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Risperidone slow-release microsphere, preparation method and application thereof

A technology of slow-release microspheres and risperidone, which is applied in the direction of pharmaceutical formulations, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., can solve the problems of burst release and low drug loading, and achieve Improve compliance, maintain blood drug concentration, and reduce adverse reactions

Active Publication Date: 2013-03-20
SHANDONG LUYE PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the drug loading of the microspheres is low, and there is still a problem of burst release at low drug loading

Method used

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  • Risperidone slow-release microsphere, preparation method and application thereof
  • Risperidone slow-release microsphere, preparation method and application thereof
  • Risperidone slow-release microsphere, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Weigh 4.0g PLGA-S (75 / 25, 0.31) molecular weight 33,000, 6.0g risperidone, add to 50ml of dichloromethane and stir to dissolve to obtain a clear solution, this solution is added to a high-speed stirring cooling to 6 In 5000ml PVA solution (0.5%) at ℃, disperse and emulsify at 1000rpm for 1min, adjust the rotation speed to 300rpm, and the rotation speed of the stirring paddle is 150rpm, volatilize to remove the organic solvent, and volatilize for 6hr; filter with a sieve, wash with deionized water 5 times, freeze The powdered microspheres were dried, with a drug loading of 49.4% and an encapsulation efficiency of 82.3%.

Embodiment 2

[0037] Weigh 4.0g PLGA-S (75 / 25, 0.42) molecular weight 53,000, 6.0g risperidone, add to 50ml of dichloromethane and stir to dissolve to obtain a clear solution, this solution is added to a high-speed stirring cooling to 6 In 5000ml PVA solution (0.5%) at ℃, disperse and emulsify at 1000rpm for 1min, adjust the rotation speed to 300rpm, and the rotation speed of the stirring paddle is 150rpm, volatilize to remove the organic solvent, and volatilize for 6hr; filter with a sieve, wash with deionized water 5 times, freeze The powdered microspheres were dried, with a drug loading of 49.0% and an encapsulation efficiency of 81.7%.

Embodiment 3

[0039] Weigh 4.0g PLGA-S (75 / 25, 0.52) molecular weight 74,000, 6.0g risperidone, add to 50ml of dichloromethane and stir to dissolve to obtain a clear solution; add this solution to a high-speed stirring cooling to 6 In 5000ml PVA solution (0.5%) at ℃, disperse and emulsify at 1000rpm for 1min, adjust the rotation speed to 300rpm, and the rotation speed of the stirring paddle is 150rpm, volatilize to remove the organic solvent, and volatilize for 6hr; filter with a sieve, wash with deionized water 5 times, freeze The powdered microspheres were dried, with a drug loading of 50.7% and an encapsulation efficiency of 84.5%.

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PUM

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Abstract

The invention provides a risperidone slow-release microsphere, a preparation method and an application thereof. The microsphere comprises risperidone or 9-hydroxy risperidone or the salt thereof and anon-end-capped lactide-glycollide copolymer. The risperidone slow-release microsphere provided by the invention has higher medicine-carrying quantity, no in-vivo sudden-release phenomenon, stable blood concentration and no medicine release lag period, reduces the administration frequency of a patient greatly, reduces the administration volume of each time, enhances the conformance of the patientand reduces the generation of adverse reactions.

Description

technical field [0001] The invention relates to a microsphere and its preparation method and application, in particular to risperidone long-acting sustained-release microspheres and its preparation method and application. Background technique [0002] Since the development of chlorpromazine as an antipsychotic in the 1950s, goals in the field have focused on improving the efficacy and increasing tolerance of antipsychotics. After decades of practice, traditional antipsychotic drugs have gradually revealed obvious defects, which are manifested in: ① not all psychotic patients can play an effective therapeutic effect; ② cannot comprehensively treat all symptoms of morbidity; The reaction is relatively large. [0003] Risperidone (risperidone) is a new generation of atypical antipsychotics. It has ideal effects in the above three aspects. This product was developed by the Belgian Janssen Pharmaceutical Company in 1984. Its chemical name is 3-[2-[4 -(6-fluoro-1,2-benzisoxazol-...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/519A61K47/34A61P25/18
Inventor 孙考祥梁荣才刘万卉王涛沙春洁王麒麟于宏郎跃武
Owner SHANDONG LUYE PHARMA CO LTD
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