Novel pharmaceutical compositions administering n-0923
AssigneeUCB Pharma S.A.
InventorsStephan Rimpler, Sabine Grapatin, Cliff Krein, Markus Thelen
Life of this patent
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Abstract
The invention relates to a pharmaceutical composition for administering the dopamine agonist N-0923 in depot form. The invention makes available for the first time a depot form of N-0923, which achieves a therapeutically significant plasma level over a period of at least 24 hours after administration to a patient. As a result of poor oral bio-availability and the short plasma half-life, N-0923 was previously administered either by an intravenous drip or by transdermal systems. Preferred embodiments of said invention are oily suspensions, containing the active ingredient N-0923 in a solid phase, in addition to anhydrous pharmaceutical preparations of N-0923.
Claims23
Pharmaceutical composition, characterized in that it is in depot form that contains N-0923 (rotigotine) as. the active agent and, upon application on a patient, leads to a therapeutically effective N-0923 plasma level over a period of at least 24 hours.
Pharmaceutical composition as in one of the preceding claims, characterized in that it is an anhydrous pharmaceutical composition.
Pharmaceutical composition as in one of the preceding claims, containing the N-0923 in crystalline form.
Pharmaceutical composition as in one of the preceding claims, containing the N-0923 in the form of a crystalline hydrochloride salt.
Pharmaceutical composition as in one of the preceding claims, said pharmaceutical composition being an oily suspension whose continuous phase consists essentially of polyol fatty acid esters.
Injectable anhydrous pharmaceutical composition, characterized in that it comprises crystalline N-0923 salt in a hydrophobic liquid phase and that upon administration on a patient it leads to a continuous plasma level of 0.2 to 10 ng N-0923/ml over at least 24 hours.
Pharmaceutical composition as in one of the preceding claims, designed to be applied by subcutaneous or intramuscular administration.
Pharmaceutical composition as in one of the preceding claims, serving for the treatment of diseases associated with a disorder of the dopamine metabolism.
Pharmaceutical composition as in one of the preceding claims, further characterized in that the pharmaceutical composition contains at least one additional antiparkinsonian agent.
Use of N-0923 or of an N-0923 derivative for producing an injectable depot medication which after application on a patient leads to a therapeutically effective N-0923 plasma level over a period of at least 24 hours.
Use of N-0923 in its solid phase for producing a heat-sterilizable medicament, characterized in that, when the medicament is heated to 121° C. over 20 minutes at 0.2 mPa, less than 1% of the N-0923 decomposes.
Production of a sterile pharmaceutical composition containing N-0923, characterized by the autoclaving of a pharmaceutical composition containing N-0923 in its solid phase.
Kit for treating Parkinson's disease or Restless Leg syndrome, comprising
- (a) a pharmaceutical composition as per one of the preceding claims
- (b) an injection device.
Dependencies are inferred from the claim text.