68 results about "Propranolol" patented technology

It has been discovered that the stimulation of beta-adrenergic receptors, which activate cAMP formation, give rise to increased APP and GFAP synthesis in astrocytes. Hence, the in vitro or in vivo exposure of neuronal cells to certain compositions comprising beta-adrenergic receptor ligands or agonists, including, e.g., norepinephrine, isoproterenol and the like, increases APP mRNA transcription and consequent APP overproduction. These increases are blocked by beta-adrenergic receptor antagonists, such as propranolol. The in vitro or in vivo treatment of these cells with 8Br-cAMP, prostaglandin E2 (PG E2), forskolin, and nicotine ditartrate also increased APP synthesis, including an increase in mRNA and holoprotein levels, as well as an increase in the expression of glial fibrillary acidic protein (GFAP). Compositions and methods are disclosed of regulating APP overexpression and mediating reactive astrogliosis through cAMP signaling or the activation of beta-adrenergic receptors. It has further been found that the increase in APP synthesis caused by 8Br-cAMP, PG E2, forskolin, or nicotine ditartrate is inhibited by immunosuppressants or anti-inflammatory agents, such as cyclosporin A, and FK-506 (tacrolimus), as well as ion-channel modulators, including ion chelating agents such as EGTA, or calcium / calmodulin kinase inhibitors, such as KN93. The present invention has broad implications in the alleviation, treatment, or prevention of neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.

It has been discovered that the stimulation of beta-adrenergic receptors, which activate cAMP formation, give rise to increased APP and GFAP synthesis in astrocytes. Hence, the in vitro or in vivo exposure of neuronal cells to certain compositions comprising beta-adrenergic receptor ligands or agonists, including, e.g., norepinephrine, isoproterenol and the like, increases APP mRNA transcription and consequent APP overproduction. These increases are blocked by beta-adrenergic receptor antagonists, such as propranolol. The in vitro or in vivo treatment of these cells with 8Br-cAMP, prostaglandin E2 (PG E2), forskolin, and nicotine ditartrate also increased APP synthesis, including an increase in mRNA and holoprotein levels, as well as an increase in the expression of glial fibrillary acidic protein (GFAP). Compositions and methods are disclosed of regulating APP overexpression and mediating reactive astrogliosis through cAMP signaling or the activation of beta-adrenergic receptors. It has further been found that the increase in APP synthesis caused by 8Br-cAMP, PG E2, or forskolin is inhibited by immunosuppressants, immunophilin ligands, or anti-inflammatory agents, such as cyclosporin A, and FK-506 (tacrolimus), as well as ion-channel modulators, including ion chelating agents such as EGTA, or calcium / calmodulin kinase inhibitors, such as KN93. The present invention has broad implications in the alleviation, treatment, or prevention of neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.

It has been discovered that the stimulation of beta-adrenergic receptors, which activate cAMP formation, give rise to increased APP and GFAP synthesis in astrocytes. Hence, the in vitro or in vivo exposure of neuronal cells to certain compositions comprising beta-adrenergic receptor ligands or agonists, including, e.g., norepinephrine, isoproterenol and the like, increases APP mRNA transcription and consequent APP overproduction. These increases are blocked by beta-adrenergic receptor antagonists, such as propranolol. The in vitro or in vivo treatment of these cells with 8Br-cAMP, prostaglandin E2 (PG E2), forskolin, and nicotine ditartrate also increased APP synthesis, including an increase in mRNA and holoprotein levels, as well as an increase in the expression of glial fibrillary acidic protein (GFAP). Compositions and methods are disclosed of regulating APP overexpression and mediating reactive astrogliosis through cAMP signaling or the activation of beta-adrenergic receptors. It has further been found that the increase in APP synthesis caused by 8Br-cAMP, PG E2, or forskolin is inhibited by immunosuppressants, immunophilin ligands, or anti-inflammatory agents, such as cyclosporin A, and FK-506 (tacrolimus), as well as ion-channel modulators, including ion chelating agents such as EGTA, or calcium / calmodulin kinase inhibitors, such as KN93. The present invention has broad implications in the alleviation, treatment, or prevention of neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.

