130 results about "Monomethoxypolyethylene glycol" patented technology

The invention is a bio-modified recombinant growth hormone (rhGH) complex and preparing method, making glutamine residue-containing rhGH react with amino donor polyethylene glycol alkyl amine PEG or monomethoxypolyethylene glycol (mPEG) under the catalysis of transglutaminase (mTG), to make acylamide in gamma-bit of the glutamine residue and amino in primary amine bit of the amino donor form an amido bond, thus obtaining it, namely PEG-rhGH or Mpeg-rhGH. It has high biostability and long in vivo half life, applied to prepare permanent injection drugs or develop oral drugs.

The invention discloses a saccharifying method of xylon cellulose through ultrasonic coordinated modified cellulose enzyme, which comprises the following steps: grinding and predisposoing xylon in the raw material through alkaline; reacting activated methoxy carbowax and cellulose enzyme in the citrate-sodium citrate buffer solution to obtain modified cellulose enzyme; blending modified cellulose enzyme, beta-glucosidase, amylase and pectase to obtain composite liquid; adding composite enzyme into predisposed raw material according to corresponding proportion; proceeding enzyme catalytic reaction through ultrasound; filtering; decompressing; evaporating; obtaining condensed sugar liquid.

A methoxy polyethylene glycol (mPEG) modified insulin compound is prepared from INS protein (insulin) and methoxy polyethylene glycol derivative through modifying reaction to obtain the solution of coarse product, ion exchange chromatography, collecting, centrifugal ultrafiltering, concentrating, and freeze drying to obtain high-purity product.

The invention discloses a Pep-1 peptide modified gliomas targeted nano drug delivery system and a preparation method thereof. The nano drug delivery system comprises polymer nano particles prepared by using an amphiphilic block copolymer (Pep-PEG-PLGA) as a carrier material, paclitaxel wrapped and carried by the polymer nano particles, and modified ligand Pep-1 polypeptide on the surfaces of the polymer nano particles. The amphiphilic block copolymer (Pep-PEG-PLGA) is composed of Male-PEG-PLGA and MePEG-PLGA, Pep-1 is adopted as a molecule with targeting function, the amphiphilic block copolymer PEG-PLGA is taken as a carrier material, the Pep-1 polypeptide is modified on the carrier material via covalent binding, and gliomas targeted polymer nano particles are prepared. According to the Pep-1 peptide modified gliomas targeted nano drug delivery system, gliomas targeting can be voluntarily performed, and the uptaking and accumulation of an anti-tumour drug in the gliomas part can be improved, as a result, the gliomas therapeutic effect is improved.

The invention belongs to the field of bio-pharmaceutical products, which provides a chemical modification method for recombinate human rh-Endostatin ('rh-ES' is called for short) through the way of using mPEG-propionaldehyde to be combined on the fixed point of free amino of N-terminal amino acid of rh-ES. Mono-PEG-rhES is the output material, its purity meet the requirements of biological products. It plays a key role in the hydrolysis resistance of trypsin and chymotrypsin, it can be used as long-acting formulations for its stability for pH and temperature and there is a great perspective in the clinical treatment of cancer.

A process for preparing branched polyethylene glycol used to modify macromoleculae and micromoleculae includes such steps as respectively preparing the amino acid's ethylester hydrochloride and carboxymethylated monomethoxy polyethanediol, mixing, sequentially adding TEA, DCC and NHS, reaction, removing protector, and gel separation. Its advantages are simple process, low cost, and high output rate up to 65%.

The present invention relates to a human pancreatic glucagons sample peptide-1 compound and its preparation method. The human pancreatic glucagons sample peptide-1 in said compound is human pancreatic glucagons sample peptide-1(7-37) or human pancreatic glucagons sample peptide-1(7-36)Nh2. Said compound is formed from human pancreatic glucagons sample peptide-1 and monomethoxy polyglycol containing active group activated by succinimide, namely said compound is mPEG-GLP-1.

