17 results about "Mirabegron" patented technology

The present invention relates to mirabegron substantially free from genotoxic impurities particularly nitrosamine impurities of Formula (I), (II), (III), (IV), (V) and processes for its preparation. In particular, the invention relates to processes for the preparation of high purity mirabegron free from nitrosamine impurities of Formula (I), (II), (III), (IV), (V) and other genotoxic and carcinogenic impurities below threshold concentration.

The present invention relates to extended release composition of Mirabegron and process of manufacture thereof. The extended release composition of mirabegron comprising non-polymeric hydrophobic excipient as release controlling agent along with one or more pharmaceutically acceptable excipient is used in the treatment of symptoms associated with overactive bladder.

One embodiment of the present invention provides a mirabegron-containing preparation that suppresses formation of N-nitroso mirabegron. A mirabegron-containing preparation according to one embodiment of the present invention includes a mirabegron-containing tablet, blister packaging that accommodates and encloses the mirabegron-containing tablet, pillow packaging that encloses the blister packaging that accommodates the mirabegron-containing tablet, and a zeolite that is provided in the space between the blister packaging and the pillow packaging. The N-nitroso mirabegron content of the mirabegron-containing tablet after storage for 3 months at 40°C and a relative humidity of 75% may be 50% or less of an acceptable limit value for N-nitroso mirabegron.

The present invention relates to a multi-layer pharmaceutical formulation comprising a prolonged-release mirabegron or a pharmaceutically acceptable salt thereof, an immediate- release solifenacin or a pharmaceutically acceptable salt thereof with a proper ratio of solifenacin succinate to binder in the immediate-release-layer for use in the treatment of overactive bladder.

The invention discloses a mirabegron sustained release preparation and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. The mirabegron sustained-release tablet comprises the following components in parts by mass: 60-90 parts of a mirabegron sustained-release compound, 20-80 parts of a film-forming agent, 1-20 parts of a plasticizer, 0-3 parts of a thickening agent and 0-1 part of a sweetening agent. The mirabegron sustained-release preparation prepared by the invention not only realizes the sustained-release effect of mirabegron, but also realizes accurate and controllable dosage, can be rapidly disintegrated in the oral cavity without water, is extremely convenient in administration mode, and greatly improves the medication compliance of patients.

The present invention relates to a composition for topical and / or transdermal administration comprising mirabegron or a salt thereof, the composition comprising: a) mirabegron or a salt thereof in the range of ≧0.01 wt.-% to ≦25 wt.-%; and b) a solvent, the solvent being: dimethyl sulfoxide (DMSO) in the range of ≧5 wt.-% to ≦99.99 wt.-%; or and a solvent selected from i) a monoalcohol in the range of ≧5 wt.-% to ≦94.99 wt.-%, or ii) glycerol, glycol, polyethylene glycol, glycol ether, mixtures thereof, or mixtures with monoalcohols in the range of ≧5 wt.-% to ≦60 wt.-%, or iii) a further solvent selected from water in the range of ≧2 wt.-% to ≦10 wt.-%, where the wt.-% is based on the total weight of the composition of 100 wt.-%.

The invention provides a mirabegron refining method which comprises the following steps: adding sulfite or hydrosulfite into a mirabegron solution, and separating to obtain a mirabegron finished product. The method can effectively inhibit generation of color development impurities in mirabegron or remove the color development impurities, the refining method is high in yield, low in cost and suitable for industrial mass production, and after long-term storage, the color still meets the pharmacopeia standard.

The invention discloses an HPLC analysis method for an impurity reference substance of mirabegron. The invention reports the impurity for the first time, and the provided HPLC analysis method can effectively elute and separate mirabegron and the impurity, so that the peak of the impurity is completely separated from the peak of mirabegron, thereby quickly and reliably controlling the impurities of mirabegron products.

The present invention relates to a composition for topical and / or transdermal application comprising mirabegron or a salt thereof, wherein the composition comprises: a) > = 0.01 wt.-% to < = 25 wt.-% mirabegron or a salt thereof; and b) a solvent selected from the group consisting of:-> = 5 wt.-% to < = 99.99 wt.-% dimethyl sulfoxide (DMSO); or > = 5 wt.-% to < = 97.99 wt.-% of a mixture of dimethyl sulfoxide with other solvents selected from i) > = 5 wt.-% to < = 94.99 wt.-% of a monohydric alcohol, or ii) > = 5 wt.-% to < = 60 wt.-% of glycerol, ethylene glycol, polyethylene glycol, glycol ether, mixtures thereof, or a mixture with a monohydric alcohol, or iii) > = 2 wt.-% to < = 10 wt.-% of water; wherein wt.-% is based on 100 wt.-% of the total weight of the composition.

