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Stable exenatide sustained-release microsphere preparation and preparation method thereof

A technology of slow-release microsphere preparation and exenatide, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, can solve the problems of poor patient compliance and achieve reasonable composition, The effect of good technical effects

Active Publication Date: 2011-09-28
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the half-life of exenatide is only 2.4 hours, in order to control blood sugar stably, subcutaneous injections need to be administered twice a day, and frequent injections make patients less compliant

Method used

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  • Stable exenatide sustained-release microsphere preparation and preparation method thereof
  • Stable exenatide sustained-release microsphere preparation and preparation method thereof
  • Stable exenatide sustained-release microsphere preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Weigh 800mg of exenatide and 300mg of gelatin and dissolve it in 1ml of water for injection as the inner water phase; weigh 6g of glycolide-lactide copolymer and dissolve it in 15ml of dichloromethane as the oil phase; add the oil phase to In the inner water phase, use high-speed stirring (23000rpm) for 15 seconds to obtain colostrum and store it in an environment below 20°C; add this colostrum to 6000 ml of 0.5% (W / V) polyethylene under stirring The alcohol solution was used to obtain double emulsion, and the double emulsion was continuously stirred for 3 hours to evaporate dichloromethane, centrifuged, washed and collected to obtain microspheres, the particle size of which was less than 100 microns. The drug loading capacity was 9.8%, and the encapsulation efficiency was 87.0%.

Embodiment 2

[0033]Weigh 200mg of exenatide, 300mg of carboxymethylcellulose sodium and 100mg of sucrose and dissolve in 1ml of water for injection as the inner aqueous phase; weigh 12.5g of glycolide-lactide copolymer and dissolve in 50ml of dichloromethane As the oil phase; add the oil phase to the inner water phase, and use high-speed stirring (23000rpm) for 15 seconds to obtain colostrum, which is stored in an environment below 20°C; add this colostrum to 6000 ml of 0.5 % (W / V) polyvinyl alcohol solution to obtain double emulsion. The double emulsion was continuously stirred for 3 hours to evaporate dichloromethane, centrifuged and washed to collect microspheres, and the particle size of the microspheres was less than 100 microns. The drug loading is 0.5%, and the encapsulation efficiency is 32.7%.

Embodiment 3

[0035] Weigh 500mg exenatide, 300mg gelatin and 100mg mannitol and dissolve in 2ml water for injection as the inner water phase; weigh 8g glycolide-lactide copolymer and dissolve it in 80ml of dichloromethane as the oil phase; The oil phase was added to the inner water phase, and the ultrasonic cell breaker (Branson S-250D) was used to perform ultrasonication for 30 seconds to obtain colostrum, which was stored in an environment below 20°C; the colostrum was added to 10,000 Milliliter of 1.0% (W / V) polyvinyl alcohol solution was used to obtain double emulsion, and the double emulsion was continuously stirred for 3 hours to evaporate methylene chloride, centrifuged and washed to collect microspheres, the particle size of which was less than 50 microns. The drug loading was 4.2%. The encapsulation rate is 74.7%

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Abstract

The invention provides a stable exenatide sustained-release microsphere preparation and a preparation method thereof. The preparation contains 0.1 to 12.5 mass percent of exenatide and 77.5 to 99 percent of glycolide and lactide copolymer. The preparation method comprises the following steps: (a) dissolves glycolide and lactide copolymer in an organic solvent to form an oil phase, wherein the organic solvent may be one or the combination of dichloromethane and ethyl acetate; (b) dissolving exenatide, a protective agent and a suspending aid in water to form an internal water phase; (c) mixing the internal water phase and the oil phase to form emulsion; and (d) after the organic solvent violates, obtaining exenatide-containing sustained-release microspheres. As the formula composition of the stable exenatide sustained-release microsphere preparation is reasonable, the stable exenatide sustained-release microsphere preparation is prepared by common sustained-release microsphere technique, and the sustained-release period of the sustained-release microspheres is as long as 7 to 35 days. The technical effect is better when the exenatide sustained-release microspheres are prepared by a multiple emulsion (water-oil-water) method.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations of sustained-release microspheres, in particular to exenatide sustained-release microsphere preparations and a preparation method thereof. Background technique [0002] Exenatide is a natural incretin mimetic secreted from the saliva of giant monster lizard in the southwestern United States, which can simulate the action of glucagon-like peptide-1 (GLP-1), so as to achieve The effect of controlling blood sugar is jointly developed by American Amylin and Lilly Pharmaceutical Company. Synthetic exenatide is the first incretin analog approved for marketing. Its new drug application was approved by the US FDA in April 2005. It is mainly used to improve the unsatisfactory treatment of metformin and sulfonylurea drugs. Glycemic control in type 2 diabetes. Exenatide is a polypeptide containing 39 amino acids, which is only 53% homologous to the amino acid sequence of mammalian GLP-1; mammalia...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K38/22A61K47/34A61K47/36A61K47/38A61K47/42A61P3/04A61P3/10
Inventor 陶安进马亚平袁建成
Owner HYBIO PHARMA
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