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Novel method for preparing galanthamine sustained-release microspheres

A technology of galantamine microspheres and microspheres, applied in the field of preparing galantamine sustained-release microspheres, achieves the effects of high encapsulation efficiency, less residual solvent and simple operation

Active Publication Date: 2020-09-11
UNIV OF JINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report about propylene carbonate being used to prepare galantamine microspheres

Method used

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  • Novel method for preparing galanthamine sustained-release microspheres
  • Novel method for preparing galanthamine sustained-release microspheres
  • Novel method for preparing galanthamine sustained-release microspheres

Examples

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Effect test

preparation example 1

[0033] Preparation Example 1: Preparation of Known Galanthamine Pamoate Sustained Release Microspheres

[0034] The known sustained-release microspheres of galantamine pamoate were prepared according to the method described in Example 1 of Patent Application No. 201911144830.0. Specifically: take 1.25g galantamine pamoate and 1.25g PLGA (75 / 25), add to the mixed system of benzyl alcohol and dichloromethane (8ml, 45 / 55, v / v) to dissolve, and prepare Solution 1. Weigh 6.4g of PVA and dissolve it in water for injection to make 0.8% PVA aqueous solution. Slowly add solution 1 to 0.8% PVA solution, homogeneously emulsify at 2000rpm for 1min; stir for 3h to evaporate the solvent after the end; wash with 0.25% poloxamer ethanol aqueous solution, continue stirring for 1h, and filter the obtained suspension with a sieve to collect micro The microspheres were washed with water for injection and freeze-dried in a freeze dryer; after freeze-drying, they were filtered through a mesh.

Embodiment 1

[0035] Embodiment 1: Preparation of galantamine sustained-release microspheres

[0036] Accurately weigh 1.25g of galantamine pamoate, polylactic-glycolic acid (PLGA) 1.00g (LA:GA=75:25), be dissolved in the mixed solvent of propylene carbonate and dichloromethane (8ml, 20 / 80, v / v), vortex to dissolve completely, and sonicate as the dispersed phase. Drop the dispersed phase into the continuous phase of 200ml 0.8% PVA17-88 aqueous solution, and shear at high speed while adding, until it is completely added. Stir under reduced pressure for 3 hours, solidify the microspheres and remove the organic solvent, collect the microspheres by centrifugation, wash with water, and dry in vacuum to obtain the galantamine sustained-release microspheres.

[0037] Solvent residues were detected by gas chromatography on the galantamine sustained-release spheres made in Example 1 and the galantamine sustained-release microspheres for injection made in Example 1 of Patent Application No. 2019111...

Embodiment 2

[0041] Embodiment 2: Preparation of galantamine sustained-release microspheres

[0042] Accurately weigh 1.0 g of galantamine pamoate, 1.0 g of PLGA (LA:GA=75:25), and put it in a mixed solvent (8ml, 33 / 67, v / v) of propylene carbonate and dichloromethane , vortex to dissolve completely, and sonicate as the dispersed phase. Drop the dispersed phase into the continuous phase of 200ml 0.8% PVA17-88 aqueous solution, and shear at high speed while adding, until it is completely added. Stir under reduced pressure for 3 hours, solidify the microspheres and remove the organic solvent, collect the microspheres by centrifugation, wash with water, and dry in vacuum to obtain the galantamine sustained-release microspheres.

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Abstract

The invention discloses a novel method for preparing galanthamine sustained-release microspheres, and particularly relates to a method for preparing galanthamine microspheres by adopting a novel solvent propylene carbonate. Galanthamine pamoate is used as a raw material, and the galanthamine sustained-release microspheres prepared by using an emulsification-solvent volatilization method have the advantages of high encapsulation efficiency, high product yield, less residual solvent and the like.

Description

technical field [0001] The invention belongs to the technical field of drug sustained-release preparations, and relates to a new method for preparing galantamine sustained-release microspheres. Background technique [0002] Galantamine, also known as Nivalin and Qiangjining, is derived from the leaves of Amaryllidaceae plants Amaryllidaceae purple flower, Snow Lotus, etc. It can also be synthesized by chemical methods. It is a phenanthridine alkaloid. Galantamine is a second-generation reversible cholinesterase inhibitor, which can increase the level of acetylcholine, easily penetrate the blood-brain barrier, restore blocked neuromuscular conduction, and improve the paralysis of various peripheral neuromuscular disorders. Clinically used to treat Alzheimer's disease. Since Alzheimer's disease requires long-term treatment, the patient's memory declines, and the existing oral dosage forms often miss or take more than one dose, resulting in large fluctuations in blood medicine...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/34A61K31/55A61P25/28
CPCA61K9/5089A61K9/5031A61K31/55A61P25/28
Inventor 刘善奎杨冰王海龙柳宇红
Owner UNIV OF JINAN
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