177 results about "Isosorbide mononitrate" patented technology

A slow-releasing tablet of isosorbide mononitrate for treating coronary heart disease and angina pectoris is prepared proportionally from isosorbide mononitrate, slow releasing agent, adhesive, filler and lubricant through proportional mixing, granulating, and tabletting.

The invention describes methods for treating blood disorders or for treating the symptoms and/or complications associated with blood disorders by administering a therapeutically effective amount of at least one nitric oxide donor compound and optionally at least one antioxidant, or a pharmaceutically acceptable salt thereof, and/or at least one therapeutic agent. The antioxidant is preferably a hydralazine compound or a pharmaceutically acceptable salt thereof. The nitric oxide donor compound is preferably N-hydroxy-L-arginine and/or isosorbide dinitrate and/or isosorbide mononitrate. The blood disorder is preferably sickle cell anemia. The complication resulting from a blood disorder is preferably pulmonary hypertension.

The invention describes novel compositions comprising at least one apocynin compound or a pharmaceutically acceptable salt thereof, and at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The invention also provides novel kits comprising at least one apocynin compound or a pharmaceutically acceptable salt thereof, and at least one nitric oxide donor compound, and, optionally, at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating gastrointestinal disorders; (h) treating inflammatory disorders; and (j) treating respiratory disorders. The apocynin compound may preferably be apocynin. The nitric oxide donor compound may preferably be isosorbide dinitrate and/or isosorbide mononitrate.

Novel derivatives of isosorbide mononitrate and its pharmaceutically acceptable salts, which have vasodilating activity with a reduced effect of tolerance, of the general formula (I)

in which A and B independently represent any of the groups

—ONO₂ and —Z—CO—R, wherein Z is an oxygen atom or sulphur atom and R is an alkyl C₁-C₄ group, an aryl group or an aralkyl group, eventually substituted, or the group

in which R¹ is hydrogen, or an alkyl C₁-C₄ group, an aryl group or an aralkyl group, eventually substituted, with the proviso that one of A or B is always —ONO₂, but never both of them at the same time, when Z is an sulphur atom R is an alkyl C₁-C₄ group, an aryl group or an aralkyl group, eventually substituted, and when Z is an oxygen atom R is the group

The invention discloses a time quick-release and slow-release preparation of isosorbide mononitrate. The technical problem for the invention to solve is to provide a time quick-release and slow-release preparation, which is provided with long time of retaining the effective plasma-drug concentration and a low interval of 5-ISMN plasma-drug concentration. Each structure layer of the invention is orderly arranged from the inside to the outside as a parent nuclear of a pill core, a drug layer of a second dosage, an insulating layer, a slow-release coating layer, a drug layer of a first dosage, an expanding layer and a release controlling layer. The weight percentages of each layer are 15 to 40 percent of the parent nuclear of the pill core, 0.3 to 5.7 percent of the drug layer of the second dosage, 0 to 20 percent of the insulating layer, 5 to 40 percent of the slow-release coating layer, 0.7 to 13.4 percent of the drug layer of the first dosage, 5 to 30 percent of the expanding layer and 5 to 40 percent of the release controlling layer. The invention combines the characteristics of a time quick-release and slow-release medication system to avoid the drug resistance as well as accurately meet the clinical requirement of the angina treatment of the patient of the coronary heart disease.

The invention provides a method for synthesizing and purifying 5-isosorbide mononitrate. The method comprises the steps of: (1) preparing a nitrifying reagent from concentrated nitric acid, acetic acid and acetic anhydride, and directly nitrifying isosorbide to obtain an isosorbide nitride mixture; (2) adding water to arouse a quenching reaction, separating out 2,5-isoscrbide dinifrate at a temperature ranging from 0 to 5 DEG C, and filtering out the 2,5-isoscrbide dinifrate; (3) reacting the filtrate with sodium hydroxide to prepare an isosorbide mononitrate sodium salt aquo-complex, filtering, and hydrolyzing the sodium salt; and (4) extracting, concentrating and recrystallizing to obtain high-purity 5-isosorbide mononitrate. The preparation method provided by the invention is simple, safe, easy to operate and short in reaction period; impurities are easy to remove, and the yield and the purity are high; therefore, the method lays a foundation for industrial production.

