41 results about "Tocopherol succinate" patented technology

Tocol-based compositions of charged amphiphilic and water soluble pharmaceutically active compounds or their charged precursors are prepared by forming a tocol-soluble ion pair with an oppositely charged ion-pair forming compound capable of forming a tocol-soluble ion-pair with the active compound.Also disclosed are novel compounds tocopherolsuccinate-aspartate and tocopherolsuccinate-glutamate, which are useful as ion-pair forming compounds.

Tocol-based compositions of charged amphiphilic and water soluble pharmaceutically active compounds or their charged precursors are prepared by forming a tocol-soluble ion pair with an oppositely charged ion-pair forming compound capable of forming a tocol-soluble ion-pair with the active compound. Also disclosed are novel compounds tocopherolsuccinate-aspartate and tocopherolsuccinate-glutamate, which are useful as ion-pair forming compounds.

The present invention relates to a liquid pest control system that includes a synthetic pyrethroid as a pest control active ingredient and an agent selected from the group consisting of purified diethylene glycol monoethyl ether, tocopherol nicotinate and tocopherol succinate, and combinations thereof, to reduce or eliminate paraesthesia of the synthetic pyrethroid. The system releases the synthetic pyrethroid efficiently and uniformly. The pest control system is less irritating to the animal's skin as compared to prior art systems, particularly to the small breeds of dogs. The system is useful for making liquid spot-on treatments, sprays and the like.

The invention relates to an environmental response type anti-tumor nanometer medicine with high medicine loading capacity, a carrier and a preparation method thereof. The nanometer medicine comprisesan amphiphilic polymer carrier and a medicine prodrug; the amphiphilic polymer carrier comprises a hydrophilic segment and a hydrophobic segment which are connected mutually; the hydrophilic segment comprises polyethylene glycol or poly(N-(2-hydroxypropyl)methacrylamide); the hydrophobic segment comprises D-alpha-tocopherol succinate; the medicine prodrug comprises a medicine for treating tumor aswell as a hydrophobic chain segment which is connected with the medicine through a chemical bond; and the hydrophobic chain segment comprises D-alpha-tocopherol succinate. The nanometer medicine hasthe characteristics of high medicine loading capacity, environmental responsiveness and adjustable and controllable grain size, and can achieve the properties that the tumor penetration ability is high, the tumor cell multidrug resistance is achieved, drug-resistant cells are killed in advance, tumor related fibroblast is not killed and tumor stem cells can be killed effectively according to composition of different polymers and the loaded prodrug molecule types.

The invention provides a nano-micelle drug carrier based on a vitamin E derivative, a nano-micelle drug composition as well as a preparation method and application of the nano-micelle drug composition. The nano-micelle drug carrier based on the vitamin E derivative is a nano-micelle formed by D-alpha-tocopherol polyethylene glycol 1000 succinate, D-alpha-tocopherol polyethylene glycol 2000 succinate and alpha-tocopherol succinate; and the carrier entraps a hydrophobic anti-tumor drug to obtain the nano-micelle drug composition. The D-alpha-tocopherol polyethylene glycol 1000 succinate, D-alpha-tocopherol polyethylene glycol 2000 succinate and alpha-tocopherol succinate are matched with one another and cooperate, so that the formed nano-micelle is good in stability, is small and uniform in grain size, improves drug encapsulation efficiency, has relatively good P-glycoprotein inhibiting ability, has good anti-tumor effect, is small in toxicity to normal cells and has good biocompatibility. The preparation method is simple and is wide in application prospect.

The present invention relates to methods for the prevention and treatment of a mammal from radiation-induced internal injury using γ-tocotrienol, α-tocopherol succinate or γ-tocotrienol succinate. Specifically, the present invention relates to methods for preventing and treating radiation-induced injuries in a mammal by (1) subcutaneous, intramuscular, intraperitoneal, or intravascular injection of a therapeutically effective amount of γ-tocotrienol; or (2) oral administration of a therapeutically effective amount of α-tocopherol succinate or γ-tocotrienol succinate or both.

