73 results about "Fat solubility" patented technology

The invention provides a pyrazole amide derivative. Based on the existing pyrazole amide compound, ether bonds or ester bonds are introduced; furthermore, nitryl or heptafluoro-iso-propyl is introduced into the pyrazole amide compound; and the pyrazole amide compound has a general formula shown at the right-lower part. The pyrazole amide compound has the technical effects that the fat-solubility of the existing compound is improved, simultaneously the insecticidal activity is also improved, the pyrazole amide compound is particularly effective to the lepidopterous pests such as oriental armyworm, diamondback moth, beet armyworm and the like, and is a pesticide with wide application prospects.

The present invention relates to a preparation method of fat-soluble tea polyphenol and aims to expand the use of the tea polyphenol by using the water-soluble tea polyphenol as raw material to prepare the fat-soluble tea polyphenol. In the preparation method, carbon acylation is used for preparing the fat-soluble tea polyphenol. More accurately, the preparation of the fat-soluble tea polyphenol causes no loss of phenolic hydroxyl of the raw material of tea polyphenol. Thus the product has improved fat-solubility and original antioxidant properties. The product can be dissolved in oil, fat and organic solvents but can not be dissolved in water. The antioxidant free group and anti-lipid overoxidation performance are similar to the tea polyphenol. The present invention also relates to a preparation method and conditions therefore for the esterification of class formation of catechin through carbon acylation. And the fat-soluble tea polyphenol has the performances that are superior to the products of the same class in the prior art.

The invention discloses a ginsenoside Rg 3 and phospholipid complex and a preparing method thereof, belonging to the filed of medicines and health care products. The components comprise ginsenoside Rg 3 and phospholipid, and the mol ratio of the ginsenoside Rg 3 to the phospholipid is 1 : 1 to 10. The preparing method adopts organic solvent with small dielectric constant to dissolve the mixture of the ginsenoside Rg 3 and the phospholipid, and then the ginsenoside Rg 3 and phospholipid complex is prepared after the technical processes of solvent evaporation and the like. The ginsenoside Rg 3 and phospholipid complex has fat solubility and high bioavailability, and can be easily absorbed by human bodies and made into preparations such as emulsion and the like.

The invention discloses acyclic nucleoside compounds with an HIV-1 / HBV viral replication inhibition activity, preparation methods thereof, and antiviral applications thereof. The invention also discloses a general formula I of the compounds. R1 is hydrogen, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C5-6 aryl, or C5-12 aralkyl. R2 is a side chain of any natural or pharmaceutically acceptable amino acid. When the side chain contains carboxyl, the carboxyl is esterified optionally by using alkyl or aryl. The invention also discloses preparation methods of the compounds represented by the structural general formula I and a structural general formula II, and medicine compositions comprising the compounds. As a result of experiments, the compounds provided by the invention have the activity of inhibiting HIV-1 / HBV viral replication. One of the compounds has activity higher by more than 385 times that of a current AIDS-treating medicine tenofovir disoproxil fumarate (TDF), and higher fat-solubility than TDF. The compounds can be used in developments of medicines used for treating AIDS or hepatitis B.

The invention discloses an apigenin polylactic acid sustained release microsphere and a preparation method of the apigenin polylactic acid sustained release microsphere. The preparation method comprises the following steps: dissolving hydroxyl-terminated racemic polylactic acid and soybean lecithin in an organic solvent; stirring the liquid, and slowly adding the apigenin mixed liquid subjected to ultrasonic treatment in an emulsifier aqueous solution to be emulsified; reducing the pressure, removing the solvent with steam, concentrating the volume; centrifuging at high speed, washing and drying the obtained mixed liquid to prepare the polylactic acid entrapped apigenin acid sustained release microsphere, wherein the microsphere particle size is 1-5 microns, the drug loading ratio is larger than 25%, the encapsulation efficiency is larger than 79%, and the sustained release time is more than 550 hours. According to the polylactic acid with good biocompatibility and biodegradability is taken as a clad material to prepare the apigenin polylactic acid sustained release microsphere, so that the microsphere is uniform in shape, smooth and adhesion-free on the surface, uniformly distributed in the particle size, and good in slow-release effect, can keep continuous release time in vitro 550 h above, conquers the defects that the drug is poor in water solubility and fat solubility, improves the oral administration availability, prolongs the drug action time and improves the drug therapeutic effect.

