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Continuous release composition made of hyaluronic acid and its therapeutic use

A technology of hyaluronic acid and hyaluronic acid salt, applied in the field of preventing skin aging and/or repairing dermal tissue, which can solve problems such as uncontrollable size

Active Publication Date: 2021-09-28
伊伯萨制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The method of preparing this emulsion also showed reproducibility problems due to the uncontrollable size of the droplets formed
Finally, another disadvantage of this method is that once the emulsion is prepared, it needs to be stored at low temperature for several days

Method used

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  • Continuous release composition made of hyaluronic acid and its therapeutic use
  • Continuous release composition made of hyaluronic acid and its therapeutic use
  • Continuous release composition made of hyaluronic acid and its therapeutic use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Preparation of polymer particles according to the invention:

[0075] Step 1: "Primary" Emulsification

[0076] An aqueous hyaluronic acid solution was prepared by dissolving 50 mg of hyaluronic acid in 5 ml of a 4 wt % polyvinyl alcohol (PVA) solution. Separately, an organic solution of the polymer was prepared by dissolving 900 mg of PLGA-PEG-PLGA triblock polymer in 12 ml of dichloromethane / acetone (3 / 1 v / v) mixture. use The two solutions were emulsified at room temperature for two minutes with an IKA T25 basic stirrer at 16,000 rpm while magnetically stirring at a rate of 500 rpm with a magnetic bar. A second stirring cycle was performed in the same manner in an ice bath.

[0077] Step 2: "Secondary" Emulsification

[0078] The stable emulsion obtained from step 1 was introduced into a glass syringe and injected into a formulation reactor containing 450 ml of 4 wt% polyvinyl alcohol (PVA) under magnetic stirring at a rate of 750 rpm.

[0079] Step 3: Addition ...

Embodiment 2

[0114] Preparation of polymer particles according to the invention:

[0115] The polymer particles according to the invention were prepared in a similar manner to Example 1. The only change relative to the method of Example 1 is that a Silverson stirrer at a rate of 2800 rpm was used instead of the magnetic stirring at 750 rpm in Example 1 in the "secondary" emulsification preparation in the second step.

[0116] Analysis of the inventive polymer particles according to Example 2:

[0117] Ten batches of polymer particles according to the invention were analyzed. The results obtained are as follows:

[0118] - according to use 3 Particle size analysis of a Coulter counter (Beckman Coulter), the size of the particles obtained from polydispersity: 34.98 μm ± 7.02 μm (before irradiation) and 34.12 μm ± 7.23 μm (after irradiation),

[0119] - content of hyaluronic acid: 16 μg of hyaluronic acid loaded per mg of freeze-dried polymer particles, and

[0120] - The binding yield ...

Embodiment 3

[0128] Preparation of polymer particles according to the invention:

[0129] A method similar to that of Example 2 was used for the preparation of the polymer particles according to the invention. The only change relative to the method of Example 2 is the addition of a pharmaceutically acceptable excipient which is also anti-inflammatory (radical scavenger), i.e. 1 ml of sorbitol in the form of an ultrapure aqueous solution of 10 wt% sorbitol Substitute the ultrapure water used in Example 2.

[0130] Analysis of the inventive polymer particles according to Example 3:

[0131] Six batches of polymer particles according to the invention were analyzed. The results obtained are as follows:

[0132] - according to use 3 Particle size analysis by Coulter counter (Beckman Coulter), the size of the particles obtained from the polydispersity: 31.15 μm ± 7.80 μm, and

[0133] - The content of hyaluronic acid is: 13.94 μg of hyaluronic acid is loaded per mg of freeze-dried polymer ...

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Abstract

The invention relates to polymer particles combined with hyaluronic acid molecules or hyaluronate and a preparation method thereof, the polymer particles are composed of poly(lactic acid-co-glycolic acid) (PLGA) polymers, poly(lactic acid-co -glycolic acid)-polyethylene glycol-poly(lactic acid-co-glycolic acid) (PLGA-PEG-PLGA) copolymer, or mixtures thereof. The invention also relates to injectable cosmetic or pharmaceutical compositions containing such polymer particles, processes for the preparation of such compositions and their use as medicines (in particular for the prophylaxis and / or Treatment of: musculoskeletal disorders, traumatic conditions of the skin and skin diseases, oral symptoms, dryness of the vaginal mucous membranes and urinary tract infections or cystitis, dry eye membranes and eye infections, and obesity), and their role in preventing skin aging and / or repairing the dermis Use in tissue (mesotherapy). More specifically, the compositions of the present invention may be aimed at replenishing joint fluid, especially synovial fluid, reestablishing the rheological and physiological conditions of pathological joints (e.g. arthritic joints), or effectively remodeling, moisturizing and protecting the skin. Treats and repairs the epidermis.

Description

technical field [0001] The present invention relates to polymer particles combined with hyaluronic acid molecules or hyaluronate, based on poly(lactic acid-co-glycolic acid)-polyethylene glycol-poly(lactic acid- co-glycolic acid) (PLGA-PEG-PLGA) copolymer, or based on poly(lactic-co-glycolic acid) (PLGA) polymers and poly(lactic-co-glycolic acid)-polyethylene glycol-poly(lactic acid -co-glycolic acid) (PLGA-PEG-PLGA) copolymer mixture. Another subject of the present invention are injectable cosmetic or pharmaceutical compositions containing such polymer particles, processes for the preparation of such compositions and their use as medicaments (in particular for the prophylaxis of and / or treatment of: musculoskeletal disorders, traumatic conditions of the skin and skin diseases, oral symptoms, dry vaginal mucosa and urinary tract infections or cystitis, dry eye membranes and eye infections, and obesity), and their role in preventing skin aging and / or Or use in repairing derma...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/728A61K9/10
CPCA61K9/0019A61K9/0024A61K9/1641A61K8/86A61K2800/91A61K31/728A61K8/735A61Q19/08A61P17/00A61P19/00A61K9/10A61K9/14A61K47/10A61K9/5084A61K9/5089
Inventor 扬尼斯·吉尔曼多米尼克·瓦谢托马斯·佩里厄莫德·贡内特让-诺埃尔·古兹
Owner 伊伯萨制药有限公司
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