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Method of manufacturing fulvestrant sustained-release microspheres

A technology of fulvestrant and sustained-release microspheres, which is applied in the field of preparation of fulvestrant sustained-release microspheres, can solve the problems of short biological half-life, poor stability, hindered application, etc., and achieves round shape and particle size distribution. uniform effect

Inactive Publication Date: 2008-01-23
XIAN LIBANG PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the short biological half-life and poor stability of these drugs, long-term large-scale administration is required, which hinders their clinical application.

Method used

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  • Method of manufacturing fulvestrant sustained-release microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Accurately weigh PLA 750mg and medicine fulvestrant 75mg and dissolve in the mixed solution of 15ml dichloromethane and ethyl acetate (the volume percentage of dichloromethane and ethyl acetate is 4: 1) to make oil phase, the relative molecular mass of PLA is in 1.0×10 4 ~1.5×10 5 Between; inject the oil phase into 400ml containing 1% (g / ml) PVA and 0.1% (g / ml) Tween80 aqueous solution (water phase) and stir 1h under 800rpm, form O / W type emulsion, again under 400rpm Stir for 4 hours until the organic solvent is completely evaporated, centrifuge at 6000 rpm for 10 minutes, wash with distilled water 4 times, collect the microspheres, and vacuum dry at room temperature for 24 hours to obtain the fulvestrant sustained-release microspheres. The average particle size of the microspheres is 23.7 μm, the drug loading capacity is 7.29%, and the encapsulation efficiency is 80.2%.

Embodiment 2

[0027] Accurately weigh 350mg of PLGA and 50mg of drug fulvestrant and dissolve in 5ml of dichloromethane to make an oil phase. The relative molecular mass of PLGA is 1.0×10 4 ~1.5×10 5 Between; The oil phase is injected into 400ml and contains 2% (g / ml) PVA, 0.1% (g / ml) Tween80 and 1% (g / ml) NaCl aqueous solution (water phase) and stir 2h under 1100rpm, form O / W type emulsion, then stirred at 400rpm for 12h until the organic solvent evaporated completely, centrifuged at 3500rpm for 15min, washed 4 times with distilled water, collected microspheres, -40°C, 4h; -30°C, 10h; -10°C, 20h freeze-dried The fulvestrant sustained-release microspheres were obtained. The average particle size of the microspheres is 85.4 μm, the drug loading capacity is 11.6%, and the encapsulation efficiency is 92.8%.

Embodiment 3

[0029] Accurately weigh PLGA 600mg and drug fulvestrant 100mg to be dissolved in the mixed solution of 2ml methylene chloride and ethyl acetate (the volume percentage of methylene chloride and ethyl acetate is 4: 1) to make oil phase, the relative molecular mass of PLGA is in 1.0×10 4 ~1.5×10 5 Between; inject the oil phase into 400ml containing 1% (g / ml) PVA, 0.1% (g / ml) Tween80 emulsification 30s at a high speed under 10000rpm, form O / W type emulsion, then stir 1h at 400rpm to organic The solvent was completely evaporated, centrifuged at 3500 rpm for 15 minutes, washed with distilled water 4 times, collected the microspheres, and dried in vacuum at room temperature for 48 hours to obtain fulvestrant sustained-release microspheres. The average particle size of the microspheres is 32.3 μm, the drug loading capacity is 13.0%, and the encapsulation efficiency is 91.0%.

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Abstract

The invention discloses a faslodex controlled-release microballoon preparation method. The faslodex controlled-releasemicroballoon in the invention envelopes fulvestrant takes PLA or PLGA or PCL or other biodegradable materials as the carrier materials. Besides, the invention takes PVA or the miscible liquids of PCL and Tween 80 as the disperse medium. Then, with the emulsion solvent evaporation method, finish the preparation of fulvestrant controlled-release microballoon under the action of mechanical mixing or high-speed shearing. The microballoon has spherical shape and even distribution of grain size that is controllable within the scope of 15 to 125Mu m as well as reaches a drug-loading rate of over 7 per cent and encapsulation rate of over 80 per cent.

Description

technical field [0001] The invention belongs to the cross-research field of biomedical polymer materials and drug controlled-release preparations, and specifically relates to a preparation method of fulvestrant sustained-release microspheres. The method adopts the emulsion solvent evaporation method, and uses the polymer material polylactic acid (PLA) or polylactic acid-glycolic acid copolymer (PLGA) or polycaprolactone (PCL) as the carrier to encapsulate fulvestrant (fulvestrant). The fulvestrant microspheres are prepared under the action of mechanical stirring or high-speed shearing. Background technique [0002] In recent years, with the rapid development of biotechnology, more and more peptide, protein and hormone drugs have been developed, and have shown unique curative effects in clinical applications. However, due to the short biological half-life and poor stability of these drugs, they need to be administered in large quantities for a long time, which hinders their ...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/565A61K47/34A61P35/00A61K47/26
Inventor 刘继三梁丹王惠宁王九成
Owner XIAN LIBANG PHARMA TECH
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