The invention discloses a method for synthesizing tocopherol succinate. The method comprises the following steps: by taking tocopherol and succinic acid as raw materials and taking lipase as a catalyst, adding the tocopherol and succinic acid in a mole ratio of (1: 1) to (1: 5) into a double-solvent reaction mixed solvent which is prepared by mixing a halohydrocarbon or alkane solvent and DMSO; reacting at 20-60 DEG C for 24-48h by using a method of generating water through an azeotropic removal reaction system while reacting; cooling to room temperature; washing to be neutral by diluted hydrochloric acid and pure water after the reaction is finished; standing for layering to separate out the lower water phase; removing the solvent of the oil phase under vacuum state; adding normal hexane to crystallize; and drying and grinding to obtain high-purity natural vitamin E monoester succinate.

The invention relates to a preparation method of multilevel slow-release drug-loaded short nano-fibers. According to the method, layered double hydroxides (LDH) loaded doxorubicin (DOX) serving as ananti-cancer drug and alpha-tocopherol succinate (alpha-TOS) serving as a P-gp inhibitor are mixed into polylactic acid-glycolic acid copolymer (PLGA) spinning solution, and electrostatic spinning andhomogeneous treatment are implemented to obtain the fibers. The multilevel slow-release double medicine carrying short nano-fibers are built by the aid of organic and inorganic double carriers, multilevel release of the anti-cancer drug and the P-gp inhibitor in materials can be achieved in tumor micro-acidic environments, multi-drug resistance of cancer cells is overcome, the double-carrier nano-fibers lengthen release paths of the drugs, slow release of the anti-cancer drug is achieved, and a novel method is provided for long-term and effective treatment of drug-resistant tumors.

An industrialized production method for producing high-content natural vitamin E by utilizing a hydrolysis reduction process comprises: (1) dissolving low-content natural mixed tocopherols in proper amount of a solvent, adding succinic anhydride and performing esterification reaction under an alkaline condition, so as to generate corresponding natural tocopherol esters; (2) performing reduced-pressure distillation on the product obtained in the step (1) to remove the solvent, adding an extraction reagent and performing extraction, water washing, crystallization and separation, so as to obtain natural tocopherol succinate with high content; (3) hydrolyzing natural tocopherol succinate obtained in the step (2) under an alkaline condition, and reducing to generate natural tocopherols; and (4) performing extraction, water washing, separation and distillation on the natural tocopherols obtained through hydrolysis in the step (3), so as to obtain the natural vitamin E (mixed tocopherols) with the high content up to 90% or more.

The invention discloses a method for preparing natural tocopherol succinate and a refrigeration system thereof. The method comprises the steps of pretreatment: adding acetone into raw materials containing natural tocopherol; performing treatment for 40 to 54 h at -20 to -17 DEG C through a refrigeration system to obtain pretreated raw materials; preparation: adding succinic anhydride and pyridineinto the pretreated raw materials; performing reaction for 2 to 3h at 40 to 50 DEG C; preparing a natural tocopherol succinate coarse product; crystallization: performing crystallization on the natural tocopherol succinate coarse product by n-hexane. In a product prepared by the method, the vitamin E content is high; the purity is high; the esterification rate is high.

The invention discloses a method for preparing tocopherol succinate, and a heating system. The method comprises the following steps: carrying out pretreatment, specifically, adding acetone into a rawmaterial containing natural tocopherol, and treating for 40-45h at -20 to -17 DEG C to obtain the pretreated raw material; preparing, specifically, adding succinic anhydride and pyridine into the pretreated raw material, carrying out a reaction at 40-50 DEG C for 2-3h by means of the heating system to obtain a crude product of natural tocopheryl succinate; crystallizing, specifically, crystallizing the crude product of the natural tocopheryl succinate with n-hexane. In the preparation process, almost no tocopherol is lost; furthermore, the method is high in whole reaction yield, esterificationrate and purity, mild and efficient in reaction conditions, and in line with the concept of green chemistry.