The invention discloses an oral insulin complexing preparation, which is characterized by the following: allocating 1-15% insulin raw material, 50-97% stable protecting agent, 1-15% carrying medicine carrier, 1-20% absorption promoting agent; setting the stable protecting agent as one or several of carbowax and casein, protamine, albumin and protease inhibitor; setting the carrying medicine carrier as calcium phosphate salt; setting the absorption promoting agent as one or several of salicylic acid, cholate and fatty acid; setting the insulin raw material as human retooling insulin or human retooling insulin chemical trimmed by single methoxy carbowax derivant. This invention also relates to a preparing method of oral insulin complexing preparation. This invention can increase biostability of human retooling insulin and can resist degradation of gastrointestinal tract enzyme.

A drug gel system for relieving conventional skin problems comprises two gel layers and a supporting layer. The drug gel system for relieving the conventional skin problems is characterized in that the gel layers are adsorbed on the supporting layer and located on the outer layers, and the supporting layer is located in the middle; the gel layers are prepared from, by weight, 3.0%-3.5% of chitosan, 3.0%-3.5% of methoxy polyethylene glycol and 0.01%-0.1% of collagen, and the gel layers contain effective constituents of all the drugs. The drug gel system is mainly used for relieving the conventional skin problems of the face and can be made into various-shaped masks, such as the face entirety mask, the nose mask and the eye mask, suitable for any facial skins. The drug gel system has the temperature-sensitive characteristic and can well adapt to the skin temperature to form a gel mask, and therefore the purpose of relieving the conventional skin problems is achieved.

The invention discloses a preparation method of a quaternary degradable antibacterial agent, and the preparation method comprises the following steps: homopolymerizing cyclic aliphatic carbonate monomers containing bromine functional groups, namely 2,2-dibromo-methyl trimethylene carbonate (DBTC) monomers or copolymerizing the 2,2-dibromo-methyl trimethylene carbonate monomers with aliphatic cyclic ester, or copolymerizing the 2,2-dibromo-methyl trimethylene carbonate monomers with the aliphatic cyclic ester or dihydroxy polyethylene glycol, or copolymerizing the 2,2-dibromo-methyl trimethylene carbonate monomers with the aliphatic cyclic ester or single methoxy polyethylene glycol; and further reacting an obtained polymer with alkylamine, thus obtaining the quaternary degradable polyester antibacterial agent with antibacterial performance. The antibacterial agent provided by the invention integrates the advantages of biocompatibility and degradability and not only has good antibacterial performance, but also has no harm to an environment, thereby being an environment-friendly antibacterial material; as an additive, the antibacterial agent provided by the invention has potential application prospects in food packaging materials, fibers, coatings, medical field and the like.

The invention relates to double-pH-response amphiphilic copolymer, the molecular formula of the double-pH-response amphiphilic copolymer is MPEG-Dliable-PAE-g-Chol, and the structure of the double-pH-response amphiphilic copolymer is as shown in formula I. The double-pH-response amphiphilic copolymer is copolymerized by hydrophilic block methoxy polyethylene glycol, hydrophobic cholesterol and pH response block poly(beta-amino ester). The double-pH-response amphiphilic copolymer has the advantages that the double-pH-response amphiphilic copolymer can self-assemble in an aqueous solution to obtain a nanoscale micellar system, the inner layer of the nanoscale micellar system is a hydrophobic core modified by cholesterol, the middle of the nanoscale micellar system is a pH-sensitive-response PAE layer, the shell of the nanoscale micellar system is hydrophilic block MPEG, the hydrophilic shell is connected sensitive middle layer through a pH-sensitive benzimide bond, the cell intake of a micelle drug-loading system is increased effectively while the requirements of high entrapment performance, stable system structure, long in-vivo circulation time, stability under neutral conditions and controllable drug release under weak acid conditions of hydrophobic drugs are satisfied, and accordingly drug bioavailability is increased, and a tumor treatment effect is optimized.

The invention discloses a growth factor slow release microballoon which comprises a nerve growth factor, monomethoxyl poly (ethylene glycol)-poly (lactic acid) with weight-average molecular weight of 10-10.5 ten thousand, a cosolvent, an emulsifying agent and a stabilizing agent, wherein the mass ratio of the nerve growth factor to the monomethoxy polyethylene glycol-polylactic acid is (0.8-1.2):(2.4-3.6*10<4>), and the average particle diameter of the slow release microballoon is 52.9-95.5mu m. The invention also provides a growth factor slow release microballoon preparation comprising the growth factor slow release microballoon and 6.0-9.0*10<3> parts by weight of polyoxyethylene polyoxypropylene ether. The bone injury animal experiment result shows that the growth factor slow release microballoon and the preparation thereof have preferable therapeutic effects on bone injuries, and are obviously superior to the control group and the blank group (P is less than 0.05).

