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Ketorolac implant and preparation method thereof

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

Inactive Publication Date: 2015-02-25
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 is a significant burst phenomenon
Chinese patent 200780020639.4 discloses a method to reduce the burst release effect of implants, that is, by coating polymer films on the surface of implants, but this method is difficult to realize in industrial production

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
Comparison scheme
Effect test

Embodiment 1

[0067] Example 1: Ketorolac implants (released for 2 days)

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

[0069] In terms of weight percentage, 30% of ketorolac tromethamine and 20% of poly D, L-lactic acid (carboxyl terminated, molecular weight 18kDa to 28 kDa) and 40% of poly D, L-lactic acid-CO-ethanol Acid (carboxyl end-capped, ratio of lactic acid to glycolic acid is 50:50, molecular weight range is 7kDa to 17kDa) and 10% polyethylene glycol (PEG4000) are mixed and put into Turbula three-dimensional mixer (T2F type, WAB Machinery Company) and Shake the 4 stainless steel balls twice for 15 minutes each time. Then the mixture was put into a HAAKE mini twin-screw extruder (MiniLab type, Thermo Scientific), the temperature of the extruder was set at 66°C, and the speed was set at 25 revolutions per minute. The extruded rod has a diameter of 0.5mm. Cut the small rod-shaped implant with a blade into small test specimens with a length of 2 mm.

[0070] 2) In v...

Embodiment 2

[0074] Example 2: Ketorolac implants (released for 5 days)

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

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

[0077] 2) In vitro release test:

[0078] Place each test sample (n=4) in an 8 ml g...

Embodiment 3

[0080] Example 3: Ketorolac implant (11 days release)

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

[0082] Five groups of ketorolac implants with a drug release for 11 days were prepared with different contents of ketorolac tromethamine and rate modifiers, as well as different molecular weights and different contents of carboxyl-terminated PLA and carboxyl-terminated PLGA. The details are as follows 2 shows:

[0083] Table 2: Ketorolac implants released for 11 days

[0084]

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

[0086] In terms of weight percentages, 40% ketorolac tromethamine and 25% poly D, L-lactic acid (carboxyl terminated, molecular weight 10kDa to 18kDa) and 35% poly D, L-lactic acid-CO-ethanol Acid (carboxyl end capped, ratio of lactic acid to glycolic acid is 50:50, molecular weight range is 7kDa to 17kDa), put into Turbula three-dimensional mixer (T2F type, WAB Machinery Company) and 4 stainless steel balls shake twice, 15 times each ...

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Abstract

The present invention provides a ketorolac implant and a method of preparing same. The implant comprises ketorolac and a degradable carrier, is prepared by adopting a hot melt extrusion method, can release drugs in a manner of zero-order kineics within a preset releasing time period, and can be used to prevent or treat acute and chronic ache and inflammation. The ketorolac implant prepared in the present invention has stable release, does not have a burst release effect, and has significant advantages in clinical use.

Description

Technical field: [0001] The present invention belongs to the technical field of medicine. Specifically, the present invention relates to a ketorolac implant with zero-order kinetics 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, and the molecular weight is 225g / mol. Ketorolac, as a non-steroidal anti-inflammatory drug (NSAIDs), 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 caused by benzoquinone, the relative analgesic intensity of ketorolac is 350 times that of aspirin. It is caused by flexion of the adjuvant-induced inflammation of the paw in rats. In the pain test, the relative analgesic intensity of ketorolac is 800 times that of aspirin; ketorolac 30mg shows analgesic effect better than m...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/407A61K47/34A61P29/00A61P19/04
CPCA61K31/407A61K47/34A61K9/0024A61P19/04A61P29/00
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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