A unit dosage form, such as a capsule or the like for delivering drugs into the body in a circadian release fashion, is comprising of one or more populations of propranolol-containing particles (beads, pellets, granules, etc.). Each bead population exhibits a pre-designed rapid or sustained release profile with or without a predetermined lag time of 3 to 5 hours. Such a circadian rhythm release cardiovascular drug delivery system is designed to provide a plasma concentration-time profile, which varies according to physiological need during the day, i.e., mimicking the circadian rhythm and severity / manifestation of a cardiovascular disease, predicted based on pharmaco-kinetic and pharmaco-dynamic considerations and in vitro / in vivo correlations.

The present invention provides an ophthalmic composition comprising a hyperbranched polyester. The ophthalmic compositions may also comprise carbonic anhydrase inhibitors, wherein the hyperbranched polyester increases the aqueous solubility of the carbonic anhydrase inhibitor, and increases corneal permeation of the active agent. The ophthalmic compositions may also comprise non-ionic surfactants, such as PEG, Polysorbate, HPMC or HEC, and beta-blockers, such as Carteolol, Levobunolol, Betaxolol, Metipranolol, Timolol or Propranolol. The concentration of the hyperbranched polyester in the ophthalmic formulation should be less than or equal to 4% (w / v) in order to avoid any cytotoxic effects on human corneal cells and thus the eye irritation.

A unit dosage form, such as a capsule or the like for delivering drugs into the body in a circadian release fashion, is comprising of one or more populations of propranolol-containing particles (beads, pellets, granules, etc.). Each bead population exhibits a pre-designed rapid or sustained release profile with or without a predetermined lag time of 3 to 5 hours. Such a circadian rhythm release cardiovascular drug delivery system is designed to provide a plasma concentration-time profile, which varies according to physiological need during the day, i.e., mimicking the circadian rhythm and severity / manifestation of a cardiovascular disease, predicted based on pharmaco-kinetic and pharmaco-dynamic considerations and in vitro / in vivo correlations.

The invention discloses an epoxide hydrolase mutant as well as a gene and an application of the epoxide hydrolase mutant. The epoxide hydrolase mutant is protein which is obtained by substituting one amino acid at one site or multiple sites of the 123th, 128th, 144th 145th, 168th, 219th and 221st amino acid of the protein with an amino acid sequence as shown in SEQ ID No: 1 in a sequence table and deriving from the protein with the amino acid sequence as shown in SEQ ID No: 1 and has epoxide hydrolase activity. Compared with wild type epoxide hydrolase, the epoxide hydrolase mutant provided by the invention can greatly improve hydrolytic activity and enantioselectivity of the racemization epoxide, and is particularly suitable for splitting and catalyzing the racemization naphthyl glycidyl ether to prepare (S)- naphthyl glycidyl ether and further synthesize racemic medicament (S)-propranolol. The hydrolase mutant has good industrial application prospect.

The invention discloses a delayed-release preparation of propranolol for treating cardiovascular diseases such as abnormal heart rate, angina, myocardial infarction and the like or a salt thereof. The aim of the invention is to provide a drug preparation which meets the intentions of chrono-pharmacology and chrono-therapeutics and has the delayed and impulse drug-release effects and a method for preparing the same. The delayed-release preparation comprises: a tablet core containing the active component propranolol with effective treating dose or the salt thereof and other auxiliary materials and one or two coating layers which are coated in a coating pan by the rollover method or coated by the fluidization coating method or dry pressing coating method. The composition and the thickness of the coating layers decide the time lag of releasing the drug.

Modified or extended release formulations containing propanolol compounds and associated methods are disclosed and described. In some aspects, such formulations may be substantially bioequivalent to known FDA approved propanolol formulations such as INDERAL LA®.

The bradyrhythmia treating Chinese medicine is orally taken preparation obtained with astragalus root and aconite root as main material. Two types of pharmacodynamic bradyrhythmia model test, including amiodaronum rat and propranolol rat show that the bradyrhythmia treating Chinese medicine can raise the heart rate obviously and has no toxic side effect produced after being taken regularly.

The invention discloses a compound preparation for treating BRAF inhibitor-resistant melanoma. Medicinal ingredients in the compound preparation include vemurafenib and propranolol, wherein the weightratio of the vemurafenib to the propranolol is at (5-15) to 1. The compound preparation provided by the invention is more economic and effective, so that family burdens of patients can be reduced.

