Novel polyorthoester medicinal auxiliary material and slow-release new preparation thereof

A technology for polyorthoesters and pharmaceutical excipients, which is applied in the directions of drug combinations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., which can solve moisture sensitivity, difficulty in preparation and storage, and polymer functions Problems such as difference

Active Publication Date: 2014-05-21
唐汝培
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The reaction conditions of these two methods are harsh. The transesterification method needs to react for a long time under high temperature and high pressure (US Patent 4079038; US Patent 4108646). The monomers required for the synthesis of the addition polymerization method are sensitive to light and moisture, and difficult to prepare and store. , the further functionalization of the polymer is poor (Chinese Patent 101052376A; Chinese Patent 1726043A; U.S. Patent 4304767; U.S. Patent 4957998). DETOSU (Chinese Patent 1726177A; US Patent 4513143; US Patent 4532335), this monomer is very sensitive to light and moisture, and requires harsh conditions for preparation, storage and use

Method used

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  • Novel polyorthoester medicinal auxiliary material and slow-release new preparation thereof
  • Novel polyorthoester medicinal auxiliary material and slow-release new preparation thereof
  • Novel polyorthoester medicinal auxiliary material and slow-release new preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Under a nitrogen atmosphere, weigh 0.979g of diamine monomer (4,4'-dimethylene oxide-bis-(2-aminoethoxy-1,3-dioxolane) in a 50mL two-necked reaction flask Add 5mL DMF to dissolve, then add 1.36mL triethylamine, then add 1.348g succinyl heavy amido dodecanoate, then add 5mL DMF to react for 1-5 days; after the reaction is completed, add the reaction solution dropwise to 100mL containing In the ethyl acetate of triethylamine, leave standstill 10min after dropping, filter, wash 3 times with ethyl acetate, vacuum-dry to obtain 1.04g white solid powder, namely polyorthoester-polyamide copolymer (POEd-1), The yield was 65%.

Embodiment 2

[0023] Preparation of New Drug Preparations for Sustained Release

[0024] 1) Preparation method of a pharmaceutical composition using bupivacaine as an active agent: after mechanically mixing a selected amount of polyorthoester-polyamide copolymer (POEAd) with bupivacaine, heating to Dissolving at 50-90° C., and then allowing the solution to cool naturally to room temperature to obtain a uniformly mixed solid pharmaceutical composition, wherein the weight content of the active agent is 5% to 30%.

[0025] 2) Preparation method of a pharmaceutical composition using bupivacaine as an active agent: after a selected amount of polyorthoester-polyamide copolymer (POEAd), bupivacaine and polyethylene glycol monomethyl ether are mechanically mixed, Heating to 50-90°C under nitrogen atmosphere and stirring to dissolve, then allowing the solution to cool naturally to room temperature to obtain a uniformly mixed solid pharmaceutical composition, wherein the active agent has a weight con...

Embodiment 3

[0031] Release Properties of Pharmaceutical Compositions

[0032]Weigh the pharmaceutical composition of Example 2 and place it in a bottle with a lid. Add 50ml of 50mMPBS (pH7.4) into each bottle, and culture in a 37°C incubator with shaking at 60rpm. At selected time points, approximately 2 ml of culture broth was withdrawn and analyzed for active agent content by HPLC. Remove the residual medium and add the same volume of fresh buffer. Drug release rate for pharmaceutical compositions with the same active agent content and copolymer: group 3>group 2>group 1; group 6>group 5>group 4; for pharmaceutical composition 1 with the same active agent content, drug release Rate: POEAd-1>POEAd-2>POEAd-3.

[0033] The experimental results confirm that the pharmaceutical composition of the present invention can adjust and control the drug release rate of the composition in various ways, such as changing the main chain affinity / hydrophobic properties of the copolymer, the type and con...

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PUM

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Abstract

The invention relates to a synthesis method of surface etched polyorthoester-polyamide copolymer (POEAd), a delivery carrier thereof and a controlled-release composition containing an active agent, which belongs to the technical field of polymer carriers and slow-release and controlled-release materials. The pharmaceutical composition can be a locally controllable delivery or injectable preparation applied to the active agent.

Description

technical field [0001] The invention relates to a synthesis method of a surface-impregnated polyorthoester-polyamide copolymer, the delivery carrier thereof, and a controlled-release pharmaceutical composition containing an active agent. The pharmaceutical composition may be in a locally controlled delivery or injectable form for the active agent. The invention belongs to the technical field of polymer carriers and sustained-release materials. Background technique [0002] There are two main types of erosion of biodegradable materials: bulk erosion and surface erosion. The overall erosion occurs in the whole of the material. Not only the surface of the material is degraded, but also the interior is simultaneously occurred. The loaded drug is released through diffusion, and the release rate is uncontrollable. The degradation of surface erosion only occurs on the surface of the material, the drug release conforms to the first-order kinetic process, and the drug release rate ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G69/40A61K47/34A61K45/06A61P27/02A61P29/02A61P35/00
Inventor 唐汝培陶扬洋
Owner 唐汝培
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