43results about How to "Enhance amphipathic" patented technology

The present invention relates to amphiphilic drug-oligomer conjugates capable of traversing the blood-brain barrier ("BBB") and to methods of making and using such conjugates. An amphiphilic drug-oligomer conjugates comprise a therapeutic compound conjugated to an oligomer, wherein the oligomer comprises a lipophilic moiety coupled to a hydrophilic moiety. The conjugates of the invention further comprise therapeutic agents such as proteins, peptides, nucleosides, nucleotides, antiviral agents, antineoplastic agents, antibiotics, etc., and prodrugs, precursors, derivatives and intermediates thereof, chemically coupled to amphiphilic oligomers.

Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, enteral, subcutaneous, pulmonary, and intravenous forms of the compounds and conjugates may be prepared as treatments and/or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the natriuretic compound are also disclosed, having an amino acid sequence that is other than the native sequence.

Modified n atriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, subcutaneous, and intravenous forms of the compounds and conjugates may be prepared as treatments and/or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the n atriuretic compound are also disclosed, having an amino acid sequence that is other than the native sequence.

The invention discloses a preparation method of chiral nanometer copper oxide with optical activity. The preparation method comprises the following steps of: (1) dissolving an achiral anionic surface-active agent and a chiral small molecule into water at room temperature to obtain an achiral anionic surface-active agent and chiral small molecule water solution; (2) adding inorganic copper salt to the achiral anionic surface-active agent and chiral small molecule water solution, and stirring to react for 10-60 minutes; (3) adding alkali to reaction liquid obtained from the step (2), then increasing temperature to 100-200 DEG C, and reacting for 30 minutes-6 hours; (4) after the reaction is finished, centrifugalizing or filtering the reaction liquid obtained from the step (3), and washing and drying to obtain the chiral nanometer copper oxide with the optical activity. The prepared chiral nanometer copper oxide with the optical activity shows very uniform flower-shaped appearance and shows outstanding optical activity by having chirality.

Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, decreasing arterial blood pressure and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, enteral, subcutaneous, pulmonary, and intravenous forms of the compounds and conjugates may be prepared as treatments and/or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the hBNP compound are also disclosed, having an amino acid sequence that is other than the native sequence.

The application relates to antimicrobial agents against Gram-negative bacteria, in particular to fusion proteins composed of an enzyme having the activity of degrading the cell wall of Gram-negative bacteria and a peptide stretch fused to the enzyme at the N- or C-terminus, as well as pharmaceutical compositions comprising the same. Moreover, it relates to nucleic acid molecules encoding such a fusion protein, vectors comprising said nucleic acid molecules and host cells comprising either said nucleic acid molecules or said vectors. In addition, it relates to such a fusion protein for use as a medicament, in particular for the treatment or prevention of Gram-negative bacterial infections, as diagnostic means or as cosmetic substance. The application also relates to the treatment or prevention of Gram-negative bacterial contamination of foodstuff, of food processing equipment, of food processing plants, of surfaces coming into contact with foodstuff, of medical devices, of surfaces in hospitals and surgeries.

The invention discloses a micromolecular thick oil viscosity reduction polymer and a preparation method thereof. The micromolecular thick oil viscosity reduction polymer comprises the following raw material components: 10 wt.% to 20 wt.% of an acrylamide (AM) monomer, 1 wt.% to 10 wt.% of a sodium acrylate monomer, 1 wt.% to 3 wt.% of a hydrophobic monomer, 1 wt.% to 3 wt.% of a temperature-resistant monomer, 0.5 wt.% to 2.5 wt.% of a surface active monomer, 0.7 wt.% to 2.5 wt.% of a chain transfer agent, 0.08 wt.% to 2 wt.% of an initiator and the balance being water. The micromolecular thick/oil viscosity reduction polymer has quick dissolving performance and good injection performance, can emulsify thick oil, has oil displacement and profile control performance at the same time, and canbe suitable for thick oil recovery of offshore oil reservoirs and low-permeability oil reservoirs.

The invention discloses a poloxamer-adriamycin conjugate with an anti-tumor effect and a preparation method thereof. The poloxamer-adriamycin conjugate has micelle property, is a high-molecular polymer which contains terminal carboxyl group and is prepared by reaction between poloxamer and succinic anhydride, and the terminal carboxyl group in the polymer and primary amino radical in adriamycin are directly bound in an amido link way. Compared with an adriamycin raw material drug, the poloxamer-adriamycin conjugate has the following advantages: the anti-tumor activity of the covalent bonding adriamycin in the poloxamer-adriamycin conjugate is maintained, the drug resistance of tumor is reduced; the poloxamer-adriamycin conjugate has the property of self-assembly formed micelle, and the critical micelle concentration of the conjugate is lower than that of polyxamer; and the micelle of the poloxamer-adriamycin conjugate can be entrapped with other medicaments with the anti-tumor effect in a physical entrapping mode, so that the aim of combined treatment of anti-tumor medicaments can be achieved.

