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Biodegradation type introducing agent of hardly water-soluble steroid, nonsteroid anti-inflammatory medicine, and its prepn. method

A non-steroidal anti-inflammatory drug, non-steroidal anti-inflammatory technology, applied in anti-inflammatory agents, drug combinations, non-central analgesics, etc., can solve the problems that affect the research of biodegradable controlled-release microspheres, low drug loading, Porous microspheres and other issues

Inactive Publication Date: 2005-01-19
ZHEJIANG ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, classic preparation methods such as organic solvent volatilization technology to prepare microspheres (capsules) are not only complicated but also require the use of toxic solvents such as chloroform and dichloromethane, and it takes a long time to volatilize these organic solvents under natural conditions. The volatilized microspheres are often porous but not dense, which affects drug release
The low drug loading of microspheres (generally less than 20%), unstable yield, and difficulty in scale-up experiments all affect further research on biodegradable controlled-release microspheres.

Method used

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  • Biodegradation type introducing agent of hardly water-soluble steroid, nonsteroid anti-inflammatory medicine, and its prepn. method
  • Biodegradation type introducing agent of hardly water-soluble steroid, nonsteroid anti-inflammatory medicine, and its prepn. method
  • Biodegradation type introducing agent of hardly water-soluble steroid, nonsteroid anti-inflammatory medicine, and its prepn. method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] 5% Ketoprofen Biodegradable Implant

[0016] Ketoprofen 0.5g

[0017] Lactic acid-glycolic acid copolymer (7:3) 1.5g

[0018] Dimethyl sulfoxide 10g

[0019] 10 bottles in total

[0020] Weigh 1.5 g of lactic acid-glycolic acid copolymer (7:3), add 10 g of dimethyl sulfoxide, dissolve it by ultrasonication, add 0.5 g of dried ketoprofen, dissolve, shake well, filter, and pack.

[0021] In vitro release:

[0022] The in vitro drug release research results of 5% ketoprofen biodegradable implants are shown in Figure 1: as can be seen from this figure, ketoprofen can be released slowly from the implants, and release about 30% (burst release effect) on the 0.8th day , about 50% of the drug was released cumulatively on the 25th day, and about 80% on the 52nd day.

[0023] Release conditions: LAB-LINE oscillator, dissolution medium: water; temperature: 37°C; speed: 50rpm.

Embodiment 2

[0025] 10% Ketoprofen Biodegradable Implant

[0026] Ketoprofen 1.0g

[0027] Lactic acid-glycolic acid copolymer (7:3) 1.5g

[0028] Dimethyl sulfoxide 10g

[0029] 10 bottles in total

[0030] Weigh 1.5 g of lactic acid-glycolic acid copolymer (7:3), add 10 g of dimethyl sulfoxide, dissolve it by ultrasonication, add 1.0 g of dried ketoprofen, dissolve, shake well, filter, and pack.

[0031] In vitro release:

[0032] The results of the in vitro drug release study of 10% ketoprofen biodegradable implants are shown in Figure 2: As can be seen from this figure, ketoprofen can be slowly released from the implants, releasing about 30% on the 8th day, and accumulating on the 20th day About 50% of the drug was released, and about 80% on the 60th day.

[0033] Release conditions: LAB-LINE oscillator, dissolution medium: water; temperature: 37°C; speed: 50rpm.

Embodiment 3

[0035] 15% Ketoprofen Biodegradable Implant

[0036] Ketoprofen 1.5g

[0037] Lactic acid-glycolic acid copolymer (7:3) 1.5g

[0038] Dimethyl sulfoxide 10g

[0039] 10 bottles in total

[0040] Weigh 1.5 g of lactic acid-glycolic acid copolymer (7:3), add 10 g of dimethyl sulfoxide, dissolve it by ultrasonication, add 1.5 g of dried ketoprofen, dissolve, shake well, filter, and pack.

[0041] In vitro release:

[0042] The in vitro drug release study results of 15% ketoprofen biodegradable implants are shown in Figure 3: as can be seen from this figure, ketoprofen can be slowly released from the implants, releasing about 30% on the 2nd day and accumulating on the 10th day About 50% of the drug was released, and it was about 80% on the 32nd day.

[0043] Release conditions: LAB-LINE oscillator, dissolution medium: water; temperature: 37°C; speed: 50rpm.

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Abstract

A biodegradable implantative medicine in the form of injection for treating chronical or progressive diseases, such as arthritis, is prepared from the lactic acid-alcoholic acid copolymer as skeleton, water-insoluble anti-inflammatory medicine (such as ketoibuprofen), and dimethylsulfoxide as solvent. Its advantages are slow releasing with degradation of medicine and low toxic by-effect.

Description

technical field [0001] The invention is a pharmaceutical preparation for treating a variety of chronic or progressive diseases, which is a biodegradable implant of insoluble steroids and non-steroidal anti-inflammatory drugs and a preparation method, and is especially suitable for treating arthritis patients . Background technique [0002] In order to study the implantable controlled-release drug delivery system, scientists have tried various methods. Non-biodegradable implants are administered by subcutaneously implanting drug tablets (rods), such as silicone rubber subcutaneously implanted drug delivery systems, etc. However, these small pieces (rods) need to be implanted subcutaneously by surgery, and they still need to be removed by surgery after the drug is released, which is inconvenient to use; in addition, this non-biodegradable matrix drug delivery system, after the drug is released, will be degraded in the matrix. A hollow area is formed,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/192A61K47/34A61P29/00
Inventor 王胜浩左军斌林芳王尊元沈正荣
Owner ZHEJIANG ACAD OF MEDICAL SCI