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Glycerol-silicone elastomers as active matrices with controllable release profiles

A technology of silicone and elastomer, applied in the field of glycerol-organosilicon elastomer as active matrix with controllable release profile

Active Publication Date: 2020-06-12
DANMARKS TEKNISKE UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

First, all drug delivery systems must be biocompatible and nontoxic

Method used

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  • Glycerol-silicone elastomers as active matrices with controllable release profiles
  • Glycerol-silicone elastomers as active matrices with controllable release profiles
  • Glycerol-silicone elastomers as active matrices with controllable release profiles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0176] Example 1: Preparation of multi-compartment glycerin-silicone elastomer

[0177] experiment

[0178] The colorant was added to the glycerin and the resulting glycerin composition was mixed with the Sylgard silicone composition by rapid mixing at 3500 rpm for 5 minutes until a homogeneous solution was obtained. A silicone composition comprising a monoglycerin phase was thus prepared. The composition is in the form of an emulsion.

[0179] Gently transfer two or three different emulsions, each with a different colorant (red / blue / green) dissolved in its corresponding glycerol phase, to a larger container and mix at a relatively low speed of 500 rpm Speed ​​mix for 1 minute. Faster mixing above 1000 rpm resulted in merging of glycerol droplets. The presence of diluents (eg solvents) and / or surfactants in the glycerol phase reduces the rate of mixing at which coalescence of the droplets occurs.

[0180] The mixed emulsion was then crosslinked at 100°C for 10 minutes a...

Embodiment 2

[0189] Example 2: Release of active substances from monocompartmental glycerol-silicone elastomers containing hydroquinone

[0190] Sample Preparation

[0191] The examples provided yielded batches of 1.42 g of material that could be easily scaled up or down. Using the method described, 1 g to 80 g batches were prepared. Hydroquinone (HQ, 0.02 g, 5 wt %) was dissolved in glycerol (0.4 g) at 50° C. using magnetic stirring until a clear solution was obtained (usually about 1 hour to 2 hours). The desired amount of S184 was combined using a double asymmetric centrifuge SpeedMixerDAC 150FVZ-K (by mixing base 0.909 g and curing agent 0.091 g 10:1 according to the manufacturer's guidelines, or 0.952 g base and 0.048 g curing agent at 20 :1 mixed to form less cross-linked product) and glycerin / hydroquinone (the ratio of glycerin / silicone product is the same regardless of the presence of hydroquinone) at 3500 revolutions per minute (rpm) for 5 minutes. The obtained glycerin emuls...

Embodiment 3

[0220] Example 3: Release of active substances from double compartmentalized glycerol-silicone elastomers

[0221] experiment

[0222] The double partitioned glycerol-silicone elastomer was prepared in four steps. The examples presented hereinafter illustrate the preparation of dual compartmentalized glycerol-silicone elastomers each comprising erythrosin B and hydroquinone as active substances in respective different glycerol phases. The amounts of all compounds are given by examples, and can be scaled up or down according to actual needs.

[0223] At least one glycerol-miscible or soluble excipient is added to glycerol at a given concentration and stirred with a mechanical stirrer until a homogeneous and clear solution is obtained. In some cases, stirring at elevated temperature is required to dissolve the active excipients. The solution obtained in this way will form a type of glycerol compartment.

[0224] Incorporation of the active substance into glycerin:

[0225...

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Abstract

Herein is disclosed an elastomeric silicone composition comprising at least a first and a second glycerol phase which are distinct from each other and a method of making the same. The elastomeric compositions are special therein that zero-order active substance release can reversibly be obtained by modifying the glycerol content of the silicone composition.

Description

technical field [0001] In the field of active matrices for controlled release of active substances, silicone elastomers comprising glycerol having a controlled release profile are described as active matrices. Background technique [0002] The active substance release regime, especially the drug regimen, has to be controlled in order to achieve an optimal effect of the released active substance, in particular an optimal therapeutic effect. While generating a first-order release matrix is ​​relatively straightforward, avoiding initial burst release can be challenging. Matrices with zero-order curves are considered beneficial in many cases, but are more difficult to formulate. [0003] In the present disclosure, a simple synthesis of elastomeric composites prepared from silicones in which the active substance is dispersed in glycerin is described. It was surprisingly found that the release of glycerol-soluble excipients from the films of these materials is tunable with respe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08K5/00C08K5/053C08K5/13C08K5/1545C08J3/205A61K9/70
CPCC08J3/2053C08K5/0008C08K5/053C08K5/13C08K5/1545C08J2383/04A61K47/34A61K9/7007A61K9/0014A61K47/10C08L83/04A61K31/05
Inventor 安娜·拉德高·斯科乌米凯尔·阿德里安·布鲁克彼得·斯坦尼斯瓦夫·马祖雷克
Owner DANMARKS TEKNISKE UNIV