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Cariprazine hydrochloride long-acting sustained-release microspheres with high drug loading capacity and preparation method of Cariprazine hydrochloride long-acting sustained-release microspheres

A technology of cariprazine hydrochloride and slow-release microspheres, applied in the field of medicine, can solve the problems of large difference in theoretical drug loading, low utilization rate of raw materials, difficult control of blood drug concentration, etc., and reduce the burden of nursing care , reduce the frequency of administration and improve compliance

Active Publication Date: 2022-07-15
SHANGHAI JINGXIN BIOLOGICAL MEDICAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Ethyl acetate, methylene chloride, benzyl alcohol ethyl acetate or benzyl alcohol methylene chloride are mentioned in the examples as mixed solvents, and microspheres are prepared by emulsification-solvent evaporation method, as in Example 1, the theoretical drug loading is 40% , the measured drug loading is 10.3%, and the burst release in 1 day is 9%. Although the pores of the microspheres are continuous and complete, and can be released steadily for 28 days, there is a large difference between the theoretical drug loading and the actual drug loading. Low, and the first day burst release is high, the blood concentration in the body is not easy to control, so further research is still needed to improve the above phenomenon

Method used

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  • Cariprazine hydrochloride long-acting sustained-release microspheres with high drug loading capacity and preparation method of Cariprazine hydrochloride long-acting sustained-release microspheres
  • Cariprazine hydrochloride long-acting sustained-release microspheres with high drug loading capacity and preparation method of Cariprazine hydrochloride long-acting sustained-release microspheres
  • Cariprazine hydrochloride long-acting sustained-release microspheres with high drug loading capacity and preparation method of Cariprazine hydrochloride long-acting sustained-release microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-9

[0054] (1) Preparation of cariprazine hydrochloride long-acting sustained-release microspheres with benzyl alcohol-dichloromethane solvent system

[0055] The preparation steps are as follows:

[0056] Dissolving cariprazine hydrochloride and PLGA in an organic solvent to obtain an oil phase; dissolving polyvinyl alcohol (PVA) in purified water to prepare a solution with a concentration of 0.5-5wt%, and then filtering the solution through a filter membrane to obtain an aqueous phase ; At 25°C, the stirring speed is 350 rpm, and the oil phase is added to the water phase to make a microsphere emulsion; continue to stir for 10min, adjust the speed to 200 rpm, adjust the temperature to 40°C, and control the vacuum to -0.095 MPa, solidified under reduced pressure and stirred for 12 hours, the particles were collected by filtration, washed with purified water, and freeze-dried.

[0057] Wherein, organic solvent is the mixing of benzyl alcohol and dichloromethane, embodiment 1~9, th...

Embodiment 10～17

[0083] Cariprazine hydrochloride long-acting sustained-release microspheres are prepared by benzyl alcohol-ethyl acetate solvent system, and the preparation steps are as follows: dissolving cariprazine hydrochloride and PLGA in an organic solvent to obtain an oil phase; polyvinyl alcohol (PVA) ) dissolved in purified water to prepare a solution with a concentration of 0.5 to 5 wt %, and then the solution was filtered through a filter membrane to obtain an aqueous phase; at 25 ° C, the stirring speed was 350 rpm, and the oil phase was added to the aqueous phase. Continue to stir for 10min, adjust the rotation speed to 200 rpm, adjust the temperature to 40°C, control the vacuum to -0.095MPa, solidify and stir under reduced pressure for 12 hours, filter and collect the particles, wash with purified water, and freeze-dry.

[0084] Wherein, the organic solvent is the mixture of benzyl alcohol and ethyl acetate, embodiment 10~17, the consumption of cariprazine hydrochloride, the cons...

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Abstract

The invention relates to the technical field of medicines, and discloses a high-drug-loading-capacity cariprazine hydrochloride long-acting sustained-release microsphere which is characterized by comprising cariprazine hydrochloride and a polylactic acid-glycolic acid copolymer, the content of the cariprazine hydrochloride is 20-80%; an organic solvent used for dissolving the cariprazine hydrochloride and the polylactic acid-glycolic acid copolymer during preparation of the microspheres is a combination of benzyl alcohol and dichloromethane or benzyl alcohol and ethyl acetate. The cariprazine hydrochloride microsphere long-acting injection provided by the invention has a long-acting slow release effect, can realize slow release from one week to three months in an animal body, and can reduce the administration frequency of a patient, improve the compliance of the patient and reduce the nursing burden of family members of the patient and a national medical institution.

Description

technical field [0001] The invention relates to the technical field of medicine, and specifically discloses cariprazine hydrochloride long-acting sustained-release microspheres with high drug loading and a preparation method thereof. Background technique [0002] The pathogenesis of schizophrenia and bipolar disorder [0003] Schizophrenia (schizophrenia, SCH) is the most common, most complex, and most difficult to fully define major psychotic disorder, with a low incidence but high prevalence. According to the International Pilot Schizophrenia Survey (IPSS), the incidence of schizophrenia in the general population is 0.2‰ to 0.6‰, with an average of 0.3‰ [1] The latest research results of Tusang et al. in 2011 show that the global prevalence rate is about 5‰, and the overall social burden ranks fourth among various diseases. [2] . According to the figures provided by the Ministry of Health, there are about 16 million people with various mental illnesses in China, includi...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/495A61K47/34A61P25/18
CPCA61K31/495A61K9/0053A61K9/1647A61P25/18
Inventor 陈琰鹿月钱怡文刘调调刘烁华侯建
Owner SHANGHAI JINGXIN BIOLOGICAL MEDICAL