The preparation process of isosorbide mononitrate as angina pectoris resisting medicine includes the following steps: directly nitrating sorbitol with fuming nitric acid and concentrated sulfuric acid in 0-0.5 time to obtain 2, 5-dinitro isosorbate; and the subsequent catalytic hydrogenation with ruthenium complex as catalyst and selective reduction of 2-nitro group. The present invention has simple process and high yield.

The invention discloses an isosorbide mononitrate timing controlled release preparation and a preparation method thereof. The isosorbide mononitrate timing controlled release preparation of the present invention has certain time-lag and long-acting stationary release, and comprises a semi-permeable membrane with drug release apertures, an isolating coating and a double layer label including a drug contained layer and a boosting layer. The isosorbide mononitrate timing controlled release preparation of the present invention is an osmotic pump tablet with certain time-lag and long-acting stationary release, and can provide a more lasting and stationary plasma concentration and is bioequivalent compared with a sale long-acting preparation Elantan.

The invention relates to a tablet of isosorbide mononitrate, in particular to a double-layer osmotic pump controlled release tablet of isosorbide mononitrate, which belongs to the field of medicine preparation. A single-chamber double-layer osmotic pump tablet of the isosorbide mononitrate is characterized in that a semi-transparent coating film cover a double-layer core body consisting of a medicine-containing layer and a boosting layer; and the coating film is provided with a medicine releasing pore on the surface of the medicine-containing layer. The gastrointestinal tract water enters a double-layer tablet chip through the semi-transparent film; the medicines forms a mixed suspension liquid or solution when contacting water in the medicine-containing layer; a penetration enhancer enables the solution of the medicine-containing layer to be hypertonic so that an osmotic pressure difference exists between the inner side and the outer side of the film, which is beneficial to pumping the medicines out; and the pressure is generated in the boosting layer through water absorption, dissolution and expansion of a penetrating agent so as to further boost a medicine liquid to eject the pore.

The invention relates to the field of medicaments, and in particular relates to isosorbide mononitrate sustained-release pallets, a preparation prepared from the same and a preparation method for the isosorbide mononitrate sustained-release pallets. Each sustained-release pallet consists of a blank pallet core, a medicament-carrying layer, a sustained-release layer and a quick-release layer, wherein the medicament-carrying layer consists of isosorbide mononitrate, a first filling agent and a first adhesive; the sustained-release layer consists of a sustained-release material, a pore-forming agent, an anti-sticking agent, a plasticizer and a second adhesive; the quick-release layer consists of isosorbide mononitrate, a second filling agent and a third adhesive. The isosorbide mononitrate sustained-release pallets and the preparation prepared from the same are stable in property, reliable in quality and high in bioavailability, remarkable changes in the in-vitro release of a medicament caused by the crystallization of isosorbide mononitrate can be avoided, and the stability of the isosorbide mononitrate sustained-release pallets and the preparation prepared from the same is improved.

A liquid sodium chloride injection of isosorbide mononitrate for treating coronary heart disease and angina pectoris is prepared from isosorbide mononitrate and sodium chloride. It can quickly take its high curative effect.

The invention belongs to the field of pharmaceutic preparation, and particularly relates to an isosorbide mononitrate sustained release tablet and a preparation method thereof. The tablet prescription of the sustained release tablet in the application comprises the following components: isosorbide mononitrate, hydroxypropyl methylcellulose K4M, microcrystalline cellulose, silicon dioxide and sodium dodecyl sulfate. The isosorbide mononitrate sustained release tablet prepared by the components has better stability.

