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L-cepharanthine sustained-release microsphere and preparation method thereof

A technology of levothrinine and sustained-release microspheres, which is applied in the directions of pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., and can solve the problems of poor oral absorption and low bioavailability, etc.

Pending Publication Date: 2021-09-14
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In order to solve the above problems, the object of the present invention is to provide a kind of L-paternidine slow-release microspheres and its preparation method, its preparation method is simple and fast, can effectively solve the problems of poor oral absorption, low bioavailability, etc.

Method used

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  • L-cepharanthine sustained-release microsphere and preparation method thereof
  • L-cepharanthine sustained-release microsphere and preparation method thereof
  • L-cepharanthine sustained-release microsphere and preparation method thereof

Examples

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Embodiment 1

[0038] Weigh 100 mg of PLGA (molar ratio of lactide to glycolide = 75:25, Mw = 1.2wg / mol), dissolve it in 0.5 mL of dichloromethane, weigh 50 mg of L-steprenine, add the drug Ultrasonic pulverize (200W, 2s, 45s) into the dichloromethane solution of PLGA to disperse evenly. Drop by drop into 2.5mL of 1% PVA solution under stirring and emulsify quickly using a vortex device, then add it into 62.5mL of water under stirring to solidify the microspheres and volatilize the organic solvent, and collect the microspheres after 2 hours The balls were washed with water for 3-5 times, the suspension was placed in a -80°C refrigerator for 8 hours, and then freeze-dried for 48 hours to obtain microsphere powder.

Embodiment 2

[0040] Weigh 100mg of PLGA (molar ratio of lactide to glycolide = 75:25, Mw = 1.2wg / mol), dissolve in 5mL of dichloromethane, weigh 50mg of L-stephenidine, dissolve in 0.5mL Add the DMSO solution containing the drug to the dichloromethane solution of PLGA, vortex to disperse evenly, and drop it into 2.5mL of 1% PVA solution under stirring to form an O / W emulsion . Stirring was continued at room temperature for 3 h to volatilize dichloromethane, wherein the stirring rate was 300-500 rpm. After evaporating the organic solvent, add the above system into 625mL of water to solidify for 4 hours, collect the microspheres and wash them with water for 3-5 times, suspend them in a -80°C refrigerator for 8 hours, freeze-dry for 48 hours, and obtain microsphere powder .

Embodiment 3

[0042]Weigh 100mg of PLGA (molar ratio of lactide to glycolide = 75:25, Mw = 1.2wg / mol), dissolve in 5mL of dichloromethane, weigh 20mg of L-paternidine, dissolve in 0.5mL In DMSO, the DMSO solution containing the drug was added to the dichloromethane solution of PLGA, and vortexed to disperse evenly. It was added dropwise into 25 mL of 1% PVA solution under stirring to form an O / W emulsion. Stirring was continued at room temperature for 3 h to volatilize dichloromethane, wherein the stirring rate was 300-500 rpm. After evaporating the organic solvent, add the above system into 625mL of water to solidify for 4 hours, collect the microspheres and wash them with water for 3-5 times, suspend them in a -80°C refrigerator for 8 hours, freeze-dry for 48 hours, and obtain microsphere powder .

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Abstract

The invention relates to a preparation method of an L-cepharanthine sustained-release microsphere. The preparation method comprises the following steps: dissolving L-cepharanthine and a degradable polymer containing a hydrophobic chain segment in an organic solvent to obtain a drug-containing polymer solution; under a stirring condition, adding the drug-containing polymer solution into a water phase to form an O / W type emulsion and removing the organic solvent in the emulsion; wherein the water phase contains a stabilizer and a ratio of the stabilizer to the water phase is 0.1%-5% (w / v); and under the stirring condition, adding the obtained dispersion system into water to be cured to obtain a L-cepharanthine sustained-release microsphere. The L-cepharanthine sustained-release microsphere has a proper particle size, is round and free of a burst release phenomenon, and has a long-acting anti-depression effect.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a kind of L-paternidine sustained-release microspheres and a preparation method thereof. Background technique [0002] Schizophrenia is a group of mental illnesses characterized by incoordination between thinking, emotion, and behavior, and separation of mental activities from reality. Often include depression, Alzheimer's disease, and Parkinson's disease, among others. With the accelerated pace of life, social competition is intensifying, people are facing increasing pressure, and mental health problems are becoming more and more prominent, especially the incidence of mental diseases such as depression, Alzheimer's disease and Parkinson's is increasing year by year. Moreover, the recurrence rate is very high, and the patient cannot perform normal work at the same time, which will bring a heavy financial burden to the family. [0003] The chemical name of l-...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/4375A61K47/34A61P25/18
CPCA61K9/1647A61K9/1641A61K31/4375A61P25/18
Inventor 镇学初曹青日何丽雅
Owner SUZHOU UNIV
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