81 results about "Glycopyrronium bromide" patented technology

Individually packaged topical formulations comprising about 0.25 to about 6% w/w of glycopyrrolate for the treatment of hyperhidrosis, wherein said wipe is contained within a pouch resistant to leakage. The formulations may further comprise ethanol, a buffering agent and water. In addition, the formulations may further comprise a polymer system comprising a hydrophobic polymer in combination with a hydrophilic polymer.

Aerosol formulations comprising glycopyrronium bromide in combination with formoterol are useful for the prevention or treatment of chronic obstructive pulmonary disease. The formulation further comprises a HFA propellant, a co-solvent, and an amount of inorganic acid sufficient to stabilize both the glycopyrronium bromide and the formoterol components. Optionally the formulation may further comprise beclometasone dipropionate.

Glycopyrronium bromide, derivatives and/or isomers thereof in combination with one or more active substances selected from a list of substances as recited in the claims and/or in the form of a W/Si emulsion, an O/W gel, a soap gel stick, and/or a surfactant-containing cleansing formula, and corresponding cosmetic preparations, in particular deodorant/antiperspirant preparations.

Aerosol solution compositions intended for use with a pressurized metered dose inhaler, comprising glycopyrronium bromide and formoterol, or a salt thereof or a solvate of said salt, optionally in combination with one or more additional active ingredients, and stabilized by a selected amount of a mineral acid, exhibit improved stability when contained in a can internally coated by a resin comprising a fluorinated ethylene propylene (FEP) polymer.

A method for the production of crystalline glycopyrronium bromide, comprises the reaction of glycopyrronium base with methyl bromide in a solvent, in which the solvent is selected such that the diastereoisomeric ratio of the product favours the R, S and S, R diastereoisomers over the R, R, and S, S diastereoisomers, and separating the desired diastereoisomers by one or more controlled crystallisation steps. This method gives a product having a particle size of narrow distribution.

The invention belongs to the technical field of medicine, and discloses a preparation method of (3S,2'S), (3S,2'R), (3R,2'R) and (3R,2'S) four type chiral monomers of muscarine receptor antagonist racemic medicine glycopyrronium bromide. The method comprises the following steps: resolving racemic alpha-cyclopentylmandelic acid by a chemical resolution method by using L-Tyrosine methyl ester and (R)-alpha-phenylethylamine as resolution reagents to respectively prepare (S)-alpha-cyclopentylmandelic acid and (R)-alpha-cyclopentylmandelic acid; and carrying out esterification reaction to respectively obtain chiral intermediates (S)/(R)-alpha-cyclopentylmethyl mandelate. L/D-malic acid used as the raw material is subjected to four reaction steps, including condensation, carbonyl reduction, catalytic hydrogenation or transfer hydrogenation reduction debenzylation, and reduction alkylation or alkylogen alkylation, in a chiral synthesis mode to obtain another important chiral intermediate (S)/(R)-N-methyl-3-hydroxypyrrolidine. The chiral intermediate is subjected to ester exchange and quaterisation to respectively obtain the four (3S,2'S), (3S,2'R), (3R,2'R) and (3R,2'S) type glycopyrronium bromide chiral monomers. The result indicates that the (3R,2'S)-glycopyrronium bromide has the strongest cholinergic antagonistic action.

The invention belongs to the technical field of medicine and discloses a preparation method of muscarinic receptor antagonist glycopyrronium bromide. The preparation method of the muscarinic receptor antagonist glycopyrronium bromide is characterized in that Alpha-cyclopentyl mandelic acid methyl ester is obtained by aceptophenone ketonic acid Grignard reaction and esterification reaction, and then glycopyrronium bromide is obtained by N-methyl pyrrolidine-3-alcohol ester exchange and quaterisation.

Stable aerosol solution formulations comprising glycopyrronium bromide are useful for administration to patients with COPD and other respiratory conditions.

The invention relates to an atomizing agent with arformoterol and glycopyrronium bromide serving as active components and a preparation method of the atomizing agent. The invention further relates to an application of glycopyrronium bromide in improving the stability of an arformoterol water solution. Arformoterol and glycopyrronium bromide can perform a synergistic function pharmacologically while glycopyrronium bromide is used for improving the stability of arformoterol, and accordingly, the local treatment function on the lung is improved.

