pH triggered targeted controlled release systems for the delivery of pharmaceutical active ingredients
First Claim
1. A multi-component controlled release composition comprising:
- a plurality of solid nano-spheres encapsulated in a pH-sensitive or salt-sensitive micro-sphere, said pH-sensitive or salt-sensitive micro-sphere being formed of a pH-sensitive or salt-sensitive matrix material, anda first pharmaceutical active agent incorporated by dispersion into a hydrophobic matrix forming the core of said plurality of solid nano-spheres or incorporated into both said hydrophobic matrix of said plurality of solid nano-spheres by dispersion and said matrix material of said micro-sphere, wherein said nano-spheres contact said matrix material of said microsphere, wherein said solid nano-spheres are formed of a wax material that has a melting point in the range of between about 25 degrees C. and about 150 degrees C. wherein said first pharmaceutical active agent is incorporated in said hydrophobic matrix of said solid nano-spheres and further comprising a second pharmaceutical active agent homogeneously incorporated in said pH-sensitive or salt-sensitive matrix material of said microsphere wherein said pH-sensitive or salt-sensitive matrix material of said microsphere releases said second active agent upon contact with a solution having a predetermined pH or predetermined salt concentration,wherein said first pharmaceutical active agent and said second pharmaceutical active agent are not the same,wherein said first pharmaceutical active is released continuously thereafter for an extended period of time,and wherein said micro-sphere has a size of from about 20 to about 100 microns and each of said nano-spheres has an average size of about 0.01 to about 5 microns.
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Accused Products
Abstract
The present invention relates to a novel pH triggered, targeted controlled release system. The controlled delivery system of the present invention is substantially a free-flowing powder formed of solid hydrophobic nano-spheres comprising pharmaceutical active ingredients that are encapsulated in a pH sensitive micro-spheres. The invention also relates to the processes for preparing the compositions and processes for using same. The controlled release system can be used to target and control the release of pharmaceutical active ingredients onto certain regions of the gastrointestinal tract including the stomach and the small intestine. The invention further pertains to pharmaceutical products comprising the controlled release system of the present invention.
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Citations
58 Claims
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1. A multi-component controlled release composition comprising:
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a plurality of solid nano-spheres encapsulated in a pH-sensitive or salt-sensitive micro-sphere, said pH-sensitive or salt-sensitive micro-sphere being formed of a pH-sensitive or salt-sensitive matrix material, and a first pharmaceutical active agent incorporated by dispersion into a hydrophobic matrix forming the core of said plurality of solid nano-spheres or incorporated into both said hydrophobic matrix of said plurality of solid nano-spheres by dispersion and said matrix material of said micro-sphere, wherein said nano-spheres contact said matrix material of said microsphere, wherein said solid nano-spheres are formed of a wax material that has a melting point in the range of between about 25 degrees C. and about 150 degrees C. wherein said first pharmaceutical active agent is incorporated in said hydrophobic matrix of said solid nano-spheres and further comprising a second pharmaceutical active agent homogeneously incorporated in said pH-sensitive or salt-sensitive matrix material of said microsphere wherein said pH-sensitive or salt-sensitive matrix material of said microsphere releases said second active agent upon contact with a solution having a predetermined pH or predetermined salt concentration, wherein said first pharmaceutical active agent and said second pharmaceutical active agent are not the same, wherein said first pharmaceutical active is released continuously thereafter for an extended period of time, and wherein said micro-sphere has a size of from about 20 to about 100 microns and each of said nano-spheres has an average size of about 0.01 to about 5 microns. - 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, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 39)
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37. A pharmaceutical composition comprising a pharmaceutically and physiologically suitable carrier and a controlled release composition, the controlled release composition comprising:
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a plurality of solid nano-spheres encapsulated in a pH-sensitive or salt-sensitive micro-sphere, said pH-sensitive or salt-sensitive micro-sphere being formed of a pH-sensitive or salt-sensitive matrix material, wherein said micro-sphere has a size of from about 20 to about 100 microns and each of said nano-spheres has an average size of about 0.01 to about 5 microns, wherein said solid nano-spheres are formed of a wax material that has a melting point in the range of between about 25 degrees C. and about 150 degrees C. and a first pharmaceutical active agent incorporated into said plurality of solid nano-spheres or into both said microsphere or said nano-sphere, wherein said active agent is dispersed throughout a hydrophobic matrix of said solid nano-sphere or said matrix material of said micro sphere in a quantity sufficient for administration in a single or multiple dose regimen to a mammal, and wherein the hydrophobic nano-spheres contact said matrix material of said microsphere. - View Dependent Claims (38)
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40. A method for delivering an active substance to a preselected environment;
- said method comprising introducing to said environment a controlled release composition comprising;
a plurality of solid nano-spheres, said plurality of solid nano-spheres being encapsulated in a pH-sensitive or salt-sensitive microsphere, wherein said solid nano-spheres are formed of a wax material that has a melting point in the range of between about 25 degrees C. and about 150 degrees C. said pH-sensitive or salt-sensitive microsphere being formed of a pH-sensitive or salt-sensitive matrix material, and a first pharmaceutical active agent incorporated into a hydrophobic matrix of said plurality of solid nano-spheres or said microsphere or in both said hydrophobic matrix of said plurality of solid nano-spheres and said micro-sphere, wherein said active agent is dispersed throughout said solid nano-sphere or said matrix material of said microsphere, wherein said hydrophobic nano-spheres contact said pH-sensitive or salt-sensitive matrix material of said microsphere;wherein said micro-sphere has a size of from about 20 to about 100 microns and each of said nano-spheres has an average size of about 0.01 to about 5 microns, and wherein introducing said composition into said environment permits degradation of said composition and release of said active agent. - View Dependent Claims (41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57)
- said method comprising introducing to said environment a controlled release composition comprising;
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58. A controlled release composition comprising:
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a first active agent; a plurality of solid nano-spheres formed of a hydrophobic matrix at its core;
wherein said solid nano-spheres are formed of a wax material that has a melting point in the range of between about 25 degrees C. and about 150 degrees C. anda micro-sphere formed of a pH-sensitive or salt-sensitive matrix; wherein said first active agent is incorporated by dispersion in and dispersed throughout said hydrophobic matrix of said nano-spheres and said pH-sensitive or salt-sensitive matrix of said microsphere, wherein said first pharmaceutical active agent is incorporated in said hydrophobic matrix of said solid nano-spheres and further comprising a second pharmaceutical active agent homogeneously incorporated in said pH-sensitive or salt-sensitive matrix material of said micro sphere wherein said pH-sensitive or salt-sensitive matrix material of said microsphere releases said second active agent upon contact with a solution having a predetermined pH or predetermined salt concentration, wherein said first pharmaceutical active agent and said second pharmaceutical active agent are not the same, and, wherein said microsphere has a size of from about 20 to about 100 microns and each of said nano-spheres has an average size of about 0.01 to about 5 microns.
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Specification