The present invention provides methods for culturing primary hepatocytes with improved long term function and improved viability, by plating the hepatocytes in the presence of an anti-oxidants) as well as an agent(s) which is a functional inhibitor of enzymes that generate reactive oxygen and reactive nitrogen species. One preferred embodiment provides a combination of 2-oxo-thizolidine and tocopherol succinate. Another preferred embodiment provides a combination of NG-methylarginine and mannitol.

The invention discloses an antioxidant essence microcapsule and a preparation method thereof. The microcapsule is a transparent spherical soft capsule of a core-shell structure, wherein the capsule wall is a sericin shell membrane, a capsule core is antioxidant essence, the mass ratio of the capsule wall to the capsule core is (1-2):1, and the diameter of the microcapsule is 1-5 mm. The antioxidant essence comprises, by weight, 12-25 parts of astaxanthin, 11-21 parts of tocopherol, 8-16 parts of tocopherol succinate, 3-11 parts of ascorbyl stearate, 1-8 parts of ascorbyl palmitate, 2-8 parts of jojoba oil, 2-8 parts of retinol, 1-7 parts of propylene glycol propionate, 1-6 parts of glycerol and 2-6 parts of sorbitol. The antioxidant essence microcapsule is slightly influenced by environmental factors such as light and heat, and is not easy to decompose and stable in property; antioxidant essence microcapsule particles are in a regular spherical shape, the capsule wall is uniform in thickness, the microcapsule has stable strength and elasticity, and the embedding effect of the capsule core is ensured.

The invention discloses a preparation method of d-alpha-tocopherol polyethylene glycol succinate. The preparation method comprises the following steps: by taking Merrifield resin and PEG1,000 as raw materials and alkali as a catalyst, performing reaction at 45-135 DEG C in an organic solvent to obtain resin loaded with PEG1,000; under the action of the catalyst, enabling the resin loaded with PEG1,000 and d-alpha-tocopherol succinate to be subjected to water diversion reflux reaction to obtain resin loaded with TPGS; and soaking the resin loaded with TPGS in toluene, then adding ethanol, palladium on carbon and phosphopyridoxal, and performing stirring reaction at 100-110 DEG C for 24 hours in hydrogen gas of 0.8-1.5MPa to obtain the d-alpha-tocopherol polyethylene glycol succinate. By adopting the synthetic method disclosed by the invention, the yield of TPGS is as high as 99%, the monoester content of TPGS is 99%, and the diester content of TPGS is 0.

The invention discloses whitening winkle and scar removal restoration skin care cream and a preparation method thereof. The skin care cream is prepared from the following ingredients of allantoin, glycerol, isopropyl myristate, caprylic / capric triglyceride, hydroxyethyl cellulose, alkyl polyglucoside, cetearyl glucoside, tocopherol succinate, plant extracts, lipidosome comprising bioactive factors, okra polysaccharide, gynostemmapolysaccharide, moringa seed oil, evening primrose oil, behenyl alcohol, phenoxyethanol, chlorphenesin and the balance deionized water. The skin care cream has the advantages that all ingredients are mutually cooperated; the scar removal effect is obvious; no skin irritation exists; the safety is high; the effects of preserving the moisture, tendering the skin, andresisting oxidization and aging are also achieved; the pigmentation can be effectively inhibited; the punctum is reduced, so that the skin restores to the natural state; the skin color is uniform; meanwhile, the winkles can be eliminated; the skin tightness is restored.

