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Method for preparing long acting progestational hormone injection embedded agent and use

A progestogen and preparation technology, which is applied in the field of preparation of long-acting progestogen injection implants, can solve the problems of inconvenience to human liver and kidney, damage to patients, etc.

Inactive Publication Date: 2005-05-18
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 the preparation method and application of a long-acting progesterone injection implant, so as to overcome the inconvenience caused by the frequent administration of existing dosage forms to patients and the certain damage to human liver and kidney. defect

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Take 20mg gestrinone, 80mg polylactide-glycolide (lactide:glycolide=75:25), dissolve in 3ml dichloromethane, and drop it into 100ml under vigorous stirring (1000rpm) In 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, filter the precipitate under reduced pressure, and a small amount of distilled water Wash the precipitate, dry under reduced pressure at room temperature, and the diameter of the microspheres is 40-120 μm.

Embodiment 2

[0024] Take 20mg gestrinone and 80mg polylactic acid, dissolve them in 1ml dichloromethane, add 5ml 0.5% PVA aqueous solution to the high-speed homogenizer, stir vigorously at 6000rpm for 2min, pour into 100ml 0.5% PVA aqueous solution, and 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

[0026] Inhibition test of rat estrous cycle:

[0027] Method: The rats with regular estrous cycle were divided into two groups, and the following corresponding injections were given on the day when the pictures of the vaginal secretions of the rats showed anaphase (white blood cells):

[0028] Negative control group: subcutaneous (s.c.) injection of vehicle (n=5).

[0029] The microsphere group of Example 1: single dose s.c. injection of microspheres with a release rate of 0.5 mg / week / kg, a particle size of 40-120 μm, and a gestrinone content of 25% in the microspheres (n=5).

[0030] After injection, regularly observe and record vaginal cell smears every day. Rat vaginal smears continue to show white blood cells, indicating that the estrous cycle is inhibited. If keratinocytes appear, it indicates that the estrous cycle begins to recover. The vaginal smear method can be used to judge the drug effect of the preparation. time.

[0031] Results: After s.c. injection of a singl...

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Abstract

The present invention introduces the preparation process of injection microballoon with PLGA, PLA or other biodegradable polymer as skeleton material and the progestational hormone, gestrinone, as model medicine, and through solvent evaporation. The microballoon may be injected to subcutaneous part or muscle for delayed releasing for over 15 days. The microballoon skeleton material inside body degrades gradually into small molecular matter excreted to outside the body. The gestrinone microballoon injection may be administrated conveniently and is superior to conventional tablet form, which is orally taken frequently to result in damage to liver and kidney and other negative reaction. Rat experiment shows that the preparation of the present invention may be used in treating endometriosis, etc.

Description

Technical field: [0001] The invention relates to a preparation method and application of a long-acting progesterone injection implant. 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 oral...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/565A61K47/34A61P15/00
Inventor 陈庆华潘峰包泳初曹霖朱焰
Owner SHANGHAI INST OF PHARMA IND
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