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Transdermal system for simultaneous delivery of a number of active principles

A technology of active ingredients and systems, applied in the field of transdermal systems, can solve problems such as unsatisfactory and small contact surface area of ​​transdermal systems

Inactive Publication Date: 2001-10-17
LABES DHYGIENE & DE DIETETIQUE L H D
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0029] Therefore, none of the solutions in the prior art is satisfactory, because they cannot successfully reconcile the above-mentioned two problems, that is, the easy control of the release of each active ingredient, and the contact surface area of ​​the transdermal system. The small size makes the system safe and comfortable to use

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Embodiment 1 (patch 1)

[0063] 47.0g LEVAPREN  450P (ethylene / vinyl acetate copolymer produced by Bayer (hereinafter referred to as EVA)), 48g crotamiton [N-ethyl-2-N-(2-methylphenyl)-2-butenamide] (BOEHRINGERINGELHEIM produced), 0.2g IRGANOX  B215 (an antioxidant produced by Ciba-Geigy) and 115.53 g of ethyl acetate were placed in a container. The mixture was heated for 5 hours until the EVA was completely dissolved. Stir at room temperature for 1 hour, and then add 4 g of norethindrone acetate (hereinafter abbreviated as NETA) previously dissolved in 20 g of tetrahydrofuran. The resulting mixture was stirred for another 30 minutes until it was completely homogeneous; it was then left to stand until the air bubbles had completely disappeared. At room temperature (15-25°C), the substrate was coated on a silicone-coated polyester film to obtain (100 ± 10) g / m 2 deposition material. The resulting object was heated at 70°C for 30 minutes and then transferred to a ...

Embodiment 2

[0064] Embodiment 2 (patch 2)

[0065] Similar to the method of Example 1 above, using 49.8 g LEVAPREN  450P, 44gcrotamiton, 0.2g IRGANOX  B215, 116.2 g ethyl acetate, 2 g 17-β-estradiol and 4 g norethindrone acetate (added at the same time as 17-β-estradiol was added), these two hormones were dissolved together in 30 g tetrahydrofuran.

Embodiment 3

[0066] Embodiment 3 (patch 3)

[0067] 20.7g ELVAX  46L and 6.9g ELVAX  46 (ethylene / ethylene acetate copolymer from DuPont) and 6g ETHOCEL  (Ethylcellulose from DOW CHEM IC AL) was placed in a container, stirred and heated to about 130°C. Then gradually add 1.2 g of 17-β-estradiol and 18.9 g of EUTANOL at 130°C with continued stirring  G (2-octyldodecanol commercially available from HENKE), continue stirring the mixture until it is completely homogeneous. Then add 6.3g SURFADONE at 100-110℃  LP300 (N-dodecyl-2-pyrrolidone commercially available from GAF Company) and continue stirring until the mixture is completely homogeneous. At 100-140°C, the resulting mixture was (100±10) g / m 2 Thickness coating on an anti-adhesive temporary support, especially a silicone-coated polyester film. The resulting matrix was transferred to a polyethylene support.

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PUM

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Abstract

A novel system for percutaneously delivering at least two active principles, consisting of at least two juxtaposed devices. The system includes (i) a first device containing a mixture of all the active principles in which at least one first active principle (A) is present in an amount enabling the effective therapeutic dose to be delivered, and at least one second active principle (B) is present in an amount smaller than the amount needed to deliver the effective therapeutic dose; and (ii) one or more additional devices each containing a single active principle (B) selected from those in the first device and provided in an amount smaller than the amount needed to deliver the effective therapeutic dose, said additional device(s) being designed to top up the amount of each of the active principles (B) in the system until the effective therapeutic dose is achieved.

Description

field of invention [0001] The present invention relates to transdermal systems that release multiple active ingredients simultaneously. The system can be easily adjusted to release the dose of one or more active ingredients and reduce the surface area of ​​the system, thereby improving the safety and comfort of the patient in use. Background technique [0002] A number of devices are currently available for transdermal delivery of active ingredients. [0003] The components of these patches are determined to (i) ensure good physicochemical stability of the active ingredient over a long period of time, and (ii) obtain optimal transdermal absorption flux per unit surface area. The dose of active ingredient released during treatment is therefore mainly determined by the surface area of ​​the patch applied to the skin. [0004] The surface area of ​​the patch should not be made too large, because a patch with a large surface area will cause discomfort when used, and such a pat...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/565A61K31/57A61L15/44A61P5/30
CPCA61K9/703A61K9/7053A61P5/30A61K9/70
Inventor 布鲁诺·贝文塞西尔·艾劳德
Owner LABES DHYGIENE & DE DIETETIQUE L H D
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