160 results about "Anticoagulant effect" patented technology

The invention relates, in part, to methods and compositions for the intracellular delivery of polysaccharides. In particular, the methods and compositions relate to the intracellular delivery of glycosaminoglycans, such as heparin. The invention in other aspects relates to the use of glycosaminoglycans for the treatment of proliferative disorders, such as cancer. The invention is still other aspects relates to improving cell viability. The invention also relates to the delivery of polysaccharides while avoiding unwanted effects of the polysaccharides. For example, heparin can be delivered while avoiding its anticoagulant effects.

A blood coagulation system analysis device capable of analyzing a blood coagulation system with high accuracy, and a method and a program for analysis of a blood coagulation system are proposed.The blood coagulation system is observed as a temporal change in permittivity before the viscoelasticity manifestation timing (timing at which blood starts to clot from the viewpoint of viscoelasticity (in greater detail, timing at which active polymerization of fibrin monomers starts)). A permittivity of blood which is positioned between a pair of electrodes is measured at predetermined time intervals after the anticoagulant effect acting on the blood is ended, and from the measurement result, a degree of the action of the blood coagulation system is analyzed.

Aiming at the conditions that heparin has severe bleeding side effects in clinical practice and clinical application thereof is restricted, the invention discloses a technique for producing ultra-low molecular heparin sodium (calcium). The technique comprises the following steps of: taking heparin sodium solution, adding sodium nitrite solution for cracking; adjusting the lysis buffer by using alkaline; absorbing impurities by using an anion-exchange column; washing for obtaining ultra-low molecular heparin calcium; carrying out filtration by using an ultrafiltration membrane and obtaining a precipitate by using alcohol; and after desalting, dehydration, re-precipitation, cooling and drying, obtaining a finished product of ultra-low molecular heparin calcium. The product has better and safer antithrombotic effect under low level of anticoagulation, and can be widely used for preventing and treating diseases such as deep vein thrombosis, pulmonary embolism, disseminated intravascular coagulation, and the like.

Partially desulphated glycosaminoglycan derivatives are described, particularly heparin, and more particularly a compound of formula (I) where the U, R and R1 groups have the meanings indicated in the description. These glycosaminoglycan derivatives have antiangiogenic and heparanase-inhibiting activity and are devoid of anticoagulant activity.

Heparin-binding peptides are provided of the formula R1(X1B1B2X2B3X3Y1R2)nR3, R1(X1B1B2B3X2X3B4X4Y1R2)nR3, and C(X1B1B2B3X2X3B4X4)nC; wherein X1, X2, X3, and X4 are independently selected from the group consisting of hydropathic amino acids; B1, B2, B3, and B4 are independently selected from the group consisting of basic amino acids; C is cysteine; Y1 is zero or one to ten amino acid residues, wherein at least one amino acid residue is proline; n is an integer from one to ten; and R1, R2, and R3 are independently selected segments containing from zero to twenty amino acid residues, provided, at least one of the segments R1, R2, and R3 comprises at least one hydrophobic amino acid residue. The peptide C(X1B1B2B3X2X3B4X4)nC is optionally cyclized via a disulfide bond formed between cysteine residues. The peptides are administered to reduce plasma LMWH and heparin levels and to reduce the anticoagulant effects of heparin and LMWH. The peptides are also administered to inhibit microbial growth and to inhibit mast cell serine proteases involved in various diseases and disorders. The peptides are also administered as carriers to deliver active agents.

Partially desulphated glycosaminoglycan derivatives are described, particularly heparin, and more particularly formula (I) compounds, where the U, R and R1 groups have the meanings indicated in the description. Said glycosaminoglycan derivatives are endowed with antiangiogenic activity and are devoid of anticoagulant activity.

