650results about How to "Increase fat solubility" patented technology

Glycopeptide having at least one asparagine-linked oligosaccharide at a desired position of the peptide chain obtained by: (1) esterifying hydroxyl of a resin and carboxyl of an amino acid having amino group nitrogen protected with a fat-soluble protective group (AGFPG), (2) removing the protective group to form a free amino group, (3) amidating the free amino group and carboxyl of an amino acid having AGFPG, (4) removing the protective group, (5) repeating the steps (3) and (4), (6) amidating the free amino group and carboxyl of the asparagine portion of an asparagine-linked oligosaccharide having AGFPG, (7) removing the protective group, (8) amidating the free amino group and carboxyl of an amino acid having AGFPG, (9) repeating steps (7) and (8), (10) removing the protective group, and (11) cutting off the resin with an acid; glycopeptide obtained by transferring sialic acid or a derivative thereof to the above glycopeptide.

The present invention relates to a new pharmaceutical product containing an antiprogestin molecule, such as mifepristone (RU486), administered by the nasal route and to be used to modulate the timing of the spontaneous LH surge as part of follicular stimulation cycles intended for Assisted Reproductive Technology (ART). In particular, it details the route of administration and the dosages that ensure effective delay of the LH surge without incurring in the antifolliculogenetic effects of the antiprogestinic. It also details the overall treatment method as resulting from the use of the new drug product.

Pharmaceutical compositions for oral-transmucosally administering methadone. For oral transmucosal delivery, the compositions comprise an oral dissolution agent and methadone in a dosage formulation. The dissolution agent generally causes the formulation to break down or dissolve in the oral cavity. The formulation is buffered to a pH of at least 6 for substantial absorption of the methadone through the oral mucosal tissue from the dissolved dosage form.

A 3-branched asparagine-linked oligosaccharide derivative of the formula (1) wherein the nitrogen of amino group of asparagine is modified with a lipophilic protective group, biotin group or FITC group; a 3-branched asparagine-linked oligosaccharide derivative which contains at least one fucose in N-acetylglucosamine on the nonreducing terminal side of the asparagine-linked oligosaccharide of the derivative; asparagine-linked oligosaccharides and oligosaccharides thereof wherein Q is a lipophilic protective group, biotin group or FITC group.

The present invention specifically adopts a simple method for preparing a molecularly imprinted polymer and directly applies the molecularly imprinted polymer to the extraction separation of trace substance in the complex sample pre-processing. The invention adopts a chemical coprecipitation method for preparing Fe3O4 magnetofluid. Then the surface of Fe3O4 magnetofluid is modified with oleic acid. The template molecules and functional monomers are realized with preassembling and are mixed with the cross linker and modified magnetofluid. Then the mixture is added into the polymer solvent containing dispersing agent. After the reaction is finished, magnetic field separation is executed. The polymer is dried after eluting the formwork molecules. A three-phase extraction system which is established on the base of magnetic molecularly imprinted polymer can be directly applied to the extraction separation of complex samples of food, environment and biological sample. The method of the invention has excellent selectivity and can eliminate the matrix interference in the sample. Furthermore as the polymer has excellent magnetism, the polymer can excellently realize the separation to the sample matrix after the extraction, and the polymer has broad application prospect in the complex sample pre-processing.

Provided are methods of treatment of many different diseases and disorders using micelle and sterically stabilized crystalline compounds of the invention.

A freeze-dried liposoluble vitamin with high water solubility and stability and its preparing process is also disclosed.

The invention discloses tenofovir diester compounds with activity of inhibiting HIV-1 (human immunodeficiency virus-1) virus replication and a preparation method and pharmaceutical use thereof. The structure of the compounds is shown in Formula (I), wherein m is 0-4, n is 12-16, and the structural formula is fixed when m is 1 and n is 14. The invention also discloses a preparation method of the compounds shown in the structural formula (I) and a pharmaceutical composition with the compounds. Tests show that the compounds have the activity of inhibiting HIV-1 replication and also much higher lipophilicity than the current HIV treatment drug tenofovir fumarate, and can be applied in development of drugs for treatment of HIV infection.