The invention belongs to the technical field of organic synthetic chemistry, and provides a plurality of puerarin derivatives and preparation methods thereof. The prepared puerarin derivatives have good water solubility or fat solubility, and can be quickly converted into puerarin in blood or in vivo, the bioavailability is high, the preparation technology is simple, a target product has a high yield, and the product safety is high.

The invention relates to designing and application of a prodrug based on a gemcitabine structure. According to the prodrug, a phosphate ester long-chain group is introduced to the position 5'-OH of a gemcitabine five-membered sugar ring, so fat-solubility and membrane permeability of the prodrug are improved. In tumors lacking nucleic acid transport protein, the fat-soluble prodrug can enter the tumors through passive diffusion and active transport to inhibit growth of the tumors. Moreover, the prodrug can be orally taken, thereby obtaining a better or same curative effect of tumor growth inhibition compared with intraperitoneal injection of gemcitabine.

The invention provides a lipid-modified substance of chlorogenic acid and a derivative thereof, and a preparation and purification method of the lipid-modified substance, wherein the lipid-modified substance includes the chlorogenic acid or the derivative thereof and phosphoglyceride. A preparation process includes steps of performing constant-temperature magnetic stirring reflux for a certain time to the chlorogenic acid or the derivative thereof and the phosphoglyceride with an aprotic solvent and drying an obtained reaction liquid to obtain a crude product. A purification process includes the steps of re-dissolving the crude product with filtration to obtain a filtrate and then drying the filtrate. The lipid-modified substance of the chlorogenic acid and the derivative thereof is high in composition rate and can significantly improve the fat-solubility of the chlorogenic acid and the derivative thereof, so that a subsequent preparation is convenient to process and shape. The lipid-modified substance can be used as an intermediate for preparing a lipidosome, nano particles, polymer micelles or a dendritic polymer and the like nano drug-delivery systems and micro emulsion, self-micro emulsion and the like micron drug-delivery systems, thereby enhancing in-vivo absorption of the chlorogenic acid and the derivative thereof and further increasing the bioavailability of the medicines in a preparation.

A puerarin derivative and a synthetic method and an application thereof belong to the field of cerebrovascular diseases. Selectivity of a vascular dementia therapeutic target is improved by decorating puerarin. The puerarin derivative is indicated through a formula (1) which is as follows. By means of a chemical synthetic method, products are applied to treatment of vascular dementia. Fat solubility and water solubility of the puerarin are improved, receptor selectivity of the puerarin is improved, osmotic pressures inside and outside brain cells are balanced, cellular swelling caused by inflammatory injury is improved, a pharmacologic action of the puerarin itself of improving microcirculation and cholinergic nerve system functions is highlighted, and learning and memory disorders caused by damage caused by ischemia reperfusion are avoided.

The invention discloses pharmaceutical application of a phenoxy acid derivative and belongs to the field of biomedicine.The phenoxy acid derivative and berberine are chemically synthesized into salt, the problem that phenoxy acid derivative medicine is poor in water solubility and low in oral bioavailability, and consequently full play of the pharmaceutical effect of the medicine is limited is solved, and the problems that berberine hydrochloride is low in water solubility and lower in fat solubility, malabsorption by the gastrointestinal tract is caused, as a result, the oral bioavailability of berberine hydrochloride is low, and the systematic treatment effect of berberine hydrochloride is affected are solved.The derivative shows an excellent effect on regulating the blood glucose and blood fat of a rat with 2-type diabetes in an animal experiment.The derivative has the main effects of improving the oral glucose tolerance, promoting insulin secretion, improving insulin resistance, reducing the amount of triglyceride and the like.

The present invention discloses a molecular modification method of active fat-soluble plant polyphenols substance. It is characterized by that said method includes the following steps: protecting phenolic hydroxyl group of plant polyphenols substance, then making alkylation, introducing long-chain alkyl group on its benzene ring to raise fat-solubility, finally, hydrolyzing the product obtained after alkylation reaction to remove protective group and restore phenolic hydroxyl group so as to obtain active fat-soluble plant polyphenols substance.