The present invention provides one kind of compound with anticoagulant effect, and is especially new preparation process of clopidogrel and its pharmaceutical salt. The preparation process includes the following four steps: 1. resolving recemized methyl o-chlorophenyl glycinate to obtain (+)-methyl o-chlorophenyl glycinate and (-)-methyl o-chlorophenyl glycinate; 2. recemizing (-)-methyl o-chlorophenyl glycinate to obtain recemized (-)-methyl o-chlorophenyl glycinate; 3. repeating the steps 1 and 2; and 4. preparing clopidogrel with (+)-methyl o-chlorophenyl glycinate obtained in the step 1 and preparing the obtained clopidogrel into corresponding salt. The process of the present invention has simple path, short circulating period, low cost, high product purity, less toxic side effect and corrosion to the production apparatus.

Partially desulphated glycosaminoglycan derivatives are described, particularly heparin, and more particularly formula (I) compounds where the U, R and R1 groups have the meanings indicated in the description. Said glycosaminoglycan derivatives are endowed with antiangiogenic and heparanase-inhibiting activity ans are devoid of anticoagulant activity.

The present invention provides compounds and methods for antagonizing the anticoagulant effect of an anticoagulant agent that is selected from UFH, LMWH, and a heparin / LMWH derivative in a patient comprising administering to the patient a compound of the invention or a salt thereof, or a composition comprising the same.

The invention belongs to the technical field of plant extraction, and particularly relates to anticoagulant blackberry seed polysaccharides, and an extraction separation method and application thereof. The extraction separation method comprises the following steps: after pulverizing blackberry seeds, carrying out water extraction and alcohol precipitation to obtain crude polysaccharides, and respectively carrying out DEAE-52 cellulose column chromatography and SephadexG-100 gel column chromatography to obtain the three polysaccharides. The special extraction separation method is adopted to separate the three polysaccharides from the blackberry seeds; and the inspection on the in-vitro coagulation effect of the three polysaccharides proves that the three polysaccharides have favorable anticoagulant effect.

The invention discloses a dentritic heparin nano-material and a modified biological type artificial blood vessel. The dentritic heparin nano-material provided by the invention has a terminal branch unit shown in formula I, and is obtained by a reaction between polyamidoaminedendrimers using hydrazide group as a terminal group and heparin, wherein the inner core of the polyamidoaminedendrimers is cystamine, and the dentritic frame of the polyamidoamine dendrimers is hydrazide modified polyamidoamine including -0.5, 0.5, 1.5, 2.5, 3.5, 4.5, 5.5, 6.5 and 7.5; and the connection between the heparin and polyamidoamine is a glycosidic bond formed a reaction between the hydrazide on the surface of the polyamidoamine and the heparin reducing terminal. The disulfide bond in the dentritic heparin nano-material is cut through a reducing agent to obtain a sulfydryl site which can react with an intravascular stent material; and the surface in a blood vessel can be activated through a coupling agent of a two-way functional group, and the heparin with a branch structure can be fixed on the inner surface of the blood vessel material through chemical bond covalence, so that a composite artificial blood vessel with an anticoagulation effect can be obtained.

The invention discloses a synthesis method of a 6-O-carboxymethyl chitosan sulfation product. The method comprises the following steps: (1) chitin alkaline treatment of chitin; (2) carboxymethylation of C6-O site of chitin; (3) deacetylation reaction of 6-O-carboxymethyl chitin; and (4) sulfation of 6-O-carboxymethyl chitosan. The synthesis method disclosed by the invention is a bran-new method for selectively replacing and controlling the replacement rate by using chitin. The synthesis product of the method provides N-site -SO3H with main anticoagulant activity and introduces -COOH, so that a lot of -COOH and SO3H which have negative electricity in the molecular structure are regularly distributed, and an anticoagulant effect of heparinoid is generated by the synergistic effect. High molecular polysaccharide is a heparinoid drug which is selectively modified by chitin via a safe reagent, so that reagent pollution of bulk drugs is reduced, the virus contamination risk of heparin biological extraction is avoided, the safety performance of the drug in the clinical experiment is more excellent in theory as compared with heparin sodium, so the 6-O-carboxymethyl chitosan sulfation product provided by the invention is expected to serve as a cheap direct thrombin inhibitor to replace heparin sodium anti coagulation drugs.