The present invention relates to the use of conjugated linoleic acid (CLA) for the topical treatment of fatty deposits and cellulite and to new topical compositions and to cosmetic and dermatological topical compositions for the treatment of fatty deposits and cellulite comprising CLA as well as kits comprising CLA for said treatment.

The invention relates to a lenalidomide derivative and a use thereof as a medicine, and in particular relates to a compound shown as a formula (I), a solvate, a hydrate, a stereoisomer or pharmaceutically acceptable salt thereof. The invention further relates to a pharmaceutical composition comprising the compound, and the use of the compound in preparing medicines for preventing or treating malignant tumors, in particular malignant tumors in the blood-lymphatic system. Compared with lenalidomide, the compound provided by the invention has a longer half-life period and can be used for preparing long-acting preparations.

The invention discloses a group of tenofovir disoproxil compounds with activity for inhibiting HIV-1 / HBV virus replication and pharmaceutically acceptable salts thereof, and a preparation method and pharmaceutical applications thereof. The group of the compounds have a general formula I, wherein X=H, Y=H, R1=-CH2(CH2)mCH2O(CH2)nCH3, m=0-4, n=10-20, and R2, R3 and R4 are respectively described in the specification. The invention also discloses a pharmaceutical composition containing the group of the compounds. Experiments show that one of the compounds has the advantages that an activity for inhibiting HIV-1 virus replication is 20 times that of a positive control medicine zidovudine (AZT), 1,000 times that of TDF that is the best medicine for treating Aids and about 9 times that of CMX157 in a clinical stage, and lipid solubility is about 2 times that of CMX157. Experiments also show that the compounds provided by the invention have the activity for inhibiting HBV virus replication, and can be used for development of drugs for treating the Aids and hepatitis B.

The invention discloses a compound vitamin lipid nanoparticle. The lipid nanoparticle is loaded with three active ingredients, i.e. vitamin A, vitamin C, vitamin E and is characterized by comprising the following ingredients in percentage by weight: 1-2% of vitamin A, 1-4% of vitamin C, 1-5% of vitamin E, 2-10% of emulsifying agent, 1-12% of compound lipid material and the rest of water, wherein the compound lipid material is a mixture of a solid lipid material and a liquid lipid material; and the lipid materials are selected from at least one or several of glycerol monolaurate, caprylic capric triglyceride, olive oil, soybean oil, corn oil, sunflower seed oil, acetylation monoglyceride, glycerin monostearate and stearic acid. The lipid nanoparticle has good stability, water solubility and repeatability and can be applied to the preparation of daily chemical products and health care foods containing the vitamin A, vitamin C and vitamin E; and a preparation method is simple and controlled.

The present invention uses puerarin as main medicine, phospholipid as absorption-promoting agent, polysorbate 80 as solubilization agent, and the weight ratio of puerarin and phospholipid is 1-20:1-4, and the weight ratio of puerarin and polysorbate 80 is 1-20:1-15, and adopts a certain preparation method to obtain the invented puerarin oral preparation which can be made into granules, tablet, capsule and soft capsule, etc. Said invention also provides its preparation method, including preparation of puerarin and phospholipid composite and its preparation. Said invention preparation is stable in quality, has no toxicity and irritation to body, and its biological utilization rate can be obviously raised.

The invention relates to the technology of phosphorescence chemical probe, in particular to a water-soluble cationic iridium complex phosphorescence probe and a preparation method. Iridium metal is not used for cell marking in the prior art. The structural formula of the water-soluble cationic iridium complex phosphorescence probe of the invention is as shown in the attached figure. The preparation of the invention is as follows: preparing 2-phenylpyridine iridium dichlorendic complex Ir2 (ppy) 4Cl2; preparing 3, 8-diacetylene o-phenanthroline; preparing 3, 8-diacetylene o-phenanthroline iridium 2-phenylpyridine complex; and preparing the objective complex. The invention has the advantages that with good water solubility and lipid solubility, the complex can quickly enter cells; and with long luminescent lifetime of iridium complex, the interference of the background fluorescence can be effectively eliminated through the time-resolved fluorescence technique, and thereby improving the detection sensitivity can be improved.

