105 results about "Carvedilol" patented technology

A controlled release pharmaceutical composition for oral use comprising a solid dispersion of: i) at least one therapeutically, prophylactically and/or diagnostically active substance, which at least partially is in an amorphous form, ii) a pharmaceutically acceptable polymer that has plasticizing properties, and iii) optionally, a stabilizing agent, the at least one active substance having a limited water solubility, and the composition being designed to release the active substance with a substantially zero order release. The polymer is typically a polyethylene glycol and/or polyethylene oxide having a molecular weight of at least about 20,000 in crystalline and/or amorphous form or a mixture of such polymers, and the active substance is typically carvedilol. The composition may comprise a coated matrix, the coating comprising a first cellulose derivative which is substantially insoluble in the aqueous medium, and at least one of a) a second cellulose derivative which is soluble or dispersible in water, b) a plasticizer, and c) a filler.

The present invention is directed to nanoparticulate carvedilol compositions having improved pharmacokinetic profiles, improved bioavailability, dissolution rates and efficacy. In one embodiment, the nanoparticulate carvedilol composition has an effective average particle size of less than about 2000 nm.

The present invention relates to compositions and methods of treating human subjects with a beta-adrenergic receptor blocking agent (“beta-blocker”) provided in a time-sustained-release delivery system. The time-sustained-release drug delivery systems includes at least three populations of beads, where each population of beads includes a beta-blocker. The beads may be selected from immediate-release beads, enteric-release beads, sustained-release beads, and time-sustained-release beads. The beta-blocker may be selected from acebutolol, atenolol, betaxolol, bisoprolol, esmolol, metoprolol, nebivolol, butoxamine, carteolol, carvedilol, labetalol, nadolol, oxprenolol, penbutolol, propranolol, pindolol, sotalol, and timolol. According to presently preferred embodiments, the beta-blocker is propranolol. The dosage forms of the present invention are useful for treating conditions including hypertension, angina pectoris due to coronary atherosclerosis, hypertrophic subaortic stenosis, congestive heart failure, arrhythmias, angina, anxiety, glaucoma, migraines, esophageal varices, alcohol withdrawal syndrome, irregular heartbeat, tachycardia, tremor, and neuroleptic-induced akathisia. They are also useful in the prophylaxis of migraine headaches.

The present invention also relates to carvedilol free base, salts, anhydrous forms, or solvates thereof, corresponding pharmaceutical compositions or controlled release formulations, and methods delivery of carvedilol forms to the lower gastrointestingal tract or methods to treat cardiovascular diseases, which may include, but are not limited to hypertension, congestive heart failure, and angina. The present invention relates to control release formulations, which comprise various cavedilol forms, which may include, but are not limited to carvedilol free base and corresponding carvedilol salts, anhydrous forms or solvates thereof.

The present invention provides for pharmaceutical compositions comprising carvedilol for treatment of cancer. More particularly the invention relates to the use of carvedilol for treatment of cancers of the colon, ovary, breast, prostate, pancreas, lung, melanoma, glioblastoma, oral cancer and leukemias. Although not bound to any theory, the anticancer activity of carvedilol appears to be attributed to the inhibition of Epidermal Growth Factor and Platelet derived growth factor dependent proliferation of cancer cells. Further, carvedilol exerts anticancer effect by inhibition of the Protein kinase C (PKC) activity and that of the cyclooxygenase 2 enzyme. The invention also relates to the anticancer activity of the optically pure isomers S(-) and R(+) of carvedilol and the use of carvedilol and its isomers in pharmaceutical compositions for the treatment of cancer.</PTEXT>

A controlled release pharmaceutical composition for oral use comprising carvedilol. The composition releases carvedilol after oral administration to a mammal, including a human, in such a manner that a prolonged residence of carvedilol is obtained in the circulatory system compared with the known compositions of carvedilol. Furthermore, a composition according to the present invention makes available to the body a suitable plasma concentration of one or both of the enantiomeric species, namely R(+) and/or S(−) carvedilol for obtaining the desired therapeutic effect.

The invention solves a new method of preparation of Carvedilol for pharmaceutical use. In the synthesis of Carvedilol a reaction of 4-(oxirane-2-ylmethoxy)-9H-arbazole (II) with 2-(2-methoxyphenoxy)ethylamine salts (IV) in the presence of a base, in an alcohol having the number of carbons C2 to C5 as a solvent, at an elevated temperature, is used. After processing of the crude reaction mixture crude Carvedilol is obtained, which is purified by crystallization from ethylacetate with an addition of activated carbon and the final substance is formulated by crystallization from ethylacetate.

This invention relates to a method of maintaining glycemic control in diabetic hypertensive patients which comprises administering carvedilol to a subject in need thereof.

Compounds having bi-cyclic structure comprising a partially unsaturated 6-carbon first cyclic moiety interconnected to a 6-carbon second cyclic moiety second via a divalent linking moiety are provided. The compounds can be used as intermediates compounds in methods for the synthesis of carbazoles and derviatives thereof, including carvedilol, and tricyclic alkylhydroxamates, which do not require Fischer indole synthetic steps. Methods of preparing the compounds having bi-cyclic structures are also provided.