Modified or extended release formulations containing propanolol compounds and associated methods are disclosed and described. In some aspects, such formulations may be substantially bioequivalent to known FDA approved propanolol formulations such as INDERAL LA®.

The invention relates to a compound of propranolol or a medicinal salt thereof and ion exchange resin and a preparation method of the compound. The compound comprises propranolol and a salt thereof and ion exchange resin, wherein the ion exchange resin is selected from one or more of polacrilin (polacrilin), polacrilin potassium (polacrilin potassium) and sodium polystyrenesulfonate. The compound of the propranolol and the salt thereof provided by the invention can be further prepared into an oral preparation, especially an oral suspension; the bitter taste and the thrill of a propranolol medicine solution can be removed; meanwhile, the stability of the compound is greatly improved; harmful impurities are reduced when the taking compliance is improved; the product quality is improved; and the medication safety of a patient is ensured.

The invention discloses a novel propranolol synthesis method. The method includes the following steps that 3-(1-naphthoxy)-1, 2-epoxypropane and isopropylamine generate a ring-opening reaction in the presence of a catalyst, propranolol is obtained, the yield is larger than or equal to 93%, and the purity is larger than or equal to 99%. Compared with an existing preparation method, the method has the advantages that the method is easy and convenient to implement, the reaction condition is mild, the catalytic activity and selectivity of the catalyst are high, few side reactions happen, products can be separated and purified easily, less device corrosion and less pollution to the environment are caused, end products with the high purity can be obtained, the yield is high, and the method is suitable for industrial production.

The invention discloses a propranolol-eugenol type basil oil nano-emulsion medicament, which consists of the following raw materials in percentage by mass: 1-10 percent of propranolol, 10-30 percent of surfactant, 0-25 percent of cosurfactant, 1-15 percent of eugenol type basil oil and the balance of distilled water, wherein the mass percentage sum of the raw materials is 100 percent. A nano-emulsion has the characteristics of small emulsion drop particles, uniform distribution, low viscosity and high flowability. In a nano-emulsion dosage form, propranolol serving as a water-soluble medicament is organically combined with fat-soluble eugenol type basil oil, so that the dissolving and permeation capabilities of eugenol type basil oil are increased, and the stability and medicament effect of propranolol are enhanced. After the propranolol and the eugenol type basil oil are prepared into a nano-emulsion dosage form, the advantages of the propranolol and the eugenol type basil oil are combined, the hypertension resisting effect is enhanced remarkably, the half-life period of a medicament is prolonged, and the administration times are reduced.

The invention provides a preparation method of a graphene oxide / attapulgite magnetic composite material for removing propranolol in a water body. Graphene oxide is prepared by utilizing an improved Hummers method, and then a composite material is prepared by mixing and reaction with attapulgite. The prepared composite material is taken as an adsorbent, propranolol is taken as an adsorption object,and experimental results show that the composite material has efficient adsorption and removal effects; compared with single graphene oxide, the composite material is low in production cost, and theused attapulgite is cheap and easy to obtain. The composite material applied to treat the propranolol in the water body has the advantages of being low in price, simple to operate, high in adsorptionrate, environmentally friendly, high in stability, easy to separate and the like, and has certain practical value in industrialization. The graphene oxide / attapulgite magnetic composite material has certain practical value as an adsorbent for treating cardiovascular drugs in sewage and provides a brand-new water treatment idea in the field of water treatment.

The invention discloses a preparation method of a propranolol stealth liposome modified by a vascular endothelial growth factor receptor-2 (VEGFR-2) monoclonal antibody and casein phosphopeptides (CPP) jointly; the method comprises the following steps of: (1) confirming the composition and the proportion of liposome compound phosphatide; (2) preparing a propranolol stealth liposome modified by the CPP; and (3) connecting the VEGFR-2 monoclonal antibody and the surface of the propranolol stealth liposome modified by the CPP to obtain the propranolol stealth liposome modified by the VEGFR-2 monoclonal antibody and the CPP jointly. The preparation method has the characteristics of high stability, long circulation, active targeting, high-efficiency endocytosis and the like, and can guarantee the toxicity reducing and efficacy enhancing of anti-hemangioma medicines. The research result of the method provides a preparation technology platform for the clinical targeted therapy of the anti-hemangioma medicines.

