Exenatide slow release sustained release microsphere, and preparation method and preparation thereof

A technology of exenatide and slow-release microspheres, which is applied in the field of medicine, can solve the problems of exenatide exenatide inactivation, toxicity and immunogenicity, and increase the risk of side effects, so as to achieve optimal drug release Curve, Reduced Aggregation, Enhanced Bioavailability Effect

Active Publication Date: 2013-12-04
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Exenatide microsphere preparations that are already on the market usually use poly(lactic-co-glycolic acid) as a carrier. Although poly(lactic-co-glycolic acid) has: good biocompatibility, it is easy to cause local acidification during the degradation process in vivo , causing the aggregation of exenatide, leading to the inactivation of exenatide, and in severe cases, toxicity and immunogenicity
Moreover, the sustained release performance of the existing exenatide microspheres is not good, and the release days usually range from several hours to several days
Frequent injections bring a lot of inconvenience to patients and increase the risk of side effects

Method used

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  • Exenatide slow release sustained release microsphere, and preparation method and preparation thereof
  • Exenatide slow release sustained release microsphere, and preparation method and preparation thereof
  • Exenatide slow release sustained release microsphere, and preparation method and preparation thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0048] Embodiment 1 Preparation of Exenatide Sustained-release Microspheres

[0049] Weigh 400mg of exenatide and 60mg of lysine and dissolve them in 4mL of water as the inner water phase; weigh 16g of poly(lactic-co-glycolic acid) copolymer (the ratio of lactide to glycolide is 50:50, 0.2dL / g ) was dissolved in 80 mL of dichloromethane, the inner water phase and the oil phase were vortex mixed for 30 s, and the colostrum was formed by ultrasonic emulsification with an ultrasonic cell disruptor (Branson S-250D) for 1 min under ice bath conditions. Add colostrum into 5000mL of 0.5% polyvinyl alcohol and 1.5% lysine aqueous solution under mechanical stirring to obtain double emulsion, keep stirring this double emulsion for more than 3 hours to volatilize and remove the organic solvent, discard the supernatant after centrifugation, The crude microspheres were obtained, and the exenatide sustained-release microspheres were obtained after washing and drying. After testing, the par...

Embodiment 2

[0050] Embodiment 2 Preparation of Exenatide Sustained-release Microspheres

[0051] Weigh 100 mg of exenatide and 100 mg of glycine, dissolve them in 0.2 mL of water as the inner water phase; weigh 9.9 g of poly(lactic-co-glycolic acid) copolymer (the ratio of lactide to glycolide is 25:75, 0.1dL / g) Dissolve in 19.8 mL of ethyl acetate, vortex mix the inner water phase and oil phase for 30 s, and ultrasonically emulsify for 1 min with an ultrasonic cell disruptor (Branson S-250D) in an ice bath to form colostrum. Add the colostrum into the aqueous solution of 20L of 0.5% polyvinyl alcohol and 10kg of arginine under mechanical stirring to obtain the double emulsion, keep stirring the double emulsion for more than 3 hours to volatilize and remove the organic solvent, discard the supernatant after centrifugation, that is Crude microspheres were obtained, and exenatide sustained-release microspheres were obtained after washing and drying. After testing, the particle size of the...

Embodiment 3

[0052] Embodiment 3 Preparation of Exenatide Sustained-release Microspheres

[0053] Weigh 500 mg of exenatide and 500 mg of histidine, dissolve them in 10 mL of water as the inner water phase; weigh 80 g of poly(lactic-co-glycolic acid) copolymer (the ratio of lactide to glycolide is 75:25, 0.5 dL / g) Dissolve in a mixture of 800mL ethyl acetate and dichloromethane (the volume ratio of ethyl acetate to dichloromethane is 1:1), vortex mix the inner water phase and oil phase for 30s, and use in ice bath Ultrasonic cell breaker (Branson S-250D) phacoemulsification for 1min to form colostrum. Add the colostrum into the aqueous solution of 8.1L 0.1% polyvinyl alcohol and 4.05g histidine under mechanical stirring to obtain the double emulsion, keep stirring the double emulsion for more than 3 hours to volatilize and remove the organic solvent, discard the supernatant after centrifugation, The crude microspheres were obtained, and the exenatide sustained-release microspheres were o...

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Abstract

The invention relates to the technical field of medicine and particularly relates to an exenatide slow release sustained release microsphere, and a preparation method and a preparation thereof. The exenatide slow release sustained release microsphere comprises the following components in parts by mass: 0.5-10 parts of exenatide, 0.5-10 parts of protecting agent and 80-99 parts of polylactic glycollic acid copolymer, wherein the protecting agent is one of or the combination of more than two of glycine, lysine, arginine or histidine. The exenatide slow release sustained release microsphere adopts the alkali protecting agent which can neutralize local acidation caused by degradation of the polylactic glycollic acid copolymer during release in vitro and degradation in vivo of the microsphere, so that aggregation of polypeptide is reduced and the stability of exenatide is maintained.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an exenatide sustained-release microsphere, a preparation method and a preparation thereof. Background technique [0002] Diabetes is currently becoming prevalent in the world. The World Health Organization estimates that the number of diabetic patients in 2011 was 346 million. The International Diabetes Federation estimates that the number of diabetics will reach 439 million in 2030. According to estimates by the International Diabetes Federation, by 2030 there will be more than 40 million diabetic patients in China, and the annual medical expenses will reach 28 billion US dollars. The Shanghai-based consultant of IMS Healthcare Consulting believes that China's diabetes drug market will expand at an annual rate of 20%, reaching 20 billion US dollars by 2016. On January 27, 2012, Bydureon, the exenatide sustained-release microsphere preparation of Amylin Corporation of the Unit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/26A61K9/10A61K9/16A61K47/34A61K47/18A61P3/10
Inventor 刘慧陶安进马亚平袁建成
Owner HYBIO PHARMA
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