The invention discloses a thickened oil cold-water-injected fat-soluble dissolving nano oil-displacing agent HCD that comprises the following components in percentage by weight: 10-50% of ester compound, 5-30% of alcohol compound, 0-20% of amine compound or ether compound, 0-35% of sodium salt or ammonium salt, 0-20% of wetting agent, 0-20% of aldehyde compound, 0-20% of biosurfactant and 0-20% ofacidic substance. The invention further discloses a preparation method of the HCD and application of the HCD in oil field exploitation and rapid pipeline petroleum transportation. The HCD prepared bythe invention has the characteristics of strong fat solubility, water solubility, viscosity reduction, through-seam throat expansion, weak oil wetness, low tension, high oil displacement efficiency,safety and environmental protection; according to the invention, the oil displacing agent enters the nanometer gaps of the thickened oil; paraffin, asphalt and colloid are dissolved in a non-polar fat-soluble manner, the thickened oil is thinned by rapid viscosity reduction, the production is easy, the pipeline transportation is easy, and the low-cost and high-benefit large-scale industrial production of naphthenic thickened oil, super thickened oil and other thickened oil is realized.

The invention belongs to the technical field of medicaments, and relates to novel azulene compounds and application thereof, in particular to novel azulene compounds which treat diseases of the immune system, have anti-aging effect and take I and II as chemical formulas. The azulene compounds have steadier structures and stronger fat solubility, and can be prepared into various pharmaceutically acceptable preparations when proper pharmaceutical excipients are matched. Immunological experimental results show that the compound I and the compound II have stronger effect on improving immune function; and antioxidation experiments show that the compound I and the compound II have stronger removal of the activity of free radicals. The azulene compounds and preparations thereof are mainly used for various diseases caused by low immunity, and can also be used for aging resistance.

The invention discloses a self-emulsifier containing a breviscapine phosphatidylcholine complex, and a preparation method and a use thereof. The self-emulsifier comprises the following components, by mass, 0.1-16% of breviscapine, 0.1-32% of phosphatidylcholine, 20-70% of an oily phase, 10-50% of a surfactant, and 0-40% of a cosurfactant. An insoluble dug breviscapine is processed to prepare a breviscapine phosphatidylcholine complex, and the breviscapine phosphatidylcholine complex is treated as an intermediate carrier to prepare the self-emulsifier containing the breviscapine phosphatidylcholine complex. The breviscapine phosphatidylcholine complex can effectively solve a bad fat solubility problem of breviscapine and substantially improve the drug loading capability of the self-emulsifier; and the self-emulsifier can increase the dissolution rate of breviscapine, promote breviscapine to penetrate epithelial cells, promote the lymphatic transport of drugs to a certain degree, reduce the hepatic first pass metabolism of the drugs and improve the oral bioavailability of breviscapine. Oral administration tests of rats show that the self-emulsifier containing the breviscapine phosphatidylcholine complex can substantially improve the absorption of breviscapine and improve the oral bioavailability of breviscapine.

The invention relates to a nanometer gel preparation with a dual slow release effect and a preparation method thereof. The nanometer gel preparation is prepared from 0.001 to 10 weight percent of preloaded medicine, 40 to 70 weight percent of ingredient A liquid crystal materials and 20 to 50 weight percent of ingredient B rheology control agents. The nanometer gel preparation has the dual slow release effect, and has the advantages that the water solubility and the fat solubility of the medicine can be greatly improved; in addition, the rheology control agents are used, so that the gel viscosity can be obviously improved along the temperature rising; at the skin temperature, good viscosity can be maintained; the nanometer gel preparation is applicable to a transdermal drug delivery system; the formed gel preparation can realize the long release time in the body; the absorption speed of the medicine in the body can be obviously improved; the medicine bioavailability is improved.

The invention relates to the application of flavonoids compound baicalein in skin cicatrisation inhibition. The invention verifies the fact that baicalein can be combined with TGFbetaRI(ALK5) to inhibit a TGFbeta1 signal channel in a cell, and accordingly abnormal proliferation, activation, shrinking and migration ability of human cicatrisation fibroblast are inhibited. An animal in-vivo experiment verifies the fact that after baicalein has an effect on mouse skin, mouse skin cicatrisation induced by tension can be inhibited. Baicalein is small in molecular weight and high in fat solubility, transdermal absorption capacity is good, accordingly, the molecules can be used for preparing medicine for skin cicatrisation inhibition, and the baicalein has wide application prospect in the field of medical treatment, plastic surgery and cosmetics.