One of the tasks of the invention is to define an effective part for using cotinus coggygria, and provide pharmacodynamics usages of the effective part and various preparations. The new usage of the effective part of the cotinus coggygria is that the leaves, stems, branches and roots of the cotinus coggygria are collected to extract general flavone as a drug which can improve animal organism hypoxia tolerance or thrombolysis, etc. The invention has the advantages that the effective part of the cotinus coggygria is defined, and the effective components are separated for medical use, thus obviously improving the therapeutic effect. Experiments prove that the preparation of the invention can obviously improve animal hypoxia tolerance and the effect thereof is equal to a western medicine antianginal drug Propranolol, thus avoiding the toxic side effect of the western medicine and having the actions of improving blood circulation and reducing whole blood viscosity. Therefore, the preparation can be applicable for preventing and curing coronary heart disease, angina pectoris, miocardial infarction, as well as obstruction of Qi in chest, dizziness, brachypnea, palpitation, chest distress or thoracodynia caused by internal resistance of congestion. Meanwhile, the preparation of the invention also has the actions of anticoagulation in vitro and thrombus dissolving.

The invention discloses an improved preparation method of propranolol, which comprises the following step: in an organic solvent, 3-(1-naphthoxy)-1,2-propylene oxide reacts with isopropylamine under the action of a catalyst so as to obtain the propranolol. Compared with an existing preparation method, the method has the advantages that the preparation method is simple and convenient, reaction conditions are mild, the process is easy to control and the preparation method has small side effects; the catalyst has high catalytic activity and selectivity, is environmental-friendly and can be repeatedly used; a product is easy to separate and purify, the finished product with high purity can be obtained, yield is high, a small quantity of three wastes are generated, and the preparation method has low pollution and is suitable for industrial production.

The invention relates to a graphene oxide / molecular imprinting filtering membrane for detecting propranolol, as well as a preparation and an application thereof. Specifically, the invention discloses a method for detecting propranolol in a detected sample by adopting the graphene oxide / molecular imprinting filtering membrane and a metallic nanometer grain combined raman technique. The detection method has the advantages of high sensitivity, simple and convenient operation, less time consumption, low cost, and the like.

The invention discloses a preparation method for propranolol. The preparation method is characterized by comprising the following preparation steps: naphthol (I), epichlorohydrin and isopropylamine are used as initial raw materials, a reaction is performed under effects of a reaction solvent, an alkali and a phase transfer catalyst, and therefore the propranolol (TM) is obtained. According to thepreparation process, the reaction is finished in one step, thus the process steps are greatly simplified and easy to control, industrialized production can be realized, and process costs are reduced.

The invention discloses a delayed-release preparation of propranolol for treating cardiovascular diseases such as abnormal heart rate, angina, myocardial infarction and the like or a salt thereof. The aim of the invention is to provide a drug preparation which meets the intentions of chrono-pharmacology and chrono-therapeutics and has the delayed and impulse drug-release effects and a method for preparing the same. The delayed-release preparation comprises: a tablet core containing the active component propranolol with effective treating dose or the salt thereof and other auxiliary materials and one or two coating layers which are coated in a coating pan by the rollover method or coated by the fluidization coating method or dry pressing coating method. The composition and the thickness ofthe coating layers decide the time lag of releasing the drug.

The present invention provides an ophthalmic composition comprising a hyperbranched polymer. The ophthalmic compositions may also comprise carbonic anhydrase inhibitors, wherein the hyperbranched polymer increases the aqueous solubility of the carbonic anhydrase inhibitor, and increases corneal permeation of the active agent. The ophthalmic compositions may also comprise non-ionic surfactants, such as polysorbate, hydroxypropyl methyl cellulose or hydroxyethyl cellulose, and beta-blockers, such as carteolol, levobunolol, betaxolol, metipranolol, timolol or propranolol.

The invention discloses a method for simulated moving bed chromatography-based resolution of a propranolol enantiomer. The method is characterized in that through a simulated moving bed chromatography system, a propranolol enantiomer is resolved under the normal phase conditions in the presence of cellulose-tris(3,5-dimethylphenylcarbamate) as a filler and n-hexane and alcohol organic modifiers as mobile phases so that high-purity R-propranolol and S-propranolol are obtained. The simulated moving bed chromatography system has the advantages of continuous production, high automation degree and high production efficiency.

