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103results about How to "Prolonged plasma half-life" patented technology

Antidotes for factor xa inhibitors and methods of using the same

ActiveUS20090098119A1Reduce and remove intrinsic procoagulantReduce and remove and anticoagulant activityOrganic active ingredientsHydrolasesMedicineAntidote
The present invention relates antidotes to anticoagulants targeting factor Xa. The antidotes are factor Xa protein derivatives that bind to the factor Xa inhibitors thereby substantially neutralizing them but do not assemble into the prothrombinase complex. The derivatives describe herein lack or have reduced intrinsic coagulant activity. Disclosed herein are methods of stopping or preventing bleeding in a patient that is currently undergoing anticoagulant therapy with a factor Xa inhibitor.
Owner:ALEXION PHARMA INC

Cellular fibronectin as a diagnostic marker in cardiovascular disease and methods of use thereof

Thrombolytic therapy in the treatment of a cardiovascular event such as myocardial infarction (MI) carries with it a chance of suffering a hemorrhagic incident leading to severe disability and often death. Methods for the evaluation of proper therapy for a specific patient who has suffered a cardiovascular event employ a variety of bio-markers including cellular fibronectin (c-Fn) assembled as a panel for evaluation. Methods are disclosed for selecting markers and correlating their combined levels with a clinical outcome of interest. In various aspects the methods permit early detection of potential bleeding events, determination of the prognosis of a patient presenting cardiovascular damage, and identification of a patient at risk for hemorrhage when given thrombolytic therapy. The disclosed methods provide rapid, sensitive and specific assays to greatly reduce the risk of bleeding or the number of patients that can receive the most beneficial treatment for their cardiovascular event, and to reduce the human and economic costs associated with bleeding following such treatments.
Owner:PREDICTION SCI

Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents

The present invention relates to antidotes of anticoagulants targeting factor Xa which antidotes are used in combination with blood coagulating agents or other heparin antidotes to prevent or reduce bleeding in a subject. The antidotes described herein have reduced or no intrinsic coagulant activity. Disclosed herein are methods of stopping or preventing bleeding in a patient that is or will be undergoing anticoagulant therapy with a factor Xa inhibitor.
Owner:ALEXION PHARMA INC

Method for preparing enoxaparin sodium

The invention discloses a method for preparing enoxaparin sodium, comprising the steps of salinizing, drying, esterfying, alcohol precipitating, oxidizing, alcohol precipitating, fine filtering and freeze drying. In the method provided by the invention, a hydrophilic liquid phase reaction, a hydrophobic liquid phase reaction and a solid phase reaction are adopted, so that macromolecule sodium heparin is degraded into micromolecule sodium heparin with a specific structure, and the molecular weights of products and molecular weight distribution ranges are controlled, thus anti-FIIa activity resulting in bleeding risk is greatly reduced, the anti-FXa activity is relatively improved, and the product effectiveness and safety advantages are obvious. The enoxaparin sodium can be used for effectively preventing venous thromboembolism and pulmonary embolism, can be used for thrombosis before and after operations of orthopedic surgery and neurosurgery, and can be used for greatly reducing apoplexy risk, more effectively reducing death, cardiac failure and recurrent angina of patients suffering from unstable coronary artery syndromes, reducing hypertriglyceridemia and effectively eliminating the side effects of haemorrhage, osteoporosis and induced thrombocytopenia after long-term use of common unfractionated heparin sodium and derivates of common unfractionated heparin sodium.
Owner:HEBEI CHANGSHAN BIOCHEM PHARMA

Glucagon-like peptide 1 (GLP-1) analogues with long-acting effect and application thereof

The invention relates to glucagon-like peptide 1 (GLP-1) analogues with a long-acting effect and a synthesis method thereof. GLP-1 analogues with longer pharmacological action time are obtained through replacing / modifying 17th, 26th, 34th and 37th amino acids of natural GLP-1, the synthesis of target polypeptides is quickly realized through a microwave-promoted solid-phase synthesis method, and crude products are purified and freeze-dried to obtain the GLP-1 analogues.
Owner:CHINA PHARM UNIV

Method for preparing enoxaparin sodium

The invention discloses a method for preparing enoxaparin sodium, comprising the steps of salinizing, drying, esterfying, alcohol precipitating, oxidizing, alcohol precipitating, fine filtering and freeze drying. In the method provided by the invention, a hydrophilic liquid phase reaction, a hydrophobic liquid phase reaction and a solid phase reaction are adopted, so that macromolecule sodium heparin is degraded into micromolecule sodium heparin with a specific structure, and the molecular weights of products and molecular weight distribution ranges are controlled, thus anti-FIIa activity resulting in bleeding risk is greatly reduced, the anti-FXa activity is relatively improved, and the product effectiveness and safety advantages are obvious. The enoxaparin sodium can be used for effectively preventing venous thromboembolism and pulmonary embolism, can be used for thrombosis before and after operations of orthopedic surgery and neurosurgery, and can be used for greatly reducing apoplexy risk, more effectively reducing death, cardiac failure and recurrent angina of patients suffering from unstable coronary artery syndromes, reducing hypertriglyceridemia and effectively eliminatingthe side effects of haemorrhage, osteoporosis and induced thrombocytopenia after long-term use of common unfractionated heparin sodium and derivates of common unfractionated heparin sodium.
Owner:HEBEI CHANGSHAN BIOCHEM PHARMA

