Liraglutide long-acting microsphere injection and preparation method thereof

A technology of liraglutide and injection, which is applied in the field of liraglutide long-acting microsphere injection and its preparation, can solve the problems of long half-life, no industrial production, and inability to guarantee rapid release of drugs, etc., to reduce treatment costs , Improve medication compliance and reduce treatment burden

Active Publication Date: 2011-06-08
蚌埠丰原涂山制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Chinese patent CN1562356 discloses a biodegradable polymer microsphere loaded with insulin, which can be used clinically for oral or mucosal administration, and there is no report of industrial production
[0021] In view of the advantage of liraglutide's long half-life, if it is prepared as a long-acting preparation, it cannot guarantee that the drug can be released quickly and maintain a certain concentration during the drug effect period, which is why there are few long-acting microsphere injections on the market at home and abroad. one of the reasons

Method used

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  • Liraglutide long-acting microsphere injection and preparation method thereof
  • Liraglutide long-acting microsphere injection and preparation method thereof
  • Liraglutide long-acting microsphere injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0074] 1. Weigh 400mg of liraglutide, add it to 80ml of water for injection, and heat it on a water bath at 45°C to completely dissolve the drug as the inner water phase;

[0075] 2. Weigh 4 g of PLGA (75 / 25, molecular weight: 10,000 Daltons), add 100 ml of acetone to completely dissolve PLGA (75 / 25), and use it as the organic phase;

[0076] 3. Add the organic phase of step 2 to the inner water phase of step 1, mix the inner water phase and the organic phase evenly, heat on a water bath at 40°C, ultrasonically emulsify, cool to 13°C, and obtain colostrum;

[0077] 4. According to the volume ratio of colostrum and polyvinyl alcohol solution is 1:10, add colostrum to 2% polyvinyl alcohol solution (containing the mass volume ratio of polyvinyl alcohol and normal saline 2g / 100ml, the same below), stir at high speed (6000r / min) for 2 minutes to obtain double emulsion;

[0078] 5. According to the volume ratio of double emulsion and normal saline as 1:50, put the double emulsion ...

Embodiment 2

[0083] 1. Weigh 600mg of liraglutide, add it to 120ml water for injection, and heat it on a water bath at 45°C to completely dissolve the drug as the inner water phase;

[0084] 2. Weigh 6 g of PLGA (75 / 25, molecular weight: 50,000 Daltons), add 130 ml of ethyl acetate to completely dissolve PLGA (75 / 25), and use it as the organic phase;

[0085] 3. Add the organic phase of step 2 to the inner water phase of step 1, mix the inner water phase and the organic phase evenly, heat on a water bath at 48°C, ultrasonically emulsify, cool to 12°C, and obtain colostrum;

[0086] 4. According to the volume ratio of colostrum and polyvinyl alcohol solution is 1:15, add colostrum into 1.5% polyvinyl alcohol solution that has been cooled to 12°C, stir at high speed (5500r / min) for 2 minutes to obtain double emulsion ;

[0087] 5. According to the volume ratio of double emulsion and normal saline is 1:100, put double emulsion into normal saline, heat in water bath at 30°C, stir at low speed...

Embodiment 3

[0092] 1. Weigh 500mg of liraglutide, add 100ml of water for injection, heat on a water bath at 45°C to completely dissolve the drug, and use it as the inner water phase;

[0093] 2. Weigh 5 g of PLGA (75 / 25, molecular weight: 50,000 Daltons), add 110 ml of dichloromethane to completely dissolve PLGA (75 / 25), and use it as the organic phase;

[0094] 3. Add the organic phase of step 2 to the inner water phase of step 1, mix the inner water phase and the organic phase evenly, heat on a water bath at 45°C, ultrasonically emulsify, cool to 14°C, and obtain colostrum;

[0095] 4. According to the volume ratio of colostrum and polyvinyl alcohol solution is 1:10, add colostrum into 2.5% polyvinyl alcohol solution that has been cooled to 14°C, stir at high speed (6500r / min) for 2 minutes to obtain double emulsion ;

[0096] 5. According to the volume ratio of double emulsion and normal saline is 1:50, put double emulsion into normal saline, heat in water bath at 30°C, stir at low sp...

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Abstract

The invention provides a long-acting microsphere injection as an antidiabetic medicament, the long-acting microsphere injection comprises liraglutide, PLGA (poly(lactic-co-glycolic acid)), excipients and a surfactant, and the invention simultaneously relates to a preparation method of the injection. Liraglutide long-acting sustained-release microspheres provided by the invention are designed to perform subcutaneous injection once every 28 days, thereby greatly reducing treatment burden on a patient, improving medication compliance and reducing treatment cost; simultaneously, results of in vitro release studies, animal experiments and the like prove that the obtained sustained-release microspheres can slowly release a medicament for a long time in vitro and in vivo.

Description

technical field [0001] The invention relates to a long-acting preparation of a hypoglycemic drug, in particular to a liraglutide long-acting microsphere injection and a preparation method thereof. Background technique [0002] Diabetes (Diabetes Mellitus, DM) is a global high incidence. According to the latest data released by the World Health Organization, the number of diabetic patients in the world has reached 180 million in 2007, and the incidence rate is still increasing year by year. It is predicted that by 2025, the global diabetes The number of patients will reach 300 million. [0003] With the rapid development of my country's economy, the incidence of diabetes in my country has increased year by year, especially in recent years, the annual incidence has increased by more than 10%. According to epidemiological statistics, there are currently nearly 50 million diabetic patients in my country. Because diabetes involves system, and even induce many fatal complications,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/26A61K47/34A61K9/19A61P3/10
Inventor 李士桥汪洪湖
Owner 蚌埠丰原涂山制药有限公司
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