The invention discloses a curcumin nanoparticle preparation. Curcumin is taken as a raw material, linear-dendritic monomethoxypolyethylene glycol-polycaprolactone is taken as a medicament carrier, and the curcumin nanoparticle preparation comprises the following components in parts by weight: 1 part of curcumin and 5-10 parts of linear-dendritic monomethoxypolyethylene glycol-polycaprolactone. A preparation method comprises the following steps: dissolving curcumin and linear-dendritic monomethoxypolyethylene glycol-polycaprolactone in an organic solvent, performing rotary evaporation to remove the organic solvent after full dissolution to obtain a medicament-containing thin film, adding into a water phase, performing hydratation at 50-80 DEG C to obtain a nanoparticle solution, and filtering by a microporous filter membrane to obtain the curcumin nanoparticle preparation. The nanoparticle preparation disclosed by the invention can ensure that the nanoparticle preparation is less prone to being swallowed by a reticuloendothelial system in vivo, can realize a slow-release effect and is conductive to clinical application.

The invention relates to the biomedical technical field, in particular to polyethylene glycol modified human serum albumin and a preparation method thereof. The polyethylene glycol modified human serum albumin comprises sulfydryl of 34-bit cysteine residues on albumin molecules and N-terminal amino or free amino group combined polyethylene glycol. Modifiers adopted by the fixed-point single modification are respectively polyethylene glycol-maleimide and polyethylene glycol-propionaldehyde; modifiers adopted by the free amino group random modification are respectively polyethylene glycol-succinimide active ester or methoxy-polyethylene glycol activated by cyanuric chloride; and the modification rate of the free amino group on the albumin molecules combined with the polyethylene glycol is 3%-7%. Compared with the natural albumin, the polyethylene glycol modified human serum albumin has the excellent characteristics of prolonged half-life period, slow plasma elimination, and the like and is beneficial to reducing the medication frequency and releasing the rare albumin source.

The invention belongs to the technical field of biology, relating to a modified glutathione peroxidase and a preparation method thereof. The preparation method comprises the following steps of: reacting single-chain monomethoxypolyethylene glycol (mPEG1) with amino-groups of glutathione peroxidase through free chlorine atoms so as to connect the mPEG1 to the glutathione peroxidase, wherein the activated single-chain mPEG1 is used as a modifier to react with the glutathione peroxidase at 4-37 DEG C with a pH value of 7.0-10.0, and the mass ratio of the single-chain mPEG1 to the glutathione peroxidase is (20-100):1; adding glutathione (GSH) by a proportion of 1:1 of the modifier to the GSH used as a terminator to terminate the reaction after reacting for 15-60min; and then removing the terminator by using 30 thousands of ultrafiltration membranes for ultrafiltering to obtain the modified glutathione peroxidase. The amino-group modification rate of the modified glutathione peroxidase is controlled to be 40-45 percent, and the enzymatic activity retention rate exceeds 100 percent.

The invention discloses a sterilization / endotoxin neutralization polypeptide modified by polyethylene glycol, which consists of a formula as follows: X-Y-BNEP-OH or H-BNEP(i-Y-X)-OH, wherein, X is polyethylene glycol or single-methoxy polyethylene glycol, Y is a linking group, i is 1 or 3 or 13 or 14, representing the position number of lysine with a modified on side-chain amino group in an amino acid sequence; and BNEP is the sterilization / endotoxin neutralization polypeptide which has an amino acid sequence shown by SEQ ID No.1; the modification polypeptide, while maintaining the endotoxin neutralization activity of BNEP, prolongs the half-life in vivo of BNEP, and shows potential for being developed into new endotoxin neutralization medicaments, thus being capable of providing new curative medicaments for treating patients of severe diseases such as pyaemia, septic shock and the like. The invention also discloses a preparation method of the modification polypeptide, which has high product yield and high purity, thus being capable of realizing fixed-point modification of polyethylene glycol of synthetic polypeptide.

