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Temperature sensitive injectable drug-loading controlled release system

A technology of controlled release and sensitivity, applied in the field of injectable vaginal drug-loaded controlled-release system and temperature-sensitive injectable drug-loaded controlled-release system, it can solve the problems of controlled release that have not been reported in literature, and achieve high drug coating. Quantity, low viscosity, effect of high copolymer concentration

Inactive Publication Date: 2012-10-31
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are few reports in the field of controlled release of contraceptive drugs, especially the controlled release of three compound contraceptive anti-inflammatory drugs of estrogen, progesterone and indomethacin has not been reported in the literature

Method used

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  • Temperature sensitive injectable drug-loading controlled release system
  • Temperature sensitive injectable drug-loading controlled release system
  • Temperature sensitive injectable drug-loading controlled release system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Star-shaped polyethylene lactide (PLGA)-polyethylene glycol monomethyl ether (mPEG) block copolymer, the molar ratio of lactide in the polyglycolide (PLGA) block is 90%, glycolide The molar ratio is 10%, and it is completely dissolved in simulated vaginal fluid at 2-4°C to prepare a star-shaped copolymer solution with a concentration of 30wt%. 2.0 mg ethinyl estradiol, 4.80 mg gestodene and 12 mg indomethacin were dissolved in 1 ml of the star-shaped copolymer solution with a concentration of 30 wt % to prepare a vaginal drug-loaded controlled release system.

[0038] The sol-gel transition behavior of vaginal drug-loaded controlled release system was observed at elevated temperature and the viscosity change was studied by static rheometer. The state in which the vaginal drug-loaded controlled-release system could not flow when the glass bottle was inverted was defined as the gel state. figure 1 It is the rheological curve of the vaginal drug-loaded controlled release ...

Embodiment 2

[0040] Star-shaped polyethylene lactide (PLGA)-polyethylene glycol monomethyl ether (mPEG) block copolymer, the molar ratio of lactide in the polyglycolide (PLGA) block is 75%, glycolide The molar ratio is 25%, and it is completely dissolved in simulated vaginal fluid at 2-4°C to prepare a star-shaped copolymer solution with a concentration of 30wt%. 2.0 mg ethinyl estradiol, 4.80 mg gestodene and 12 mg indomethacin were dissolved in 1 ml of the star-shaped copolymer solution with a concentration of 30 wt % to prepare a vaginal drug-loaded controlled release system.

Embodiment 3

[0042] Star-shaped polyethylene lactide (PLGA)-polyethylene glycol monomethyl ether (mPEG) block copolymer, the molar ratio of lactide in the polyglycolide (PLGA) block is 50%, glycolide The molar ratio is 50%, and it is completely dissolved in simulated vaginal fluid at 2-4°C to prepare a star-shaped copolymer solution with a concentration of 30wt%. 2.0 mg ethinyl estradiol, 4.80 mg gestodene and 12 mg indomethacin were dissolved in 1 ml of the star-shaped copolymer solution with a concentration of 30 wt % to prepare a vaginal drug-loaded controlled release system.

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Abstract

The invention discloses a temperature sensitive injectable drug-loading controlled release system, which comprises a star-shaped poly-lactic-co-glycolic acid-methoxy polyethylene glycol segmented copolymer and a simulated body fluid, and the content of the copolymer accounts for 15-40 weight by percent. The drug-loading controlled release system exists in a state of liquid which can freely flow in or below room temperature, is rapidly changed into oyster white physical crosslinking hydrogel which cannot flow at a human body temperature, and expresses a reversible sol- gel conversion behavior; the drug-loading controlled release system can uniformly disperse a loaded drug, and exists in a state of liquid which can freely flow in or below room temperature and gel which cannot freely flow at the body temperature; as a vagina drug-loading controlled release system, the temperature sensitive injectable drug-loading controlled release system has the characteristics that contraceptive compound estrogen, progestogen and an anti-inflammation drug are loaded into a copolymer hydrogel carrier by adopting a solution blending method, and the prepared drug-loading system serves as a birth control spraying agent; the drug-loading system is sprayed into vagina after women menses, and is shaped into mesh gel and attached into a wall, and the drug is slowly and controllably released and have an effect of birth control.

Description

technical field [0001] The invention belongs to the field of biodegradable polymer materials and drug controlled release, in particular to a temperature-sensitive injectable drug-loaded controlled release system, and the invention is especially suitable as an injectable vaginal drug-loaded controlled release system. Background technique [0002] With the improvement of living standards and the development of science and technology, people's demand for various short-term flexible birth control measures is increasing, and the research on vaginal flexible birth control measures is also more active. Vaginal gel, as a carrier of various drugs, has been a research hotspot in the past few decades. The scientific research achievements of various contraceptive drugs and vaginal bactericides coated by it have promoted the progress of female physiology and reproductive safety and biomedical materials. subject development. At present, the vaginal gels used for the coating and release o...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/34A61P15/18
Inventor 索进平邹鹏聂磊封水彬
Owner HUAZHONG UNIV OF SCI & TECH
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