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Subcutaneous implant of mifespristone and use thereof in treatment of endometriosis

A technology of mifepristone and pore preparations, applied in the field of preparation of drugs for treating endometriosis, mifepristone subcutaneous implants, and can solve the problems that there are no reports of mifepristone subcutaneous implants , to achieve the effect of alleviating the pain of patients and controlling the condition of patients

Inactive Publication Date: 2006-11-22
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Currently, there is no report on mifepristone subcutaneous implants

Method used

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  • Subcutaneous implant of mifespristone and use thereof in treatment of endometriosis
  • Subcutaneous implant of mifespristone and use thereof in treatment of endometriosis
  • Subcutaneous implant of mifespristone and use thereof in treatment of endometriosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1: Preparation of Mifepristone Subcutaneous Implant with Polycaprolactone Capsule

[0031] Mifepristone was provided by Shanghai Hualian Pharmaceutical Co., Ltd. The preparation method and literature of polycaprolactone capsule [9] The method for preparing levonorgestrel long-acting sustained-release implant is the same. After Pluronic F68 is treated with acetic anhydride to treat the hydroxyl group of the blocked end group, it is mixed with caprolactone monomer (CL) at a weight ratio of 10:90, and 400 ppm of stannous octoate is added as a polymerization catalyst. 2 ) Polymerize at 140°C for 24 hours in a protected polymerizer. The polymerized product is melt-extruded and pelletized to obtain PCL / F68 raw material. A pipe with an outer diameter of 2.5mm and an inner diameter of 2.1mm is made by a plastic extruder. The tube was cut and the lengths of the prepared implants were 0.75cm, 1.5cm, and 3.0cm, respectively, and the corresponding mifepristone contents were 3.0...

Embodiment 2

[0032] Example 2: In vitro drug release test on mifepristone subcutaneous implant

[0033] Put the 3cm-long mifepristone subcutaneous implant prepared in Example 1 into 100ml of distilled water, keep the stirring speed of 130 rpm in a constant temperature shaker at 37±2℃, and replace it at regular intervals. Release fluid. The concentration of mifepristone in the released solution was determined by HPLC on the 15, 30, 45, 60, 90, 120 and 180 days. The chromatographic determination conditions were in accordance with the literature. [12] According to the measurement results, the average daily drug release rate can be calculated [9] .

[0034] Such as figure 1 As shown, the mifepristone subcutaneous implant releases the drug at a faster rate in the first 15 days in vitro, and then the release rate gradually decreases. At 30 days, the drug release can basically maintain a constant release rate and can be maintained for 6 months. As mentioned above, since the drug release rate of the ...

Embodiment 3

[0035] Example 3: Test of blood concentration in rats after implantation of mifepristone subcutaneous implants in rats

[0036] Wister female normal rats weighing 170-190g were randomly divided into experimental group and control group. The experimental group is divided into four groups, namely groups I-IV, each group of 8-10 rats, respectively, in the back of group I-group IV rats were implanted 1 0.75cm (group I) and 1 1.5cm (group I) subcutaneously on the back of the rats. Group II), 1 3.0cm (Group III) and 2 3.0cm (6.0cm total) (Group IV) implants. At 2, 4, 7, 10, 14, 30, 45, 60, 98, 120, 150, and 180 days after implantation, 2ml of blood was taken from the rat’s orbit, centrifuged to separate the serum, and stored at -40°C for later measuring. According to the literature [12] The method described in to measure the concentration of mifepristone in the blood. The control group consisted of 6 normal rats, and two 3.0cm non-medicated implants were implanted into them respectively...

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Abstract

The present invention provides one kind of subdermal embedded mifepristone preparation containing mifepristone in effective treating amount and mifepristone holding sac. The sac has pharmaceutically acceptable polymer as basic material and dispersed pore creating agent, and the polymer may be polylactic acid, polylactide, polylactic acid-hydroxyacetic acid, polycaprolactone, etc. and is preferably polycaprolactone. The present invention also provides the use of the subdermal embedded mifepristone preparation in preparing medicine for treating endometriosis.

Description

Technical field [0001] The present invention relates to a subcutaneous implant of mifepristone. More specifically, the present invention relates to a subcutaneous implant obtained by filling mifepristone into a capsular tube containing a porogen with a polymer material as a base material . The invention also relates to the use of the subcutaneous implant in the preparation of a medicine for treating endometriosis. Background technique [0002] When the endometrium is not in its normal part but appears in any other part of the body, it is called endometriosis (MET). Endometriosis is an aggressive gynecological common disease that can invade the peritoneum surrounding the pelvic cavity, the ligaments that suspend the uterus, the neighbors of the uterus-the bladder, rectum, and the greater omentum, appendix, small intestine and abdominal wall Incision, as far as the liver, gallbladder, kidney, lung, thoracic cavity, limb muscles and bones and other organs, and even ectopic lesions i...

Claims

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Application Information

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IPC IPC(8): A61K31/565A61K9/00A61P15/00
Inventor 孙洪范宋存先于祖茹
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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