The invention relates to a method for preparing amphoteric chitosan water reducing agents. The amphoteric chitosan water reducing agents are prepared from chitosan, methoxy polyethylene glycol, acetic anhydride and chlorosulfonic acid through reaction. The method has the innovation point that the natural chitosan is used as raw materials, methoxy polyethylene glycol (MPEG) and hydrophilic sulfo groups are introduced, and the novel amphoteric chitosan water reducing agents are prepared. The prepared amphoteric chitosan water reducing agents have the advantages that the product performance is stable, the cement adaptability is high, the compatibility is good, the cement initial net pulp flowability can reach a value higher than 250mm (W / C=0.29), the concrete water reducing rate can reach about 25 percent, the one-hour collapsbillity can reach 140mm, and in addition, no pollution is caused on the environment. The preparation method has the advantages that the preparation process is noveland unique, the industrial production is convenient, and the like.

The invention discloses a hydrophilic polymer of resveratrol conjugate and a preparing method thereof. The hydrophilic polymer of resveratrol conjugate has the following structure, wherein P represents monomethoxy-polyethylene glycol acyl, monomethoxy-polypropylene glycol acyl, polyglutamic acid acyl or poly aspartic acid acyl; n represents 1-3; D represents resveratrol monomer; and L represents connecting ester bond of -O-. In the invention, insoluble resveratrol is modified to soluble hydrophilic polymer of resveratrol conjugate, so that the application range of resveratrol is widened.

The invention relates to a monomethoxy carbowax silane derivant, the method and usage for it. The structural formula ó±of such alkoxy silane carbowax derivant is (R1O)zR2(3-z)Si(CH2)nA(CH2CH2O)mCH3, wherein R1ú¼R2 represent separately linear or branched chain alkane with 1-10 carbon atoms, aralkyl or aryl radicals; A means oxygen atom or sulfur atom; z equals to 1, 2 or 3; while n is an integral between 1 and 12; m also is an integral between 1 and 15. Such a derivant can be produced by reacting monomethoxy carbowax with organic amine and p-toluene sulfonyl chloride to get monomethoxy carbowax ethyl p-toluenesulfonate; then with alkoxy silane compound and sodium alcoholate to obtain the derivant of the invention. Such derivant can be used as an absorb depressant to block non-specific absorption of biomolecule on the surface of inorganic material, with gentle condition and simple process.

The invention discloses a method for synthesis of monomethoxy poly(ethylene glycol), including the steps that ethylene oxide is transferred to a dried ethylene oxide tank after calcium-hydrogen treatment, the autoclave is processed, dried methyl alcohol is added into the potassium methoxide to prepare solution with 10-30 percent of mass fractions; the achieved solution is added into the autoclave, the autoclave is heated to 90 DEG C, the ethylene oxide is added into the autoclave and stirred under 120 plus and minus 2 DEG C continuously until the pressure of the reaction system approaches to normal pressure, then the temperature is lowered to 80 DEG C, and the product of reaction is transferred out; the pH of the reaction product is adjusted to be 7.0 by citric acid; finally, the desired monomethoxy poly(ethylene glycol) is achieved after being dried. The purity of the product is proved very high by gel permeation chromatography, and the molecular weight distribution is very narrow. The polyoxyethylene compound used as the initial medical material is mainly applied to drug release system.

The invention discloses a prodrug of oridonin with polyethylene glycol serving as a vector. The prodrug has the structural formula shown in the specification, wherein n is an integer from 110 to 910. The preparation method comprises the following steps: (1) preparing carboxylation oridonin: performing reaction to oridonin and succinic anhydride, thus obtaining carboxylation oridonin; and (2) synthesizing prodrug of oridonin modified via methoxypolyethylene glycol amine: reacting the mono-methoxypolyethylene glycol amine with carboxylation oridonin, thus obtaining the prodrug of oridonin which is in form of white solid. According to the prodrug of oridonin with polyethylene glycol serving as the vector disclosed by the invention, the succinic acid serves as a joint arm for combining the oridonin with the hydrophilic polyethylene glycol derivative, so that the dissolubility of the oridonin is improved, the performance of the medicine is enhanced and improved, and the stability of the oridonin is improved; and the prodrug can be decomposed and fallen at a proper environment, so as to release the oridonin, so that the acting time in the organism can be increased, and the purpose of long circulation can be achieved.