The invention relates to novel hydrazide derivatives as well as a preparation method and application thereof. The novel hydrazide derivatives have a general formula as shown in the specification, wherein each group is as shown in the claim 1. The novel hydrazide derivatives provided by the invention are improved in insecticidal activity while the previous compound lipid solubility thereof is improved; the derivatives have excellent insecticidal activity; instantly after the derivatives are applied, insects can lose control on muscle and stop eating, and are obviously shrank and paralyzed; at last, the insects can be caused to die, and in the meantime, abnormal ecdysis of insects also can be induced; the novel hydrazide derivatives are very effective especially for lepidoptera pests such as mythimna separata, plutella xylostella and asparagus caterpillar, and thus are pesticides having wide application prospect.

The invention discloses a compound bifonazole nano-emulsion spray preparation. The nano-emulsion spray preparation has the grain size of 1 nm to 100 nm and is formed by the following raw materials in mass percent: 30%-40% of surfactant, 3%-14% of cosurfactant, 5%-10% of oil phase, 0.8%-2% of bifonazole, 0.02%-0.1% of clobetasol propionate, 0.01%-0.2% of cinnamyl aldehyde and the balance of deionized water, wherein the sum of the mass percents of the raw materials is 100%. The compound bifonazole nano-emulsion spray preparation has multiple actions, such as fungicide, bactericide, anti-bacterial, anti-fungal, antiinflammation, itching relieving and the like, treats superficial skin fungous infection, fungous paronychia and candidal vulvovaginitis, and is also effective to external otitis and bacterial skin infection. The compound bifonazole nano-emulsion spray preparation prepared by a preparation method of the compound bifonazole nano-emulsion spray preparation has the advantages that: the activity of the three drugs is remarkably improved, the effect of sterilization and itching relieving is rapid, the recurrence is difficult, and the preparation method is simple, so that the compound bifonazole nano-emulsion spray preparation and the preparation method thereof have broad market prospects in the medicine field.

The invention provides a W / O microemulsion with stable properties and a particle size less than 100nm. The weight of the W / O microemulsion is taken as a standard, the W / O microemulsion comprises, by weight, 10 to 42% of a complex emulsifier, 2 to 40% of an aqueous solution, and the balance isopropyl myristate; the complex emulsifier is made from Span80 and Tween80 at a weight ratio of 1.02-1.27:1; and the aqueous solution is formed by water and ethanol at a weight ratio of 1-3:1. The invention also provides a preparation method and applications of the W / O microemulsion. The preparation method of the W / O microemulsion is simple; and the W / O microemulsion is an excellent carrier of active substances or functional substances which possess poor stability and lipid solubility, and are represented by tea polyphenol, and is capable of increasing stability of the active substances or the functional substances in food and medicinal preparations, and improving slow release behavior of the active substances or the functional substances.

The invention relates to a method and a device for extracting an aroma component. The method comprises the following steps of: (1) performing pretreatment on a material, and then performing pressure reduction treatment on the treated material in an extraction container; (2) introducing a solvent into the extraction container to mix the solvent and the material, and extracting the mixture to obtain extract liquor; (3) putting the extract liquor into a vaporization separation device to separate out a crude extract of the aroma component, and simultaneously separating the solvent, compressing and cooling the solvent, and then reclaiming the solvent for cyclic utilization; and (4) putting the crude extract of the aroma component into a refining system to perform refining treatment to prepare a refined extract. The extraction device comprises an extraction separation system, the refining system, a solvent purification system, a vacuum system and a heat exchange system. The aroma component extracted by the method and the device has no solvent residue, and the effective active components of a natural plant raw material can be maintained to the utmost extent.

