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Composition of micro-array drug delivery system of glucagon-like peptide-1 receptor stimulating agent

A technology of glucagon and receptor agonist, applied in the field of microarray drug delivery system, can solve the problem of inability to deliver GLP-1 receptor agonist, and achieve the effect of process stability

Pending Publication Date: 2021-05-04
南京百劲企业管理咨询有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to address the deficiencies in the existing GLP-1 receptor agonist drug delivery system and utilize the advantages of the microarray drug delivery system to solve the problem that the existing microarray preparation materials cannot deliver GLP-1 receptor agonists

Method used

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  • Composition of micro-array drug delivery system of glucagon-like peptide-1 receptor stimulating agent
  • Composition of micro-array drug delivery system of glucagon-like peptide-1 receptor stimulating agent
  • Composition of micro-array drug delivery system of glucagon-like peptide-1 receptor stimulating agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: Safety and irritation evaluation of microarray membrane

[0029] Using thermoplastic polyurethane, ethylene-vinyl acetate copolymer, polyvinylpyrrolidone-vinyl acetate copolymer, polylactic acid glycolic acid, hypromellose acetate succinate, and polyoxyethylene microfabricated arrays to evaluate safety and irritation , silicon wafer, PDMS material as the control group.

[0030] The details are as follows: 80 ICR mice were randomly divided into 8 groups, 10 in each group. The abdomen and back hair were manually shaved to expose the epidermis. Take a thermoplastic polyurethane microarray, b ethylene-vinyl acetate copolymer microarray, c polyvinylpyrrolidone-ethylene acetic acid copolymer microarray, d polylactic acid glycolic acid microarray, e hypromellose acetate succinate microarray , f polyoxyethylene microarray, g silicon chip microarray, h PDMS microarray, press the exposed epidermis for 5 minutes, let the above microarray act on the skin, observe the w...

Embodiment 2

[0037] Embodiment 2: Research on the glass transition temperature and melting point of the composition

[0038] The microarray membranes of 5 different materials provided by the present invention were taken to form compositions with semaglutide, exenatide, liraglutide, and dulaglutide respectively, and the glass transition temperature and melting point of the compositions were studied. Compared with the glass transition temperature and melting point of the existing published microarray membranes, as well as the degradation research of the prepared samples, it is shown that the existing disclosed technology cannot achieve semaglutide, exenatide, liraglutide , Epidermal drug delivery of dulaglutide.

[0039] as shown in the table below

[0040]

[0041] Note: A thermoplastic polyurethane 41D, B ethylene-vinyl acetate copolymer 150, C polyvinylpyrrolidone-ethylene acetate copolymer, D polyoxyethylene, E hypromellose acetate succinate, F glass, G PDMS.

[0042] The results sh...

Embodiment 3

[0043] Example 3: Test proof of mechanical strength and epidermis penetration ability

[0044] Furthermore, the epidermis drug delivery ability of the composition provided by the invention was studied, and compared with the existing microarray technology products.

[0045] The mechanical properties of polyvinylpyrrolidone-ethylene acetic acid copolymer-liraglutide microarray composition and glass-liraglutide microarray composition were analyzed by Agilent Nano Indenter G200. Test the load-displacement curve diagram of a loading-unloading cycle process of synapses of different sizes, and summarize the maximum load of the pressurized section in the curve, the deformation of the synapse and whether it is broken or not, and tabulate it as follows:

[0046]

[0047] Note: A polyvinylpyrrolidone-ethylene acetic acid copolymer-liraglutide microarray composition, B glass-liraglutide microarray composition.

[0048] According to the common knowledge of the prior art, drug delivery ...

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Abstract

The invention relates to a composition of a micro-array drug delivery system of a glucagon-like peptide-1 receptor stimulating agent and belongs to the technical field of pharmacy. The composition disclosed by the invention at least comprises two parts, i.e., a part A and a part B, wherein the A is a micro-array film, and the B is the glucagon-like peptide-1 receptor stimulating agent. The composition has the advantages that preparation materials, morphologies and use performance of the existing micro-array systems are broken through by researching interaction between the system and drugs based on morphologies of the existing micro-arrays, and thus, the composition is more applicable to drug delivery. The final-provided composition of the micro-array drug delivery system for delivering the GLP-1 receptor stimulating agent is stable in process, high in drug load amount and uniform in drug distribution, and the problem of the existing micro-array preparation materials that the GLP-1 receptor stimulating agent cannot be delivered is solved.

Description

technical field [0001] The invention relates to a microarray drug delivery system for a glucagon-like peptide-1 receptor agonist, belonging to the technical field of pharmacy. Background technique [0002] GLP-1 receptor agonist (GLP-1 receptor agonist, GLP-1RA) can play a hypoglycemic effect by activating the GLP-1 receptor. At present, 8 GLP-1 receptor agonist hypoglycemic drugs have been approved for marketing in the world. The main products are: exenatide, liraglutide, lixisenatide, dulaglutide, albiglutide, Semaglutide, benaglutide, polyethylene glycol loxenatide, among which: 6 products have been launched in the domestic market, and imported products include exenatide, liraglutide, lixisenatide, and dulaglutide Peptides; domestically produced benaglutide and polyethylene glycol loxenatide. Whether the preparations of the above-mentioned GLP-1 receptor agonist drugs are long-acting preparations or short-acting preparations, the dosage forms are all injections, and the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/26A61K9/70A61K47/34A61K47/10A61K47/38A61K47/32A61P3/10A61P3/04
CPCA61K9/0021A61K9/7007A61K38/26A61K47/10A61K47/32A61K47/34A61K47/38A61P3/04A61P3/10
Inventor 靳翔
Owner 南京百劲企业管理咨询有限公司
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