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Long-acting sustained-release preparation for resisting Parkinson's disease and preparation method thereof

A slow-release preparation, Parkinson's disease technology, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of prescription compatibility, product burst release, increase prescription complexity, etc., achieve delayed release period, reduce The effect of fluctuations in concentration

Active Publication Date: 2017-08-18
AC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, on the one hand, the method of adding a release regulator also increases the complexity of the prescription, which may cause problems with prescription compatibility. On the other hand, the method used in the present invention will still cause the problem of product burst release.

Method used

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  • Long-acting sustained-release preparation for resisting Parkinson's disease and preparation method thereof
  • Long-acting sustained-release preparation for resisting Parkinson's disease and preparation method thereof
  • Long-acting sustained-release preparation for resisting Parkinson's disease and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1. Preparation of sustained-release microspheres.

[0059] Dissolve 8.00g PLGA (lactide / glycolide=65 / 35, hereinafter the same, all are lactide / glycolide, 0.65dl / g, 71kDa, ester end group) in 80.00g dichloromethane, get Homogeneous solution A; dissolve 2.00 g of rasagiline in 10.00 g of ethanol to obtain homogeneous solution B; under the vortex condition of 3000 rpm, add solution A to solution B to obtain homogeneous emulsion C. The homogeneous solution C was added into 1.0% polyvinyl alcohol aqueous solution at 4° C., and stirred with a mechanical stirrer at 2000 rpm to prepare microspheres. Then the temperature was raised to 40° C. to volatilize the organic solvent, and then the microspheres were filtered, washed with water for injection for 7 times, and then freeze-dried to obtain sustained-release microspheres.

Embodiment 2

[0060] Example 2. Preparation of sustained-release microspheres.

[0061] Dissolve 8.00g PLGA (65 / 35, 0.65dl / g, 71kDa, ester end group) in 80.00g dichloromethane to obtain a homogeneous solution A; dissolve 2.00g rasagiline in 10.00g ethanol to obtain a homogeneous solution B: Under ultrasonic conditions, with a power of 300w, add solution A to solution B to obtain a homogeneous emulsion C. The homogeneous solution C was added into the 1.0% polyvinyl alcohol continuous aqueous phase at 4° C., and the microspheres were homogeneously prepared under high pressure under a pressure of 900 bar. Then the temperature was raised to 40°C to volatilize the organic solvent, and then the microspheres were filtered to remove the continuous water phase, and the microspheres were washed 7 times with water for injection, and then freeze-dried to obtain sustained-release microspheres.

Embodiment 3

[0062] Example 3. Preparation of sustained release microspheres.

[0063] Dissolve 7.00g PLGA (75 / 25, 0.5dl / g, 57kDa, carboxyl end group) in 70.00g ethyl acetate to obtain homogeneous solution A; dissolve 3.00g rasagiline in 15.00g acetic acid to obtain homogeneous solution B ; Under the vortex condition of 3000rpm, solution A was added to solution B to obtain uniform emulsion C. The homogeneous solution C was added into the 0.5% polyvinyl alcohol continuous aqueous phase at 4°C, and a 4000rpm homogenizer was used to homogeneously prepare microspheres. Then the temperature was raised to 40° C. to volatilize the organic solvent, and then the microspheres were filtered, washed with water for injection for 7 times, and then freeze-dried to obtain sustained-release microspheres.

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Abstract

The invention discloses a long-acting sustained-release preparation for resisting Parkinson's disease and a preparation method thereof. The long-acting sustained-release preparation refers to microspheres, each microsphere comprises rasagiline or pharmaceutically acceptable salt thereof and biodegradable high-biocompatibility molecular polymer, and the microspheres includes the microspheres with the average particle size of 0.5-5 micrometers and the microspheres with the average particle size of 20-150 micrometers. The two kinds of microspheres different in particle size are properly matched and used in the pharmaceutical composition, the fluctuation of the concentration of rasagiline in plasma can be significantly reduced, and there is no obvious delayed release period. At the same time, the long-acting sustained-release preparation has no drug releasing phenomenon under the condition of high drug loading.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a long-acting sustained-release preparation of an anti-Parkinson's disease drug and a preparation method thereof. Background technique [0002] Rasagiline is a second-generation monoamine oxidase inhibitor, which can block the decomposition of neurotransmitter dopamine. The inhibitory effect is stronger, and it can also improve the effect of long-term application of dopa preparations on patients with declining efficacy. In addition, the metabolite of rasagiline is an inactive non-amphetamine substance with few side effects. More importantly, the drug has a certain effect of relieving symptoms, and there is a lot of evidence that this kind of drug has certain neurological effects. The role of protection. [0003] Rasagiline is currently only available in oral tablets. Although oral tablets are convenient to take, as the disease progresses, Parkinson's patients are often acco...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/135A61K47/34A61P25/16
CPCA61K9/0002A61K9/5031A61K9/5084A61K31/135
Inventor 郑阳赖树挺曺付春连远发刘锋
Owner AC PHARMA CO LTD
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