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Method of preparing simvastatin sustained-release microsphere carried series

A technology of slow-release microspheres and simvastatin, applied in the biological field, can solve the problems that have not yet been studied and reported on simvastatin sustained-release microsphere preparations, and achieve improved bioavailability, controllable particle size, and adjustment range wide effect

Inactive Publication Date: 2010-01-13
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, the microsphere sustained-release system has begun to be applied to tissue engineering scaffolds, and has achieved certain effects in promoting cell growth, proliferation and tissue repair, but there is no report on the study of simvastatin sustained-release microsphere preparations

Method used

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  • Method of preparing simvastatin sustained-release microsphere carried series
  • Method of preparing simvastatin sustained-release microsphere carried series
  • Method of preparing simvastatin sustained-release microsphere carried series

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Dissolve 0.09 gram of polylactic acid (molecular weight 0.2 million) in 3ml of dichloromethane to make a homogeneous mixture, slowly add it to 30ml of PVA aqueous solution (containing 0.6ml of Tween80) with a mass concentration of 1.5% stirred at a speed of 700rpm , continue to stir for 1.5 hours, 37 ° C vacuum rotary evaporation for 1 hour, remove the organic solvent, centrifuge at 18,000 rpm, wash with deionized water 3 times, and vacuum dry for 48 hours to obtain about 0.078 grams of polylactic acid blank microsphere powder. The average particle size of the microspheres is 2100nm.

[0030] Microspheres of different particle sizes obtained by applying polylactic acid of other molecular weights and other biodegradable polymer materials according to the above steps, the average particle size ranges from 358nm to 2100nm, and the results are shown in Table 1, which can meet the requirements for preparing drug-loaded microspheres with different degradation rates. need.

...

Embodiment 2

[0035] (1) A mixture of PLA (0.05 grams, molecular weight 1.0w) and simvastatin (0.01 grams) with a mass ratio of 5:1 was dissolved in 3 milliliters of dichloromethane to make a uniform mixture;

[0036] (2) Slowly add the above mixed solution into 30ml of PVA aqueous solution with a mass concentration of 1.5% (containing 0.6ml of Tween80, 0.3g of sodium chloride, used after stirring at 700rpm for 15 minutes) in stirring (700rpm), and continue stirring for 1.5 hours ;

[0037] (3) Rotary evaporation under reduced pressure at 37°C for 1 hour to remove the organic solvent; centrifuge at 18,000 rpm for 10 minutes, wash with water, and dry in vacuum for 48 hours to obtain about 0.06 g of simvastatin-loaded microsphere powder with an average particle size of 102 nm. The sealing rate is 20.89%.

[0038] Get dry loaded simvastatin microsphere powder 0.03g, add 1 milliliter of acetonitrile and 2 milliliters, 0.1M phosphate buffer saline, after 24 hours, ultraviolet spectrophotometer de...

Embodiment 3

[0042] A mixture of PLGA7525 (0.05 gram, molecular weight 2w) and simvastatin (0.01 gram) with a mass ratio of 5:1 was dissolved in 3 milliliters of dichloromethane to make a homogeneous mixture, which was slowly added to the stirring (700rpm ) in 30 milliliters, 1% PVA aqueous solution (containing 0.6 milliliters of Tween80, 0.3 grams of sodium chloride, used after stirring at 700 rpm for 15 minutes) in 30 milliliters, mass concentration 1%, continue to stir for 1.5 hours, 37 ℃ of decompression, rotary evaporation 1 hour, remove Clean organic solvent; centrifuge at 18,000 rpm for 10 minutes, wash with water, and dry in vacuum for 48 hours to obtain 0.062 g of simvastatin-loaded microsphere powder with an average particle size of 1,400 nm and an encapsulation efficiency of 35.27%.

[0043] Change the stirring speed and prepare microspheres under other conditions unchanged, in order to explore the influence of stirring speed on the preparation of microspheres. A series of exper...

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Abstract

The invention relates to a method that a functional drug is enveloped into a polymeric material with biodegradability to form a nano-micron microsphere system. The method comprises that the polymeric material and simvastatin are dissolved in an organic liquor to form uniform dispersion which is then added into an liquor containing emulsifier Tween 80 and biologically nontoxic electrolytic polyvinyl alcohol or sodium dodecyl benzene sulfonate (SDBS), and then the obtained liquor is stirred, evaporated at a reduced pressure, centrifugalized, washed and vacuum dried, finally the simvastatin-contained delayed-release microsphere system is obtained. The surface of the microsphere is smooth and round, the granule thereof is regular without conglutination, and the granule diameter, the drug-loading rate (1-10 percent) and the encapsulation rate (above 40 percent) are all controllable, and the delayed-release time exceeds 2 months. The prepared simvastatin-contained delayed-release microsphere system can be processed into various preparations used in bony tissue absorption or bony defect parts, the microsphere system is degraded at a proper speed, thus the simvastatin can be further released; the degradation of the polymer can provide bony tissue with subsequent recuperating space to complete the repair of the bony defect parts.

Description

technical field [0001] The invention belongs to the field of biotechnology, and in particular relates to a method for encapsulating functional drugs into biodegradable polymer materials to form a nano-micron microsphere system by adopting an emulsification-drying method. Background technique [0002] Simvastatin is an inhibitor of hydroxymethylglutaryl-CoA reductase, and is currently a commonly used drug for clinically lowering cholesterol and preventing cardiovascular diseases. Mundy et al first reported that statins can induce the expression of bone morphological protein 2 (Bone morphological protein 2, BMP-2) gene in osteoblasts and bone marrow cells, indicating that statins can promote osteogenesis. [0003] In this research group, rats with extracted mandibular central incisors were used as an animal model to evaluate the resorption of the remaining alveolar ridge, and a simvastatin-loaded scaffold material with polylactic acid-glycolic acid as a carrier was prepared an...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/366A61K9/50A61K9/16A61K47/34A61L27/44A61L27/54A61L27/58A61L31/12A61L31/16A61P19/08A61P1/02A61P3/06
Inventor 孙宏晨李祥伟林权杨柏
Owner JILIN UNIV
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