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Method for preparing alternate lamellar bio-degraded polymer drug controlled-release composite

A polymer material and biodegradation technology, which is applied in the field of preparation of alternate layered biodegradable polymer drug slow-release materials, can solve the problems of low drug efficacy, complex process, poor preparation stability, etc. Good compatibility and the effect of refining the size of the dispersed phase

Active Publication Date: 2017-02-22
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are many deficiencies in these traditional homogeneous sustained-release preparations: the drug release of some preparation methods is nonlinear; the preparation form is relatively single, and it is difficult to flexibly and effectively control the dosage and administration plan, which increases the difficulty of compound administration; some preparations have poor stability, low efficacy
[0005] Although the above studies can overcome the problems of the traditional homogeneous drug-loading materials, such as the difficulty in flexible and effective control of the drug dosage and drug regimen, but due to the multi-use solution method for preparation, there are difficulties in solvent removal, and there are relatively large limitations in the choice of matrix and drugs. , The process is complex, it is difficult to meet the needs of industrial mass production

Method used

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  • Method for preparing alternate lamellar bio-degraded polymer drug controlled-release composite
  • Method for preparing alternate lamellar bio-degraded polymer drug controlled-release composite

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] In the first step, the polymer-based drug immediate-release layer (hereinafter referred to as the immediate-release layer) uses polycaprolactone as the matrix of the immediate-release layer (molecular weight: 80,000), and polyethylene oxide as the dispersed phase of the immediate-release layer (molecular weight: 100,000), and The ingredients are 60%:40% by weight; metoprolol tartrate is the drug of the immediate release layer, and the ingredients are formulated according to 10% of the total weight of the polymer of the immediate release layer. The above-mentioned polymer and drug were mixed in a high-speed mixer for 5 minutes at a speed of 100 rpm to obtain a polymer-based drug immediate-release layer material.

[0050] The polymer-based drug slow-release layer (hereinafter referred to as the slow-release layer) selects polycaprolactone as the slow-release layer matrix (molecular weight is 80000), and metoprolol tartrate is the slow-release layer drug, and the percentage...

Embodiment 2

[0055] The polymer-based drug immediate-release layer (hereinafter referred to as the immediate-release layer) uses polybutylene succinate as the matrix of the immediate-release layer (molecular weight is 100,000); polyethylene oxide is the dispersed phase of the immediate-release layer (molecular weight is 200,000); and Percentage by weight 80%: 20% batching; Ibuprofen is an immediate-release layer medicine, and is batched according to 35% of the total weight of the immediate-release layer macromolecule. The above-mentioned polymer and drug were mixed in a high-speed mixer for 5 minutes at a speed of 100 rpm to obtain a polymer-based drug immediate-release layer material.

[0056] The polymer-based drug slow-release layer (hereinafter referred to as the slow-release layer) uses polycaprolactone as the matrix of the slow-release layer (molecular weight is 50000); polyethylene glycol is the dispersed phase of the slow-release layer (molecular weight is 6000); 95%: 5% batching; ...

Embodiment 3

[0061] In the first step, the polymer-based drug immediate-release layer (hereinafter referred to as the immediate-release layer) uses ethyl cellulose as the matrix of the immediate-release layer (molecular weight: 130,000), and polyethylene glycol as the dispersed phase of the immediate-release layer (molecular weight: 6,000). And with weight percentage 75%: 25% batching; Hydrochlorothiazide is the immediate-release layer medicine, carries out batching according to 30% of the macromolecule gross weight of the quick-release layer. The above-mentioned polymer and drug were mixed in a high-speed mixer for 5 minutes at a speed of 100 rpm to obtain a polymer-based drug immediate-release layer material.

[0062] The polymer-based drug sustained-release layer (hereinafter referred to as the sustained-release layer) selects ethyl cellulose as the matrix of the sustained-release layer (molecular weight is 130000), and metoprolol tartrate as the drug, 91% by weight: 9% in high blender ...

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Abstract

The invention provides a method for preparing an alternate lamellar bio-degraded polymer drug controlled-release composite. The method mainly includes the steps that polymer-based drug quick release layers and polymer-based drug slow release layers with different release behaviors are alternately and orderly arranged in a melt co-extrusion mode, polymers deform and are oriented in the extrusion process through the shear and stretching effects of a layer multiplier during multiple times of lamellar overlapping, drug diffusion and release channels are improved, and the obtained alternate lamellar bio-degraded polymer drug controlled release composite has the reasonable initial release concentration and required long-term release rate and achieves controllable, flexible and effective release of drugs to meet different drug release requirements. The alternate lamellar bio-degraded polymer drug controlled release composite is controllable in form and adjustable in formula; the mechanical property is excellent; continuous volume production can be achieved, and the production efficiency can be improved; the application range is wide, and wide industrial and market prospects are achieved.

Description

technical field [0001] The invention relates to the preparation of an alternate layered biodegradable polymer drug slow-release material with configurable structure, designable performance, continuous production and flexible and controllable drug release behavior, which belongs to the field of functional composite material preparation. Background technique [0002] Compared with traditional drug delivery systems, drug sustained-release preparations do not require frequent drug administration, can maintain effective drug concentrations in the body for a long time, reduce the pain and inconvenience caused by frequent drug use, and can greatly improve drug efficacy and reduce toxic side effect. Polymer drug sustained-release materials are generally divided into two categories: non-biodegradable materials and biodegradable materials. Among them, biodegradable polymer materials do not require secondary surgery due to their good biocompatibility and non-toxicity, and metabolites h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K47/38A61K47/10A61K47/36A61K47/32A61K9/00A61K9/20A61K31/192A61K31/138A61K31/4402A61K31/196A61K31/549
CPCA61K47/10A61K47/32A61K47/34A61K47/36A61K47/38A61K9/0002A61K9/2086A61K31/138A61K31/192A61K31/196A61K31/4402A61K31/549
Inventor 陈蓉郭少云张聪
Owner SICHUAN UNIV
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