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Transdermal therapeutic system with activatable oversaturation and controlled permeation promotion

一种治疗系统、渗透增强剂的技术，应用在经皮治疗系统领域，能够解决系统不可控制、稳定性问题、活性物质生物利用度降低等问题

Active Publication Date: 2007-12-12
LTS LOHMANN THERAPIE-SYST AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, the method most frequently used in practice to improve the transdermal penetration of active substances also involves a number of disadvantages
[0009] The main disadvantage of adding permeation enhancers is that, since said enhancers are usually easily volatile organic compounds, the use of the delivery system very quickly puts the system in an uncontrollable manner, especially at the initial stage of use
This uncontrolled excess of penetration enhancer (enhancer dose dumping) often causes skin irritation
In addition, the inclusion of penetration enhancers in the matrix of transdermal therapeutic systems often leads to stability problems because active substances can interact with penetration enhancers
[0010] The specific disadvantages of iontophoresis and phonophoresis are, first and foremost, their potential for skin irritation since electrical current and ultrasound interfere with the skin barrier function more than chemical penetration enhancers
[0011] The disadvantage of supersaturated systems with active substances is that they are only metastable and that the recrystallization processes that occur in the matrix containing the active substance lead to a reduction in the bioavailability of the active substance and to the adhesion of transdermal therapeutic systems Negative Effects

Method used

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  • Transdermal therapeutic system with activatable oversaturation and controlled permeation promotion
  • Transdermal therapeutic system with activatable oversaturation and controlled permeation promotion
  • Transdermal therapeutic system with activatable oversaturation and controlled permeation promotion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1 : Manufacturing of active parts

[0060] With 54g containing the vinyl acetate of 40wt% and melt index be the EVA copolymer of 55 (EVATANE 40 / 55  ) into 80 g of a solvent mixture comprising 2 parts of 80 / 110 type specific boiling point gasoline and 1 part of propyl acetate and stirred at 50° C. by heating. After stirring for about 30 minutes, a viscous, colorless to slightly opaque solution was obtained. Next, 66g of binder resin Foral  85E was added and stirred again at 50°C until it completely dissolved (about 15 minutes). This yielded a 45.7%, low-viscosity, yellowish and slightly opaque solution (binder solution A), which remained as a stirrable binder solution even after cooling.

[0061] To prepare a self-adhesive active substance-containing matrix, 8.75 g of binder solution A are provided, to which 1.0 g of the lipophilic, sparingly water-soluble medical active substance moxonidine base are added in portions while stirring. The preparation was th...

Embodiment 2

[0066] Example 2 : Preparation of reinforcement part including self-adhesive control film

[0067] To prepare the self-adhesive enhancer part (liquid reservoir system), first, the active substance-free adhesive solution A (Example 1) was spread onto siliconized polyethylene terephthalate with a wet layer thickness of 300 μm using a spatula. on the ester film. Then, the solvent was removed by drying in a drying cabinet at 50° C. for 30 minutes using an exhaust pipe. The solvent-free and active-substance-free adhesive film was then bonded with a 35 μm thick polyurethane film (Opraflex  , from the Lohmann company in Germany) (according to the embodiment of the invention EB1) or with a 25 μm thick polypropylene film (Celgard X-20  , US Celanese Seperation Products) coverage. These films ultimately form the control film. Thereafter, the polyester film (Scotchpak No.1220  , from 3M Company in Germany) was placed on this Opraflex or Celgard film and made into a bag with a c...

Embodiment 3

[0069] Example 3: Permeation diagram of TTS

[0070] In order to be able to test the permeation properties of the TTS according to the invention and to compare these properties with each other, permeation tests were carried out on an in vitro diffusion model of human full-thickness skin by using a modified Franz diffusion cell, the results of which are graphically represented in FIG. 2 .

[0071] The receiving medium used was the addition of 0.1% NaN at a temperature controlled to 32°C 3 Physiological sodium chloride solution as preservative.

[0072] The enhancer mixture used in the reservoir of the enhancer section was 300 mg of a mixture of ethanol:oleic acid:N-methylpyrrolidone in a ratio of 2:1.5:1.5 (v / v / v).

[0073] For the embodiment EB / 1 of the TTS according to the invention, after removal of the siliconized polyethylene terephthalate film, the reinforcing part EB1 according to Example 2 is applied as a cover patch to the TTS according to Example 1. on the active pa...

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Abstract

The invention relates to a transdermal therapeutic system (TTS) that is essentially composed of two compartments and that is provided with activatable oversaturation and controlled permeation promotion. The invention more particularly relates to a TTS, wherein an oversaturated active ingredient solution is produced in an active-substance-containing polymer matrix when the system is applied to theskin, caused by the controlled supply of one or several substances promoting permeation of the pharmaceutical active ingredient; the two compartments which make up the inventive transdermal therapeutic system; and the production of said transdermal therapeutic system from the two compartments.

Description

technical field [0001] The present invention relates to a transdermal therapeutic system (TTS), which essentially consists of two parts and which has activatable supersaturation and controllable penetration enhancement. More specifically, the present invention relates to a TTS in which, when the system is applied to the skin, a supersaturated solution of the active substance is produced in an active substance-containing polymer matrix, which is composed of one or several substances that promote the penetration of the pharmaceutical active substance. caused by the controlled supply of substances (penetration enhancers). The invention also relates to two parts combined to form a transdermal therapeutic system according to the invention and to the preparation of said transdermal therapeutic system from said two parts. Background technique [0002] In fact, it is usually difficult to achieve the penetration of pharmaceutical active substances into the blood circulation through ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70
CPCA61K47/10A61K47/22A61K9/7092A61K47/12A61K9/7053A61K9/70
Inventor 安德烈亚斯·科赫
Owner LTS LOHMANN THERAPIE-SYST AG
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