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2-methoxy estradiol injectable hydrogel implant

A technology of methoxyestradiol and implants, which is applied in the field of medicine, can solve the problems of strong fat solubility, poor water solubility, and no improvement in the treatment effect, and achieve the effects of improving the treatment effect, easy production and scientific formula

Inactive Publication Date: 2011-01-26
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The drug has poor water solubility and strong fat solubility, and has a certain liver first-pass effect. It is widely distributed in the body, and it is difficult to maintain an effective blood drug concentration, so it is difficult to maintain an effective therapeutic concentration at the target site, and the curative effect of oral administration is not ideal.
No improvement in therapeutic effect even after doubling the dose

Method used

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  • 2-methoxy estradiol injectable hydrogel implant
  • 2-methoxy estradiol injectable hydrogel implant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0008] When the 2-methoxyestradiol injectable hydrogel implant of the present invention is specifically implemented, the percentage by weight is: temperature-sensitive PLGA-PEG-PLGA block copolymer 24.6%, ultrapure water 73.9%, 2-Methoxyestradiol 1.5% is made, wherein first temperature-sensitive PLGA-PEG-PLGA block copolymer and ultrapure water are mixed, put 2 days (48 hours, hereinafter the same at low temperature) in the refrigerator ), to fully swell the temperature-sensitive PLGA-PEG-PLGA block copolymer, add 2-methoxyestradiol and mix well before subcutaneous injection; or mix 0.75g temperature-sensitive PLGA-PEG-PLGA block copolymer The copolymer is mixed with 2.25g of ultrapure water, placed in the refrigerator at low temperature for 2 days, so that the temperature-sensitive PLGA-PEG-PLGA block copolymer is fully swollen, and 0.045g of 2-methoxyestradiol is added before subcutaneous injection Alcohol can be mixed;

[0009] The molecular weight of said temperature-sens...

Embodiment 2

[0011] When the present invention is implemented, it can also be made by weight percentage: temperature-sensitive PLGA-PEG-PLGA block copolymer 14.8%, ultrapure water 83.7%, 2-methoxyestradiol 1.5%, wherein first Mix the temperature-sensitive PLGA-PEG-PLGA block copolymer with ultrapure water, and place it in the refrigerator at low temperature for 2 days to fully swell the temperature-sensitive PLGA-PEG-PLGA block copolymer, 12 hours before use Add 2-methoxyestradiol and mix well before subcutaneous injection; or mix 0.45g of temperature-sensitive PLGA-PEG-PLGA block copolymer with 2.55g of ultrapure water, put it in the refrigerator at low temperature For 2 days, fully swell the temperature-sensitive PLGA-PEG-PLGA block copolymer, add 0.045g of 2-methoxyestradiol 12 hours before use, and mix well before subcutaneous injection;

[0012] The molecular weight of said temperature-sensitive PLGA-PEG-PLGA block copolymer is 4500, the molar ratio of lactic acid:glycolic acid is 6:1...

Embodiment 3

[0014] When the present invention is implemented, it can also be made by weight percentage: temperature-sensitive PLGA-PEG-PLGA block copolymer 24.3%, ultrapure water 72.8%, 2-methoxyestradiol 2.9%, wherein, First mix the temperature-sensitive PLGA-PEG-PLGA block copolymer with ultrapure water, and place it in the refrigerator at low temperature for 2 days to fully swell the temperature-sensitive PLGA-PEG-PLGA block copolymer. Before use, 6 Add 2-methoxyestradiol within 1 hour and mix well before subcutaneous injection; or mix 0.75g of temperature-sensitive PLGA-PEG-PLGA block copolymer with 2.25g of ultrapure water, and put it in the refrigerator at low temperature Leave it for 2 days to fully swell the temperature-sensitive PLGA-PEG-PLGA block copolymer, add 0.090g of 2-methoxyestradiol 6 hours before use, and mix well before subcutaneous injection;

[0015] The molecular weight of said temperature-sensitive PLGA-PEG-PLGA block copolymer is 5000, the molar ratio of lactic ac...

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Abstract

The invention relates to a 2-methoxy estradiol injectable hydrogel implant which can effectively solve the problems of maintaining the effective concentration of the target part of 2-methoxy estradiol and enhancing the treatment effect. The invention has the technical scheme that a temperature sensitive type PLGA-PEG-PLGA segmented copolymer having temperature sensitive hydrogel properties is adopted to be mixed with water to prepare dissolution swelling solution; the solution is mixed with the 2-methoxy estradiol to prepare an injection; the temperature sensitive type PLGA-PEG-PLGA segmented copolymer is uniformly mixed with the water to be kept stewing at 0 to 25 DEG C; the temperature sensitive type PLGA-PEG-PLGA segmented copolymer is fully dissolved and swelled into the solution; and the 2-methoxy estradiol is added to be uniformly mixed with solution at 0 to 25 DEG C on the use day or one day before use. The invention has scientific formula, easy production, low cost and good injection effect, can effectively maintain the effective concentration of the target part of the 2-methoxy estradiol and enhance the treatment effect is enhanced and is the innovation on the path of cancer treatment drug forms and drug administration.

Description

1. Technical field [0001] The invention relates to medicine, in particular to a 2-methoxyestradiol injectable hydrogel implant. 2. Background technology [0002] 2-Methoxyestradiol is an anticancer drug, which is mainly used to treat breast cancer, prostate cancer and other diseases through anti-angiogenesis and anti-tumor effects. The drug resistance is very good, and the side effects are very small , which is an unsatisfactory advantage of other anticancer drugs, and also the biggest advantage that this anticancer drug is worth developing. At the same time, it is an anti-inflammatory drug, which is used to treat arthritis and so on. In current foreign clinical trials, its dosage forms are oral tablets and capsules, which are taken once or twice a day, and the dosage is relatively large, 400mg-1200mg each time. The drug has poor water solubility and strong fat solubility, and has a certain liver first-pass effect. It is widely distributed in the body, and it is difficult ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/565A61K47/34A61P35/00
Inventor 张振中郭新红张正全张红岭胡海英邢亚兵梅芊
Owner ZHENGZHOU UNIV
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