The invention relates to a mirabegron taste-masking preparation as well as a preparation method and application thereof, mirabegron or pharmaceutically acceptable salt thereof is taken as an active pharmaceutical ingredient, and a functional auxiliary material glyceryl behenate is added into a prescription, so that various effects of masking taste, lubricating and aiding flow and defoaming are achieved; performance tests show that the mirabegron taste-masking preparation is sufficient in taste masking, better in lubricating performance, better in defoaming performance, more stable in chemical property, less in use variety of preparation auxiliary materials, more stable in product quality and easier to commercially produce and implement. In addition, the preparation method of the mirabegron taste-masking preparation is simple, convenient and economical, a simple three-in-one equipment one-pot compound preparation mode, a fluidized bed granulation mode and a physical mixing mode are adopted in production, and compared with a traditional method, the mirabegron taste-masking preparation is simpler, more convenient and easier to industrialize and has great economic and social benefits.

The present invention belongs to the technical field of pharmaceutical chemistry, and particularly relates to a mirabegron sustained-release tablet degradation impurity, its preparation method and application. The mirabegron sustained-release tablet degradation impurity N-(4-{2-[acetyl-((2R)-2-hydroxy-2-phenylethyl)-amino]-ethyl}-phenyl)-2-(2-aminothiazol-4-yl)-acetamide provided by the present invention is a new mirabegron sustained-release tablet degradation impurity and can be used for the quality standard control of related substances of mirabegron sustained-release tablets. The mirabegron sustained-release tablet degradation impurity of the present invention increases during the forced degradation experiment, the compatibility experiment of raw materials and excipients, the stress test and the stability experiment of the preparation product, and there is a risk of exceeding the quality control limit during the stability period. Therefore, it is necessary to conduct qualitative research and quality control on it, include it in the quality standard of related substances of mirabegron sustained-release tablets, and the control standard is accurate and reliable.

The present invention relates to bilayer tablet pharmaceutical compositions comprising an immediate-release layer comprising solifenacin succinate as active ingredient, a binder, a distintegrant and at least one pharmaceutically acceptable excipient, a prolonged-release layer comprising mirabegron as active substance and at least one pharmaceutically acceptable excipient.

The present invention relates to prolonged-release tablet compositions comprising 25 mg mirabegron, polyethylene oxide and hydroxypropyl methylcellulose as release modifying agents.

The present invention relates to an extended release pharmaceutical composition of mirabegron comprising mirabegron or a pharmaceutically acceptable salt thereof, polyethylene glycol having an average molecular weight of 1,800 to 9,000, polyethylene oxide having an average molecular weight of 70,00,000 to 1,00,00,000 and a viscosity of more than 7,500 mPa·s in a 1% aqueous solution at 25 °C and at least one pharmaceutical acceptable excipient.

The present invention relates to an extended release pharmaceutical composition of mirabegron comprising mirabegron or a pharmaceutically acceptable salt thereof, polyethylene glycol having an average molecular weight of 1,800 to 9,000, polyethylene oxide having an average molecular weight of 70,00,000 to 1,00,00,000 and a viscosity of more than 7,500 mPa·s in a 1% aqueous solution at 25 °C and at least one pharmaceutical acceptable excipient.

The present invention discloses a mirabegron sustained-release tablet and a preparation method thereof. The weight percentage contents of the components of the mirabegron sustained-release tablet are as follows: mirabegron 0.5% to 25%, hydroxypropyl methylcellulose 1% to 40%, sodium alginate 1% to 40%, polyethylene glycol 10% to 60%, stearic acid 0.5% to 30%, hydroxypropyl cellulose 0.1% to 20%, magnesium stearate 0.01% to 5%, and coating premix 0.5% to 20%. The mirabegron sustained-release tablet provided by the present invention has a long release time, high safety, and complete release, improves the bioavailability, and is simple to prepare and suitable for industrial production.

The invention provides an analysis method for detecting nitrosamine impurities in mirabegron. The two nitrosamine impurities, namely an impurity A and an impurity B, can be separated and detected at the same time. The method is high in sensitivity and good in specificity, repeatability and durability, and quantitative detection of nitrosamine impurities A and B in mirabegron can be rapidly and accurately achieved.