Synthesis and applications of an albumin bounding type 5-fluorouracil prodrug

The invention relates to an albumin bounding type 5-fluorouracil prodrug, and applications thereof in anti-tumor drug transfer. The prodrug is a compound formed by bridging 4-maleimidobutyric acid, 6-maleimidocaproic acid or 8-maleimido octanoic acid and N1-hydroxymethyl-5-fluorouracil through an ester bond, wherein the maleimido group is adopted as a bonding target of free sulfydryl of 34-site cysteine of albumin. The prodrug compound can be rapidly specifically bonded with albumin in blood to form an albumin prodrug composite, and therefore the drug metabolism speed is reduced, drug half life is significantly prolonged, and a long circulation function is achieved. In addition, under EPR effects and albumin acceptor mediation, tumor targeting is achieved and antitumor effects are improved. The 5-fluorouracil prodrug is used for intravenous injection and has a wide market application prospect.
Owner:SHENYANG PHARMA UNIVERSITY

Oxycontin controlled release formulations and methods of using same

The compositions disclosed herein are of use for the treatment of a wide variety of diseases. In particular, the compositions provide oxytocin and oxytocin analogs in sustained release formulations. In particular embodiments, the disclosed compositions concern oxytocin and oxytocin analogs, each of which may be associated with a biodegradable polymer and / or attached to a hydrophilic polymer. The methods include treatment of a wide variety of diseases and conditions. In particular, the methods include treatment of sexual dysfunction and disorders associated with repetitive behaviors, such as autism. The usefulness of the present invention is that the oxytocin, oxytocin analogs and mixtures thereof can be administered in a pharmaceutical formulation that increases their half-life and also provides for sustained release.
Owner:PR PHARMA

Novel long-acting glucagon-like peptide 1 (GLP-1) analogues and application thereof

The invention relates to novel long-acting glucagon-like peptide 1 (GLP-1) analogues and a synthesis method thereof. GLP-1 analogues with longer pharmacological action time are obtained through replacing / modifying 17th, 26th, 34th and 37th amino acids of natural GLP-1, the synthesis of target polypeptides is quickly realized through a microwave-promoted solid-phase synthesis method, and crude products are purified and freeze-dried to the GLP-1 analogues.
Owner:CHINA PHARM UNIV

Isomorellic acid polylactic acid nano particle preparation and preparing method thereof

InactiveCN101229130ANanoparticles with low drug loadingPossesses liver passive targeting propertiesOrganic active ingredientsPowder deliverySide effectTherapeutic effect
The invention discloses a gamboges acid nanometer particle preparation and is prepared by the components of raw material gamboges acid 0.05 to 1.5 percent, polylactic acid 0.05 to 1.5 percent, surfactant 0.1 to 1.5 percent, organic solvent 33 to 50 percent and the allowance of water with the following steps: dissolving the polylactic acid into the organic solvent and dispersing the gamboges acid in the mixed solution of the polylactic acid and the organic solvent; the preparation is obtained by adding the mixed solution with the gamboges acid into water phase with the surfactant, stirring magnetically for 4 hours, vacuum distillation and filtering with a 0.22Mum micro-porous filtering film after the organic solvent and part of water are distillated. The drug with a clear system, the particle size between 10 to 100nm and good dispersion and stability can significantly solubilize drugs, has a targeting effect for reticuloendothelial cells and concentrate at lesion sites, thus improving the curing effect of the drug and reduces the side effect of the drug. Additionally, the drug has a slowly releasing effect, can maintain constant plasma concentration or pharmacologic effect for a long time and improve drug bioavailability.
Owner:NORTHWEST A & F UNIV

Nanocrystal of camptothecin drugs and preparation method thereof

The invention provides a nanocrystal composition of a slightly-soluble antitumor drug, i.e., camptothecin and derivatives thereof, and a preparation method thereof. According to the invention, an optimized alkali-dissolution acid-precipitation high-pressure-homogenization process is employed; drug powder is subjected to alkali dissolution and then acid is added at a gradient speed to allow a nanocrystal to be precipitated; acid precipitation is carried out in two steps, and a produced salt is removed through a centrifugation step; and high-pressure homogenization is carried out to further decease a particle size. Preferably, the camptothecin nanocrystal has an average particle size of 100 to 150 m and is uniformly distributed; the camptothecin nanocrystal can be preserved for a long time in the form of freeze-drying powder only by adding a minute quantity of poloxamer 188 as a freeze-drying protection agent; and in use of the camptothecin nanocrystal, a glucose solution with a concentration of 5% is added and shaken out, so the camptothecin nanocrystal directly recovers to a state before freeze-drying. The method is simple, good in repeatability and suitable for large-scale production. The prepared nanocrystal has good slow release effect; and compared with commercially available injections, the nanocrystal has prolonged circulation time in blood plasma, improves distribution of the drug in human tissue and has beeter antineoplastic effect and good development prospects.
Owner:INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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