The invention discloses a PCL-PLGA slow-release preparation and a preparation method thereof. The preparation method comprises the following steps: dissolving an antitumor medicine and a PCL-PLGA copolymer in a spinning solvent, stretching a spinning solution into micro / nanofiber under the action of a high-voltage electric field by an electrostatic spinning technology, and receiving the micro / nanofiber on the surface of a fixed receiver to obtain the PCL-PLGA slow-release preparation. The slow-release preparation provided by the invention gives full play to excellent biocompatibility and fat solubility of a PLGA material, further solves the problems of low mechanical toughness and too short degradation cycle through PCL-PLGA copolymerization, and has the advantages of capabilities of prolonging the circulation time of a chemotherapeutic medicine in a body, improving the blood concentration at a tumor site and reducing adverse effects of the chemotherapeutic medicine, and the like.

The invention discloses a ferulic acid and phospholipid complex and application thereof to preparation of skin-whitening cosmetics. The ferulic acid and phospholipid complex is obtained after ferulic acid and phospholipid are heated, stirred and compounded in a non-protonic solvent and the non-protonic solvent is removed. The invention also provides the skin-whitening cosmetics containing the ferulic acid and phospholipid complex. The cosmetics include skin oil, emulsion and cream with the skin whitening effect. According to the ferulic acid and phospholipid complex, ferulic acid and phospholipid are compounded, so that physicochemical properties of ferulic acid are changed, fat solubility, stability and water dispersibility of the complex are enhanced, the transmembrane transport performance of the complex is improved, and then the bioavailability of the complex is increased. After 30 female volunteers at the age of 25-45 use the skin-whitening and skin-caring emulsion containing the ferulic acid and phospholipid complex for 30 days, the melanin content of their faces is lowered obviously, the brightness of their skin is increased, the MI value, L* value and ITA degree value of their skin are remarkably different from original values (P<0.05), and it is indicated that the skin-whitening emulsion has a good human body skin whitening effect.

The invention discloses an application of a polygonin atomizing agent as asthma-treating medicine. Each 1000 ml of polygonin spraying agent comprises 1 g of polygonin, 50 ml of propylene glycol, 1 g of sodium pyrosulfite, and the balance of water. Polygonin is prepared in the atomizing agent for the first time in the invention, and thus, the curative effect of asthma treatment is greatly increased through an administration method of atomizing inhalation. The molecular mass of polygonin is small, and the polygonin has the characteristics of fat solubility and no taste; the polygonin has certain solubility in airway secretion fluid or alveolar fluid, can be quickly absorbed through the membrane of an epithelial cell so as to arrive at a target cell and exert the efficacy for relieving asthma and diminishing inflammation, and is suitably prepared into the atomizing agent without adding more additives; asthma is treated through the administration method of atomizing inhalation, and the curative effect of the polygonin atomizing agent is superior to a peroral dosage form of polygonin. Compared with other various dosage forms, the polygonin atomizing agent effectively saves dosage and manufacturing cost, reduces bad effect on patients, and is beneficial to environment protection.

The invention provides a fat-soluble tea polyphenol preparation method. The method comprises the following steps: 1, taking tea polyphenol, adding ethyl acetate, uniformly mixing, adding lipase and protease, and adding a disodium hydrogen phosphate-sodium dihydrogen phosphate buffer solution to obtain a reaction solution; 2, carrying out microwave radiation on the reaction solution, and reacting at a temperature of 35-45DEG C for 10-20min; and 3, adding water after the reaction ends to remove water-soluble impurities, standing for layering, taking the obtained ethyl acetate layer, carrying out reduced pressure distillation, and carrying out vacuum freeze-drying to obtain fat-soluble tea polyphenol. Compared with the prior art, the method adopting a microwave radiation-enzyme coupling catalysis technology to prepare the fat-soluble tea polyphenol has the advantages of avoiding of use of a large amount of severely toxic organic solvents, great shortening of the reaction time, and great improvement of the fat solubility of tea polyphenol.

