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Injectable celecoxib formulations based on microspheres

A technology of celecoxib and microspheres, applied in the field of injectable celecoxib preparations based on microspheres

Pending Publication Date: 2022-03-18
AVIDENCE THERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] unmet needs

Method used

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  • Injectable celecoxib formulations based on microspheres
  • Injectable celecoxib formulations based on microspheres
  • Injectable celecoxib formulations based on microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0151] The present invention addresses an unmet need in the art by providing a surprisingly superior way of using celecoxib to treat joint-related diseases. The present invention does this by releasing celecoxib over time from celecoxib-bearing microspheres.

[0152] Specifically, the present invention provides biodegradable microspheres, wherein the microspheres (i) have a diameter of 1 μm to 500 μm; (ii) comprise a polylactic-co-glycolic acid (PLGA) matrix; (iii) carry the drug celecoxib and (iv) release celecoxib for at least one month when present in suitable joint-related tissues.

[0153] In one embodiment of the biodegradable microspheres of the present invention, they have a molar ratio of lactic acid to glycolic acid of 100:0 to 50:50. Preferably, the microspheres of the present invention (i) have a diameter of 20 μm to 200 μm; and (ii) have a molar ratio of lactic acid to glycolic acid of 75:25.

[0154] In another embodiment of the biodegradable microspheres of th...

Embodiment 1

[0180] Example 1. General Experimental Materials and Methods

[0181] PLGA refers to polylactic acid-glycolic acid copolymer; PDLA refers to poly-D-lactic acid, which is a type of polylactic acid (PLA); DMSO refers to dimethyl sulfoxide; PVA refers to polyvinyl alcohol (molecular weight: 31K to 50K, 98% to 99% hydrolyzed); PBS refers to phosphate buffered saline (pH 7.4); and MW refers to molecular weight. The magnetic stir bar used in all the following examples has a length of 2 cm and a diameter of 0.7 cm.

[0182] (i) PDLA (0.4 dl / g, ester-terminated): intrinsic viscosity = 0.35 dl / g to 0.45 dl / g. MW: 20,000 to 30,000; (ii) PDLA (0.6dl / g, ester-terminated): intrinsic viscosity = 0.55dl / g to 0.65dl / g; (iii) PDLA (2dl / g, ester-terminated): intrinsic viscosity = 1.6 dl / g to 2.4 dl / g. MW: 300,000 to 600,000; (iv) PLGA (50:50, 0.2 dl / g, acid-terminated): intrinsic viscosity = 0.16 dl / g to 0.24 dl / g. MW: 7,000 to 17,000; (v) PLGA (50:50, 0.2 dl / g, ester-terminated): intrins...

Embodiment 2

[0184] Example 2. Microsphere Formulation of Diclofenac: Effect of Polymer Composition on Release of Diclofenac (I)

[0185] A drug depot comprising NSAID, diclofenac (2-[2-(2,6-dichloroaniline)phenyl]acetic acid) was prepared and incorporated into microspheres. Formulations were prepared by dissolving 50 mg PLGA or PDLA and 20 mg diclofenac in 440 μl dichloromethane and 60 μl DMSO. 500 μl of the solution was injected into the center of 200 ml of 1% PVA (w / v, pH adjusted to 2) in a 250 ml beaker, stirred with a magnetic stirring bar at 2,000 rpm to form an emulsion. The emulsion was stirred at 2,000 rpm for 2 minutes and at about 500 rpm for 2 hours to evaporate the dichloromethane. Microspheres were harvested by centrifugation at 4,000g for 5 minutes and washed three times with water.

[0186] To test the release of diclofenac from the microspheres, all prepared microspheres were added to 250 ml of 10 mM PBS and shaken at 80 rpm at 37 °C. At each time point in the releas...

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Abstract

The present invention provides biodegradable microspheres, wherein microspheres (i) have a diameter of from 1 [mu] m to 500 [mu] m; (ii) a matrix comprising a polylactic acid-glycolic acid copolymer (PLGA); (iii) carrying the medicine celecoxib; and (iv) releasing the celecoxib for at least one month when present in a suitable joint-related tissue. The invention also provides related injectable formulations, methods for treating joint-related diseases, and kits.

Description

[0001] This application claims the benefit of U.S. Provisional Application No. 62 / 884,526, filed August 8, 2019, the contents of which are incorporated herein by reference. [0002] Throughout this application, various publications are referenced. The disclosures of these publications are hereby incorporated by reference into this application to more fully describe the state of the art to which this invention pertains. technical field [0003] The present invention relates to a method of treating joint-related diseases by local injection of biodegradable microspheres comprising celecoxib. Background technique [0004] NSAIDs and celecoxib [0005] Non-steroidal anti-inflammatory drugs (NSAIDs) treat inflammation and pain. For the treatment of joint disease, oral NSAID drugs have been widely used to reduce pain and improve physical function. However, the vast majority of NSAIDs cause severe side effects due to inhibition of COX-1 and COX-2 targets. In fact, every drug tha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/575A61K47/12A61Q1/00
CPCA61K9/19A61K9/1647A61K9/1694A61K9/0019A61K31/415A61P19/02A61K9/5031A61K9/16A61K47/10
Inventor 李昂
Owner AVIDENCE THERAPEUTICS INC
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