Felodipine transdermal device and methods
AssigneeEuro-Celtique S.A.
InventorsLino Tavares, Ihor Shevchuk, Mark Alfonso, Geraldine Marcenyac, Kirti Valia
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Abstract
A method of effectively treating hypertension in humans is achieved by administering felodipine via a transdermal formulation. Preferably, the transdermal formulation is applied to the skin of the patient and maintained in contact with the skin for at least about 24 hours days, and preferably for about 3 to about 8 days.
Claims37
A method of effectively treating hypertension, angina, or both conditions in a human patient, comprising:
- administering felodipine transdermally to the human patient by applying a transdermal delivery system containing felodipine to the skin of a patient, and maintaining said transdermal delivery system in contact with the skin of said patient for at least 3 days, said transdermal delivery system maintaining an effective mean relative release rate to provide a therapeutic blood level of said felodipine within 36 hours from the initiation of the dosing interval, and thereafter maintaining a therapeutic blood level until the end of at least the three-day dosing interval.
- said transdermal delivery system having a mean relative release rate of from about 4.2 μg/cm2/hr to about 20.0 μg/cm2/hr at 24 hours;
- from about 3.3 μg/cm2/hr to about 14.0 μg/cm2/hr at 48 hours;
- and
- from about 2.7 μtg/cm2/hr to about 10.8 μg/cm2/hr at 72 hours;
- as determined via an in-vitro permeation test utilizing a Valia-Chien cell where the membrane is a human cadaver skin and said cell has a receptor chamber containing a 40:60 mixture of Ethanol:water;
- said transdermal delivery system providing a mean relative release rate of felodipine to provide a plasma level of felodipine of at least 0.1 ng/ml within about 6 hours after application of said transdermal delivery system onto the skin of said patient.
A transdermal delivery system containing felodipine or a pharmaceutically acceptable salt thereof which provides a mean relative release rate of from about 4.2 μg/cm2/hr to about 20.0 μg/cm2/hr at 24 hours;
- from about 3.3 μg/cm2/hr to about 14.0 μg/cm2/hr at 48 hours;
- and
- from about 2.7 μg/cm2/hr to about 10.8 μg/cm2/hr at 72 hours;
- as determined via an in-vitro permeation test utilizing a Valia-Chien cell where the membrane is a human cadaver skin and said cell has a receptor chamber containing a 40:60 mixture of ethanol:water;
- said transdermal delivery system providing a plasma level of felodipine of at least about 0.1 ng/ml by about 6 hours after application of said transdermal delivery system onto the skin of a human patient;
- said transdermal delivery system maintaining a therapeutic blood level until the end of at least a three-day dosing interval and said transdermal delivery system maintaining a plasma level of felodipine at steady-state from about 0.1 to about 3.3 ng/ml.
Dependencies are inferred from the claim text.