The present invention relates to a copper imidazole-4-carboxylic acid phenanthroline coordination compound, a preparation method and an application thereof, wherein the coordination structure formula is . The preparation method comprises: in an aqueous phase, an organic phase or a mixed phase of an aqueous phase and an organic phase, carrying out a reaction of a copper compound, imidazole-4,5-dicarboxylic acid, phenanthroline, and an inorganic alkali or organic alkali or inorganic ammonium or organic ammonium to obtain the product. According to the present invention, the coordination compound can stably exist under a natural state, has a certain water-solubility and good fat-solubility, exhibits excellent blue light emitting specificity, can be used as a fluorescent or phosphorescent material or used for preparing a fluorescent or phosphorescent material, and can further be used for illumination lights, display screens and the like; and the preparation method has characteristics of easily available raw materials, low cost, product precipitation in a crystal form, high product purity and high yield.

The invention relates to a N-benzyl-N-benzyloxy urea, the general formula of which is as follows: R1 symbolizes H, CH3, OCH3, halogen R2 symbolizes H, CH3 and OCH3; the halogen N-benzyl-N-benzyloxy urea is obtained through the reaction between the benzyloxy urea and the benzyl chloride. The invention has the advantages that the aromatic base or replaced aromatic base is added on the basis of the hydroxyurea so as to increase both the molecular weight and fat solubility of the compounds, change the spatial structure of the compounds, enhance the bioavailability of the target compounds to a certain extent, strength the activity of the compounds and lower the side effect of the compounds.

The invention provides a novel method for synthesizing a 9-O-aryl substituted berberine derivative 5 and a 9-O-phenyl bridged berberine dimer 7. The method comprises the steps: removing methyl of a site 9 from berberine 1, which serves as a raw material, so as to obtain berberrubine 2, and subjecting the berberrubine 2 to protonation and reduction, so as to prepare tetrahydro berberrubine 3; subjecting the tetrahydro berberrubine 3 and iodo aromatic hydrocarbon to a C-O cross-coupling reaction under nitrogen protection so as to obtain a product 4, and then, carrying out oxidation, so as to obtain the target 9-O-aryl substituted berberine derivative 5; coupling the tetrahydro berberrubine 3 and 4o, and carrying out oxidation, thereby obtaining the berberine dimer 7. The berberine derivatives synthesized by the method have the advantages of good fat solubility, simple preparation method, high yield and the like. Discovered by in-vitro experiments, this kind of berberine derivatives havea relatively good inhibiting action on staphylococcus aureus, thereby having a potential application value in the field of antibacterial drugs.

The invention discloses a production method of a W / O blueberry anthocyanin micro-emulsion. The method includes the steps of: 1) adding the following raw materials at 25 DEG C according to ratio: 8-12 g of a compound surfactant being 7.5 in HLB value, 4-6 g of a co-surfactant anhydrous ethanol, 1.15-4.59 g of deionized water, and 12-18 g of isopropyl myristate, and uniformly mixing the components in a vortex mixer until a homogeneous and transparent solution is formed; and 2) maintaining the temperature at 25 DEG C, adding prepared anthocyanin to a W / O blank micro-emulsion in different ratios, performing centrifugation to obtain a supernatant, which is the W / O blueberry anthocyanin micro-emulsion. The method is simple in operations. The micro-emulsion is 10-100 nm in particle size and is easy to absorb due to the small particle size, and has good stability, wherein active components are in the inner layer of the micro-emulsion, so that influence on degradation of the anthocyanin due to light irradiation and pH value. The micro-emulsion has good fat solubility, which is improved by 30%, so that the applications of anthocyanin in lipid foods are increased.

The invention relates to a synthesis method of a nicotinamide modified polyaspartic acid derivative. The nicotinamide modified polyaspartic acid derivative is synthesized by using L-aspartic acid as araw material, phosphoric acid as a catalyst, and nicotinamide as a modifier. The synthesis method mainly comprises the following steps: stirring L-aspartic acid and phosphoric acid, heating to obtainpolysuccinimide (PSI), adding nicotinamide into a PSI reaction kettle, reacting to enable PSI to be subjected to ring-opening grafting to achieve the purpose of modification, and finally adding an alkali solution for hydrolysis to obtain a nicotinamide grafted and modified polyaspartic acid derivative sodium salt aqueous solution. The synthesis method disclosed by the invention is simple and easyto operate, and the grafting modification step and the polymerization step are coupled in one reactor, so that the process steps can be simplified, and the polymerization degree and the grafting ratecan be regulated and controlled. The synthesized nicotinamide modified polyaspartic acid derivative has good hydrophilicity, fat solubility and chelation, has the effects of moisturizing, removing freckles, whitening, improving skin quality, removing heavy metals and the like, and is a multifunctional and high-value polyaspartic acid derivative product.

