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GLP-1 analogue composition for microneedle devices

A technology of GLP-1 and analogs, which is applied in the field of GLP-1 analog compositions for microneedle devices, can solve the problems of increased burden on patients, and achieve the effects of suppressing liquid dripping, good release, and high viscosity

Inactive Publication Date: 2013-11-13
HISAMITSU PHARM CO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since this drug requires multiple doses of once / day to once / week, when administered by injection, the burden on the patient (pain) tends to increase

Method used

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  • GLP-1 analogue composition for microneedle devices
  • GLP-1 analogue composition for microneedle devices
  • GLP-1 analogue composition for microneedle devices

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～6

[0081] In a test tube, lixisenatide and a solvent were mixed at the content ratio shown in Table 1. The prepared mixed solution was stirred with a stirrer (1500 rpm, 12 hours, 25° C.), and the solubility of the polymer compound was visually observed and evaluated according to the following criteria. The evaluation results are shown in Table 1.

[0082] A: completely dissolved

[0083] B: partially dissolved

[0084] C: not dissolved

[0085] Based on the feeling when mixing, the viscosity of the prepared mixture was evaluated according to the criteria described later.

[0086] a: suitable for coating

[0087] b: not suitable for coating

[0088] [Table 1]

[0089]

[0090] Macrogol 200 and macrogol 400 in the table are polyethylene glycols with molecular weights of 200 and 400, respectively.

Embodiment 7

[0092] The solvent is water, and the polymer carrier is added, and mixed with the content ratio shown in Table 2. Compatibility and viscosity of the mixture were evaluated in the same manner as in Examples 1-6. The evaluation results are shown in Table 2.

[0093] [Table 2]

[0094]

[0095]

[0096] PEG400 and PEG4000 in the table are polyethylene glycol with a weight average molecular weight of 400 and 4,000 respectively, D×40 and D×70 are dextran with a weight average molecular weight of 40,000 and 70,000 respectively, and HPC─M is a weight average molecular weight of 110,000-150,000 hydroxypropyl cellulose, CMC (250,000) is sodium carboxymethyl cellulose with a weight average molecular weight of 250,000.

[0097] Examples 1-6 showed excellent solubility and viscosity. Example 7 also shows excellent solubility and viscosity. In Example 7, no viscosity-increasing effect was observed by adding the polymer carrier, but it is believed that the viscosity-increasing eff...

Embodiment 8～10

[0100] In a test tube, lixisenatide and a solvent (and a polymer carrier) were mixed at the mass ratio shown in Table 3 to obtain a GLP-1 analog composition. Example 8 is a water formula composition using water as a solvent, Example 9 is a PG formula composition using propylene glycol (PG) as a solvent, and Example 10 is a G formula composition using glycerin (G) as a solvent.

[0101] [table 3]

[0102]

[0103] The aforementioned GLP-1 analog composition was coated on the microneedles from the needle tip to a height of 100 μm to obtain a coated microneedle array.

[0104] In Example 9 of the PG formulation and Example 10 of the G formulation, in addition to the high viscosity of the solvent itself, plus the viscosity from lixisenatide, a GLP-1 analog combination with a good viscosity of about 10,000 cps can be prepared things. On the other hand, in Example 8, a GLP-1 analog composition with good viscosity was prepared by the effect of pullulan as a viscosity-imparting a...

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Abstract

A GLP-1 analogue composition for microneedle devices, which contains a GLP-1 analogue and at least one kind of solvent that is selected from the group consisting of water, glycerol, propylene glycol, ethylene glycol, 1,3-butylene glycol and polyethylene glycol.

Description

[0001] [Technical field to which the invention belongs] [0002] The present invention relates to GLP-1 analog compositions for microneedle devices. [Background technique] [0003] In recent years, incretin-related drugs have attracted attention as therapeutic drugs for type 2 diabetes, and various GLP-1 analog preparations have been actively developed and their use approved. The so-called GLP is a glucagon-like peptide (Glucagon-like peptide), originally an incretin hormone secreted by the human digestive tract mucosa. The analog preparation of GLP-1 (glucagon-like peptide-1) is a GLP-1 receptor agonist, which is secreted by the small intestine in the body, promotes the secretion of insulin by the pancreatic β cells at the end, and inhibits the pancreatic α Cells secrete glucagon, which acts as a hormone that inhibits food intake in the central nervous system. Through these actions, GLP-1 only promotes insulin secretion and effectively lowers blood sugar when it reaches the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61M37/00A61K38/26
CPCA61M2037/0046A61M2037/0061A61K47/10A61K47/02A61M37/00A61M2037/0023A61K38/26A61K9/0021A61P3/10
Inventor 梅本拓也松户俊之德本诚治
Owner HISAMITSU PHARM CO INC
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