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Long-acting naltrexone implant and preparation method thereof

A technology for naltrexone and implants, applied in the field of long-acting naltrexone implants and their preparation, can solve the problems of different solution components, inability to carry out large-scale production, etc., achieves good release completion, and improves clinical treatment Effect, good process control effect

Active Publication Date: 2012-06-27
SHENZHEN SCIENCARE MEDICAL INDUSTRIES CO. LTD.
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Based on the current research and public literature technologies, they are all laboratory-level preparation processes, which cannot be used for large-scale production. Among them, many influencing factors and conditions obtained for screening are not suitable for large-scale production. This is because microspheres Different active ingredients in the package, different ways of adding the internal phase emulsion to the external phase solution, different components of the solution, and different components of the specific excipients used will lead to unpredictable changes in the optimal preparation process conditions, and it is necessary to redo the process. In order to obtain the sustained-release microspheres with ideal sustained-release effect and therapeutic effect

Method used

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  • Long-acting naltrexone implant and preparation method thereof
  • Long-acting naltrexone implant and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] DL-polylactic acid, the selected viscosity coefficient is 0.9dl / g, and the average molecular weight is about 50,000 Daltons. Dissolve DL-polylactic acid (20g) and naltrexone (20g) in dichloromethane (200mL) as the DP phase; prepare 6000ml of a 0.5% polyvinyl alcohol solution and saturate it with 10% sucrose as the CP phase ;The speed of the peristaltic pump is set to 180rpm, the nitrogen pressure is set to 2Kpa, and the stirrer speed is set to 180rpm; the DP phase is pressed into the CP phase from the outside through nitrogen, heated to 37°C, decompressed to a vacuum of -0.08Mpa, and continuously Stir; after the microspheres are solidified, cool to below 10°C in an ice-water bath, filter, wash the microspheres with distilled water 3 times, and vacuum-dry for 48 hours; combine the microspheres, pass through a 40-mesh sieve, mix well, and press into tablets with an appropriate pressure , the tablet diameter is 6.8mm; the surface is coated with DL-polylactic acid, the weig...

Embodiment 2

[0035] DL-polylactic acid, select viscosity coefficient 1.5dl / g (chloroform, 30°C), dissolve DL-polylactic acid (20g) and naltrexone (30g) in dichloromethane (200mL) as DP phase; prepare concentration It is 6000ml of 1% polyvinyl alcohol solution and saturated with 10% sucrose as the CP phase; the speed of the peristaltic pump is set to 200rpm, the nitrogen pressure is set to 8Kpa, and the stirrer speed is set to 180rpm; the DP phase is pressed into the CP from the outside by nitrogen phase, heated to 37°C, decompressed to a vacuum of -0.08Mpa, and continued to stir; after the microspheres solidified, cooled to below 10°C in an ice-water bath, filtered, washed the microspheres with distilled water 3 times, and dried in vacuum for 48 hours Merge the microspheres, pass through a 30-mesh sieve, mix well, and press into tablets with an appropriate pressure. Denaltrexone implant.

Embodiment 3

[0037] DL-polylactic acid, select viscosity coefficient 0.7dl / g, dissolve DL-polylactic acid (25g) and naltrexone (20g) in dichloromethane (250mL) as DP phase; prepare polyethylene with a concentration of 0.8% 6000ml of alcohol solution was saturated with 10% sucrose as CP phase; the speed of peristaltic pump was set to 200rpm, the pressure of nitrogen gas was set to 15Kpa, and the speed of stirrer was set to 180rpm; the DP phase was pressed into the CP phase from the outside by nitrogen gas, and heated to 37 ℃, reduce the pressure to a vacuum degree of -0.08Mpa, and continue to stir; after the microspheres are solidified, cool them in an ice-water bath to below 10°C, filter, wash the microspheres with distilled water three times, and dry them in vacuum for 48 hours; combine the microspheres, pass 60-mesh sieve, mixed, and pressed with appropriate pressure, the tablet diameter is 5.5mm; the surface is coated with DL-polylactic acid, the weight of each tablet is 280mg, the hardn...

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Abstract

The invention relates to a long-acting naltrexone implant and a preparation method thereof, which belong to the field of pharmaceutical preparations. The long-acting naltrexone implant comprises a polylactic acid and naltrexone, and is characterized in that the viscosity coefficient of the polylactic acid is 0.5-2.5dl / g (chloroform, 30 DEG C); the ratio of the polylactic acid to the naltrexone is1:(0.5-1.8) in parts by weight; the composition structure of the long-acting naltrexone implant is a particle tabletted and coated structure; coated particles are slow release pellets which can be sieved by a 20-60 mesh screen in particle size; the slow release pellets comprise the polylactic acid and the naltrexone; the ratio of the polylactic acid to the naltrexone in the slow release pellets is 1:(1-2) in part by weight; and a coating layer is a DL-polylactic acid. The long-acting naltrexone implant has a good curative effect, better drug-loading rate and better drug release completeness, and has small side effect on human bodies.

Description

technical field [0001] The invention relates to a long-acting naltrexone implant (Naltrexone Implant) and a preparation method thereof, belonging to the field of pharmaceutical preparations. technical background [0002] At present, biodegradable sustained-release drug loading technology has been extensively studied. This technology not only provides a better way of drug delivery for a variety of drugs, but also reduces adverse drug reactions and improves patient compliance. The biodegradable sustained-release drug-carrying system is a new type of drug delivery system that can slowly and stably release drugs after local administration. There are microsphere injection type, tablet implantation type and other drug delivery systems. The release behavior of the drug is not affected by the characteristics of the drug (molecular weight, molecular size, water solubility, etc.), the properties of polylactic acid and its copolymers (composition, molecular weight, crystallinity, degra...

Claims

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Application Information

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IPC IPC(8): A61K9/32A61K47/34A61K31/485A61P25/32A61P25/36
Inventor 尹述贵李金禄贾少微王实强刘庆哲张涛
Owner SHENZHEN SCIENCARE MEDICAL INDUSTRIES CO. LTD.
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