Disclosed herein is a process for preparation of carvedilol substantially free from its bis-impurity comprises the reaction of 4-(2,3-epoxypropoxy)carbazole and 2-(2-methoxyphenoxy)ethylamine in a polar aprotic solvent media; followed by isolation of carvediol from the reaction mass as an acid addition salt and subsequent conversion into pure carvedilol.

This invention relates to carvedilol monocitrate monohydrate, compositions containing this salt of carvedilol and methods of using this compound to treat hypertension, congestive heart failure and angina.

The invention discloses a simple synthetic method of expanded mesoporous silicon dioxide with a large specific surface area and a dissolution promoting application of expanded mesoporous silicon dioxide on an insoluble drug carvedilol. The method comprises the following steps: firstly dissolving a template in deionized water, dissolving a pore-enlarging agent in ethanol, then mixing the two solutions, adding sodium hydroxide and a silicon source into the mixed solution at 80 DEG C and filtering the reaction liquid and washing the filter cake after reaction for two hours; and finally, putting the filter cake in a hydrochloric acid/ethanol solution for refluxing for 3 hours to obtain an expanded silicon dioxide product with the large specific surface area. The preparation method is easy to operate, simple in process, mild in reaction and low in cost. The prepared expanded mesoporous silicon dioxide is in a mono-dispersive spherical shape, the specific surface area reaches up to 1234.4m<2>/g and the pore diameter is 3.7nm. Finally, the mesoporous silicon dioxide and carvedilol are used for preparing a solid dispersion, and dissolution of the medicinal raw material carvedilol is obviously improved, so that the dissolution rate of carvedilol within 15 minutes reaches near 80%.

An improved controlled release dosage form for once-daily administration of carvedilol is described. The controlled release dosage form comprises a therapeutically effective amount of carvedilol and/or a pharmaceutically acceptable salt thereof; one or more hydrophilic polymers; one or more pharmaceutically acceptable excipients; and a polyoxyalkylene block copolymer, a solid dispersion of carvedilol and an extrusion material or a combination of a polyoxyalkylene block copolymer, a solid dispersion of carvedilol and an extrusion material.

The use of β-adrenergic inverse agonists provides a new and highly efficient way of treating a number of pulmonary airway diseases, including asthma, emphysema, and chronic obstructive pulmonary diseases. In general, such a method comprises administering a therapeutically effective amount of a β-adrenergic inverse agonist to the subject to treat the pulmonary airway disease. Particularly preferred inverse agonists include nadolol and carvedilol. In addition, methods are described for long-term administration of such inverse agonists and for determining the suitability of patients for long-term inverse agonist therapy.

The invention discloses a method for preparing carvedilol solid dispersions by virtue of a supercritical anti-solvent technique. The method comprises the following steps: (S1) dissolving carvedilol and a water-soluble carrier into an organic solvent, so as to obtain a carvedilol-carrier mixed solution; (S2) introducing CO2 into a crystallization kettle, and regulating the temperature and pressure in the crystallization kettle; (S3) continuing to introduce CO2 to keep the temperature and pressure in the crystallization kettle constant, and simultaneously introducing the mixed solution prepared in the step (S1) into the crystallization kettle; and (S4) after the carvedilol-carrier mixed solution is introduced, continuing to introduce CO2 to keep the temperature and pressure in the crystallization kettle constant, finally relieving the pressure, and after the pressure in the crystallization kettle is decreased to the atmospheric pressure, opening the crystallization kettle, and collecting the carvedilol solid dispersions. By virtue of the method, the carvedilol solid dispersions with obviously improved dissolution characteristics can be prepared, and furthermore, the bioavailability of indissolvable drugs can be improved.

The present invention relates to extended release matrix tablets for oral administration that include a cationic polymer, a water-swellable polymer, and an alginic acid derivative to cause the release rate of the active ingredient of the tablets to be independent of pH and gastric residence time. The active pharmaceutical ingredient may be one or more of antibiotics, sympathomimetics, sympatholytic agents, cholinergic agents, antimuscarinics, gastro-intestinal drugs, gentio-urinary smooth muscle relaxants, cardiac drugs, anticonvulsants, tranquilizers and sedatives, and in particular may be an antibiotic, such as cefaclor, or may be a sympatholytic agent, such as carvedilol.

The invention relates to the technical field of pharmaceutic preparations, in particular to carvedilol supersaturatable self-microemulsion dispersible tablets and a preparing method thereof. A carvedilol supersaturatable self-microemulsion preparation is prepared by combining an oil phase, a surfactant, a cosurfactant and a supersaturation promoter according to a certain ratio and mixed with other auxiliary materials after being adsorbed by an excipient, and then tabletting is conducted on powder directly to obtain the carvedilol supersaturatable self-microemulsion dispersible tablets. The prepared carvedilol supersaturatable self-microemulsion dispersible tablets can form microemulsion with particle size within 200 nm through spontaneous emulsification in the body after being orally taken. By the adoption of the supersaturatable self-microemulsion dispersible tablets, the dissolution rate of carvedilol in the gastrointestinal tract can be increased, bioavailability can be improved, usage of the surfactant and the cosurfactant in the prescription can be reduced, irritation to the gastrointestinal tract can be reduced, drug use safety can be improved, and market prospects are broad.