Oral preparation with controlled release
Inventors
Schlutermann, Burkhard • Kohlmeyer, Manfred
Assignees
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Publication Number
US-11311490-B2
Publication Date
2022-04-26
Expiration Date
Abstract
A pharmaceutical pellet is disclosed, comprising a spherical core containing active ingredient with a smooth surface and a coating on the core which controls the release of the active ingredient in a pH-independent manner. With such a pellet the release of the active ingredient can follow a profile with a lag phase of 60 minutes to 840 minutes, a proportion of 5 wt. % or less of the active ingredient being released during the lag phase. The active ingredient can furthermore be released from the pellet with a profile such that after the lag phase the release of the active ingredient amounts to between 3 and 25 wt. % per hour.
Core Innovation
The invention relates to a pharmaceutical pellet having a spherical core with a smooth surface, where the spherical core is homogeneous and comprises an active substance that is uniformly distributed in the core. The core has a diameter in the range of 0.2 to 2.0 mm, and the core surface has a mean roughness of less than 10 μm and a relative mean roughness of less than 2%.
The pellet includes a coating on the core that controls pH-independent release of the active substance and does not comprise the active substance. The pellet additionally has an outer protective coating comprising a water-soluble film-forming agent, and the release profile includes a lag phase and thereafter a controlled release of the active substance.
In a further aspect, the pellet includes an interlayer comprising a water-soluble film forming agent provided between the core comprising the active substance and the coating that controls the release of the active substance. The document also characterizes core smoothness and geometry using quantitative criteria such as mean roughness, relative mean roughness, and a length-width ratio of less than about 1.4.
Claims Coverage
The independent claim set covers three distinct subjects: a pharmaceutical pellet with a smooth homogeneous active-containing spherical core and a pH-independent release-controlling coating, a collection of cores meeting population-level smoothness and geometry constraints, and a pharmaceutical pellet in which an interlayer with a water-soluble film forming agent is provided between the core and the pH-independent release-controlling coating. Across these independent claims, five main inventive feature areas are specified.
Spherical homogeneous active-containing core with smooth surface
A spherical core with a smooth surface, wherein the spherical core is homogeneous and comprises an active substance, wherein the active substance is uniformly distributed in the core, and wherein the core has a diameter in the range of from 0.2 to 2.0 mm.
Smoothness-limited core surface
The surface of the core has a mean roughness of less than 10 μm and a relative mean roughness of less than 2%.
pH-independent release-controlling coating without active substance
A coating, on the core, which controls pH-independent release of the active substance, and which does not comprise the active substance.
Outer protective water-soluble film-forming layer
The pellet additionally has an outer protective coating which comprises a water-soluble film-forming agent.
Population-level collection of compliant homogeneous smooth cores
At least 90% of the cores are homogeneous, comprise an active substance that is uniformly distributed in each core, have a diameter in the range of from 0.2 to 2.0 mm, have a smooth surface with a mean roughness of less than 10 μm and a relative mean roughness of less than 2%, and have a length-width ratio of less than about 1.4.
Interlayer of water-soluble film forming agent between core and release-coating
An interlayer, which comprises a water-soluble film forming agent, provided between the core comprising the active substance and the coating that controls the release of the active substance.
Overall, the claim coverage centers on pellets and collections of cores that combine a smooth homogeneous spherical active-containing core with quantitative smoothness and size/geometry limits, together with a coating that controls pH-independent release without containing the active substance, optionally supplemented by a water-soluble film-forming protective outer coating and/or an interlayer of a water-soluble film forming agent between the core and the release-controlling coating.
Stated Advantages
Provides pH-independent release of the active substance.
Documented Applications
Use in producing tablets by mixing pellets with selected pharmaceutical ingredient types and compressing the mixture into a tablet.
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