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Purpose <p>Cariprazine (CPZ) is a drug used in the treatment of schizophrenia and manic/mixed episodes of bipolar I disorder; however, its absolute bioavailability is low (52–63%) due to first-pass metabolism. To overcome the limitations of the oral route, a transdermal patch of CPZ was prepared to maintain a constant drug plasma level concentration.</p> Methods <p>Transdermal patches of CPZ were prepared using a solvent evaporation method using different pressure-sensitive adhesives (PSA), penetration enhancers, and crystal inhibitors. The patches were checked for drug crystallisation, and a composition that prevented the drug from crystallising was selected. The next step involved the identification of process parameters, such as mixing time, drying time, and drying temperature, that caused the evaporation of solvents but did not strip off the penetration enhancer from the patch. Furthermore, the composition was optimised for flux and adhesion characteristics. The optimised patch was characterised for its heat effect, rat skin irritation potential, and stability testing.</p> Results <p>The selected batch included a combination of Duro-Tak-87-2287 and Bio PSA-AC7-4302 as PSA, a mixture of propylene glycol and lauroglycol (1:1) as penetration enhancer, Povidone K-29/32 (PVP) as a crystal inhibitor, and 12% CPZ. The patch with acceptable levels of residual solvents and penetration enhancers required a mixing time of 45&#xa0;min for the blend and drying time of 20&#xa0;min at 56&#xa0;°C. The composition was optimised using a face-centred central composite design, and found acceptable for assay, flux, adhesion parameters, and drug release at the 6th hour, residual drug content, degradation product, impact of heat, and stability. </p> Graphical Abstract <p></p>

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Systematic approach to optimise components and process parameters in the development of transdermal patch containing cariprazine for weekly administration

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  • 发表日期：

    2026年7月6日

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  • Punitkumar Rathod,
  • Anita Lalwani

摘要

Purpose

Cariprazine (CPZ) is a drug used in the treatment of schizophrenia and manic/mixed episodes of bipolar I disorder; however, its absolute bioavailability is low (52–63%) due to first-pass metabolism. To overcome the limitations of the oral route, a transdermal patch of CPZ was prepared to maintain a constant drug plasma level concentration.

Methods

Transdermal patches of CPZ were prepared using a solvent evaporation method using different pressure-sensitive adhesives (PSA), penetration enhancers, and crystal inhibitors. The patches were checked for drug crystallisation, and a composition that prevented the drug from crystallising was selected. The next step involved the identification of process parameters, such as mixing time, drying time, and drying temperature, that caused the evaporation of solvents but did not strip off the penetration enhancer from the patch. Furthermore, the composition was optimised for flux and adhesion characteristics. The optimised patch was characterised for its heat effect, rat skin irritation potential, and stability testing.

Results

The selected batch included a combination of Duro-Tak-87-2287 and Bio PSA-AC7-4302 as PSA, a mixture of propylene glycol and lauroglycol (1:1) as penetration enhancer, Povidone K-29/32 (PVP) as a crystal inhibitor, and 12% CPZ. The patch with acceptable levels of residual solvents and penetration enhancers required a mixing time of 45 min for the blend and drying time of 20 min at 56 °C. The composition was optimised using a face-centred central composite design, and found acceptable for assay, flux, adhesion parameters, and drug release at the 6th hour, residual drug content, degradation product, impact of heat, and stability.

Graphical Abstract