The invention provides a pharmaceutical composition containing active procyanidins and prasugrel or the pharmacologically acceptable salt thereof. The procyanidins and the prasugrel are used in a combined manner, a more effective method for curing thrombotic diseases is found, after trail for many times, the prasugrel and the procyanidins (an extract of traditional Chinese medicine) are creatively and effectively combined together, the effect of applying the procyanidins to inhibit the thrombosis in a combined manner is discovered unexpected in the process of applying the prasugrel to cure the thrombotic diseases, and not only the anticoagulant effect of the prasugrel is free from the influence of the procyanidins, but also a good effect is achieved in the aspect of reducing the adverse reaction of bleeding after the use of the prasugrel and the procyanidins in a combined manner, therefore, the risk of bleeding is greatly reduced when the advantages of good anticoagulant activity and fast effect of the prasugrel during the antiplatelet aggregation are fully exerted, the risk of bleeding of the prasugrel during the antiplatelet aggregation is effectively reduced and the adverse reaction of the prasugrel is greatly reduced.

The invention discloses an anticoagulant hydrogel coating capable of catalyzing the release of nitric oxide and a preparation method of the anticoagulant hydrogel coating capable of catalyzing releaseof nitric oxide. The method comprises the following steps: (1) pretreating a substrate material; (2) sequentially placing the pretreated substrate material in a polycation electrolyte, a mixed solution of polyphenol and a compound A, and a polyanion electrolyte at room temperature to react for 20 minutes, and washing for 3 to 5 times; (3) using a product obtained in step (2) as a substrate at room temperature, repeating the operation of step (2) for 5 to 20 times, after drying by nitrogen, obtaining the anticoagulant hydrogel coating capable of catalyzing the release of nitric oxide. The hydrogel coating prepared by the method disclosed by the invention has the advantages of simple method, stable structure, and good biocompatibility, can stably catalyze NO to release for a long time to protect endothelial cells and has an anticoagulant effect. The coating can be used for surface modification of cardiovascular stent materials and heart valves.

The invention provides a coating method for an activated carbon adsorbent for blood perfusion. Firstly, coating film is formed on the surface of activated carbon with chitosan, then crosslinking is executed with epichlorohydrin to increase the strength of the film, and finally heparin sodium having an anticoagulant effect is grafted to the surface of the film. The crosslinked chitosan film can improve the blood compatibility of the activated carbon and decrease particle falling of the activated carbon; the heparin sodium having an excellent anticoagulant property is grafted on the film so thatthe blood coagulation phenomenon occurring when blood is in contact with the surface of the activated carbon can be decreased, and the safety of a perfusion device is improved.

The invention discloses a dialysis membrane used for hemodialysis and relates to the field of medical equipment. The dialysis membrane that is used for hemodialysis of the present invention, its raw material comprises by mass fraction: Its raw material comprises by mass fraction: chitosan quaternary ammonium salt 26-33 parts, polylactic acid 107-111 parts, polylactic acid 29-34 parts of ethylene glycol, 0.5-0.8 parts of heparin, 0.10-0.14 parts of ethylenediamine, 0.4-0.7 parts of glycidyl methacrylate, 0.05-0.08 parts of N,N-dicyclohexylcarbodiimide, butyl Diimide 0.02-0.04 parts. The dialysis membrane of the present invention is made of modified polylactic acid composite material and has good biocompatibility; heparin is fixed on the dialysis membrane and has anticoagulant effect; the chitosan quaternary ammonium salt in the raw material makes the composite membrane positively charged, Form a positive charge barrier, effectively resist the bacteria in the dialysate from entering the blood, reduce the chance of infection, and improve the safety of clinical application.

The invention refers to a manmade materials for medicial anticoagulant and the manufacturing method. It solves the problem that anticoagulant problem of blood osculant materials. It is used to produce osculant blood pipe, medicinal appliance and manmade blood vessel. It comprises polyamine ester and metallic oxide nano materials. The method is that the polyamine ester is resolve in N,N-dimethylacetamide or N,N-dimethylformamide and forms the polyamine ester liquid, the metallic oxide nano materials are put into the liquid. Through high-speed mixing, shocking, and moulding, then the solvent is eliminated. The invention has good anticoagulant effect, high stretching intensity and rupture tensibility. The method and craft and the device is simple and the cost is low.