The invention relates to an isosorbide mononitrate sustained-release tablet and a preparation method thereof, belonging to the technical field of medicinal preparations. The sustained-release tablet comprises a coating of isosorbide mononitrate drug loaded microballoons which account for 48% to 55% of the total weight of the tablet and a quick-release layer which accounts for 45% to 52% and comprises isosorbide mononitrate, a binder, a filler and a lubricant. According to the invention, isosorbide mononitrate is divided into two parts, i.e., the part of quick release and the part of sustained release, which enables the tablet to take effect rapidly at an initial stage of administration, maintain an effective plasma concentration after the effective plasma concentration is reached and retain the effective plasma concentration at a low level so as to reduce residual quantity of the tablet at administration time of the tablet the next day, thereby effectively avoiding generation of drug resistance.

The invention relates to an isosorbide mononitrate osmotic pump type controlled release preparation and a preparation method thereof. The osmotic pump type controlled release preparation is composed of a tablet core and semipermeable film coating with medicine releasing holes; wherein, the tablet core is composed of isosorbide mononitrate, penetration enhancer, bond and other excipient, and the semipermeable film includes coating material and plasticizer; the punching mode includes mechanical drilling and laser drilling. The preparation of the invention can effectively control the constant speed release rate of medicine and has the advantages of few administration times, less side effect, long efficacy lasting time, avoidance of medicine tolerance, etc.

The invention provides methods for (a) reducing mortality associated with heart failure; (b) improving oxygen consumption; (c) treating heart failure; (d) treating hypertension; (e) improving the quality of life in a heart failure patient; (f) inhibiting left ventricular remodeling; (g) reducing hospitalizations related to heart failure; (h) improving exercise tolerance; (j) increasing left ventricular ejection fraction; (k) decreasing levels of B-type natriuretic protein; (l) treating renovascular diseases; (m) treating end-stage renal diseases; (n) reducing cardiomegaly; (o) treating diseases resulting from oxidative stress; (p) treating endothelial dysfunctions; (q) treating diseases caused by endothelial dysfunctions; or (r) treating cardiovascular diseases; in a patient in need thereof, wherein the patient has a Arg389Arg polymorphism and/or a Gly389Gly polymorphism in the beta 1 adrenergic receptor gene, comprising administering to the patient (i) at least one antioxidant compound or a pharmaceutically acceptable salt thereof; (ii) at least one nitric oxide enhancing compound; and (iii) optionally the best current therapy for the treatment of cardiovascular diseases. In one embodiment the antioxidant is a hydralazine compound or a pharmaceutically acceptable salt thereof and the nitric oxide enhancing compound is isosorbide dinitrate and/or isosorbide mononitrate.

The invention provides a preparation method for isosorbide 5-mononitrate. The preparation method comprises the following steps: with isosorbide dinitrate as a raw materials and Pd/C as a catalyst in a special mixed solvent, carrying out selective hydrogenation reduction on 2-nitro, filtering after reaction, steaming to remove ethyl alcohol in filtrate, extracting residual concentrated liquid through ethyl acetate, washing extracting liquid through dilute acid, washing to be neutral through water, drying through anhydrous magnesium sulfate, filtering to remove a drying agent and steaming to remove ethyl acetate so as to obtain high-purity isosorbide 5-mononitrate. Compared with the prior art, the synthetic method provided by the invention is simple and easy to operate, impurities are easy to remove, the yield and purity are higher, the cost is reduced since the Pd/C and the solvent can be recycled and reused, isosorbide generated through over reduction can be recycled and the preparation method is suitable for industrial production.