The present invention relates to the AAAPT bioconjugate of general Formula 1 or 2, whereinA may be a small molecule such as, but is not limited to α-tocopherol succinate (1), benzamide riboside (2), bortezomib (3), cycloheximide (4), or hispolone (5) or a macromolecule such as, but not limited to TRAIL, or AIF1 Flavoprotein. L is an alkylene or polyoxaalkyene chain selected from the group comprising —OC(CH2)aCO—, —HN(CH2)bCO—, —OC(CH2)cNH—, —HN(CH2)dNH—, —HN(CH2)e—, —O(CH2)f(CH2CH2O)g(CH2)hO—, —OC(CH2)i(CH2CH2O)j(CH2)kCO—, and —HN(CH2)i(CH2CH2O)j(CH2)kNH—. L may optionally contain acid enzymatically cleavable polypeptide sequences. T is selected from the group comprising somatostatin receptor binding agents, folate receptor binding agents, cathepsin B binding agents, matrix metalloprotein-2 (MMP-2) binding agents, GRP receptors, estrogen receptors, epidermal growth factor receptors (EGFR), and benzodiazepine.

The invention relates to a preparation method of a polyacrylic acid-tocopherol succinate self-assembly drug loading system for slow drug release. The preparation method comprises the following steps:preparing cystamine modified polyacrylic acid, preparing polyacrylic acid-tocopherol succinate and preparing drug-loading polyacrylic acid-tocopherol succinate. The preparation method has the advantages that the polyacrylic acid-tocopherol succinate self-assembly drug loading system is simple to prepare and can be prepared through two-step amidation reaction, the self-assembled drug loading systemhas dual sensitivity of pH and redox, and a drug can be slowly released through stimulation of pH and glutathione.

Tocopheryl succinate derivatives according to formula I:are described. These compounds increase the activity of protein phosphatase 2A, can be included in pharmaceutical compositions, and can be used for the treatment of androgen receptor-dependent cancers such as prostate cancer.

The invention relates to a concentration method for low-content natural mixed tocopherol. The method comprises: adding succinic anhydride, sodium hydroxide and butanone into natural mixed tocopherols with the mixed tocopherols content of 10%-45%, and stirring at 40-70 DEG C for 3-6 h; after the reaction is finished, performing reduced-pressure distillation to remove butanone, adding cyclohexane, performing water washing to neutral, cooling to 10-15 DEG C, standing for crystallization for 12-24 h, performing solid separation on the crystal and drying to obtain natural tocopherol succinate; adding ethanol and a potassium hydroxide solution with the concentration of 50% into natural tocopherol succinate to perform hydrolysis, controlling the hydrolysis temperature to be 60-70 DEG C and the hydrolysis time to be 4-6 h, after hydrolysis, adding cyclohexane and performing water washing to neutral, separating and performing reduced-pressure distillation on the solvent layer to recover cyclohexane, so as to obtain the mixed tocopherol concentrated liquid with the mixed tocopherol content larger than 90%.

The invention belongs to the technical field of paint removal of a metal material and particularly relates to a paint removal method of a waste metal material. The method comprises the following steps: preparation of a paint remover, applying of the paint remover and paint removal again. Compared with the prior art, the method provided by the invention has the following advantages: in the invention, the prepared paint remover has good paint removal property and relatively strong ability of permeating into the gaps of macromolecular chain segment and easily generates an internal acting force with macromolecules in a paint film so as to destroy the adhesion between the paint film and a substrate and strip the paint film from the metal substrate; the addition of furoic acid and tocopherol succinate is conducive to accelerating the damage of macromolecular chain segment and enhancing the paint removal effect of the paint remover; the paint remover has moderate viscosity; through repeated paint removal and in cooperation with corresponding conditions of paint removal, the paint removal effect is enhanced; the paint removal process causes relatively little damage to the surface substrate; and according to inspection, the content of harmful substances in the paint remover conforms to national standard, and the paint remover can be promoted for application.

The present invention relates to methods for the prevention and treatment of a mammal from radiation-induced internal injury using γ-tocotrienol, α-tocopherol succinate or γ-tocotrienol succinate. Specifically, the present invention relates to methods for preventing and treating radiation-induced injuries in a mammal by (1) subcutaneous, intramuscular, intraperitoneal, or intravascular injection of a therapeutically effective amount of γ-tocotrienol; or (2) oral administration of a therapeutically effective amount of α-tocopherol succinate or γ-tocotrienol succinate or both.