The invention belongs to the biotechnology field, which particularly relates to a deuterohemin short peptide compound modified by the Monomethoxy-Polyethylene Glycol Succinimidyl Ester derivatives and the preparation method for the compound, which adds phosphate buffer into the water solution prepared by a deuterohemin 6-mer peptide, and then reacts by adding the solid powder of active Polyethylene Glycol derivatives or the acetonitrile solution of the Polyethylene Glycol derivatives and obtains the deuterohemin 6-mer peptide modified by the Polyethylene Glycol by chromatographic separating of the reaction mixture with the reversed-phase high performance Liquid Chromatography. The deuterohemin 6-mer peptide modified by the Polyethylene Glycol of the invention can basically maintain the biological activity of the deuterohemin 6-mer peptide, and has better stability than the deuterohemin 6-mer peptide without any modification. The preparation method of the deuterohemin 6-mer peptide modified by the Polyethylene Glycol of the invention is simple and easy to operate, while the structure general formula of the deuterohemin 6-mer peptide modified by the Polyethylene Glycol is shown on the right, wherein, R stands for a DhHP-6 molecule eliminating an NH2.

The invention discloses oral insulin micelle nanoparticles and a preparation method thereof. The preparation method comprises the following steps: dissolving an amphiphilic block copolymer with pH (Potential of Hydrogen) sensitivity, i.e., [poly(methyl methacrylate-co-methacrylate)-b-monomethoxypolyethylene glycol polymethacrylate P(MMA-co-MAA)-b-PPEGMA], into an organic solvent; dissolving insulin into a diluted acid solution with the concentration of 0.0001mol / L; then slowly dropwise adding an insulin solution into a polymer solution; sufficiently stirring; then transferring a mixed solutioninto a dialysis bag and dialyzing for 24 to 48h in the environment with the pH (Potential of Hydrogen) of 4.5 to 6.0; removing an organic solvent to form a polymer drug-loading micelle; centrifuging,freeing and drying to obtain the oral insulin micelle nanoparticles which have relatively uniform sizes, are micro-spherical and have the remarkable pH sensitivity and the quality entrapment rate of85 percent or above.

The invention relates to a tumor microenvironment reduction responsive nano-drug and a preparation method thereof. The nano-drug is a nano-scale monomethoxypolyethylene glycol and celastrol compound (MPEG2k-SS-Cel) drug which takes safe and non-toxic monomethoxypolyethylene glycol (MPEG2k) with the molecular weight of about 2000 as a hydrophilic material, hydrophobic natural antitumor drug celastrol is chemically bonded through-SS-, MPEG2k-SS-Cel can be self-assembled into a nano-micelle with the particle size of about 140 nm, and the monomethoxypolyethylene glycol is used as a hydrophilic segment to embed the celastrol outside the micelle. The drug is bonded with the celastrol through the hydrophilic monomethoxypolyethylene glycol so as to overcome the defect that celastrol is difficult to effectively utilize in vivo due to hydrophobicity of the celastrol, and the nano-micelle has the characteristic that the micelle disintegrates and releases the drug in a tumor microenvironment due to fracture response under the condition of high-concentration glutathione (GSH) through the -SS- in the middle. Cell experiments detect that the nano-drug has efficient treatment effects.

The invention discloses an mPEG-MAL-aGLP-1 composite. The mPEG-MAL-aGLP-1 composite is formed by connecting human glucagon-like peptide-1 derivative aGLP-1 with monomethoxypolyethylene glycol-maleimide mPEG-MAL by virtue of an addition reaction, wherein a sulfydryl -SH of amino acid of a terminal C of aGLP-1 and a terminal double bond of mPEG-MAL form a covalent bond, so that aGLP-1 and mPEG-MAL are connected; aGLP-1 is of any structure shown in Seq ID No.2, Seq ID No.3 or Seq ID No.4. The mPEG-MAL-aGLP-1 composite avoids polymorphism of a modification site, so that follow-up purification is extremely simple, yield is high, and cost is low; a half-life period of the composite is further prolonged, continuous blood sugar level reducing time is 24 hours, and administration can be realized in an oral manner, so that the mPEG-MAL-aGLP-1 composite can be applied to treatment on diabetes.

