PMX‑53 gelatin composite particles and preparation method thereof

A technology of PMX-53 and composite particles, which is applied in the direction of drug combinations, pharmaceutical formulas, and non-effective ingredients of polymer compounds, can solve the problems of large dosage, difficulty in maintaining drug concentration, and low bioavailability, so as to reduce drug administration The effect of increasing the number of times, improving bioavailability, and maintaining drug concentration

Inactive Publication Date: 2017-06-30
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to aim at the shortcomings of PMX-53, such as large drug dosage and low bioavailability when applied to the whole body, and it is difficult to maintain its drug concentration when it is applied locally alone. Using gelatin as a carrier, PMX-53 is prepared after compounding with gelatin A PMX-53 gelatin composite particle that can be locally applied to the lesion environment and can be released for a long time

Method used

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  • PMX‑53 gelatin composite particles and preparation method thereof
  • PMX‑53 gelatin composite particles and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Take 500mg of type A gelatin (with an isoelectric point of 7-9) and add it to 10mL of deionized water, heat-dissolve at 60°C to form an aqueous gelatin solution, add 10mL of acetone to the aqueous gelatin solution, remove the upper suspension, and obtain 200mg of precipitated gelatin. Dissolve the precipitated gelatin again in 10 mL of deionized water, adjust the pH value of the reaction system to 7.0 with aqueous hydrochloric acid and sodium hydroxide solution, add 2 mg of PMX-53 to the aqueous gelatin solution, and stir magnetically at 800rmp / min for 3min; under magnetic stirring at 1500rmp / min Add 40 mL of acetone to the above system to emulsify the system to form gelatin particles, add 200 μL of 50% glutaraldehyde aqueous solution, and stir in an ice bath for 6 hours to solidify the gelatin particles; centrifuge at 15000 rpm, remove the supernatant, and use acetone under ultrasonic The precipitate was washed 4 times, and vacuum-dried to obtain PMX-53-loaded gelatin c...

Embodiment 2

[0028] Take 1000mg type A gelatin (isoelectric point is 7~9) and add it into 10mL deionized water, heat-dissolve at 60°C to form a gelatin aqueous solution, add 10mL acetone to the gelatin aqueous solution, remove the upper suspension, take 800mg of precipitated gelatin, and use Dissolve the precipitated gelatin again with 10 mL of deionized water, adjust the pH value of the reaction system to 8.0 with hydrochloric acid and sodium hydroxide aqueous solution, add 1 mg of PMX-53 to the gelatin aqueous solution, and stir magnetically at 800rmp for 3min; Emulsify the system into the above system to form gelatin particles, add 500 μL of glutaraldehyde aqueous solution with a mass fraction of 50%, and stir in an ice bath for 6 hours to solidify the gelatin particles; centrifuge at 15,000 rpm, remove the supernatant, and wash the precipitate with acetone under ultrasound for 4 times , vacuum-dried to obtain PMX-53-loaded gelatin composite microparticles, detected by a scanning electro...

Embodiment 3

[0030] Take 800mg of type A gelatin (with an isoelectric point of 7-9) and add it to 10mL of deionized water, heat-dissolve it at 60°C to form an aqueous gelatin solution, add 10mL of acetone to the aqueous gelatin solution, remove the upper suspension, and obtain 400mg of precipitated gelatin. Dissolve the precipitated gelatin again in 10mL of deionized water, adjust the pH value of the reaction system to 7.5 with hydrochloric acid and sodium hydroxide aqueous solution, add 1mg of PMX-53 to the gelatin aqueous solution, stir magnetically at 800rmp / min for 3min, and magnetically stir at 1500rmp / min Add 40mL of acetone to the above system to emulsify the system to form gelatin particles under certain conditions, add 400 μL of 50% glutaraldehyde aqueous solution, and stir in an ice bath for 12 hours to solidify the gelatin particles; centrifuge at 15000rmp, remove the supernatant, and use acetone The precipitate was cleaned 4 times under ultrasound, and vacuum-dried to obtain com...

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Abstract

The invention discloses a PMX-53 and gelatin composite particle and a preparation method thereof, and belongs to the technical fields of gelatin composite particles and preparation thereof. The method comprises the following steps: firstly, adding gelatin to deionized water, heating and dissolving to prepare a gelatin water solution; adding acetone to the gelatin water solution to obtain precipitated gelatin; dissolving with the deionized water again to prepare the gelatin water solution; adjusting the pH value of the solution to be 7.0-8.0; adding PMX-53 to the gelatin water solution, dropwise adding the acetone to the formed system under a magnetic stirring condition, and emulsifying the system to form gelatin particles; adding a glutaraldehyde water solution, further stirring in ice bath, and solidifying the gelatin particles; and centrifuging the formed gelatin particles, cleaning and precipitating with acetone for 3-5 times, and drying in vacuum to obtain the PMX-53 and gelatin composite particle. The PMX-53 is applied to the processes of treating rheumatoid arthritis, promoting severe bone trauma healing and treating related diseases such as periodontitis, so as to obtain a relatively good treatment effect.

Description

technical field [0001] The invention belongs to the technical field of gelatin composite microparticles and its preparation, and in particular relates to a PMX-53 gelatin composite microparticle with slow-release function and a preparation method thereof. Background technique [0002] PMX-53 is a chemically synthesized polypeptide substance. By simulating the structure of the complement C5 receptor, the polypeptide acts as an antagonist of the complement C5 receptor. In the immune inflammatory response of the body, it acts on the axis reaction of C5a-C5aR to inhibit the occurrence and development of local tissue inflammation, thereby exerting Anti-inflammatory effect. Related studies have shown that oral administration of PMX-53 can treat rheumatoid arthritis, inhibit the development of immune inflammation, and at the same time promote the healing of severe bone trauma. In addition, local injection of PMX-53 in periodontal tissue can not only effectively inhibit periodonta...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/00A61K9/14A61K47/42A61P29/00A61P19/02A61P19/08A61P1/02
Inventor 于维先李娜倪世磊刘歆婵张恺侯玉帛唐秋玲
Owner JILIN UNIV
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