The invention relates to the field of organic synthesis, specifically to a preparation method for tocopherol succinate salt. The preparation method for the tocopherol succinate salt provided by the invention comprises the following steps: hydrogenating dl-alpha-tocopherol in the presence of a precious metal catalyst, subjecting a hydrogenated product and succinic anhydride to an esterification reaction in the presence of alkali so as to prepare a tocopherol succinate intermediate; and subjecting the tocopherol succinate intermediate to salt-forming. The preparation method for the tocopherol succinate salt provided by the invention can effectively improve the purity of a target product, can effectively reduce the content of a single impurity, and can prepare a calcium salt product with a purity capable of reaching 99.9% or above.

The invention discloses an environment-friendly refining preparation process of d-alpha-tocopherol succinate, which comprises the following steps: S1, carrying out esterification reaction on d-alpha-tocopherol and succinic anhydride to obtain d-alpha-tocopherol succinate, heating and dissolving the d-alpha-tocopherol succinate with ethanol, cooling, keeping the temperature below 0 DEG C, adding a proper amount of water, and cooling; s2, carrying out solid-liquid separation, adding a proper amount of water into the separated solid, uniformly mixing, and filtering to obtain water-containing d-alpha-tocopherol succinate; and S3, performing freeze drying to obtain d-alpha-tocopherol succinate powder. According to the method, firstly, ethanol-water is adopted as an organic solvent to crystallize and refine the d-alpha-tocopherol succinate, and the toxicity of the solvent is low; after solid-liquid separation, residual ethanol in the solid is replaced by water, so that only water is discharged in the drying process, and no organic solvent is discharged; and a freeze drying technology is subsequently adopted, so that the product can be in a loose powder shape, a subsequent crushing step is not needed, the generation of dust is reduced, and meanwhile, low-temperature drying is beneficial to reducing oxidative deterioration of the product.

The invention belongs to the field of natural tocopherol succinate preparation, and particularly relates to a method for recovering high-content natural d-alpha-tocopherol succinate from leftovers. The method comprises the following steps of adding 2-10 times by weight of methanol into the pretreated leftovers, adding 0.5-5% of acid catalyst, carrying out esterification reaction at 60-70 DEG C to obtain a corresponding methyl ester product, carrying out reduced pressure distillation to recover methanol, washing with water until the methanol is neutral, carrying out secondary molecular distillation to obtain a secondary light phase which is a methyl ester product, hydrolyzing the methyl ester product in a water-organic solvent system under the catalysis of lipase, and carrying out post-treatment to obtain the high-content natural d-alpha-tocopherol succinate. The method is simple in process, environmentally friendly and high in operability, has very good industrial feasibility, can recover the natural alpha-tocopherol succinate from the leftovers, is used for recycling waste resources, and has important economic value and social value.

The invention belongs to the field of pharmaceutical preparations, and particularly relates to an oxaliplatin-containing nano-micelle preparation and a medical application thereof. The oxaliplatin-containing nano-micelle preparation contains oxaliplatin and an amphiphilic block copolymer micelle, wherein the hydrophilic segment of the amphiphilic block copolymer micelle is pluronic, and the hydrophobic segment of the amphiphilic block copolymer micelle is tocopherol succinate. The oxaliplatin is effectively loaded through a nano-micelle drug carrier, the drug loading capacity is improved, the impurity content in the product is reduced, meanwhile, product stability is enhanced, and the inhibition effect of the oxaliplatin for cancer cells is remarkably improved.

