Oral formulations of branaplam
A composition and drug technology, applied in the field of treatment, cyclodextrin, prevention or improvement of diseases related to SMN deficiency, can solve the problems of incompatibility of preservatives, poor stability, poor solubility and the like
Pending Publication Date: 2021-08-06
NOVARTIS AG
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- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Indeed, the development of such formulations has been severely hampered by several technical challenges, such as the poor solubility of brenalan in aqueous media (even in the presence of surfactants), pH-dependent stability ( poor stability at pH 4) and the incompatibility of brenella with some preservatives (such as potassium sorbate)
Method used
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Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
[0114] Embodiment 1: a kind of pharmaceutical composition, described pharmaceutical composition comprises
[0115] A) compounds of formula (I)
[0116]
[0117] or a pharmaceutically acceptable salt thereof, and
[0118] B) A pharmaceutically acceptable cyclodextrin or a combination of pharmaceutically acceptable cyclodextrins.
Embodiment 2
[0119] Embodiment 2: The pharmaceutical composition according to embodiment 1, wherein the compound of formula (I) is in the form of its hydrochloride salt.
Embodiment 3
[0120] Embodiment 3: The pharmaceutical composition according to embodiment 1 or 2, wherein the cyclodextrin is β-cyclodextrin.
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The present invention relates to pharmaceutical compositions suitable for oral administration comprising 5-(1H-pyrazol-4-yl)-2-(6-((2,2,6,6-tetramethylpiperidin-4-yl)oxy)pyridazin-3-yl)phenol (branaplam) and a pharmaceutically acceptable cyclodextrin.
Description
technical field [0001] The present invention relates to a pediatric pharmaceutical composition suitable for oral administration comprising 5-(1H-pyrazol-4-yl)-2-(6-((2,2,6,6-tetramethylpiperidine-4 -yl)oxy)pyridazin-3-yl)phenol (INN: branaplam) and pharmaceutically acceptable cyclodextrin. In particular, the present invention relates to such compositions comprising hydroxypropyl-beta-cyclodextrin, one or more flavor enhancers / taste-masking agents and being free of preservatives. The present invention further provides a method of treating, preventing or ameliorating a disorder associated with SMN deficiency, the method comprising administering to a subject in need thereof an effective amount of a pharmaceutical composition disclosed herein. Background technique [0002] Proximal spinal muscular atrophy (SMA) is a group of inherited, clinically heterogeneous neuromuscular disorders characterized by degeneration of the anterior horn cells of the spinal cord. Muscle weakness i...
Claims
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IPC IPC(8): A61K9/00A61K9/08A61K31/00A61K47/40
CPCA61K9/0095A61K9/08A61K47/40A61K9/0053A61K31/501A61K47/26A61P25/28A61P21/00A61K47/46
Inventor R·洛瓦莱卡M·德拉斯皮德T·法勒C·豪格P·A·费尔南德斯戈麦斯多斯桑托斯
Owner NOVARTIS AG