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Process for preparing graft copolymer excipients with excellent peptide and protein binding properties

A technology of graft copolymers and copolymers, applied in the field of preparation of graft copolymer excipients with excellent peptide and protein binding properties

Active Publication Date: 2020-12-01
PHARMAIN CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Example 2 has a saturation of 55%, but was produced using NHS rather than NHSS as in this disclosure, so it is a different process and the product may have a different distribution of PEG along the polylysine backbone

Method used

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  • Process for preparing graft copolymer excipients with excellent peptide and protein binding properties
  • Process for preparing graft copolymer excipients with excellent peptide and protein binding properties
  • Process for preparing graft copolymer excipients with excellent peptide and protein binding properties

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0171] Example 1 (Samples 1-A, 1-B and 1-C)

[0172] The graft copolymers 1-A, 1-B and 1-C were synthesized by PEGylation using MPEG-CM (5 kDa MPEG-CM; 20 kDa PL; the amino groups were 59, 53 and 54% saturated with PEG, and the remaining The primary amino groups were modified with stearic acid). Syntheses were performed as described in the Overview section unless otherwise indicated. Activation of Sol B was allowed to proceed for 20 minutes. After 2 and 3 hours, additional EDC was added to Sol C (total EDC for each batch is reported in the ratio table). The table below provides the properties of the products and the ratios of each reagent used in the synthesis.

[0173] Table 13: Properties of the synthesized materials

[0174]

[0175] *The corresponding method failed to provide a product with the desired properties.

[0176] At 10% peptide loading, the moderate incorporation of the as-synthesized graft copolymers was not within the acceptable range of 13% or less fre...

Embodiment 2

[0185] Example 2 (Samples 2-A, 2-B and 2-C)

[0186] The graft copolymers 2-A, 2-B and 2-C were synthesized by PEGylation using MPEG-CM (5 kDa MPEG-CM; 20 kDa PL; the primary amino groups were 45, 44 and 44% saturated with PEG, the remaining The primary amino groups are modified with stearic acid). Syntheses were performed as described in the Overview section unless otherwise indicated. Activation of Sol B was allowed to proceed for 20 minutes. After 2 and 3 hours, additional EDC was added to SolC (total EDC for each batch is reported in the ratio table).

[0187] Table 17: Properties of the synthesized materials

[0188]

[0189] *The corresponding method failed to provide a product with the desired properties.

[0190] At 10% peptide loading, the moderate incorporation of the as-synthesized graft copolymers was not within the acceptable range of 13% or less free ANP. Thus, the ratios of reagents used by this method provided inferior products to those produced by the me...

Embodiment 3

[0199] Example 3 (Samples 3-A, 3-B and 3-C)

[0200] The graft copolymers 3-A, 3-B and 3-C were synthesized by PEGylation using MPEG-CM (5 kDa MPEG-CM; 20 kDa PL; the primary amino groups were 54, 60 and 56% saturated with PEG, the remaining The primary amino groups are modified with stearic acid). Syntheses were performed as described in the Overview section unless otherwise indicated. Activation of Sol B was allowed to proceed for 20 minutes. After 2 and 3 hours, additional EDC was added to SolC (total EDC for each batch is reported in the ratio table).

[0201] Table 21: Properties of the synthesized materials

[0202]

[0203] *The corresponding method failed to provide a product with the desired properties.

[0204] At 10% peptide loading, the moderate incorporation of the as-synthesized graft copolymers was not within the acceptable range of 13% or less free ANP. Thus, the ratios of reagents used by this method provided inferior products to those produced by the ...

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Abstract

This article presents a method for the preparation of semirandom graft copolymers whose products are difficult to fully characterize chemically. The products of the present disclosure have the following unique and useful properties: 1) bind to the peptide; and 2) when the product is co-administered to an animal with the peptide, the product will Increases blood circulation time and increases peptide levels.

Description

Background technique [0001] The development of new pharmaceutical agents for physiologically active peptides and proteins has focused on maintaining biological activity, but even these are limited by the inherently short half-lives or instability of peptides and proteins in vivo. This is especially true for small peptides and proteins with hydrodynamic diameters of less than about 5 nm. It has long been desired to alleviate this short half-life or instability of peptides and proteins in the body by using infusion devices that continuously deliver rapidly degrading peptide or protein drugs or by providing erosive depots of drugs under the skin. The development of excipients that prolong the half-life and / or provide stability of peptides and proteins in vivo and in blood is a new area of ​​research. [0002] Liposomes entraining unstable or short half-life drugs rely on degradation of the liposome structure before the drug can be released. Poly(lactic-co-glycolic acid) particl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08L77/00
CPCC08G73/02C08G81/025C08G69/10C08G69/48C08G81/00A61P13/12A61P5/48A61P9/04A61P9/12A61K47/59A61K47/34C08G73/0206
Inventor C·C·约内斯J·F·阿尔法罗G·M·卡斯蒂洛
Owner PHARMAIN CORP