The invention relates to a method for separating glycopyrronium bromide enantiomers through a capillary electrophoresis technique, and inspecting impurities of the enantiomers. The glycopyrronium bromide enantiomers are separated through capillary electrophoresis, the positions of the peaks of four glycopyrronium bromide enantiomer monomers are confirmed, and the limit of enantiomers in glycopyrronium bromide is calculated according to an impurity control technique; and water is used to prepare all tested samples, a capillary electrophoresis buffer solution is a sodium dihydrogen phosphate buffer solution, and sulfonated-beta-cyclodextrin (S-beta-C-D) is added to the above buffer salt. The method adopting the capillary electrophoresis technique to separate glycopyrronium bromide has the advantages of good separation effect, low amount of the samples, no pollution and low cost, and is suitable for separating racemic glycopyrronium bromide.

The invention discloses a solution type metered dose inhalation aerosol of glycopyrronium bromide or derivatives thereof and a preparation method thereof. The aerosol comprises a main drug, a cosolvent, a surfactant and a propellant. The aerosol is high in fine particle fraction (FPF) and good in placement stability under long-term reserving and accelerating conditions, and the FPF does not have remarkable variation. Pharmacodynamic test results indicate that the aerosol is quick in response, can be used for treating bronchial asthma and chronic obstructive pulmonary disease, and has excellent effects of resisting airway inflammation, airway fibrosis and airway remodeling.

The invention discloses glycopyrronium bromide injection and a preparation method thereof. The preparation method disclosed by the invention comprises the following steps of: (1), adding 50-90% of injection water into a preparation tank, adding sodium chloride, adding a pH adjusting agent after dissolving to adjust the pH value to 1.0-4.0, and then, diluting to total weight by adding injection water to obtain solution A; (2), adding glycopyrronium bromide into the solution A at the constant temperature of 30-40 DEG C, stirring till dissolving completely, crudely filtering in a filtrate tank through a milliporous filtration membrane which is 0.45 mu m, and finally filtering through a milliporous filtration membrane which is 0.22 mu m to obtain an intermediate product; (3), filling the filtrate tank into a neutral boron-silicon container, sealing, and sterilizing through steam at 115-121 DEG C for 8-30 min to obtain the glycopyrronium bromide injection. The glycopyrronium bromide injection disclosed by the invention has the characteristics of being good in stability, high in safety and the like.

Aerosol formulations comprising glycopyrronium bromide, formoterol or a salt thereof, and beclometasone dipropionate are useful for the prevention or treatment of moderate/severe chronic obstructive pulmonary disease.

The invention discloses a method for purifying a glycopyrronium bromide intermediate 2-cyclopentyl-2-hydroxyphenylacetic acid. The method comprises the following steps: (1) heating and dissolving crude 2-cyclopentyl-2-hydroxyphenylacetic acid in a mixed solvent of ethanol and water, cooling, crystallizing, and filtering to obtain a solid; (2) heating and dissolving the solid obtained in the step (1), cooling, crystallizing, and filtering, thereby obtaining the solid 2-cyclopentyl-2-hydroxyphenylacetic acid. According to the method, the various impurities can be effectively removed, the productpurity is obviously improved, the purity of HPLC (High Performance Liquid Chromatography) is more than 98.0%, the loss of the 2-cyclopentyl-2-hydroxyphenylacetic acid is reduced to the greatest degree, the yield is improved, and the method is suitable for industrial production.

The invention discloses glycopyrronium bromide injection and a preparation method thereof. The glycopyrronium bromide injection comprises glycopyrronium bromide, a pH adjusting agent and water for injection, and no benzyl alcohol or sodium chloride is contained. The glycopyrronium bromide injection prepared through the preparation method is controllable in quality, good in stability and suitable for industrial production.

The invention discloses a preparation method of glycopyrronium bromide. The preparation method comprises the following steps: firstly, protecting hydroxyl of alpha-cyclopentyl mandelic acid with benzyl; then carrying out esterification with 1-methyl-3-pyrrolidinol by means of a conventional method to obtain a key intermediate ester of pyrrolidinol; carrying out debenzylation on the key intermediate ester under a condition of Pd/C; and finally, carrying out quaterniziation and salification on methyl bromide to separate out a solid, filtering the solid to obtain a coarse product of glycopyrronium bromide, and refining the coarse product to obtain a qualified product of glycopyrronium bromide. In order to prevent side reactions, hydroxyl is introduced with a very low cost to protect benzyl, so that the yield is improved greatly, the post-treatment is reduced, and the wastewater amount is reduced. The method disclosed by the invention has the characteristics of being simple in production operation, low in production cost, easily available in raw material, high in yield, small in pollution and the like. The obtained product meets the drug standard.