The invention provides a liquorice pigment and a preparation method thereof. Based on traditional Chinese medicine liquorice as a raw material, the preparation method comprises a series of steps such as extracting, removing impurities by quaternization, leaching, concentrating and drying and the like. The prepared liquorice pigment is high in content and good in fat solubility. A medicament preparation, a functional food additive and the like can be further prepared from the liquorice pigment which is used as the raw material and have the effects of antibiosis and antiphlogosis and virus resistance. The liquorice pigment preparation method provided by the invention is novel in process, good in stability and is suitable for industrial production, and has strong practicability.

The invention discloses a quercetin derivative chemically modified by dodecanoyl chloride and a synthesis method thereof, belonging to the field of pharmaceutical synthesis. The method comprises the following steps of: adding raw materials namely quercetin and dodecanoyl chloride into a solvent, adding a proper amount of catalyst and acidity regulator, reacting for 8-10 hours under the condition of ice water bath to room temperature, adjusting the pH value to 6-7 with acid after the reaction is finished, adding water, extracting with ethyl acetate, separating liquid, and continuously extracting a water layer with ethyl acetate for 2-3 times. Combine ethyl acetate layers, adde water absorbing agent, overnight, suction filtering, distil to remove ethyl acetate to obtain crude product, purifying with 200-300 mesh silica gel column chromatography, preparing liquid phase, and purifying again to obtain quercetin derivative with high purity. The quercetin derivative obtained by the inventioncarries out chemical modification on natural quercetin, and is favorable for improving water solubility and fat solubility and improving bioavailability through substitution reaction at the 4'-OH hydroxyl position. The quercetin derivative can be used for treating diseases such as hypertension, myocardial ischemia and cancer.

The invention relates to the technical field of pharmaceutical preparations, in particular to an external preparation of simvastatin and an application of the external preparation. The external preparation is composed of simvastatin and pharmaceutically acceptable auxiliary materials. The preparation can effectively treat CHILD (congenital hemidysplasia with ichthyosiform erythroderma and limb defects) syndrome and xanthomatosis. The preparation has the advantages of convenient treatment, safety, low price, fat solubility, no trauma, easy observation of curative effect and low recurrence rate;high concentration of drugs in the target site of the skin increases the curative effect and reduces the systematic side effects of a simvastatin oral preparation; for patients with xanthomatosis whoare not suitable for or unwilling to be treated with oral lipid-lowering drugs for a long time, the effect of treating skin lesions is achieved, and adverse reactions caused by the absorption of thedrug system is avoided.

The invention relates to corn SOD molecule finishing method. Its features are that finishing agent and weight proportion are as follows: polyethylene glycol 8, anhydrous sodium sulfate 1, cyanogens urea acyl chloride 1, and anhydrous benzene 6.6; water and fat solubility polymers polyethylene glycol is used as the main finishing agent; the cyanogens urea acyl chloride is used as activator. The manufacturing method is simple. And it can increase stability, prolong half life, remove immunizing source and toxicity, increase film permeability, improve biochores and metabolism behavior, and increase solubility and organic solvent proof denaturing to make corn SOD can be extensively applied to food service, light, and medicine industries.

The invention discloses a photoresist resin monomer synthesized from alpha-cedrene and a synthesis method thereof, which belong to the field of chemical synthesis and photoetching materials. The structural general formula of the photoresist resin monomer is shown in the specification, wherein R is a connecting bond or a heteroalkyl group. The synthesis method of the photoresist resin monomer comprises the following steps: reacting alpha-cedrene with peroxide to obtain a first intermediate with an epoxy structure; and carrying out a ring-opening esterification reaction on the first intermediateto obtain the photoresist resin monomer. The photoresist resin monomer provided by the invention comprises a tert-butyl structure and a polycyclic polyester structure, can improve the edge roughness,increase the contrast ratio and improve the resolution ratio, has excellent etching resistance and fat solubility, and is simple and convenient in preparation method.