The invention belongs to medical field, and more specifically relates to a product used for evaluating effect of propranolol in treatment of infant hemangioma. The product is a kit, equipment, an operating system, and / or a composition of the kit, the equipment, and the operating system. The product comprises 1, a reagent, an instrument and / or a system used for measuring expressive abundances of ID1 and beta-actin in cells of a measurement object; 2, a module and / or a processor used for calculating ID1 relative expression quantity; and 3, a module and / or a processor used for evaluation of treatment effect of propranolol on infant hemangioma based on the ID1 relative expression quantity. The product is capable of detecting whether drug resistance of infant patients with hemangioma on propranolol is caused, can be used for effective evaluation on treatment effect of propranolol on infant hemangioma, and is capable of providing an effective evaluation method. The evaluation method possesses important meaning in in-time detecting whether drug resistance of patients on propranolol is caused, and adjusting of treatment schemes.

The invention discloses application of propranolol and derivatives or pharmaceutically acceptable salts thereof in preparation of drugs for preventing or treating coronavirus infection. Researches show that propranolol can effectively inhibit or degrade virus replication organelles and inhibit virus replication, has clear and remarkable prevention and resistance effects on coronaviruses including SARS-CoV-2, SARS-CoV and MERS-CoV, and can relieve various diseases caused by new coronavirus sequelae. Meanwhile, the invention also discloses application of propranolol and the derivatives thereof or pharmaceutically acceptable salts thereof in preparation of medicines for preventing or treating coronavirus infection in combination with other anti-new coronavirus medicines, including anti-new coronavirus medicines which are approved to appear on the market or enter clinic. After combined use, the virus load can be obviously reduced at a low dosage. The invention has important application and popularization significance on the treatment and prevention and control of the current novel coronavirus COVID-19.

The invention discloses a nano-emulsion oral solution containing propranolol or a salt thereof and a preparation method thereof, wherein the prescription of the nano-emulsion oral solution containingpropranolol or the salt thereof includes propranolol or the salt thereof, and pharmaceutically acceptable pharmaceutical excipients, wherein the pharmaceutical excipients include an oil phase medium,an emulsifier, a taste masking agent and purified water. The nano-emulsion oral solution containing propranolol or the salt thereof belongs to an oral taste masking preparation high in compliance, high in safety, good in stability and suitable for infants and young children to take for a long period of time, and conforms to clinical needs.

This invention relates to a method for preventing and treating morning migraine headaches. Pursuant to this method, a therapeutic amount of β-adrenergic-blocking agent is administered nightly to a person that suffers from migraine attacks such that the blocking agent is first released during morning hours when the person is most susceptible to morning migraine.

The invention discloses a method for detecting contents of epicatechin and mercapto epicatechin in plasma according to the liquid-mass chromatography. The method comprises the following steps: (1) preparing a medicated plasma sample; (2) preparing a working curve sample; (3) setting LC determination conditions; (4) setting MS / MS conditions; (5) quantifying according to an internal standard method, taking the concentrations of series of epicatechin and mercapto epicatechin in blank plasma as horizontal coordinates, and the peak area ratios of the epicatechin and the mercapto epicatechin to an internal standard substance propranolol as vertical coordinates, and carrying out regressing calculation according to a weighted least square method, so as to obtain a linear regression equation, namely a working curve, wherein the weighting coefficient is 1 / x2; calculating the concentrations of the epicatechin and the mercapto epicatechin in the medicated plasma sample according to the working curve. The method provided by the invention is fast, dedicated, precise and highly sensitive.

A compound preparation for treating hypertension and a preparation method thereof. The product of the present invention overcomes the obvious increase in side effects caused by increasing the dose of the drug when propranolol and hydrochlorothiazide are used clinically to ensure the curative effect when the drug is used alone; At the same time, because there is no pharmaceutical preparation that meets the combined dosage, the clinical dosage is not accurate, which affects the efficacy of the drug. The combined use of propranolol and hydrochlorothiazide has synergistic and complementary effects in curative effect; the dosage is reduced, the adverse reactions are alleviated, and it is convenient to take and the price is low.