In-situ implantation drug delivery system of naltrexone microsphere-hydrogel matrix

A drug delivery system and technology of naltrexone, which is applied in the field of microsphere-hydrogel skeleton implanted drug delivery system in situ, can solve the problems of easy displacement and short duration, and reduce disintegration and release. The rate is stable and the effect of solving the problem of relapse

Inactive Publication Date: 2009-12-30
TSINGHUA UNIV
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

Developed by American Alkermes company Using PLGA as the microsphere carrier material, a biodegradable microsphere injection implant has been developed for intramuscular inject

Method used

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  • In-situ implantation drug delivery system of naltrexone microsphere-hydrogel matrix
  • In-situ implantation drug delivery system of naltrexone microsphere-hydrogel matrix
  • In-situ implantation drug delivery system of naltrexone microsphere-hydrogel matrix

Examples

Experimental program
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Effect test

specific Embodiment approach

[0023] First, PLGA microspheres loaded with naltrexone were prepared. The substance quantity ratio of lactic acid and glycolic acid in the microsphere material PLGA is 50:50-75:25, and the molecular weight is 20k-80k. The mass ratio of the drug naltrexone and the carrier material lactic acid / glycolic acid copolymer in the microsphere is 1:1-1:6. The preparation method can adopt an O / W emulsification solvent evaporation method, the solvent can be dichloromethane, and the emulsification aid can be PVA. By adjusting the concentration of PLGA and PVA, microspheres with a particle size of 10-100 μm can be prepared. Microspheres can be stored lyophilized.

[0024] Then prepare methyl cellulose sol, its preparation method can refer to Chinese invention patent CN 1698902A. The sol is composed of methylcellulose (viscosity 400mPa·S), polyethylene glycol (molecular weight 11000), citrate and alginate (low viscosity), and the mass ratio of the four (wherein citrate and alginate As so...

Embodiment 1

[0028] This example shows the solidification characteristics of the naltrexone microsphere-hydrogel framework in situ implantation system.

[0029] The ratio of microspheres: lactic acid and glycolic acid in PLGA is 75:25, and the molecular weight is 80k. The mass ratio of the drug naltrexone and the carrier material lactic acid / glycolic acid copolymer in the microspheres is 1:2. The average particle size of the microspheres is 52±2 μm, and the encapsulation efficiency is 95%.

[0030] Gel skeleton: methylcellulose: polyethylene glycol: citrate: alginate = 2:8:1:3.5, the content of methylcellulose is 20mg methylcellulose per mL of hydrosol.

[0031] The content of microspheres in the gel matrix is: 30mg / mL

[0032] The viscosity change curve of the naltrexone microsphere-hydrogel matrix in situ implantation system at body temperature is as follows: figure 1 As shown, the curve is divided into two sections of slow speed and fast increase. The time corresponding to the inters...

Embodiment 2

[0034]This example is the effect of microsphere content in the naltrexone microsphere-hydrogel framework in situ implantation system on the solidification characteristics. The microspheres and gel skeleton are the same as in Example 3. The contents of microspheres in the gel matrix are respectively: 10mg / mL, 30mg / mL and 50mg / mL microsphere contents are different, and the solidification time of the naltrexone microsphere-hydrogel matrix in situ implantation system at body temperature is listed in the table 1. Although the coagulation time increased with the increase of the microsphere content, but when the microsphere content reached 50mg / mL, the coagulation time was still within 10min.

[0035] Table 1 The coagulation time of naltrexone microspheres-hydrogel matrix system at body temperature at different times

[0036] Microsphere content / mg·mL -1

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Abstract

The invention discloses an in-situ implantation drug delivery system of microsphere-hydrogel matrix of detoxification drug naltrexone, belonging to the field of medicinal preparation. The drug naltrexone is embedded in microspheres of biodegradable materials polylactic acid/glycolic acid polymer; the microspheres disperse in reverse temperature sensitive hydrosol of methylcellulose; the hydrosol is solidified into a hydrogel matrix at body temperature during hypodermic injection to form a composite system of microsphere-hydrogel matrix and to control the release of naltrexone. The invention integrates the advantages of medicine carrying controlled release particles and temperature sensitive gel matrix in-situ implantation system, realizes injected implantation, realizes release at a constant speed for 60 days after implantation, and can adjust drug release speed by adjusting the content of naltrexone microspheres in hydrogel, thus having great significance in improving clinical application effect of naltrexone and in solving the problem of relapse in the detoxification process.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, specifically a microsphere-hydrogel framework in-situ implanted drug delivery system. Background technique [0002] In vivo implantable drug release system is a kind of controlled release drug implanted in the body or subcutaneously, which is suitable for long-term drug delivery system. The early implanted drug delivery systems were mainly constructed of non-biodegradable materials, such as silicone rubber, etc. The carrier was injected into the implanted site by surgery or a special injection device, and the carrier was taken out after the drug was released. Due to the good stability of the material and the relatively stable release rate of the drug, this kind of implanted drug delivery system has been applied clinically. However, due to the poor biocompatibility of the material, the serious foreign body sensation at the implant site, and the complicated procedure of implanting and re...

Claims

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Application Information

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IPC IPC(8): A61M31/00A61K9/00A61L31/14
Inventor 蒋国强林莹孙佳丽丁富新
Owner TSINGHUA UNIV
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