Osmotic delivery of therapeutic compounds by solubility enhancement
First Claim
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1. An oral osmotic pharmaceutical delivery dosage form comprising:
- (a) a semipermeable wall; and
(b) a single, solid core composition within said wall consisting essentially of;
at least one pharmaceutically active agent that has solubility limitations due to inherent hydrophobicity or to high drug load, wherein high drug load means that at least 30% by weight of the dosage form is the at least one active agent, and, homogenously mixed with said pharmaceutically active agent, (1) a non-swelling osmotic agent, and (2) from 1 to 10% by weight of the core of meglumine, as a solubilizer, wherein said wall maintains its integrity during pharmaceutical delivery and has at least one passageway through it, connecting the core of the dosage form with the external environment, wherein the size of the passageway(s) is from 100μ
to 1000μ
.
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Abstract
The present invention is directed to the oral osmotic delivery of therapeutic compounds that have limited solubility in an aqueous environment due to inherent hydrophobicity or to saturation limitations in the core of the osmotic system. The present invention is suitable for the osmotic delivery of glipizide and other hydrophobic drugs, but runs the spectrum to other therapeutic agents with higher aqueous solubilities, yet having a solubility limitation in an osmotic dosage unit due to high drug load.
105 Citations
17 Claims
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1. An oral osmotic pharmaceutical delivery dosage form comprising:
- (a) a semipermeable wall; and
(b) a single, solid core composition within said wall consisting essentially of;
at least one pharmaceutically active agent that has solubility limitations due to inherent hydrophobicity or to high drug load, wherein high drug load means that at least 30% by weight of the dosage form is the at least one active agent, and, homogenously mixed with said pharmaceutically active agent, (1) a non-swelling osmotic agent, and (2) from 1 to 10% by weight of the core of meglumine, as a solubilizer, wherein said wall maintains its integrity during pharmaceutical delivery and has at least one passageway through it, connecting the core of the dosage form with the external environment, wherein the size of the passageway(s) is from 100μ
to 1000μ
. - View Dependent Claims (3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17)
- (a) a semipermeable wall; and
-
2. An oral osmotic pharmaceutical delivery dosage form comprising:
- (a) a solid core comprising a pharmaceutically active agent that has solubility limitations due to inherent hydrophobicity or to high drug load, wherein high drug load means that at least 30% by weight of the dosage form is the at least one active agent, a non-swelling osmotic agent and from 1 to 10% by weight of the core of meglumine, as a solubilizer, wherein the pharmaceutically active agent, non-swelling osmotic agent and meglumine are all present as a homogeneous mixture in at least one layer, and when said core comprises more than one layer, each layer comprises at least one pharmaceutically active agent, and (b) a semipermeable wall that surrounds the core, maintains its integrity during pharmaceutical delivery and has at least one passageway through it, connecting the core of the dosage form with the external environment, wherein a size of the passageway(s) is from 100μ
to 1000μ
.
- (a) a solid core comprising a pharmaceutically active agent that has solubility limitations due to inherent hydrophobicity or to high drug load, wherein high drug load means that at least 30% by weight of the dosage form is the at least one active agent, a non-swelling osmotic agent and from 1 to 10% by weight of the core of meglumine, as a solubilizer, wherein the pharmaceutically active agent, non-swelling osmotic agent and meglumine are all present as a homogeneous mixture in at least one layer, and when said core comprises more than one layer, each layer comprises at least one pharmaceutically active agent, and (b) a semipermeable wall that surrounds the core, maintains its integrity during pharmaceutical delivery and has at least one passageway through it, connecting the core of the dosage form with the external environment, wherein a size of the passageway(s) is from 100μ
Specification