The invention discloses a mixed gel with an anticoagulation effect, and a preparation method and an application thereof, and relates to the technical field of 3D printing. The mixed gel with the anticoagulation effect comprises a photo-curing polymer formed by methacrylic anhydride modified gelatin, functionalized anticoagulant molecules are covalently connected to the light-cured polymer, the functionalized anticoagulant molecules are a product obtained after amidation chemical reaction and covalent crosslinking of heparin and alginate, the mixed gel with a slow release effect and the anticoagulant effect is formed, and the mixed gel can be applied to light-cured 3D printing. The preparation method of the mixed gel with the anticoagulation effect comprises the following steps: the methacrylic anhydride modified gelatin, alginate and heparin are subjected to a photocuring reaction and then subjected to a covalent cross-linking reaction. The finally formed photocuring polymer contains heparin and alginate, so the anticoagulation effect is achieved, and heparin can be slowly released in the application process to solve the burst release problem to a large extent.

The invention discloses a coronary artery stent with anticoagulant effect and a preparation method thereof. The hyperbranched star-shaped amphiphilic SPLA-b-PMPC polymer nano particle coating is arranged on the support. Dissolve the treated stent in an organic solvent of hyperbranched star-shaped amphiphilic SPLA-b-PMPC polymer nanoparticles to prepare a coating solution; then take out the stent; place the stent on a centrifuge device and load it into a centrifuge tube , centrifuged, and dried under reduced pressure at room temperature to complete the coating. The 2-methacryloyloxyethylphosphorylcholine contained in the coating liquid of this coronary artery stent has little interaction with blood components, which can effectively inhibit blood coagulation and complement activation, and reduce protein adsorption , Inhibit the denaturation of adsorbed protein and platelet adhesion, can inhibit cell adsorption and inflammatory response, has good blood and tissue compatibility, and has a good anticoagulant effect, and has good application in cardiovascular and cerebrovascular diseases prospect.

Heparin-binding peptides are provided of the formula R1(X1B1B2X2B3X3Y1R2)RnR3, R1(X1B1B2B3X2X3B4X4Y1R2)RnR3, and C(X1B1B2B3X2X3B4X4)nC; wherein X1, X2, X3, and X4 are independently selected from the group consisting of hydropathic amino acids; B1, B2, B3, and B4 are independently selected from the group consisting of basic amino acids; C is cysteine; Y1 is zero or one to ten amino acid residues, wherein at least one amino acid residue is proline; n is an integer from one to ten; and R1, R2, and R3 are independently selected segments containing from zero to twenty amino acid residues, provided, at least one of the segments R1, R2, and R3 comprises at least one hydrophobic amino acid residue. The peptide C(X1B1B2B3X2X3B4X4)nC is optionally cyclized via a disulfide bond formed between cysteine residues. The peptides are administered to reduce plasma LMWH and heparin levels and to reduce the anticoagulant effects of heparin and LMWH. The peptides are also administered to inhibit microbial growth and to inhibit mast cell serine proteases involved in various diseases and disorders. The peptides are also administered as carriers to deliver active agents.

The invention belongs to the field of Chinese medicine, relates to Prunella vulgaris polysaccharide, and a preparation method and purpose thereof in preparing anticomplement medicines. The Prunella vulgaris polysaccharide including uniform polysaccharide PW-PS1 and PW-PS2 is prepared from a dry fruit aqueous extract of a labiatae plant Prunella vulgaris Linn. Through in vitro tests, the uniform polysaccharide is proved to have strong anticomplement activity and inhibition effects on classical pathway and alternative pathway of a complement system; besides, the polysaccharide does not have the anticoagulant effect influencing in vivo activity and can be used for the preparation of complement inhibition medicaments. The PW-PS1 effects on C1q, C3 and C9 components of the complement system, and the PW-PS2 effects on the C1q, C2, C3, C5 and C9 components of the complement system.

