Preparation of acidum citricum tamoxifen polylactic acid-glycolic co-polymer microballoons

A technology of moxifen polymerization and tamoxifen, which is applied in the field of preparation of tamoxifen citrate microspheres, can solve the problems of large gastrointestinal irritation and short drug release time, and achieve good sustained release effect, good Effects of biocompatibility and good biodegradability

Inactive Publication Date: 2012-03-21
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But so far, the dosage form of tamoxifen citrate is mainly tablet, which has the shortcomings of short drug release time and large gastrointestinal irritation, so it is of great significance to develop a new drug dosage form

Method used

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  • Preparation of acidum citricum tamoxifen polylactic acid-glycolic co-polymer microballoons
  • Preparation of acidum citricum tamoxifen polylactic acid-glycolic co-polymer microballoons
  • Preparation of acidum citricum tamoxifen polylactic acid-glycolic co-polymer microballoons

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Embodiment 1

[0025] (1) Preparation of tamoxifen citrate poly(lactic-co-glycolic acid) PLGA microspheres

[0026] Accurately weigh 100 mg of polylactic acid-glycolic acid copolymer PLGA (LA: GA = 50: 50, Mr = 20000), dissolve it in 2 ml of acetonitrile, then add 20 mg of tamoxifen citrate, and ultrasonically dissolve it as the organic phase; Prepare 60 ml of 1% PVA aqueous solution, and then add 0.45 g of NaCl as the water phase. Under stirring conditions (600rpm), slowly (1ml / min) add the organic phase to the water phase, continue to stir at room temperature for 24h, then centrifuge, wash with double distilled water for 3 times, freeze-dry to obtain he citrate Moxifen poly(lactic-co-glycolic acid) PLGA microspheres.

[0027] (2) Morphology and particle size of microspheres

[0028] Photographs of microspheres taken by optical microscope and scanning electron microscope ( figure 1 , figure 2 ), it can be seen that the obtained microspheres have a good circular shape. Measure the part...

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Abstract

The invention relates to a preparation method of tamoxifen citrate polylactic acid-glycolic acid copolymer microspheres. The method comprises the following steps: 1) dissolving polylactic acid-glycolic acid copolymer (PLGA) in an organic solvent, adding tamoxifen citrate, and dissolving under ultrasonic action to obtain a solution as organic phase; 2) adding slowly the organic phase into aqueous solution of polyvinyl alcohol (PVA) as water phase under stirring, adding electrolytes, stirring at room temperature until the organic solvent volatilizes completely, centrifugating, washing, and freeze-drying to obtain tamoxifen citrate polylactic acid-glycolic acid copolymer microspheres. The microsphere has round shape, uniform particle size distribution (below 10 micrometers), high drug content (above 10%), high encapsulation rate (about 80%), and in vitro release characteristics of long-acting preparations; and is suitable for the use as implant for prevention and treatment of breast cancer.

Description

technical field [0001] The invention belongs to the field of preparing pharmaceutical preparations for preventing and treating breast cancer, and in particular relates to a preparation method of tamoxifen citrate microspheres. Background technique [0002] In recent years, the incidence of breast cancer has increased dramatically. In Western countries, breast cancer has become the number one cause of death among women. In recent years, the incidence of breast cancer in my country has also been on the rise. According to the latest report from the health department, the incidence of breast cancer has become the No. It still ranks 9th among tumor diseases. In recent years, there are about 1.6 million to 1.8 million new cancer patients in my country every year, and the total number of cancer patients is about 4.5 million to 6 million. [0003] At present, the main means of breast cancer treatment include: surgery, radiotherapy, chemotherapy and endocrine therapy. Among them...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/138A61K47/34A61K9/00A61P35/00
Inventor 朱利民马宗会余灯广周毓婷
Owner DONGHUA UNIV
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