The invention discloses water-soluble O-hydroxyethyl chitosan nanoparticles as well as a preparation method and application thereof. The preparation method comprises the following steps: 1), carrying out oxidative degradation on chitosan in an acidic aqueous solution, adjusting the pH value of the system, adding ethylene oxide, and carrying out ethoxyl etherification I so as to obtain an O-hydroxyethyl chitosan aqueous solution; 2), mixing the O-hydroxyethyl chitosan aqueous solution with a D-alpha-tocopherol succinate solution, and carrying out covalent linkage reaction so as to obtain an aqueous solution of chitosan derivative nanoparticles; 3), mixing the aqueous solution of chitosan derivative nanoparticles with ethylene oxide and carrying out ethoxyl etherification II so as to obtain the water-soluble O-hydroxyethyl chitosan nanoparticles. The prepared water-soluble O-hydroxyethyl chitosan nanoparticles have good water solubility, are relatively small in particle size and controllable in size and have good biocompatibility and anticancer selectivity; when the water-soluble O-hydroxyethyl chitosan nanoparticles are used as drug carriers, the solubility of drugs is increased and bioavailability of the drugs is improved.

The invention provides a whitening, moisturizing, wrinkle-resisting and repairing micro-emulsion, which is prepared from the following components in parts by weight: 1 to 5 parts of marine algae extract, 0.5 to 3 parts of panthenol, 3 to 5 parts of hydroxyethyl urea, 1 to 3 parts of sweet almond oil, 1 to 2 parts of sunflower oil, 1 to 2 parts of tocopherol succinate, 1 to 3 parts of jojoba oil, 1to 5 parts of hyaluronic acid, 0.3 to 1 part of calcium gluconate, 0.3 to 1 part of magnesium gluconate and 0.5 to 1 part of glycyrrhizin. All the components of the whitening, moisturizing, wrinkle-resisting and repairing micro-emulsion supplement each other, so that the compatibility and the permeability between a product and skin of a human body are better; the absorption is more facilitated; the elasticity of the skin is increased, and the effects of moisturization, whitening, wrinkle resisting and the like can be achieved.

The invention discloses a multi-effect care antioxidant night cream and a preparation method thereof. The night cream is prepared from jojoba oil, hydroxypropyl tetrahydrofurantriol, glycine betaine, bio-saccharide gum-1, platinum powder, tocopherol succinate, malachite extract, ascorbyl tetraisopalmitate, aspartic acid, carnosine, scutellaria baicalensis root extract, silybum marianum fruit extract, crithmum maritimum extract, oat peptide, white-flower lily flower extract, tranexamic acid and the balance of water. The multi-effect anti-oxidation care night cream has relatively good skin feeling, moisture retention, spreading property and stability, can moisturize skin cuticle at night, enables the skin to be sufficiently maintained, enables the skin to be moisturized and beautiful, keeps fine, clean, tender, smooth and glossy, and has the effects of moisturizing and meticulous and smooth effects.

The invention discloses a nano organic selenium tablet, which is prepared from the following raw materials in parts by weight: 150 to 170 parts of nano organic selenium powder, 75 to 95 parts of L-ascorbic acid C, 25 to 35 parts of vitamin K2 (fermentation method), 20 to 30 parts of D-alpha-tocopherol succinate, 20 to 195 parts of sorbitol, 10 to 70 parts of lactose, 10 to 35 parts of silicon dioxide, microcrystalline cellulose, and 1 to 3 parts of povidone. The preparation method is characterized by comprising the following steps: weighing main and auxiliary materials according to a certain ratio, carrying out primary crushing and primary grinding and secondary fine grinding to guarantee that the particle size after fine grinding is not larger than 20 nanometer, carrying out boiling granulation after fine grinding, adding a lubricant, and carrying out total mixing, tabletting, coating and packaging. The adopted formula is scientific, the adopted nanocrystallization processing method is a pure physical method, no chemical reaction exists, substances in selenium yeast cells cannot be damaged, harmful substances cannot be brought in, and the selenium-enriched yeast is clean and environmentally friendly, so that the selenium-enriched yeast has the characteristics of being safe to eat, high in selenium content, good in taste, high in bioavailability and good in selenium supplementing effect.