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Intelligent responsive sustained-release microsphere and preparation method thereof

An intelligent, microsphere technology, applied in the field of novel microspheres formed by ketal or its derivative-PLGA and its preparation, intelligent responsive slow-release microspheres and its preparation fields, can solve problems such as hypoglycemia, Achieve the effect of improving the encapsulation rate and overcoming hypoglycemia

Inactive Publication Date: 2020-07-17
YANTAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The invention provides an intelligent response slow-controlled release microsphere, which mainly solves the problem of hypoglycemia caused by the sudden release effect of ordinary microspheres and the continuous release of drugs under normal blood sugar concentration by ordinary sugar-sensitive ordinary microspheres.

Method used

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  • Intelligent responsive sustained-release microsphere and preparation method thereof
  • Intelligent responsive sustained-release microsphere and preparation method thereof
  • Intelligent responsive sustained-release microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1 Intelligent responsive slow-release microspheres loaded with insulin

[0047] (1) Prepare two separate oil phases, which are oil phase A: Accurately weigh 20 mg of insulin and dissolve it in 0.1 ml of dimethyl sulfoxide (DMSO), and add the above solution dropwise to 0.9ml of dichloromethane containing 150mg of polyketal (weight average molecular weight 4250); oil phase B: 10mg of glucose oxidase, 10mg of catalase and 300mg of PLGA were dissolved in 2ml of ethyl acetate ;

[0048] (2) Quickly drop the oil phase A into the B phase under the high-speed shear condition of 2000rpm to form the S / O / O phase; quickly drop the S / O / O phase to 200ml mass under the high-speed shear condition of 4000rpm In the PVA aqueous solution with a concentration of 1%, the S / O / O / W phase is formed;

[0049] (3) Stir the emulsion obtained above at 1000 rpm for 1 hour, then stir at 500 rpm for 2 hours, centrifuge the solidified microspheres, wash with deionized water, and freeze-dry to...

Embodiment 2

[0051] Example 2 Intelligent Responsive Slow and Controlled Release Microspheres Loaded with Exenatide

[0052] (1) Prepare two separate oil phases, which are oil phase A: accurately weighed 20 mg of exenatide dissolved in 1 ml of dichloromethane containing 200 mg of polyketal (weight average molecular weight 7250); oil phase B: the Accurately weighed 15mg of glucose oxidase, 15mg of catalase and 200mg of PLGA were dissolved in 1ml of acetone;

[0053] (2) Quickly drop the oil phase A into the B phase under the condition of 3000rpm high-speed shear to form the O / O phase; quickly drop the O / O phase into 200ml of 1% mass concentration under the condition of high-speed shear of 5000rpm In PVA aqueous solution, O / O / W phase is formed;

[0054] (3) Stir the emulsion obtained above at 1200rpm for 1h, then stir rapidly at 600rpm for 2h, centrifuge the solidified microspheres, wash with deionized water, and freeze-dry to obtain the product.

[0055] After testing, the particle size o...

Embodiment 3

[0056] Example 3 Intelligent response slow and controlled release microspheres loaded with glibenclamide

[0057] (1) Prepare two separate oil phases, which are oil phase A: precisely weighed glibenclamide 30mg dissolved in 1.5ml dichloromethane containing 300mg polyketal (weight average molecular weight 6500); oil phase B: mix Accurately weighed 20mg of glucose oxidase, 20mg of catalase and 300mg of PLGA were dissolved in 1.5ml of tetrahydrofuran;

[0058] (2) Quickly drop the oil phase A into the B phase under the condition of 4000rpm high-speed shear to form the O / O phase; quickly drop the O / O phase into 300ml of 1% mass concentration under the condition of high-speed shear of 6000rpm In PVA aqueous solution, O / O / W phase is formed;

[0059] (3) Stir the emulsion obtained above at 1500rpm for 1h, then stir rapidly at 700rpm for 2h, centrifuge the solidified microspheres, wash with deionized water, and freeze-dry to obtain the product.

[0060] After testing, the particle s...

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Abstract

The invention relates to an intelligent responsive sustained-release microsphere and a preparation method thereof. A novel microsphere preparation is characterized in that the microsphere contains a microsphere with small particle size, the outer microsphere takes polylactic acid-glycolic acid copolymer (PLGA) as a carrier material, the microsphere with small particle size takes polyketal or derivatives thereof as a skeleton, a model medicine is embedded in the skeleton, and a glucose oxidase trigger and a catalase trigger are dispersed on the outer part of the microsphere with small particlesize. According to the preparation method, an intelligent responsive novel microsphere is prepared, the serious situation of sudden release of an ordinary microsphere preparation for treating diabetesis solved, especially hypoglycemia caused by continuous medicine release under normal blood glucose concentration, and important clinical application value is achieved.

Description

technical field [0001] The invention relates to an intelligent response type slow-controlled release microsphere and a preparation method thereof, based on the acid-sensitive characteristics of polyketal or its derivative materials and the diffusion or erosion mechanism of polymer materials to regulate drug release, specifically relates to a ketal or The novel microsphere formed by its derivative-PLGA and its preparation method belong to the technical field of medicine production. Background technique [0002] Diabetes is a major health problem facing humans in modern life. The prevalence of diabetes is increasing year by year in both developed and developing countries. According to the 2017 Global Diabetes Map Report released by the International Diabetes Federation (IDF), the global About 425 million adults have diabetes. Among them, the situation in my country is particularly severe, with more than 114 million people suffering from diabetes, and one in every ten people h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/34A61K47/32A61K47/42A61K38/28A61K38/22A61K31/64A61P3/10
CPCA61K9/5031A61K9/5052A61K9/5089A61K31/64A61K38/22A61K38/28A61K47/32A61P3/10
Inventor 慕宏杰张婕张艳文郑霞邵永珠王雪邢佳丽徐婷黄莉洁孔玉彤崔千艺
Owner YANTAI UNIV
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