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17beta-estradiol/PLGA sustained release microsphere and preparation method thereof

A technology of slow-release microspheres and estradiol, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of high price, short half-life, poor patient compliance, etc. To achieve the effect of reducing drug costs

Inactive Publication Date: 2014-04-30
CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the short half-life of the introduced factors, the systemic and local applications are quickly degraded, and the desired biological effects cannot be achieved.
Moreover, there are many drugs currently recognized for the treatment of osteoporosis, which are expensive, ordinary families cannot afford long-term use, and patients have poor compliance.

Method used

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  • 17beta-estradiol/PLGA sustained release microsphere and preparation method thereof
  • 17beta-estradiol/PLGA sustained release microsphere and preparation method thereof
  • 17beta-estradiol/PLGA sustained release microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Dissolve 100mg of PLGA in 5ml of dichloromethane, and disperse uniformly by ultrasonic at 4°C, then dissolve 10mg of 17β-estradiol in the above solution, and disperse evenly by ultrasonic at 4°C, add 10g / L% under stirring at a constant speed of 500rpm 40ml of polyvinyl alcohol solution was emulsified for 10 minutes to form an oil-water complex emulsion. Under the condition of ice bath (0-4 ℃), turn the evaporator up and down with medium-speed magnetic stirring overnight, volatilize and remove dichloromethane to obtain a suspension of microspheres, settle at room temperature, separate and collect, wash three times with twice distilled water, Freeze-dried at low temperature, sealed at room temperature and protected from light for future use.

[0049] In the examples and comparative examples of the present invention, in order to make the dichloromethane volatilize completely, it was stirred for 24-30 hours to make it volatilize completely, so as to maintain the shape of th...

Embodiment 2

[0051] Dissolve 150mg of PLGA in 5ml of dichloromethane, and disperse evenly by ultrasonic at 4°C, then dissolve 10mg of 17β-estradiol in the above solution, and disperse evenly by ultrasonic at 4°C, add 7.5g / L under constant stirring at 500rpm 40ml of polyvinyl alcohol solution was emulsified for 10 minutes to form an oil-water complex emulsion. Under the condition of ice bath (0-4 ℃), turn the evaporator up and down with medium-speed magnetic stirring overnight, volatilize and remove dichloromethane to obtain a suspension of microspheres, settle at room temperature, separate and collect, wash three times with twice distilled water, Freeze-dried at low temperature, sealed at room temperature and protected from light for future use.

Embodiment 3

[0053] Dissolve 150mg of PLGA in 7ml of dichloromethane, and disperse uniformly by ultrasonic at 4°C, then dissolve 15mg of 17β-estradiol in the above solution, and disperse evenly by ultrasonic at 4°C, add 10g / L poly Vinyl alcohol solution 40ml, emulsified for 10 minutes to form oil-water complex emulsion. Under the condition of ice bath (0-4 ℃), turn the evaporator up and down with medium-speed magnetic stirring overnight, volatilize and remove dichloromethane to obtain a suspension of microspheres, settle at room temperature, separate and collect, wash three times with twice distilled water, Freeze-dried at low temperature, sealed at room temperature and protected from light for future use.

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Abstract

The invention discloses a 17beta-estradiol / PLGA sustained release microsphere and a preparation method thereof. The preparation method is simple, the sustained release microsphere prepared by the method is pore-free, smooth and round in surface, uniform in sphere size, full in shape and uniform in microsphere distribution, obvious adhesion is avoided, earlier initial burst release or terminal stage rapid release can be well avoided, the 17beta-estradiol can be slowly released, and the drug loading capacity and encapsulation efficiency are high.

Description

technical field [0001] The invention relates to the technical field of biochemical pharmacy, in particular to 17β-estradiol / PLGA slow-release microspheres and a preparation method thereof. Background technique [0002] 17β-Estradiol (17β-Estradiolum, 17βE2) has the property of regulating cell proliferation and differentiation in bone formation and repair, and its application research is one of the most active topics in the field of bone tissue repair, regeneration and bone tissue engineering. The process of bone reconstruction and repair is exactly the process in which bone cells adhere, proliferate and differentiate on the scaffold material under the regulation of some factors, especially 17βE2, absorb the scaffold material, and rebuild the osteogenic tissue. In the process of bone repair, many related cytokines are expressed. These factors play an important role in bone reconstruction and repair, and it is particularly important to introduce these factors into bone materia...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K47/34A61K31/565A61P19/10
Inventor 王魁向梁芳
Owner CENT SOUTH UNIV
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