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Transdermal therapeutic system containing asenapine

a technology of asenapine and transdermal therapy, which is applied in the direction of drug compositions, heterocyclic compound active ingredients, cardiovascular disorders, etc., can solve the problems of reducing patient compliance, eating, drinking and smoking, and affecting the effect of treatment

Inactive Publication Date: 2018-07-12
LTS LOHMANN THERAPIE-SYST AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a matrix-type TTS for the transdermal administration of asenapine, which reduces fluctuations in blood plasma concentration compared to sublingual administration and is convenient for easy and cost-efficient application. The TTS complies with the needs of a convenient application in view of size and thickness and ensures an improved bioavailability of asenapine. The invention also provides an adhesive overlay that enhances the adhesive properties of the TTS and a backing layer that prevents active loss or cross-contamination in accordance with regulatory requirements.

Problems solved by technology

However, sublingual administration is associated with bitter or unpleasant taste as well as tongue / oral mucosal numbness induced by a local anesthetic effect, nausea and headaches.
Further, eating, drinking and smoking are not allowed immediately after sublingual dosing for 10 min.
These inconveniences may lead to reduced patient compliance and improper administration such as dose reduction, dose skipping, irregular drug intake or a complete abstinence from the intended asenapine intake.
Sublingual administration is also difficult to monitor in institutionalized psychiatric patients and may not be suitable for children, elderly and other patients with difficulty in swallowing, or for those not capable of taking medication on their own.
The relatively rapid concentration decrease also inevitably leads to multiple daily doses (currently twice daily), which are associated with poor patient compliance, in particular in chronic conditions.
Transdermal delivery of asenapine has been investigated, but it appears that passive transdermal delivery of asenapine, and in particular a constant release over an extended period of time, is challenging.
Up to date, no commercial asenapine TTS is available.

Method used

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  • Transdermal therapeutic system containing asenapine
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  • Transdermal therapeutic system containing asenapine

Examples

Experimental program
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Effect test

examples

[0410]The present invention will now be more fully described with reference to the accompanying examples. It should be understood, however, that the following description is illustrative only and should not be taken in any way as a restriction of the invention. Numerical values provided in the examples regarding the amount of ingredients in the composition or the area weight may vary slightly due to manufacturing variability.

examples 1a-d

Coating Composition

[0411]The formulations of the asenapine-containing coating compositions of Examples 1a-d are summarized in Table 1.1 below. The formulations are based on weight percent as also indicated in Table 1.1.

TABLE 1.1Ex. 1aEx. 1bEx. 1cEx. 1dSolidsSolidsSolidsSolidsIngredient (Trade Name)Amt [g][%]Amt [g][%]Amt [g][%]Amt [g][%]Asenapine base0.346.720.9312.340.9312.26 1.9725.93Acrylic adhesive in ethyl9.2993.2812.1481.1112.1681.0711.1374.07acetate. Solids content of50.5% by weight(Duro-Tak ™ 387-2287)Isopropyl myristate——0.496.55————Diethylene glycol————0.51 6.67——monoethyl ether(Transcutol)Ethyl acetate2.06—3.81—3.83— 3.79—Total11.69100.0017.37100.0017.43100.00 16.89100.00 Area Weight [g / m2]200.1141.5136.9149.0Asenapine content1.3451.7461.6783.864[mg / cm2]

Preparation of the Coating Composition

[0412]For Examples 1a-1c, a beaker was loaded with the asenapine base and with the solvent (ethyl acetate), and the isopropyl myristate (Example 1b) or the diethylene glycol monoethyl ...

examples 2a-d

Coating Composition

[0420]The formulations of the asenapine-containing coating compositions of Examples 2a-d are summarized in Table 2.1 below. The formulations are based on weight percent, as also indicated in Table 2.1.

TABLE 2.1Ex. 2aEx. 2bEx. 2cEx. 2dAmtSolidsAmtSolidsAmtSolidsAmtSolidsIngredient (Trade Name)[g][%][g][%][g][%][g][%]Asenapine base0.356.860.346.63 1.3413.33 1.3413.33Acrylic adhesive in ethyl8.5385.38 ——14.1371.1414.1371.14acetate. Solids content of50.5% by weight(Duro-Tak ™ 387-2287)Polyisobutylene adhesive——10.7 86.47 ————in petroleum ether,bp 80-110° C. Solidscontent of 40.9%(Oppanol B10 / B100,85 / 15)Diethylene glycol0.397.76—— 1.5615.53 1.5615.53monoethyl ether(Transcutol)Polyvinylpyrrolidone——0.356.90————(Kollidon ® 90F)Ethyl acetate2.54———3.1—3.1—Petroleum ether,——5.42—————bp 80-110° C.Total11.81 100.00 16.81 100.00 20.13100.00 20.13100.00 Area Weight [g / m2]91.385.790.15159.6Asenapine content0.6270.5681.2012.127[mg / cm2]

Preparation of the Coating Composition

[0421]...

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Abstract

The present invention relates to transdermal therapeutic systems (TTS) for the transdermal administration of asenapine comprising a self-adhesive layer structure containing a therapeutically effective amount of asenapine, such asenapine TTS for use in a method of treatment, processes of manufacture of such TTS as well as asenapine and transdermal therapeutic systems containing asenapine for use in a method of treatment and to a method of treating a human patient by transdermal administration of asenapine.

Description

TECHNICAL FIELD OF THE INVENTION[0001]The present invention relates to a transdermal therapeutic system (TTS) for the transdermal administration of asenapine to the systemic circulation, and processes of manufacture, method of treatments and uses thereof.BACKGROUND OF THE INVENTION[0002]The active agent asenapine (3aRS,12bRS)-rel-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole) is an atypical antipsychotic belonging to the dibenzo-oxepino pyrrole family, the tetracyclic structure of which is unrelated to those of other antipsychotics such as Olanzapine, Quetiapine or Clozapine (tricyclic structure), Risperidone, Ziprasidone or Aripiprazole (bicyclic structure). Asenapine is an antagonist at the dopamine D2 and serotonin 5-HT2A receptors with high affinity to the latter and has been developed by Schering-Plough / Organon for the treatment of schizophrenia and acute mania associated with bipolar disorder.[0003]Currently, asenapine is commercially availabl...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/407
CPCA61K9/7061A61K31/407A61K9/7038A61K9/7053A61P25/18A61P25/24A61P43/00A61K47/32A61K47/22A61K47/10A61K9/70A61K31/40A61K47/30A61P9/12A61K9/0014A61K9/7069A61K9/7076A61K9/7084
Inventor MOHR, PATRICKRIETSCHER, RENEEIFLER, RENEBOURQUAIN, OLGA
Owner LTS LOHMANN THERAPIE-SYST AG
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