The invention relates to monomethoxy polyethylene glycol modified ezetimibe and a preparation method thereof. The modified ezetimibe has the following general molecular formula as shown below in the specification, wherein n is the integer ranging from 1 to 24. The preparation method comprises the following steps of (1) adopting monomethoxy polyethylene glycol as a reactant to prepare a compound I;(2) carrying out condensation reaction on the compound I and the ezetimibe under the condition of the interaction of a filtrate reducer and alkali, and preparing the required modified ezetimibe. Thepreparation method is short in process flow, simple in reaction operation, less in side reaction, low in cost, high in reaction selectivity, and higher in yield.

The invention relates to a method for modifying oxalate decarboxylase, particularly a method for modifying oxalate decarboxylase with monomethoxypolyethylene glycol, belonging to the technical field of biochemical engineering. The method comprises the following steps: preparation of recombinant oxalate decarboxylase, activation of monomethoxypolyethylene glycol (mPEG), modification of oxalate decarboxylase and the like. The modified oxalate decarboxylase has higher heat stability, pH adaptability, heat resistance and trypsinase tolerance. The method solves the realistic problem that the oxalate decarboxylase in use can be influenced by digestion of gastric acid and proteinase and can be easily digested to lose activity at present. The method can be used for preparing an enzyme preparation for preventing and treating calculus caused by oxalate crystallization.

The invention discloses a tolyltriazole-containing polyethylene glycol protein modifier, a preparation method thereof and the application thereof, wherein the tolyltriazole-containing polyethylene glycol protein modifier has the following chemical general formula, wherein A is linear-chain alkyl group of which the carbon atom number is 0-20. The preparation method of the modifier comprises the following step of carrying out copper-catalyzed click chemistry on azide group-containing methoxy polyethyleneglycol and terminal acetylene link and succinimide-containing alkane derivative. The tolyltriazole-containing polyethylene glycol protein modifier provided by the invention can be used for modifying the hemoglobin, particularly used for modifying the bovine hemoglobin and the hemoglobin from human blood for human body. According to the method of the copper-catalyzed click chemistry, various functional groups can be effectively modified, and the invention is simple in technology, low in cost, and convenient for industrial production.

The invention belongs to the fields of biological materials and nano materials, and relates to a mixed micelle with hypoxia and pH double responsiveness and a preparation method of the mixed micelle.The method comprises the following specific steps: a product of an esterification reaction of carboxylated monomethoxypolyethylene glycol and p-hydroxyazobenzene is used as a macroinitiator to initiate atom transfer radical polymerization of a cyclocaprolactone monomer; ring-opening polymerization cyclohexanolide is used as a macroinitiator to initiate atom transfer radical polymerization of a N,N-diethylaminoethyl methacrylate monomer; and two block copolymers are used to prepare the mixed micelle by a solvent evaporation method according to a certain charge ratio. The mixed micelle preparedby the method provided by the invention has the hypoxia and pH dual responsiveness, and broad application prospects in biomedical applications, drug carriers, targeted therapies and the like; and thepreparation method provided by the invention is simple and easy to implement, the raw materials can be industrially produced, and the method has very good promotion and application value.

The present invention relates to one kind of polyethylene glycol modified zidovudine conjugate and its preparation process and application. The polyethylene glycol modified zidovudine conjugate with the structure as shown is prepared through dissolving zidovudine, p-dimethyl aminopyridine and dicyclohexyl carbon diimide in proper amount of dichloromethane, dropping equi-molar ratio dichloromethane solution of mPEG-SA to react, filtering, adding cold ether in 45-55 times volume into the filtrate to obtain white precipitate, filtering to separate the precipitate, and drying to obtain precursor methoxy polyethylene glycol zidovudine conjugate for preparing anti-AIDS medicine.