The invention discloses a feed additive for improving the growth performance of a nursery pig. The invention discloses a preparation method of the feed additive for improving the growth performance ofthe nursery pig, wherein the preparation method comprises the following steps: mixing Fuzhuan tea, jujube, star anise and raw ginger, crushing, adjusting the water content, adding a compound enzyme preparation, mixing evenly, carrying out enzymatic hydrolysis, and filtering to obtain a first material and an enzymatic hydrolysate; adding the first material into absolute ethyl alcohol, soaking, andcarrying out ultrasonic assisted reflux extraction to obtain an extract liquid and a filter residue; adding the filter residue to water, soaking, cooking and filtering to obtain a filtrate; mixing the enzymatic hydrolysate, the extract liquid and the filtrate, and drying at low temperature to obtain a second material; adding the second material, excipients and a cladding wall material into water,mixing evenly and spray-drying to obtain the feed additive for improving the growth performance of the nursery pig. The invention discloses an application of the feed additive for improving the growth performance of the nursery pig.

The present invention relates to an amphiphilic cyclic phosphazene trimer which is biocompatible and a method for preparing the same. The present invention also relates to pharmaceutical formulations of hydrophobic drugs that are micelle-encapsulated by the amphiphilic cyclic phosphazene trimer and a method for preparing the same.

The invention discloses poloxamer-adriamycin conjugate (DOX-P) micelle with anti-tumor drug resistance and a preparation method of the DOX-P micelle. The synthetic process of the DOX-P comprises the steps of firstly, reacting poloxamer with succinic anhydride to obtain high-molecular polymer of which the tail end contains carboxyl; and then, directly bonding the carboxyl at the tail end of the polymer with primaquine group in the adriamycin in an amido bond mode. The DOX-P has the capability of forming the micelle; and compared with the adriamycin bulk drug, the adriamycin subjected to covalent binding in the DOX-P micelle has the advantages that the anti-tumor activity of the adriamycin is maintained, the drug resistance of the tumor is overcome, and the stability of the adriamycin is better than that of poloxamer micelle.

The invention discloses a dihydroartemisinin higher fatty acid ester and a preparation method thereof. The method adopts lipase as a catalyst, carries out a structure modification on the 10th position carbon of dihydroartemisinin, and then subjecting the hydroxyl group on the 10th carbon of dihydroartemisinin to carry out an esterification reaction with higher fatty acid ester. Specifically, the preparation method takes lipase Novozyme 435 as the catalyst, stearic acid and lauric acid as the acyl group donors, tertiary butanol as the reaction solvent, and 4A molecular sieve as the water absorbing agent during the esterification reaction. The prepared artemisinin esterification product has an oil and water amphiphilicity, and shows a good specificity in the in-vitro antimicrobial tests. The dihydroartemisinin higher fatty acid ester and the preparation method thereof have an important meaning on improving artemisinin solubility in water and oil so as to make artemisinin into a proper dosage form.

The invention discloses porphyrin-modified cell-penetrating peptide and preparation and application thereof, and belongs to the technical field of design and synthesis of antitumor drugs. Carboxyl ofpyromagnesium chlorophyll a is utilized and is linked to cell-penetrating peptide with exposed amino through amidation. The pyromagnesium chlorophyll a which is a porphyrin derivative and has similarproperty to hemoporphyrin can be embedded into a cavity of human serum albumin, so that the in-vivo circulation time of polypeptide is prolonged. In combination with the photodynamic effect of porphyrin, the peptide has a more efficient killing effect on tumors. The compound is simple in synthetic method, easily available in raw materials, low in cost, less in side reaction, high in yield, easy topurify and beneficial to industrial production.

The invention provides high-gloss water-based paint and a preparation method thereof.The water-based paint is prepared from modified ethyl acrylate, a filler, a modified dispersing agent, an antifoaming agent, a thickener, a leveling agent, a wetting agent, a modified curing agent and water, and the preparation method comprises the steps that mixing the modified dispersing agent, the modified ethyl acrylate and the water to prepare a first mixed solution; and adding the filler, the antifoaming agent, the thickener, the leveling agent and the wetting agent into the first mixed solution to prepare a second mixed solution, adding the modified curing agent into the second mixed solution, and uniformly stirring to obtain the high-gloss water-based paint. According to the invention, the phenomenon that prickly heat easily occurs on the surface of a paint film of conventional water-based paint is overcome, and meanwhile, the improved water-based paint still has good surface performance and has good application prospect.