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Naltrexone long-acting sustained-release preparation with no need of coating and preparation method thereof

A technology of sustained-release preparations and naltrexone, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, which can solve toxic and side effects, residues, and short-term Months, no more than half a year, etc., to achieve a smooth surface

Inactive Publication Date: 2010-05-05
海南凤凰国际药物研究院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The earliest research on naltrexone long-acting sustained-release preparations began in the United States in the 1970s, but there has been no breakthrough in long-acting sustained-release preparations that contain harmful organic substances and have serious toxic and side effects; the sustained-release preparations have a short release time, Generally within 1-3 months, no more than half a year; polymer materials cannot be completely degraded, and form lumps with body tissues, residues and other problems

Method used

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  • Naltrexone long-acting sustained-release preparation with no need of coating and preparation method thereof
  • Naltrexone long-acting sustained-release preparation with no need of coating and preparation method thereof
  • Naltrexone long-acting sustained-release preparation with no need of coating and preparation method thereof

Examples

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Effect test

Embodiment 1

[0043] A long-acting sustained-release agent of naltrexone for long-acting anti-relapse treatment after detoxification of opioid addiction patients.

[0044] Using the W / O / W solvent volatilization method, 10g of racemic polylactic acid (the average molecular weight of polylactic acid is between 50,000 and 400,000 daltons and the intrinsic viscosity is 0.53dL / g) is dissolved in 100ml of two Then add 0.55g of stannous zincate as a catalyst and ultrasonically shake to form colostrum; then add the colostrum solution and 20g of naltrexone base to 1000ml, 1% polyvinyl alcohol (hydrolysis degree 87- 89%, 4% aqueous solution viscosity coefficient 40-46cP at 20℃) in the solution, high-speed stirring (1,500-2000rpm) until the methylene chloride is completely volatilized, then filter out the naltrexone-polylactic acid polymer, and wash with distilled water 3 Next, dehumidify and dry at 30°C to obtain naltrexone-polylactic acid microspheres. The diameter of the microspheres is between 20-200...

Embodiment 2

[0046] A long-acting sustained-release agent of naltrexone for the treatment of alcohol addiction patients.

[0047] Using the W / O / W solvent volatilization method, 10g of racemic polylactic acid (the average molecular weight of polylactic acid is between 50,000 and 300,000 Daltons, and the intrinsic viscosity is 0.53dL / g), dissolved in 100ml of two Then add 0.5g of stannous zincate as a catalyst and ultrasonically shake to form colostrum; then add 1600ml of colostrum solution and 10g of naltrexone base, 1% polyvinyl alcohol (hydrolysis degree 87- 89%, 4% aqueous solution viscosity coefficient 40-46cP at 20℃) in the solution, high-speed stirring (1,500-2000rpm) until the methylene chloride is completely volatilized, and then filtered to separate the naltrexone-polylactic acid polymer, with distilled water Wash 3 times, dehumidify and dry at 30°C to obtain naltrexone-polylactic acid microspheres. The diameter of the microspheres is between 20-200μm and shows a normal distribution (...

Embodiment 3

[0049] A long-acting sustained-release agent of naltrexone for the treatment and prevention of Alzheimer's disease.

[0050] Using the W / O / W solvent volatilization method, 10g of racemic polylactic acid (the average molecular weight of polylactic acid is between 5-25 million Daltons and the intrinsic viscosity is 0.53dL / g) is dissolved in 100ml of two Then add 0.4g of stannous zincate as a catalyst and ultrasonically shake to form colostrum; then add 1000ml of colostrum solution and 12g of naltrexone base to 1% polyvinyl alcohol (hydrolysis degree 87- 89%, 4% aqueous solution viscosity coefficient 40-46cP at 20℃) in the solution, high-speed stirring (1,500-2000rpm) until the methylene chloride is completely volatilized, and then filtered to separate the naltrexone-polylactic acid polymer, with distilled water Wash 3 times, dehumidify and dry at 30°C to obtain naltrexone-polylactic acid microspheres. The diameter of the microspheres is between 20-200μm and shows a normal distribut...

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Abstract

The invention discloses a naltrexone long-acting sustained-release preparation with no need of coating, which is prepared by naltrexone base-racemic form polylactic acid microspheres via a continuous extrusion forming technology. The preparation adopting a W / O / W solvent volatilization method comprises the following steps: dissolving the mixture of naltrexone base and racemic form polylactic acid microspheres in dichloromethane, adding catalyst, carrying out sonic oscillation to form foremilk, volatilizing solvent, filtering, separating polymer, washing, dehumidifying and drying to obtain microspheres, and performing continuous extrusion to extrude granules. In the invention, addictive is not contained, high molecular materials are absolutely degraded without residue, no coating is needed, the medicine arrangement is even, the in vitro and in vivo release of naltrexone is at a 0-level release speed, the blood concentration is stabilized above 2ng / ml of therapeutic dose, the period of sustaining effective blood concentration can be up to more than 540 to 720 days; and the content of naltrexone base is as high as 55%-80%, the sustained-release preparation can be produced in large scale, for treating rehabilitation long-acting relapse prevention and alcoholic dependence, and for treating and preventing senile dementia, and the like.

Description

Technical field [0001] The invention relates to a long-acting sustained-release preparation of naltrexone without coating and a preparation method thereof, which is suitable for long-acting anti-relapse treatment of drug detoxification, treatment of alcohol dependence, and treatment and prevention of senile dementia. Background technique [0002] Opioid dependence is characterized as a "recurrent chronic encephalopathy", which requires long-term drug treatment and psychotherapy, but whether it is opioid agonists or non-agonist drugs, the relapse rate after treatment is extremely high. Up to 95% or more. Naltrexone is a morphine (opioid) antagonist. Its mechanism of action is to produce an "insurmountable" antagonistic effect by competing with morphine to occupy the same receptor. It also blocks morphine from reaching the receptor site, which is an affinity The lack of effective drugs. Since the US FDA approved the market in 1984 (my country's naltrexone oral tablets were market...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/485A61K47/48A61K47/34A61P25/36A61P25/32A61P25/28
Inventor 刘立华谢成张松明王贤德谢佳刘卓洋宋玉炜
Owner 海南凤凰国际药物研究院
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