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Hydrophilic medicament dual-microsphere formulation and preparation method thereof

A technology of hydrophilic drugs and microspheres, which can be used in pharmaceutical formulations, medical preparations of non-active ingredients, powder delivery, etc. Rapid, increased drug loading, high encapsulation efficiency

Inactive Publication Date: 2009-02-18
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For hydrophilic small molecule drugs, although the preparation of double microspheres by this method can control the burst release effect of microsphere preparations, there is a problem of low encapsulation efficiency, resulting in waste of raw materials and failure to achieve long-term sustained release.

Method used

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  • Hydrophilic medicament dual-microsphere formulation and preparation method thereof
  • Hydrophilic medicament dual-microsphere formulation and preparation method thereof
  • Hydrophilic medicament dual-microsphere formulation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037]Accurately weigh 30 mg of gentamicin, dissolve in 30 ml of chitosan aqueous solution with a concentration of 1 mg / mL and pH=6, stir magnetically at room temperature, slowly add 12 ml of sodium tripolyphosphate aqueous solution with a concentration of 0.5 mg / mL into chitosan The sugar solution was mixed for 30 minutes, and the precipitate was collected after centrifugation at 12000 rpm at 4°C for 20 minutes, washed 3 times with distilled water, and freeze-dried to obtain chitosan nanoparticles.

[0038] Disperse the above dried 50mg chitosan nanoparticles into 2.5ml acetonitrile solution containing 300mgPLGA (the mass ratio of LA to GA is 90:10), mix evenly with 400w probe type ultrasonic instrument for 90 seconds, and use it as the suspension water phase Dissolve 1.5g Span 80 in 20ml edible oil as the oil phase; slowly drop the oil phase into the above-mentioned suspension water phase under stirring at 3500rpm, rotate and evaporate under reduced pressure for 2 hours, remo...

Embodiment 2

[0040] Accurately weighed 30mg streptomycin, and the rest were operated in the same way as in Example 1.

Embodiment 3

[0042] Accurately weigh 250 mg of tetracycline, dissolve in 25 ml of chitosan aqueous solution with a concentration of 3 mg / mL and pH=4, stir magnetically at room temperature, slowly add 20 ml of aqueous sodium tripolyphosphate solution with a concentration of 1.5 mg / mL to the chitosan solution, and mix After 40 minutes, centrifuge at 16,000 rpm at 4°C for 20 minutes to collect the precipitate, wash with distilled water three times, and freeze-dry to obtain chitosan nanoparticles.

[0043] The above dried 50mg chitosan nanoparticles were dispersed into 3ml of acetonitrile solution containing 200mgPLGA (the mass ratio of LA and GA was 85:15), and the 400w probe type ultrasonic instrument was ultrasonically mixed for 90 seconds as the suspension water phase; Dissolve 2.0g of Span 80 in 20ml of edible oil as the oil phase. Slowly drop the oil phase into the above suspension water phase under stirring at 3500rpm. Rotate and evaporate under reduced pressure for 1.5 hours to remove a...

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Abstract

The invention discloses a dual microsphere preparation of a hydrophilic drug, which consists of the hydrophilic drug, chitosan, sodium tripolyphosphate and a polylactic acid-glycolic acid copolymer. The invention also discloses a method for preparing the dual microsphere preparation: firstly, chitosan nanoparticles of the hydrophilic drug are prepared; secondly, the nanoparticles are dispersed in an acetonitrile or dichloromethane solution of PLGA and are evenly mixed to be used as suspension aqueous phase; finally, span80 is dissolved in edible oil to be used as oil phase; the oil phase is slowly dripped to the suspension aqueous phase while being stirred; acetonitrile or dichloromethane is removed; and the mixture is subjected to centrifugal collection and vacuum drying to prepare the dual microsphere preparation. The dual microsphere preparation of the hydrophilic drug has small burst effect, keeps the high encapsulation efficiency of the chitosan nanoparticles to the hydrophilic drug, is slowly released in vitro and is novel promising slow-release dosage of the hydrophilic drug.

Description

technical field [0001] The invention relates to the field of biodegradable microsphere preparations in pharmacy, in particular to a double microsphere preparation using chitosan-modified hydrophobic and degradable polylactic acid-glycolic acid copolymers to encapsulate hydrophilic drugs and a preparation method thereof . Background technique [0002] Polylactic acid-glycolic acid copolymer (PLGA) is a polymer copolymer formed by the polymerization of two monomers of lactic acid (LA) and glycolic acid (GA) under the action of a catalyst. PLGA has good biodegradability and biocompatibility, and can be degraded into lactic acid, water and carbon dioxide in the living body, participates in the metabolism in the body, and does not cause any toxic reactions in the body. It can be widely used in biomedical tissue engineering, such as controlled drug release system, bioabsorbable suture materials, orthopedic fixation and tissue repair materials, etc. The material has been approved...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/34A61K47/36
Inventor 高建青何彩霞
Owner ZHEJIANG UNIV
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