Ketorolac implant and preparation method thereof

A technology of ketorolac and implants, which is applied in the field of medicine and can solve difficult problems such as realization

Inactive Publication Date: 2013-08-28
广东欧替克生物医学科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The ketorolac implant disclosed in U.S. Patent US2009/0263319A1, although the implant claims to be capable of controlled release for 3-7 days, its in vitro release experiment shows that more than 90% of the ketorolac is released within 24 hours, and there

Method used

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  • Ketorolac implant and preparation method thereof
  • Ketorolac implant and preparation method thereof
  • Ketorolac implant and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0067] Embodiment 1: Ketorolac implant (drug release for 2 days)

[0068] 1) Preparation of ketorolac implant (drug release for 2 days)

[0069] By weight percentage, 30% of ketorolac tromethamine and 20% of poly D, L-lactic acid (carboxyl-terminated, molecular weight of 18kDa to 28kDa) and 40% of poly D, L-lactic acid-CO-ethanol Acid (carboxyl-terminated, lactic acid and glycolic acid ratio 50:50, molecular weight range 7kDa to 17kDa) and 10% polyethylene glycol (PEG4000) mixed, put into Turbula three-dimensional mixer (T2F type, WAB machinery company) and 4 stainless steel balls were shaken twice, each time for 15 minutes. The mixture was then put into a HAAKE miniature twin-screw extruder (MiniLab type, Thermo Scientific Company), the temperature of the extruder was set at 66° C., and the speed was set at 25 revolutions per minute. The diameter of the extruded rod is 0.5mm. The small stick-shaped implant was cut with a razor blade into small test samples with a length of...

Embodiment 2

[0074] Embodiment 2: Ketorolac implant (drug release for 5 days)

[0075] 1) Preparation of ketorolac implant (drug release for 5 days)

[0076] In terms of weight percentage, 50% of ketorolac tromethamine and 30% of poly D, L-lactic acid (carboxyl-terminated, with a molecular weight of 18kDa to 28kDa) and 20% of poly D, L-lactic acid-CO-ethanol Acid (carboxyl-terminated, lactic acid to glycolic acid ratio 50:50, molecular weight range 7kDa to 17kDa) mixed, put into Turbula three-dimensional mixer (T2F type, WAB Machinery Company) and 4 stainless steel balls to shake twice, each time 15 minute. Then the mixture was put into a HAAKE miniature twin-screw extruder (MiniLab type, Thermo Scientific Company), the temperature of the extruder was set at 78° C., and the speed was set at 25 revolutions per minute. The diameter of the extruded rod is 0.5mm. The small rod-shaped implants were cut with a blade into small pieces with a length of 2 mm.

[0077] 2) In vitro release test: ...

Embodiment 3

[0080] Embodiment 3: Ketorolac implant (11 days of drug release)

[0081] 1) Preparation of ketorolac implant (drug release for 11 days)

[0082] Five groups of ketorolac implants with drug release for 11 days were prepared by using different contents of ketorolac trometamol and rate modifiers, as well as different molecular weights and contents of carboxyl-terminated PLA and carboxyl-terminated PLGA, as shown in the following table 2 shows:

[0083] Table 2: Ketorolac Implants Released for 11 Days

[0084]

[0085] The preparation method of implant B is as follows:

[0086]By weight percentage, 40% of ketorolac tromethamine and 25% of poly D, L-lactic acid (carboxyl-terminated, molecular weight 10kDa to 18kDa) and 35% of poly D, L-lactic acid-CO-ethanol Acid (carboxyl-terminated, lactic acid to glycolic acid ratio 50:50, molecular weight range 7kDa to 17kDa) mixed, put into Turbula three-dimensional mixer (T2F type, WAB Machinery Company) and 4 stainless steel balls to ...

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Abstract

The invention provides a ketorolac implant and a preparation method thereof. The implant which contains ketorolac and a degradable carrier is prepared by using a hot melt extrusion method, can release drugs in a zero-level dynamic way within a preset drug release time and can be used for preventing or treating acute or chronic pain and inflammation. The ketorolac implant prepared by the invention is stable in release and free of burst release effect and has great advantages in clinic application.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, in particular, the invention relates to a ketorolac implant with zero-order kinetic release effect and a preparation method thereof. Background technique: [0002] The chemical name of ketorolac is (±)5-benzoyl-2,3-dihydro-1H-pyrrolazine-1-carboxylic acid with a molecular weight of 225 g / mol. As a non-steroidal anti-inflammatory drug (NSAIDs), ketorolac is widely used in the treatment of rheumatic diseases, inflammatory diseases, pain, soft tissue diseases and sports injuries. Ketorolac has a strong analgesic effect. In the writhing reaction experiment of mice induced by benzoquinone, the relative analgesic strength of ketorolac is 350 times that of aspirin. In the pain experiment, the relative analgesic strength of ketorolac was 800 times that of aspirin; 30 mg of ketorolac showed an analgesic effect superior to that of 6 mg of morphine, 50 and 100 mg of meperidine, and 30 mg of analgesia, an...

Claims

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Application Information

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IPC IPC(8): A61K31/407A61K47/34A61P29/00A61P19/04
CPCA61K9/0024A61K31/407A61K47/34A61P19/04A61P29/00
Inventor 林军石海涛林穗珍胡海燕
Owner 广东欧替克生物医学科技有限公司
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