The invention relates to an anticoagulant textile-based artificial blood vessel material and a preparation method thereof. The anticoagulant textile-based artificial blood vessel material is characterized in that an anticoagulant polypyrrole (PPy) coating layer is polymerized to the surface of polyester textile, the coating layer is of a micro-nano structure and has good hydrophobic property, andan anticoagulant effect is further improved; meanwhile, some low surface energy matters are further doped into the coating layer, and the anticoagulant effect is further improved. In preparation, firstly, alkali minimization or plasma pretreatment is performed on a polyester material; then, a chemical polymerization technology or electrochemical polymerization technology is utilized to coat pyrrole monomer on the surface of the pretreated material. The artificial blood vessel material disclosed by the invention has the advantages of good anticoagulant effect, simple preparation technology, lowcost, safety and reliability.

The invention provides a pharmaceutical composition containing active procyanidins and clopidogrel or the pharmacologically acceptable salt thereof. The procyanidins and the clopidogrel are used in a combined manner, a more effective method for curing thrombotic diseases is found, after trail for many times, the clopidogrel and the procyanidins (an extract of traditional Chinese medicine) are creatively and effectively combined together, the effect of applying the procyanidins to inhibit the thrombosis in a combined manner is discovered unexpected in the process of applying the clopidogrel to cure the thrombotic diseases, and not only the anticoagulant effect of the clopidogrel is free from the influence of the procyanidins, but also a good effect is achieved in the aspect of reducing the adverse reaction of bleeding after the use of the clopidogrel and the procyanidins in a combined manner, therefore, the risk of bleeding is greatly reduced when the advantages of good anticoagulant activity and fast effect of the clopidogrel during the antiplatelet aggregation are fully exerted, the risk of bleeding of the clopidogrel during the antiplatelet aggregation is effectively reduced and the adverse reaction of the clopidogrel is greatly reduced.

This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action.The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.

The invention discloses a ligustrazine derivative and a preparation method and medical application thereof. The invention synthesizes and prepares three ligustrazine derivatives with novel structures,and provides a preparation method of the ligustrazine derivatives. Pharmacological results show that the inhibitory activity of the three ligustrazine derivatives I-2, I-4 and I-6 on ADP-induced or AA-induced platelet aggregation is superior to that of a parent compound ligustrazine (TMP); compared with clinically common medicines with anticoagulant effects, the activity of the ligustrazine derivatives I-2, I-4 and I-6 in inhibition of ADP-induced platelet aggregation is equivalent to that of a positive drug thilopyrazine, and the inhibition activity of the ligustrazine derivatives I-2, I-4 and I-6 in inhibition of AA-induced platelet aggregation is obviously superior to that of a positive control drug aspirin.

A novel animal blood anticoagulant consisting of long-chain inorganic phosphates and organic phosphates. Wherein: the weight proportion of the long-chain inorganic phosphate and the organic phosphate is: the long-chain inorganic phosphate is 25-75 parts, and the organic phosphate is 25-75 parts. The method of using the above-mentioned novel animal blood anticoagulant is: dissolve the anticoagulant and water in a ratio of 1:10 (w / w) during use, and evenly sprinkle the anticoagulant solution in the blood tank before slaughtering, and then slaughter After the start, the anticoagulant solution is evenly sprayed on the surface of the original blood during the slaughtering process of the livestock and poultry, and the addition ratio of the anticoagulant solution to the original blood is 1:15-1:20 (v / v). Compared with traditional anticoagulants, the anticoagulant has stronger anticoagulant effect, can effectively inhibit hemolysis, reduces the amount of anticoagulant used, and significantly improves the anticoagulant effect of animal blood, which is beneficial to related Enterprise mass production.

The invention relates to the art of Chinese medicine processing and bio-fermentation, in particular to a fermentation method of Chinese milkvetch and an application of fermented product through the method. The invention makes the fermentation of Chinese milkvetch by taking large edible fungus as the starting fungus of Chinese medicine fermentation, Chinese milkvetch as the main material of fermentation culture medium and adding a small amount of necessary nutrients for fungus production and growth. Animal experiment show that the fermented milkvetch liquid has the anti-anoxia and anticoagulant effect. The application of the invention refers to the fermented milkvetch liquid obtained through the method can be applied in preparing anti-anoxia and anticoagulant medicine as well as corresponding health products and food.