4 results about "Brexpiprazole" patented technology

The application belongs to the technical field of chemical medicines, and particularly relates to 4,5-dichloro-3-hydroxy-6-({4-[(2-oxo-1H-quinolin-7-yl)oxy]butyl}oxy)benzene-1,2-dicarbonitrile, a preparation method and application thereof. H The 4,5-dichloro-3-hydroxy-6-({4-[(2-oxo-1H-quinolin-7-yl)oxy]butyl}oxy)benzene-1,2-dicarbonitrile has a structure shown in formula I: formula I. The impurity in brexpiprazole contains the structure shown in formula I, the content of the impurity in brexpiprazole can be effectively detected by using the novel compound provided by the application as a standard sample, and the drug quality stability and drug safety can be effectively ensured.

The application belongs to the technical field of medicine synthesis, and particularly relates to a preparation method of brexpiprazole. The application takes compound 4-amino benz[b] thiophene and 2-chloroethyl methyl sulfonate as starting materials, first carries out a double-substitution reaction to obtain an intermediate N,N-bis(2-chloroethyl) benz[b] thiophene-4-amine, then carries out a substitution reaction on the intermediate and 7-(4-aminobutoxy) quinoline-2(1H)-ketone to construct a piperazine ring to obtain the target product brexpiprazole. The product obtained through the process has high yield and purity, and is suitable for industrial production.

The present invention belongs to the field of pharmaceutical preparations, and relates to a long-acting brexpiprazole microsphere and a preparation method therefor. The method comprises the following steps: (1) dissolving brexpiprazole and a degradable polymer in an organic solvent to obtain a drug-containing polymer solution as an oil phase; (2) mixing the drug-containing polymer solution with a polyvinyl alcohol solution by means of a microfluidic technique to obtain an oil-in-water emulsion; and (3) under stirring, solidifying, washing and freeze-drying the oil-in-water emulsion to obtain the long-acting brexpiprazole microsphere. In the present invention, the in-vitro release rate of the final microsphere is adjusted by means of adjusting the volatilization and stirring time during the formation of the O / W primary emulsion, thereby screening microspheres with no burst release or lag period, and exhibiting sustained release. The long-acting brexpiprazole microsphere provided in the present invention has a simple preparation process, is readily scalable for industrial production, exhibits high encapsulation efficiency, high drug loading capacity, uniform microsphere particle size distribution, spherical morphology, good flowability, good syringeability and injectability, has a significant sustained-release effect, and can be used to reduce fluctuations in blood drug level and effectively improve the compliance of patients with psychiatric diseases.