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Naltrexone microspheres

A technology of naltrexone and microspheres, applied in the field of pharmaceutical preparations, can solve the problems of irregular shape and poor uniformity of naltrexone microspheres, and achieve the effects of low production cost, good reproducibility and high encapsulation rate

Active Publication Date: 2021-10-26
JIANG SU PHARMAMAXCORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] In view of the above-mentioned deficiencies, the object of the present invention is to provide a kind of naltrexone microspheres, its preparation method is simple and fast, can effectively solve the problems such as poor uniformity of naltrexone microspheres, irregular shape, etc.

Method used

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  • Naltrexone microspheres
  • Naltrexone microspheres
  • Naltrexone microspheres

Examples

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preparation example

[0048] A kind of naltrexone microsphere is made by following steps:

[0049] a: 2.03g naltrexone and 4g degradable polymers containing hydrophobic segments are dissolved in methylene chloride to obtain a drug-containing polymer solution; the concentration of degradable polymers in organic solvents is 2.5% to 50% ( w / v);

[0050] b: dissolving the stabilizer PVA in water to obtain an external water phase; wherein, the concentration of the stabilizer is 1% to 5% (w / v);

[0051] c: The drug-containing polymer solution and the water phase are respectively used as the A and B pump solutions of the advection pump, and the A and B pumps of the advection pump are set at a certain flow rate, and an O / W emulsion is generated through a microfluidic device, and stirred The organic solvent in the emulsion is removed in the state; among them, the flow rate of phase A is set: the flow rate of phase B is 1:2~1:5, and the two phases pass through the advection pump at a constant flow rate and ...

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Abstract

The invention discloses naltrexone microspheres. A preparation method of the naltrexone microspheres comprises the following steps: dissolving naltrexone and a degradable polymer with a hydrophobic chain segment in an organic solvent to obtain a drug-containing polymer solution; mixing the drug-containing polymer solution and water phase by using a microfluidic device to form an O / W type emulsion, and removing the organic solvent in the emulsion under a stirring condition; wherein the water phase contains a stabilizer, and a ratio of the stabilizer to the water phase is 0.1%-5% (w / v); after the organic solvent is completely volatilized, adding the obtained dispersion system into water for curing to obtain the naltrexone microspheres. The microsphere provided by the invention overcomes defects of non-uniform particle size distribution, irregular microsphere shape, high burst release and the like of microspheres prepared by a traditional preparation method. In addition, technological parameters of a microsphere synthesis process with microfluidic technology are highly controllable, and production amplification of the microspheres is facilitated.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a naltrexone microsphere. [0002] technical background [0003] Naltrexone is an opioid receptor antagonist, and its pharmacodynamics is similar to that of naloxone. It has blocking effects on κ-, δ-, μ- and other opioid receptors, and can significantly weaken or completely block opioid receptors. receptors, and even reverse the effects of intravenous opioids. Therefore, it can block the effect of retaking drugs and prevent or reduce relapse. The structural formula is shown in the following formula. [0004] [0005] Naltrexone preparations are mainly tablets, and the course of treatment lasts for half a year and must be taken daily at 50 mg. Therefore, the course of treatment is longer, and at the same time, it has certain toxicity to the liver. In order to improve patient compliance, the development of long-acting microspheres of naltrexone has a wide...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/485A61K47/34A61P25/36
CPCA61K9/5031A61K31/485A61P25/36
Inventor 蒋志君杜欢欢曹青日陆小娟于鹤云
Owner JIANG SU PHARMAMAXCORP