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Long-acting injectable microsphere based on aripiprazole microcrystal aggregate and preparation method of long-acting injectable microsphere

A technology of aripiprazole and microspheres, applied in the field of long-acting injectable microspheres and its preparation, can solve the problems of low blood drug concentration, large particle size of microspheres, difficulty in injection, etc. Good ball performance and improved compliance

Pending Publication Date: 2021-09-21
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The aripiprazole core-shell microspheres involved in this patent use dichloromethane as the solvent, the average particle size is 20-150 μm, and the drug loading is 55%-95%. Large particle size of microspheres, difficulty in injection, and low blood drug concentration in the early stage of release

Method used

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  • Long-acting injectable microsphere based on aripiprazole microcrystal aggregate and preparation method of long-acting injectable microsphere
  • Long-acting injectable microsphere based on aripiprazole microcrystal aggregate and preparation method of long-acting injectable microsphere
  • Long-acting injectable microsphere based on aripiprazole microcrystal aggregate and preparation method of long-acting injectable microsphere

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Embodiment 1: the selection of oil phase kind

[0067] Mix 315 mg of aripiprazole with 210 mg of polylactic acid-glycolic acid copolymer, wherein polylactic acid-glycolic acid copolymer (intrinsic viscosity 0.32-0.44dL / g, weight average molecular weight is 30500Da, the molar ratio of polylactic acid and glycolic acid is 50:50), add single solvent dichloromethane, ethyl acetate, acetone, chloroform, and a certain proportion of mixed solvents (dichloromethane: ethyl acetate, dichloromethane: acetone, dichloromethane: chloroform) 3mL, Heat the water bath at 55°C and shake to dissolve. Prepare 1% polyvinyl alcohol solution 450mL (w / v) simultaneously, add sodium hydroxide to adjust pH 10, under 10000rpm high-speed shearing, inject oil phase in polyvinyl alcohol to disperse, after shearing 30s, under the temperature condition of control ( The temperature is lower than 15°C for the first hour, and then maintained at 25°C) to volatilize the organic solvent; solidify for 3h, ce...

Embodiment 2

[0074] Embodiment 2: the selection of mixed solvent ratio

[0075] Mix 315 mg of aripiprazole with 210 mg of polylactic acid-glycolic acid copolymer, wherein polylactic acid-glycolic acid copolymer (intrinsic viscosity 0.32-0.44dL / g, weight average molecular weight is 30500Da, the molar ratio of polylactic acid and glycolic acid is 50:50), add a certain proportion of mixed solvent (dichloromethane: ethyl acetate, dichloromethane: acetone, dichloromethane: chloroform) 3mL, and heat the water bath at 55°C and shake to dissolve. Prepare 450mL (w / v) of 1% polyvinyl alcohol solution at the same time, add sodium hydroxide to adjust pH10, under 10000rpm high-speed shearing, inject the oil phase into polyvinyl alcohol to disperse, after shearing for 30s, under the temperature condition of control (before The temperature is lower than 15°C for one hour, and then maintained at 25°C) to volatilize the organic solvent; solidify for 3h, centrifuge and wash to harvest the microspheres, and ...

Embodiment 3

[0079] Embodiment 3: the selection of oil-water phase ratio

[0080] Mix 315 mg of aripiprazole with 210 mg of polylactic acid-glycolic acid copolymer, wherein polylactic acid-glycolic acid copolymer (intrinsic viscosity 0.32-0.44dL / g, weight average molecular weight is 30500Da, the molar ratio of polylactic acid and glycolic acid is 50:50), add 3mL of mixed solvent (dichloromethane: ethyl acetate = 4:1), heat in a water bath at 55°C and shake to dissolve. Prepare a certain volume of 1% polyvinyl alcohol solution (w / v) at the same time, add sodium hydroxide to adjust the pH to 10, inject the oil phase into the polyvinyl alcohol to disperse under the high-speed shear of 10000rpm, after shearing for 30s, under the controlled temperature condition (The temperature was lower than 15°C in the first hour, and maintained at 25°C thereafter). Volatile organic solvent; solidified for 3 hours, centrifuged and washed to harvest microspheres, and freeze-dried.

[0081] Table 3: Effect of...

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Abstract

The invention provides a long-acting injectable microsphere based on aripiprazole microcrystal aggregate and a preparation method of the long-acting injectable microsphere. The long-acting injectable microsphere is free of release lag period, is free of oral supplementation, and is of a core-shell structure. According to the long-acting injectable microsphere, a mixed solvent in a certain proportion is used as an oil phase, a polylactic acid-glycolic acid copolymer is used as an adhesive and a shell, and aripiprazole microcrystals are condensed and bonded to form a spherical entity of an inner core. According to the long-acting injectable microsphere, the microsphere drug loading capacity is 35%-65% in percentage by mass, the average particle size of the microspheres is smaller than 25 microns, the intramuscular injection needle passing performance is good, an aripiprazole preparation does not need to be additionally orally taken and supplemented, the effective blood concentration can be achieved only through half of the administration dosage of the preparation on the market, and the medicine release period can reach 30 days or above.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a long-acting injectable microsphere based on aripiprazole microcrystalline aggregates with a core-shell structure without a release lag period and without oral supplementation and a preparation method thereof. Background technique [0002] Aripiprazole (Aripiprazole) is currently one of the drugs of choice for anti-schizophrenia in clinical practice. It has effects on dopamine D2, D3, 5-HT1A and 5-HT2A receptors, and can exert biphasic effects on the nervous system. It has the advantages of good curative effect, low adverse reactions, and can reduce the recurrence rate. Due to the particularity of the treatment of psychiatric patients, long-acting injections with high compliance have higher clinical value and application convenience. The long-acting injection microspheres have a long drug release period, significantly reducing the frequency of administration, stable b...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K47/34A61K9/10A61K47/06A61K47/14A61K47/08A61K47/32A61K31/496A61P25/18
CPCA61K9/5031A61K9/5089A61K9/0019A61K9/10A61K47/06A61K47/14A61K47/08A61K47/32A61K31/496A61P25/18
Inventor 毛世瑞胡迎莉张欣李惠玲
Owner SHENYANG PHARMA UNIVERSITY
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