The invention discloses isosorbide mononitrate sustained release tablets and a preparation process thereof. According to the preparation, the sustained release aim is achieved by adopting a method for combining mesoporous carbon and membrane controlled coating. The process comprises the following steps: preparing a mesoporous carbon-isosorbide mononitrate complex; by taking ethyl cellulose as a sustained release coating material and taking hydroxyethyl cellulose as a pore-foaming agent, performing bottom-spray coating by adopting a fluidized bed to obtain sustained release coated pills; and mixing the pills with other pharmaceutically acceptable auxiliary materials, and pressing into the tablets. The sustained release tablets disclosed by the invention have the advantages that the drug release is stable, membrane aging is avoided in the storage process, the drug release stability is high, the bioavailability is high, and the preparation process is simple.

The invention relates to isosorbide mononitrate sodium chloride injection which belongs to the field of medical preparation. The isosorbide mononitrate sodium chloride injection is prepared from 10-40mg of isosorbide mononitrate, 450-1800mg of sodium chloride, an amount of pH regulator which regulates the pH to 4.0-7.0 and water for injection, wherein the volume of the water for injection is fixed to 100ml. The isosorbide mononitrate sodium chloride injection has high stability and simple preparation process.

The invention belongs to the technical field of pharmaceutical preparation and provides an isosorbide mononitrate freeze-dried power injection and a preparation method thereof. In the preparation process of the isosorbide mononitrate freeze-dried power injection of the invention, sorbic alcohol is used as a propping agent and the pH value of the solution of a middle body is adjusted to between 6.5 and 7.5 by acidic or alkaline buffer solution, so the hydrolysis of a main medicament is restrained and the stability of the main medicament is improved; and a pre-freezing initial temperature is controlled to be below 50 DEG C below zero, and the second sublimation temperature in a free-drying process is controlled to be between 5 and 15 DEG C, so the medicament content and the stability of related substances are improved. The stable isosorbide mononitrate freeze-dried power injection prepared by the method has reduced toxicity and good clinical effects.

The invention belongs to the field of pharmaceutical preparations, and particularly discloses a large-sized isosorbide mononitrate sustained release tablet and a preparation method thereof. Accordingto the prescription, the sustained release tablet is prepared from the components: isosorbide mononitrate:lactose (6:4), hydroxypropyl methylcellulose K200M, microcrystalline cellulose, mannitol, hydrogenated castor oil, silica and magnesium stearate. According to the large-sized isosorbide mononitrate sustained release tablet and the preparation method thereof, the microcrystalline cellulose, themannitol and the hydrogenated castor oil of a certain proportion are mixed to greatly improve the fluidity of mixed powder, and requirements of producing pressed tablets are met.

The invention describes novel compositions comprising nebivolol and/or at least one metabolite of nebivolol and at least one nitric oxide donor, and, optionally, at least one antioxidant or a pharmaceutically acceptable salt thereof, and/or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and/or at least one nitrosated compound used to treat cardiovascular diseases. The compounds and compositions of the invention can also be bound to a matrix. The nitric oxide donor is a compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The invention also provides methods for treating and/or preventing vascular diseases characterized by nitric oxide insufficiency; and for treating and/or preventing Raynaud's syndrome; and for treating and/or preventing cardiovascular diseases or disorders.

The invention provides a novel isosorbide mononitrate injection composition containing 1,2-propylene glycol and phosphate buffer and a preparation method thereof. Phosphate buffer is used to adjust the pH of the injection to 6.8-7.9. The injection prepared by the application of the invention improves the purity of the effective components of the medicine, reduces the content of related substances, and reduces the toxicity at the same time.

The invention belongs to the field of medicine synthesis, and particularly discloses a method for synthesizing 5-isosorbide mononitrate by the aid of micro-channel reactors. The method includes pumping nitrification reagents and isosorbide liquid into the micro-channel reactors and carrying out hybrid reaction; allowing products to flow out from outlets of the micro-channel reactors after the reaction is completely carried out; carrying out after-treatment on the products and separating and purifying the products to obtain the 5-isosorbide mononitrate which is a target product. The method hasthe advantages that the method is short in reaction time and is safe as compared with the traditional processes, and the yield of the 5-isosorbide mononitrate can be greatly increased.