31 results about "Pimobendan" patented technology

A liquid preparation includes an etherified cyclodextrin derivative and a substituted benzimidazol, where the etherified cyclodextrin derivative is one of alpha-, beta, and gamma-cyclodextrin ether.

The invention is directed to a pharmaceutical tablet formulation for the veterinary medical sector containing an instable ACE inhibitor or a pharmaceutically acceptable salt thereof as a first pharmaceutically active substance, and pimobendan or a pharmaceutically acceptable salt thereof as a second pharmaceutically active substance, comprising granules which contain carrier core particles coated with at least one layer wherein the first pharmaceutically active substance is present, the granules being embedded in a tablet matrix wherein the second pharmaceutically active substance is present. It is provided a “fixed-dose-combination” which allows to ease the treatment and administration of the medication, improves the medication compliance by reducing the pill burden to the animal holder and enables the better observation of and adherence to the therapy by decreasing the number of tablets to be administered. The lower number of tablets leads to a lower treatment failure rate, minimizes dosage mistakes and avoids confusions by false dose intake and slower development of resistance.

The invention discloses a chemical synthesis method of Pimobendan. The method comprises steps as follows: acetanilide and 2-methyl-3-(chloroformyl)propionate react to produce 3-p-acetylaminobenzoyl methyl butyrate in a mixed organic solvent under the action of a composite catalyst, 3-p-acetylaminobenzoyl methyl butyrate reacts with a nitration reagent, 3-(4-acetamido-3-nitrobenzoyl)-methyl butyrate is produced and subjected to a reflux reaction with alkali in an alcohol solvent to produce 3-(4-amino-3-nitrobenzoyl) butyrate, 3-(4-amino-3-nitrobenzoyl) butyrate and hydrazine hydrate are subjected to a reflux reaction, 4,5-dihydro-5-methyl-6-(4-amino-3-nitrophenyl)-3(2H)-pyridazinone is produced and reduced with zinc powder in absolute methanol, 4,5-dihydro-5-methyl-6-(3,4-diaminophenyl)-3(2H)-pyridazinone is produced and subjected to a reflux reaction with p-anisaldehyde, and Pimobendan is obtained. The method comprises a few reaction steps, operation is safe and convenient, and the cost is low.

Pimobendan is used for reducing the heart size and / or delaying the onset of clinical symptoms in a patient suffering from asymptomatic (occult, preclinical) heart failure, preferably congestive heart failure, due to mitral valve disease (MVD), and / or delaying the onset of heart failure, preferably congestive heart failure, in a patient suffering from asymptomatic (occult, preclinical) heart failure, preferably congestive heart failure, due to mitral valve disease (MVD), wherein the patient is preferably a mammal, more preferably a human, a dog, a cat or a horse, and most preferably a dog.

The present invention is directed to a preserved liquid aqueous pharmaceutical composition comprising one or more etherified cyclodextrin derivatives; one or more water-soluble preservatives; preferably selected from the group consisting of sorbic acid or salts thereof, preferably sodium sorbate, potassium sorbate, calcium sorbate; benzoic acid or salts thereof, preferably sodium benzoate; benzalkonium chloride; benzethonium chloride; cetylpyridinium chloride; sodium metabisulfite; sodium acetate; parabenes and salts thereof, preferably methylparabene, ethylparabene, propylparabene, butylparabene, butylparabene sodium; or combinations thereof; and at least one pharmaceutically active compound which is poorly water-soluble, very poorly water-soluble or water-insoluble. The liquid aqueous pharmaceutical composition provides an acceptable solubility of the pharmaceutically active compound, such as pimobendan, in aqueous solution whereby the water-soluble preservatives retain their effectiveness in the presence of the etherified cyclodextrin derivatives allowing the use in an oral administration form.

The invention provides a novel process, which takes substituted propiophenone and oxoacetic acid as starting raw materials, carries out condensation to obtain 3-(substituted benzoyl)-2-butenoic acid, and carries out reduction and nitrification to obtain a pimobendan intermediate 3-(substituted benzoyl) butyric acid. The method has the advantages of few steps, easy and simple operation, easy separation and purification of products, high yield and low cost, uses common reagents, and is the novel process suitable for industrialized production.

A preserved liquid aqueous pharmaceutical composition includes one or more etherified cyclodextrin derivatives, at least one water-soluble preservative, and at least one pharmaceutically active compound which is poorly water-soluble, very poorly water-soluble or water-insoluble. The liquid aqueous pharmaceutical composition provides an acceptable solubility of the pharmaceutically active compound, such as pimobendan, in aqueous solution whereby the water-soluble preservatives retain their effectiveness in the presence of the etherified cyclodextrin derivatives allowing the use in an oral administration form.

The invention relates to a preparation technology of a pimobendan key intermediate 6-(4-amino-3-nitro phenyl)-5-methyl-4, 5-dihydrogen pyridazine-3(2H)-ketone (formula V). The preparation technology is short in synthesis route and simple in operation, thus having large industrial production prospect. The chemical reaction formula is shown in the description.

The invention relates to oral pharmaceutical compositions comprising pimobendan pharmaceutically active compound. It also relates to a method for preparing the same uses thereof.

The invention relates to a novel preparation process of pimobendan. The process comprises short steps, does not refer to dangerous and highly toxic reagents such as Br2, KCN and NaH which have limitation in wide industrial use, is simple in operation and mild in reaction conditions and has obvious superiorities in industrial production.

The present invention is directed to a composition comprising particles of pimobendan with an integral coating of a carrier matrix which serve to ensure a rapid dissolution of the active substance at each pH condition representing the gastrointestinal tract and therefore a reliable absorption, and a method of pimobendan microencapsulation using the spray congealing technology and incorporating the coated particles into oral formulations, for example into tablets.

A composition includes particles of pimobendan with an integral coating of a carrier matrix which serve to ensure a rapid dissolution of the active substance at each pH condition representing the gastrointestinal tract and therefore a reliable absorption, and a method of pimobendan microencapsulation using the spray congealing technology and incorporating the coated particles into oral formulations, for example into tablets.