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Risperidone slow-release composition and preparation method thereof

A technology of sustained-release composition and risperidone, which is applied in the directions of drug combination, pharmaceutical formulation, drug delivery, etc., can solve the problems of surface collapse, high cost, difficult preparation and storage, etc.

Inactive Publication Date: 2017-06-13
AC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this polymer combination is prone to surface collapse during radiation sterilization, because PLGA with different monomer ratios and molecular weights degrades differently under radiation; It is more prone to degradation during storage, which is not conducive to the storage stability of the preparation; at the same time, the preparation and storage of PLGA excipients with low molecular weight and high proportion of GA components are relatively difficult and relatively expensive

Method used

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  • Risperidone slow-release composition and preparation method thereof
  • Risperidone slow-release composition and preparation method thereof
  • Risperidone slow-release composition and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0065] An embodiment of the risperidone sustained-release composition of the present invention, the non-solvent preparation raw material of the risperidone sustained-release composition described in this embodiment contains the following components in mass percentage: risperidone 25%, water Insoluble polymer: PLA 74.9%, release regulator: stearic acid 0.1%. Wherein, the weight average molecular weight of the PLA is 30kDa, the viscosity is 0.27dL / g, and the PLA has an ester terminal.

[0066] The risperidone sustained-release composition described in this example is prepared by the following preparation method:

[0067] (1) Dissolving the poorly water-soluble polymer in methylene chloride, the mass percentage of the poorly water-soluble polymer and methylene chloride is 10%, then adding risperidone and a release regulator, dissolving evenly, and forming an internal oil Mutually;

[0068] (2) PVA and potassium phosphate are dissolved in water to form an external water phase, t...

Embodiment 2

[0072] An embodiment of the risperidone sustained-release composition of the present invention, the non-solvent preparation raw material of the risperidone sustained-release composition described in this embodiment contains the following components in mass percentage: 30% risperidone, water Insoluble polymer: PLA 69.5%, release regulator: behenic acid 0.5%. Wherein, the PLA is composed of PLA at the ester group end (the weight average molecular weight is 40kDa, the viscosity is 0.35dL / g) and the PLA at the carboxyl end (the weight average molecular weight is 40kDa, the viscosity is 0.35dL / g). The mass ratio of PLA at the end is: 70:69.

[0073] The risperidone sustained-release composition described in this example is prepared by the following preparation method:

[0074] (1) dissolving the poorly water-soluble polymer in chloroform, the mass percentage of the poorly water-soluble polymer and chloroform being 9.5%, then adding risperidone and a release regulator, dissolving e...

Embodiment 3

[0079] An embodiment of the risperidone sustained-release composition of the present invention, the non-solvent preparation raw material of the risperidone sustained-release composition described in this embodiment contains the following components in mass percentage: 35% risperidone, water Insoluble polymer: PLA 64.2%, release regulator: behenate 0.8%. Wherein, the weight average molecular weight of the PLA is 35kDa, the viscosity is 0.32dL / g, and the PLA has a carboxyl terminal.

[0080] The risperidone sustained-release composition described in this example is prepared by the following preparation method:

[0081] (1) Dissolving the poorly water-soluble polymer in methylene chloride, the mass percentage of the poorly water-soluble polymer and tetrachlorethylene is 9%, then adding risperidone and a release regulator, dissolving evenly, and forming an inner oil Mutually;

[0082] (2) dissolving albumin in water to form an external aqueous phase, the mass percentage of the a...

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Abstract

The invention discloses a risperidone slow-release composition and a preparation method thereof. The risperidone slow-release composition disclosed by the invention comprises non-solvent preparation raw materials, namely risperidone, a water-insoluble polymer and a release regulating agent, wherein the release regulating agent comprises organic lipophilic substances. The preparation method of the risperidone slow-release composition comprises the following steps: (1) dissolving the non-solvent preparation raw materials into an organic solvent so as to form inner oil phase; (2) dissolving a surfactant into an aqueous medium so as to form outer water phase; (3) adding the inner oil phase obtained in the step (1) into the outer water phase, preparing an emulsion, performing solvent evaluation or solvent extraction to harden micro particles in the solution, collecting the micro particles, washing, and drying, thereby obtaining risperidone slow-release microspheres. The risperidone slow-release composition disclosed by the invention is stable enough, can be continuously released for weeks or longer, and can be regulated according to specific medicine properties or treatment demands.

Description

technical field [0001] The invention relates to a sustained-release composition and a preparation method thereof, in particular to a risperidone sustained-release composition and a preparation method thereof. Background technique [0002] In the past ten years, biodegradable polymer microspheres have become one of the important research fields of new drug delivery systems. The microspheres can be used as the carrier of long-acting preparations, and can be administered to humans or animals by intramuscular or subcutaneous injection, which can limit the drug release rate and release cycle, and can maintain effective therapeutic drug concentrations for a long time with only one administration. It can minimize the total dosage of drugs required for treatment, and can improve the drug treatment compliance of patients. [0003] The long-acting antipsychotic drug Risperidal Consta (Hengde) developed based on the technology disclosed in the patent CN1137756 uses PLGA with a molecul...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/519A61K47/12A61K47/44A61K47/34A61P25/18
CPCA61K9/0002A61K9/5123A61K9/5153A61K31/519
Inventor 刘锋赖树挺郑阳曹付春连远发
Owner AC PHARMA CO LTD
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