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A method for modifying release of a therapeutically active agent from an elastomeric matrix

A technology of active agent and matrix, which is applied in the field of improving the release of therapeutic active agents from elastic matrix, and can solve the problems of affecting drug release, complex preparation methods, and troubles, etc.

Active Publication Date: 2020-05-12
BAYER AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Especially for drugs that are poorly soluble in silicone polymers such as non-steroidal anti-inflammatory drugs (NSAIDs), sufficient release rates may not be obtained for thick films
[0004] Furthermore, this type of preparation method can be complex and create various problems
Another problem is that the coating may not fully adhere to the outer surface of the core, which can affect the release of the drug, which can cause trouble during use

Method used

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  • A method for modifying release of a therapeutically active agent from an elastomeric matrix
  • A method for modifying release of a therapeutically active agent from an elastomeric matrix
  • A method for modifying release of a therapeutically active agent from an elastomeric matrix

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Embodiment Construction

[0023] The present specification relates to a method of improving the release of a therapeutically active agent from an elastic matrix.

[0024] The method includes

[0025] - providing a core comprising an elastic matrix and a therapeutically active agent;

[0026] - immersion of the core in a coating solution containing 5-40% by weight of elastomer and 95-60% by weight of solvent;

[0027] - curing the dip-coated core to provide a coated core;

[0028] in

[0029] - The elastomer dissolved in the solvent contains 20-35% by weight of filler, based on the total amount of filler and elastomer; - Dip coating is carried out by a continuous process of drawing the core through the coating solution, using a method suitable for providing 5-100 μm Traction speed of coating thickness;

[0030] - the filler is selected from the group consisting of silica, titanium dioxide, barium sulfate, carbon and mixtures thereof; and

[0031] - the elastomer contained in the core and the elasto...

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Abstract

The present invention relates to a method for modifying release of a therapeutically active agent from an elastomeric matrix, comprising providing a core comprising an elastomeric matrix and a therapeutically active agent; dipping the core to a coating solution of an elastomer, wherein the elastomer comprises 20-35 wt-% of a filler, calculated from the total amount of filler and elastomer; curingthe dipped core to provide a coated core. In this method the dipping is provided as a continuous process by pulling the core through the coating solution, using a pulling speed suitable for providinga coating thickness of 5-100 mu m; the filler is selected from silica, titanium dioxide, barium sulphate, carbon and mixtures thereof; the elastomer comprised in the core and the elastomer comprised in the coating solution are independently selected from poly(dimethyl) siloxanes, polyethylene vinyl acetates (EVAs), polyurethanes (PUs), polyhydroxyethyl methacrylates (PHEMAs) and polymethyl methacrylates (PMMAs).

Description

technical field [0001] The present invention relates to improving the release of therapeutically active agents from elastic matrices, such as from elastic matrices of reservoirs in an intrauterine system. Background technique [0002] Elastomeric matrices have been used for some time as reservoirs for therapeutically active agents (ie, drugs). These reservoirs are used, for example, in subcutaneous implants and intrauterine systems (IUS). The rate of release of the therapeutically active agent can be controlled by selecting an appropriate elastic matrix material, and also by coating a core made of elastomer and containing the therapeutically active agent. The coating typically also controls the initial release of the therapeutically active agent, ie it limits the burst effect. Depending on the therapeutically active agent used and the intended use of the reservoir, the coating material can be made from a variety of elastomers. Typically, polydimethylsiloxane (PDMS) and it...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/34A61K31/192A61K31/196A61K31/405A61K31/5415A61K47/02
CPCA61K9/0036A61K47/02A61K47/34A61K31/192A61K31/196A61K31/405A61K31/5415A61K9/0039A61K9/0002A61K9/1641A61K9/485A61K9/5026
Inventor M·阿霍拉R·哈卡拉P·哈拉A·科纳伦H·科罗莱宁J·皮拉杰
Owner BAYER AG
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