine cholesterol derivative. The chloroquine cholesterol derivative provided by the invention can effectively inhibit the proliferation of rat fibroblasts and treat pulmonary fibrosis, exerts anti-inflammatory effect, and offers a novel option for preparation of anti-fibrotic, anti-inflammatory and anti-tumor drugs.

The present invention discloses a preparation method of gel emulsion and low-density fluorescent porous metal complex material prepared by templating gel emulsion. The preparation method comprises the following steps: mixing a solution formed by dissolving an aromatic carboxylic acid type cholesterol derivative serving as an organic ligand in an oil phase with a solution formed by dissolving metal salts such as terbium nitrate and europium nitrate in a water phase; and using a complex formed by an in-situ self-assembly reaction of an organic ligand and metal ions on an oil-water interface as a stabilizer to obtain a W / O type gel emulsion, wherein the gel emulsion has reversible damage-recovery thixotropic performance. When an oil phase is a polymerizable monomer (such as styrene), the gel emulsion can be used as a template, a low-density fluorescent porous metal complex material is prepared through initiation polymerization of the oil phase, the material can be dried at room temperature, some high-energy-consumption means such as supercritical drying, freeze drying and the like and large professional equipment are not needed, and the material has the characteristics of simple preparation, excellent material performance, convenient processing and the like, and is easy to realize large-scale industrial production.

The invention discloses a fluorescent sensor film preparation method based on a perylene diimide cholesterol derivative. According to the invention, cholesterol-modified perylene diimide is coated on the surface of a glass substrate, such that a fluorescent sensor film is prepared. With the film, sensitive detections upon organic amine gas can be realized. The method provided by the invention is advantaged by simple operation and mild reaction condition. With the method, prepared fluorescent sensor films are advantaged in good stability, long service life, and high sensitivity. The fluorescent sensor films are excellent organic amine gas sensor films. When the films are used in combination with commercial fluorescent devices, sensitive detections upon environmental organic amine can be realized. Also, the sensor films can be prepared into devices, and developed into special organic amine detection devices.

The invention relates to a cholesterol ramification containing azobenzene group and the compounding method, and the application as light controlling releasing material. It has simple method, and is suitable for industrializing manufacturing.

The invention provides a 5-hydroxyl tolterodine gel preparation and a preparation method thereof, and further provides a novel cholesterol derivative. One end of the molecular formula of the cholesterol derivative is provided with an uncharged diethylamine group, and cholesterol is replaced by the cholesterol derivative. As compared with lipidosome added with cholesterol, lipidosome added with cholesterol derivative has higher long-term stability and higher encapsulation efficiency. The 5-hydroxyl tolterodine gel preparation which can be absorbed percutaneously is good in drug stability and high in bioavailability; toxic and side effects caused by oral administration and suffering and discomfort to patients caused by medicine injection are both avoided. The 5-hydroxyl tolterodine lipidosome, which is prepared by ethanol injection, is easy to produce and can be prepared for use on site, is convenient in quality control, low in cost, and low in environmental pollution. Stability of the 5-hydroxyl tolterodine lipidosome can be improved by uniformly dispersing the same in gel. Compared with common gel preparations, the lipidosome gel preparation has the advantages of effectively prolonging medicine release time, reducing systematic absorption of medicines, reducing toxic and side effect of medicines, enhancing compliance of patients, and accordingly has good clinical application prospect.

The invention belongs to the field of organic synthesis, and discloses a liquid crystal material based on pillararene and a preparation method thereof. A pillar [5] arene-cholesterol derivative 1 bridged by a rigid Schiff base spacer is designed and synthesized by aldehyde amine condensation. Then, [3]-pseudorotaxane is obtained through host-guest interaction between the pillar [5] arene-cholesterol derivative 1 and a guest 2 containing a dinitrile group; as the Schiff base group can be coordinated with Cu < 2 + >, the [3]-pseudorotaxane can be further cross-linked to obtain a three-dimensional supramolecular polymer network. The supramolecular network polymer is simple and convenient in preparation method and low in cost, and has a liquid crystal behavior, so that a new method is providedfor constructing a liquid crystal material based on pillararene.