Controlled release system and method for manufacturing the same
First Claim
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1. A pharmaceutical controlled release system for administration of active substances with pH-dependent solubilities, comprising:
- a) a core material comprising one or more pharmaceutically acceptable pH modifiers, wherein at least one pharmaceutically acceptable pH modifier is an organic acid;
b) a first insulating layer, provided on the core material, comprising one or more pharmaceutically acceptable water soluble polymers;
c) a second layer comprising a pharmaceutically acceptable water-insoluble (poly(ethyl acrylate/methyl methacrylate/trimethylammonioethyl methacrylate chloride)polymer having either a 1;
2;
0.1 or 1;
2;
0.2 ratio of ethyl acrylate to methyl methacrylate to trimethylammonioethyl methacrylate chloride monomers;
d) a third layer comprising at least one active substance having a pH-dependent solubility;
e) a fourth layer comprising one or more pharmaceutically acceptable polymers having anionic or no ionic groups; and
f) optionally a fifth layer.
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Abstract
The invention is directed to a pharmaceutical controlled release system for administration, particularly oral administration, of active substances with pH-dependent solubilities, comprising
- a) a core material containing or consisting of one or more pharmaceutically acceptable pH modifiers;
- b) optionally an insulating layer,
- c) a first layer containing or consisting of one or more pharmaceutically acceptable water-insoluble polymers;
- d) a second layer containing or consisting of at least one active substance having a pH-dependent solubility;
- e) a third layer containing or consisting of one or more pharmaceutically acceptable polymers having anionic or no ionic groups; and
- f) optionally a fourth layer, preferably in form of an outer coating layer.
It is provided a pH-independent release profile of active substances having pH-dependent solubilities in vitro and vivo.
103 Citations
26 Claims
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1. A pharmaceutical controlled release system for administration of active substances with pH-dependent solubilities, comprising:
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a) a core material comprising one or more pharmaceutically acceptable pH modifiers, wherein at least one pharmaceutically acceptable pH modifier is an organic acid; b) a first insulating layer, provided on the core material, comprising one or more pharmaceutically acceptable water soluble polymers; c) a second layer comprising a pharmaceutically acceptable water-insoluble (poly(ethyl acrylate/methyl methacrylate/trimethylammonioethyl methacrylate chloride)polymer having either a 1;
2;
0.1 or 1;
2;
0.2 ratio of ethyl acrylate to methyl methacrylate to trimethylammonioethyl methacrylate chloride monomers;d) a third layer comprising at least one active substance having a pH-dependent solubility; e) a fourth layer comprising one or more pharmaceutically acceptable polymers having anionic or no ionic groups; and f) optionally a fifth layer. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26)
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Specification