Method for preparing long acting progestogen injection implant agent and use

A progestogen and preparation technology, applied in the field of long-acting progestogen injection implants, can solve problems such as damage and inconvenience to the human liver and kidney, and achieve the effects of facilitating treatment, reducing liver and kidney damage, and reducing the frequency of medication

Inactive Publication Date: 2005-01-12
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved in the present invention is to disclose a long-acting progesterone injection implant and its preparation method and application, so as to overcome the defects of frequent administration of existing dosage forms that bring a lot of inconvenience to patients and damage to human liver and kidney

Method used

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  • Method for preparing long acting progestogen injection implant agent and use

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Get 20mg gestrinone, 80mg polylactide-glycolide (lactide:glycolide=75:25, weight ratio), dissolve in 3ml dichloromethane, under vigorous stirring (1000rpm) Drop into 100ml of 0.2% sodium carboxymethylcellulose aqueous solution, continue to stir for 5-10 minutes after dripping, then reduce the stirring speed to 300rpm, evaporate at 25°C for about 12h, centrifuge, pour off the supernatant, and filter the precipitate under reduced pressure , washed with a small amount of distilled water, dried under reduced pressure at room temperature, and the diameter of the microspheres is 40-120 μm.

Embodiment 2

[0028] Take 20mg gestrinone and 80mgDL-polylactic acid, dissolve them in 1ml dichloromethane, add 5ml 0.5% PVA aqueous solution to a high-speed homogenizer, stir vigorously at 6000rpm for 2min, pour into 100ml 0.5% PVA aqueous solution, Evaporate at 300 rpm at 25°C for about 12 hours, centrifuge, pour off the supernatant, filter the precipitate under reduced pressure, rinse the precipitate with a small amount of distilled water, and dry under reduced pressure at room temperature. The diameter of the microspheres is 30-80 μm.

Embodiment 3

[0030] Take 20mg nomegestrol and 80mgDL-polylactic acid, dissolve in 1.25ml ethyl acetate, add 10ml 0.5% PVA aqueous solution to a high-speed homogenizer, stir vigorously at 8000rpm for 2min, and pour into 100ml 0.5% PVA aqueous solution , evaporated at 300rpm at 25°C for about 12h, centrifuged, poured off the supernatant, filtered the precipitate under reduced pressure, rinsed the precipitate with a small amount of distilled water, dried under reduced pressure at room temperature, and the diameter of the microspheres was 20-40 μm.

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Abstract

A slowly-releasing gestrinone injection for treating endometriosis by subcutaneous injecting or intramuscular injecting is prepared from biodegradable polymer PLGA or PLA as skeleton and gestrinon (R2323) as active component by solvent evaporation method.

Description

technical field [0001] The invention relates to a long-acting progesterone injection implant and its preparation method and application. Background technique [0002] Progestogens, such as gestrinone (Gestrinone, R2323, norethindrone, 18-methyltrienyl norethindrone) were originally moderate-strength progestogens with strong antiprogestogen and antiestrogenic activities. Experiments have proved that this product has anti-implantation and anti-early pregnancy effects, and it can also inhibit ovulation when taken orally in the early menstrual cycle. Its anti-implantation and anti-early pregnancy effects are related to changing the thickness of cervical mucus, interfering with the development of endometrium, affecting the running speed of eggs and antagonizing endometrial progesterone receptors. Clinically, it was originally used as a family-visiting contraceptive or an after-event contraceptive. [0003] In recent years, clinical studies at home and abroad have found that ora...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/56A61K31/565A61P15/00
Inventor 陈庆华潘峰包泳初曹霖朱焰
Owner SHANGHAI INST OF PHARMA IND
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