The invention discloses a Chinese herbal piece ultrasonic wall breaking method. The Chinese herbal piece ultrasonic wall breaking method comprises the following steps: 1) pretreatment: Chinese herbal medicines are put in a drying chamber from a feed port to obtain dried Chinese herbal medicines; 2) the dried Chinese herbal medicines obtained in the step 1) are roughly crushed by a 80-mesh rough crushing device to obtain rough powder of 80-100 meshes; 3) ultrasonic wall breaking: the rough powder obtained in the step 2) is controlled through a flow valve to add in a first wall breaking reaction cavity for ultrasonic crushing to reach a particle size of 10-100 microns so as to obtain wall breaking fine powder; 4) secondary ultrasonic wall breaking: the wall breaking fine powder obtained in the step 3) is added in a second wall breaking reaction cavity for secondary wall breaking by 30-90 min to obtain secondary wall breaking powder; and 5) ternary ultrasonic wall breaking: the secondary wall breaking powder is put in a third wall breaking reaction cavity for ultrasonic wall breaking by at least 20 min to obtain wall breaking ultrafine powder; and the wall breaking ultrafine powder flows out from a discharge port. The Chinese herbal piece ultrasonic wall breaking method can be applied to manufacture ultrafine wall breaking Chinese herbal pieces, and is better in wall breaking effect of the Chinese herbal pieces through three times of continuous ultrasonic wall breaking.

The invention relates to compound emulsifiable paste for treating acne and a preparation method thereof, in particular to a medicament for treating acne and a preparation method thereof. The compound emulsifiable paste solves the problems of long treatment course and skin oxidation, dim skin and formation of color spots in the healing process in the conventional medicament for treating the acne. The compound emulsifiable paste is prepared from clindamycin hydrochloride, metronidazole, vitamin A, vitamin C, an emulsifying agent, stearic acid, albolene, glycerol monostearate, lanolinum, glycerol and purifying water. The preparation method comprises the following steps of: adding the vitamin A into uniform solution prepared from the stearic acid, the albolene, the glycerol monostearate and the lanolinum to obtain an oil phase; dissolving the glycerol and the emulsifying agent into the purifying water, adding the clindamycin hydrochloride, the metronidazole and the vitamin C, and stirring uniformly to obtain a aqueous phase; and adding the oil phase into the aqueous phase, stirring, homogenizing and standing the mixture to obtain the compound emulsifiable paste for treating the acne. The treatment period of the compound emulsifiable paste is between 14 and 24 days, skin is bright and clean after healing, and the compound emulsifiable paste can treat the acne, seborrheic dermatitis, acne rosacea and folliculitis.

A lipoid nanoparticle of camptothecine-phosphatide composition is prepared from phosphatide, 10-hydroxy camptothecine or its derivative and lipoid. Its preparing process is also disclosed.

The invention provides a method for extracting lipid-soluble and water-soluble antioxidants from rosemary. The method comprises the following steps: (1) naturally drying in harvested tender stems and leaves of rosemary in shadow places; (2) distilling the naturally dried rosemary by using steam, thereby obtaining rosemary essential oil and residues; (3) crushing the residues obtained after the essential oil is extracted, adding an ethanol solution with certain concentration, performing ultrasonic auxiliary extraction for multiple times, andperforming centrifugal separation after extraction, thereby obtaining leach liquids, and combining the leach liquids; (4) decoloring the leach liquids, adding a certain amount of activated clay into the leach liquids, stirring and maintaining for a certain time at a certain temperature, and removing the activated clay, thereby obtaining a decolored leach liquid; (5) performing vacuum concentration on the decolored leach liquid till a certain volume is achieved, and separating out the precipitate; (6) centrifuging the concentrated solution to obtain precipitate and water phase; and (7) respectively drying the precipitate and the water phase in vacuum, thereby obtaining a lipid-soluble antioxidant and a water-soluble antioxidant.

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 relates to a novel berberine 9-position coupled cholic acid derivative as shown in a formula (I) and a preparation method thereof as well as application of the derivative in the aspect of being a medicament, especially treating tumour. In the formula (I), R1 is hydroxyl or carbonyl; and R2 and R3 are hydrogen, hydroxyl or carbonyl.

