Gastro-retentive levodopa delivery form

Details Gastro-retentive levodopa delivery form Gastro-retentive levodopa delivery form

A - Human Necessities

61

K

A61K 9/20 (2006.01) A61K 9/00 (2006.01) A61K 9/28 (2006.01) A61K 9/48 (2006.01) A61K 9/64 (2006.01) A61K 31/198 (2006.01)

Patent

CA 2501345

Gastro-retentive dosage forms for prolonged delivery of levodopa and carbidopa~levodopa combinations are described. The dosage forms comprise a tablet containing the active ingredient and a gas-generating agent sealed within an expandable, hydrophilic, water-permeable and substantially gas- impermeable membrane. Upon contact with gastric fluid, the membrane expands as a result of the release of gas from the gas-generating agent in the tablet. The expanded membrane is retained in the stomach for a prolonged period of time up to 24 hours or more during which period the active ingredient is released from the tablet providing delivery of levodopa to the site of optimum absorption in the upper small intestine.

L'invention concerne des formes pharmaceutiques gastro-rétentive pour une administration prolongée de levodopa et de combinaisons de carbidopa-levodopa. Les formes pharmaceutiques comprennent un comprimé contenant le principe actif et un agent produisant du gaz enfermé à l'intérieur d'une membrane extensible, hydrophile, perméable à l'eau, et sensiblement imperméable au gaz. Lors du contact avec le liquide gastrique, la membrane s'étend en raison de la libération de gaz provenant de l'agent produisant du gaz dans le comprimé. Ladite membrane extensible est retenue dans l'estomac pendant une période prolongée supérieure ou égale à 24 heures, durant laquelle le principe actif est libéré du comprimé, ce qui libère le levodopa vers le site d'absorption optimal, situé dans l'intestin grêle supérieur.

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