Gentamicin sulfate wrapped in polylactic acid/nano-hydroxyapatite composite microspheres and preparation method thereof

A technology of nano-hydroxyapatite and gentamicin sulfate, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas to overcome short sustained release time and particle size dispersion Uniform, long-term drug release effect

Inactive Publication Date: 2010-08-04
SCHOOL OF OPHTHALMOLOGY & OPTOMETRY WENZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Polylactic acid (PLA) is widely used as a drug carrier due to its good biocompatibility and biodegradability, but it has a disadvantage that it forms an acidic environment after degradation, adding bioceramic hydroxyphosphorus that releases alkaline ions in aqueous solution Limestone is expected to solve this problem, while also improving the material's biological activity
At present, polylactic acid / nano-hydroxyapatite is used as a GS carrier and made into composite microspheres, which has not been reported in China.

Method used

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  • Gentamicin sulfate wrapped in polylactic acid/nano-hydroxyapatite composite microspheres and preparation method thereof
  • Gentamicin sulfate wrapped in polylactic acid/nano-hydroxyapatite composite microspheres and preparation method thereof
  • Gentamicin sulfate wrapped in polylactic acid/nano-hydroxyapatite composite microspheres and preparation method thereof

Examples

Experimental program
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Effect test

example 1

[0025] Preparation of PLA / nHA-GS composite microspheres: ①Preparation of nHA-GS: Add 0.6g HA to 6ml aqueous solution containing 120mgGS, first mix with 60kHz ultrasonic, then magnetically stir for 24h, freeze-dry at -40°C and heat up to 10°C, The white lyophilized powder nHA-GS was obtained. ②Preparation of microspheres: Add nHA-GS lyophilized powder into 15ml dichloromethane solution dissolved with 1.5g PLA, stir at 8000rpm for 1min, mix and disperse by ultrasonic to form S / O emulsion; ③Add the above S / O emulsion Quickly pour into 750ml deionized aqueous solution dissolved with 1.2g emulsifier methyl cellulose to obtain S / O / W emulsion, and magnetically stir at 400rpm for 4h to completely volatilize dichloromethane; after standing for 4h, centrifuge at 10000rpm , the precipitate was separated, washed three times with deionized water, and then freeze-dried at -40°C to obtain the product of the present invention, which was refrigerated at -4°C. The drug loading capacity of the ...

example 2

[0030] Preparation of PLA / nHA-GS composite microspheres: ① Preparation of nHA-GS: Add 0.6g HA to 6ml aqueous solution containing 60mgGS, first mix with 80kHz ultrasonic, then magnetically stir for 24h, freeze-dry at -40°C and heat up to 10°C. The white lyophilized powder nHA-GS was obtained. ②Preparation of microspheres: Add nHA-GS freeze-dried powder into 15ml of acetone solution dissolved with 1.5g PLA, stir at 4000rpm for 1min at high speed, and form S / O emulsion after fully mixing and dispersing; ③Pour the above S / O emulsion quickly Dissolve 0.6g of emulsifier methylcellulose in 300ml of deionized aqueous solution to obtain an S / O / W emulsion, and stir it magnetically at 800rpm for 4h to make the acetone evaporate completely; after standing for 4h, centrifuge at a speed of 10000rpm to separate Precipitated, washed three times with deionized water, then freeze-dried at -40°C and warmed to 10°C, and the obtained microspheres were refrigerated at -4°C. The drug loading capaci...

example 3

[0032]Preparation of PLA / nHA-GS composite microspheres: ①Preparation of nHA-GS: Add 0.2g HA to 10ml aqueous solution containing 120mgGS, first mix with 40kHz ultrasonic, then magnetically stir for 24h, freeze-dry at -40°C and heat up to 10°C, The white lyophilized powder nHA-GS was obtained. ②Preparation of microspheres: Add nHA-GS freeze-dried powder into 15ml chloroform solution dissolved with 1.5g PLA, stir at 2000rpm at high speed for 1min, mix well and disperse to form S / O emulsion, ③Pour the above S / O emulsion quickly Dissolve 0.6g of emulsifier methyl cellulose in 300ml of deionized aqueous solution to obtain an S / O / W emulsion, stir it magnetically at 1000rpm for 4h, and let the chloroform volatilize completely; after standing for 4h, centrifuge at a speed of 10000rpm to separate Precipitated, washed three times with deionized water, then freeze-dried at -40°C and warmed to 10°C, and the obtained microspheres were refrigerated at -4°C. The drug loading capacity of the ...

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Abstract

The invention relates to a gentamicin sulfate wrapped in polylactic acid/nano-hydroxyapatite composite microspheres, which comprises the following components in parts by weight: 1-10 parts of nano-hydroxyapatite, 1 part of gentamicin sulfate, 12.5-25 parts of polylactic acid and 1-17 parts of methyl cellulose. The invention further discloses a preparation method. The prepared gentamicin sulfate has the advantages of high drug loading, high entrapment efficiency, long-term sustained release and biodegradability.

Description

technical field [0001] The invention relates to gentamicin, in particular to gentamicin sulfate wrapped by biodegradable polylactic acid / nanometer hydroxyapatite composite microspheres. Background technique [0002] Gentamicin sulfate (GS) is an antibiotic that has antibacterial and bactericidal effects on a variety of Gram-negative and positive bacteria, and is also effective against Pseudomonas aeruginosa, Bacillus aerogenes, Klebsiella pneumoniae, Salmonella, Escherichia coli and Gram-negative bacteria such as Proteus and Staphylococcus aureus have strong effects. This drug is widely used in systemic or local infections caused by sensitive bacteria, and has relieved the pain of countless patients. Caused death after anaphylactic shock, reducing the clinical application effect. Polymer drug-loaded microspheres are a new dosage form developed in recent years, which can control drug release and prolong the biological half-life of drugs, reduce toxic and side effects, and f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K47/02A61K31/7036A61K9/16A61P31/04
Inventor 陈浩魏坤
Owner SCHOOL OF OPHTHALMOLOGY & OPTOMETRY WENZHOU MEDICAL COLLEGE
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