The invention relates to the field of research into pharmaceutical chemistry, and particularly discloses a novel aromatic acid pro-drug with nitrogen monoxide donor, and a preparation method and application thereof in preventing and treating thrombotic diseases. In the invention, natural aromatic acid compounds with strong antithrombotic actions are structurally modified, and the carboxylic acid groups are incorporated with nitrogen monoxide donor to obtain the nitrogen monoxide donor type aromatic acid pro-drug with favorable liposolubility. The aromatic acid pro-drug with nitrogen monoxide donor has favorable solubility, can effectively permeate into the biomembrane lipid bimolecular layer, and can enhance the bioavailability after the human body takes the pro-drug. The pro-drug can be resolved into aromatic acid compounds and release nitrogen monoxide, and the aromatic acid compounds and nitrogen monoxide can cooperate to perform the pharmacological activities of resisting thrombi, resisting platelet aggregation and the like. The aromatic acid pro-drug with nitrogen monoxide donor can be used for preventing and treating thrombotic diseases and cerebral ischemia diseases.

The invention relates to a method for preparing coenzyme Q10 sub micro-emulsion injection, wherein said agent can treat cardiovascular disease, hepatitis, etc, while it can be injected or orally taken. And it comprises coenzyme Q10, soya oil, lecithin, glycerin, and injection water at 0.1-2:7-30:0.5-3:2-2.5:0-1:65-89; it uses high-speed mixer or ultrasonic vibration to form initial emulsion, via high-pressure mixer to prepare coenzyme Q10 sub micro-emulsion. Said agent is water-packing-oil sub micro emulsion, which packs coenzyme in water-packing-oil micro oil to reduce excited reaction and side effect, with target function.

The invention discloses an anthocyanin phospholipids compound and a preparation method thereof, comprises an anthocyanin phospholipids compound and a preparation method thereof, and belongs to the field of medicaments and health-care products. The components of the anthocyanin phospholipids compound comprise anthocyanin and phospholipids, wherein the weight ratio of the anthocyanin to the phospholipids is 1:1-20; and the preparation method adopts an organic solvent with a small dielectric constant for dissolving a mixture of the anthocyanin and the phospholipids and prepares the anthocyanin phospholipids compound through solvent evaporation and other technical processes. The anthocyanin phospholipids compound has the advantages of lipid solubility, easy absorption, high bioavailability, emulation formulation, and the like.

The present invention relates to a lipid microsphere injection containing ketoprofen or ketoprofen ester, its preparation process and prescription. It has good action for stopping pain, resisting inflammation and reducing fever. Said lipid microsphere includes ketoprofen or one ketoprofen ester, injection soybean oil, injection medium chain triglyceride, phospholipids, pure glycerin and injection water. Said invention can be used for preparing pain-stopping and inflammation-relieving medicine.

The invention relates to a natural biological composition for preventing and treating agricultural pests and a preparation method thereof. The natural biological composition is characterized by comprising the following raw materials and auxiliary materials in parts by weight: 20-50 parts of fine Elsholtzia, 60-80 parts of organic solvent (low-carbon alcohol), 4-8 parts of synergist, 1-3 parts of surfactant and 900 parts of deionized water. The effective active ingredients of the fine Elsholtzia are terpene phenolic compounds and are obtained by mixing Orthodonfordii, majoram and 2-4 kinds of vanillon, Elsholtzia stauntonii, Elsholtzia flava and Elsholtzia densa plants through ultrasonic oscillation extraction or percolation of the organic solvent. The composition of the invention is a natural biological pesticide having the advantages of safety, no environment pollution and no drug residues; the main raw materials used in the natural biological composition are effective active ingredients in two kinds of labiate accepted all around the world; and the additive, the surfactant and the organic solvent are mixed scientifically and reasonably to prepare an environment-friendly pesticide by adopting the advanced production technology.