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Preparation method of gentamicin sulphate-loading porous hydroxyapatite/PLGA (poly(DL-lactide-co-glycolide) microspheres

A technology of gentamicin sulfate and hydroxyapatite, which is applied in the field of preparation of biomedical materials, can solve the problems of large drug release burst and poor drug loading performance, and achieve small burst release effect, long release time, and preparation The effect of simple method

Active Publication Date: 2014-04-30
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the drug-loaded hydroxyapatite system prepared by the above-mentioned prior art generally has the problems of poor drug loading performance and large burst drug release.

Method used

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  • Preparation method of gentamicin sulphate-loading porous hydroxyapatite/PLGA (poly(DL-lactide-co-glycolide) microspheres
  • Preparation method of gentamicin sulphate-loading porous hydroxyapatite/PLGA (poly(DL-lactide-co-glycolide) microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] (1) Pour 1.5g of 100-200nm PLGA balls into a beaker, add 15ml of 5% acetone / ethanol blend, and place in the air for 72 hours to completely evaporate the solvent;

[0027] (2) Add 0.16mol L -1 Add 100ml of diammonium hydrogen phosphate solution into the beaker in (1), pour 0.36mol·L -1 100ml of calcium nitrate solution, adjust the pH value to 10 with ammonia water, and after aging the reactant for 5 days, wash the product 5 times with distilled water, dry it at 30°C, and then calcinate at 450°C for 4 hours to remove PLGA, and obtain porous hydroxyapatite ;

[0028](3) After grinding the porous hydroxyapatite, soak it in an aqueous solution containing 0.5 mg / ml gentamicin sulfate and 0.1% PEG, freeze-dry for 60 hours to obtain porous hydroxyapatite loaded with gentamicin sulfate, Store sealed at 4°C for later use.

[0029] (4) Mix 10ml of 10% PLGA acetone solution with 0.3g of gentamicin sulfate-loaded porous hydroxyapatite obtained in (3) to obtain a gentamicin sulfat...

Embodiment 2

[0032] (1) Pour 1.5g of 500-600nm PLGA balls into a beaker, add 30ml of 15% acetone / ethanol blend, and place in the air for 48 hours to completely evaporate the solvent;

[0033] (2) Add 0.11mol·L -1 Add 150ml of diammonium hydrogen phosphate solution into the beaker in (1), pour 0.24mol·L -1 150ml of calcium nitrate solution, adjust the pH value to 9 with ammonia water, and after aging the reactant for 6 days, wash the product 3 times with distilled water, dry it at 35°C, and then calcinate at 900°C for 2 hours to remove PLGA, and obtain porous hydroxyapatite ;

[0034] (3) After grinding the porous hydroxyapatite, soak it in an aqueous solution containing 0.8 mg / ml gentamicin sulfate and 0.5% PEG, freeze-dry for 60 hours to obtain porous hydroxyapatite loaded with gentamicin sulfate, Store sealed at 4°C for later use.

[0035] (4) Mix 10ml of 15% PLGA acetone solution with 0.4g of gentamicin sulfate-loaded porous hydroxyapatite obtained in (3) to obtain a gentamicin sulfa...

Embodiment 3

[0038] (1) Pour 3.75g of 300-400nm PLGA balls into a beaker, add 25ml of 10% acetone / ethanol blend, and place in the air for 60h to completely evaporate the solvent;

[0039] (2) Add 0.08mol·L -1 Add 200ml of diammonium hydrogen phosphate solution into the beaker in (1), pour 0.18mol·L -1 200ml of calcium nitrate solution, adjust the pH value to 8 with ammonia water, and after aging the reactant for 7 days, wash the product 4 times with distilled water, dry it at 40°C, and then calcinate at 600°C for 3 hours to remove PLGA, and obtain porous hydroxyapatite ;

[0040] (3) Grind the porous hydroxyapatite and soak it in an aqueous solution containing 1 mg / ml gentamicin sulfate and 1% PEG, and freeze-dry for 40 hours to obtain porous hydroxyapatite loaded with gentamicin sulfate. Store in a sealed container at 4°C for later use.

[0041] (4) Mix 10ml of 20% PLGA acetone solution with 0.5g of gentamicin sulfate-loaded porous hydroxyapatite obtained in (3) to obtain a gentamicin ...

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Abstract

The invention discloses a preparation method of gentamicin sulphate-loading porous hydroxyapatite / PLGA (poly(DL-lactide-co-glycolide) microspheres. The preparation method comprises the following steps: adding PLGA microspheres in an acetone / alcohol solution, adding a diammonium hydrogen phosphate solution, pouring in a calcium nitrate solution, adjusting pH, ageing, washing, drying, calcining, and grinding to obtain porous hydroxyapatite; placing the porous hydroxyapatite powder in a water solution containing gentamicin sulphate / PEG (polyethylene glycol), and carrying out freeze drying to obtain gentamicin sulphate-loading porous hydroxyapatite; and uniformly mixing the PLGA solution and the gentamicin sulphate-loading porous hydroxyapatite, pouring in a polyvinyl alcohol solution, stirring, washing, and carrying out freeze drying to obtain the gentamicin sulphate-loading porous hydroxyapatite / PLGA (poly(DL-lactide-co-glycolide) microspheres. The gentamicin sulphate-loading porous hydroxyapatite / PLGA (poly(DL-lactide-co-glycolide) microspheres prepared by adopting the preparation method are high in medicine loading rate, small in burst release, good in biocompatibility, simple in preparation process, easily available in raw materials, and low in cost; and industrialization is easily realized.

Description

technical field [0001] The invention belongs to the technical field of preparation of biomedical materials, and relates to the preparation technology of drug-loaded injectable microspheres, in particular to a preparation method of porous hydroxyapatite / PLGA microspheres loaded with gentamicin sulfate. Background technique [0002] In recent years, various open fractures are more likely to be complicated by bone defect, soft tissue infection and osteomyelitis, and severe infection often affects fracture healing. How to prevent and treat such bone defect and infection has always been a clinical concern. In recent years, the emergence of drug-loaded bone tissue engineered bone has brought new hope for the repair of bone defects. For the drug treatment of bone tissue diseases, such as anti-infection and anti-inflammation after fracture surgery, systemic administration often results in insufficient effective drug content in the "focus" of bone tissue, and the distribution of dru...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/34A61K47/04A61K31/7036A61P19/08A61P31/04
Inventor 魏坤许为康
Owner SOUTH CHINA UNIV OF TECH
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