NOVEL METHODS AND COMPOSITION FOR DELIVERING MACROMOLECULES TO OR VIA THE RESPIRATORY TRACT
First Claim
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1. A pharmaceutical composition capable of providing increased bioavailability of a macromolecule upon administration to or via the respiratory tract, the composition comprising:
- a plurality of lipid-based microstructures, the lipid-based microstructures comprising;
(a) a major lipid excipient comprising a major amount of the lipid-based microstructure based on the total weight of the microstructure, the major lipid excipient comprising at least one lipid excipient; and
(b) a minor co-excipient comprising a minor amount of the lipid-based microstructure based on the total weight of the microstructure, the minor amount being lesser than the major amount, and wherein the lipid-based microstructure is formulated so as to release at least about 95% of the macromolecule incorporated therein within about 30 minutes after administration to or via the respiratory tract to thereby at least partially avoid scavenging by bronchoalveolar macrophages and/or a mucociliary clearance after the administration to thereby improve the bioavailability of the macromolecule.
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Abstract
A composition comprises a lipid-based microstructure with at least one bioactive macromolecule. The composition provides improved bioavailability and is capable of rapidly releasing a bioactive macromolecule. It is believed that the improved bioavailability is due, at least in part, to the reduction of scavenging by bronchoalveolar macrophages and/or mucociliary clearance.
98 Citations
54 Claims
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1. A pharmaceutical composition capable of providing increased bioavailability of a macromolecule upon administration to or via the respiratory tract, the composition comprising:
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a plurality of lipid-based microstructures, the lipid-based microstructures comprising;
(a) a major lipid excipient comprising a major amount of the lipid-based microstructure based on the total weight of the microstructure, the major lipid excipient comprising at least one lipid excipient; and
(b) a minor co-excipient comprising a minor amount of the lipid-based microstructure based on the total weight of the microstructure, the minor amount being lesser than the major amount, and wherein the lipid-based microstructure is formulated so as to release at least about 95% of the macromolecule incorporated therein within about 30 minutes after administration to or via the respiratory tract to thereby at least partially avoid scavenging by bronchoalveolar macrophages and/or a mucociliary clearance after the administration to thereby improve the bioavailability of the macromolecule. - 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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27. A pharmaceutical composition capable of providing improved bioavailability, the composition comprising:
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a plurality of lipid-based microstructures comprising;
(a) about 5% to about 89% w/w of a macromolecule;
(b) about 10% to about 89% w/w of a major lipid excipient; and
(c) about 0.5% to about 5% w/w of an excipient comprising a detergent surfactant;
wherein the lipid-based microstructures are formulated so as to release at least about 95% of the macromolecule from the lipid-based microstructures within about 30 minutes after exposure to an aqueous environment. - View Dependent Claims (28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45)
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46. A pharmaceutical composition capable of providing bioavailability, the composition comprising:
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a plurality of lipid-based microstructures comprising;
(a) about 10% to about 89% w/w of a major lipid excipient comprising at least one phosphatides having a hydrocarbon chain length ranging from 5 to 10 carbon atoms;
(b) about 5% to about 89% w/w of a macromolecule; and
(c) about 5% to about 50% w/w of at least one minor carbohydrate excipient;
wherein the lipid-based microstructures are formulated so as to release at least about 95% of the bioactive macromolecules from the lipid-based microstructures within about 30 minutes after administration to or via the respiratory tract of the patient. - View Dependent Claims (47, 48, 49, 50, 51, 52, 53, 54)
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Specification
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Current AssigneeNovartis Pharma AG (Novartis Ag)
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Original AssigneeNovartis Pharma AG (Novartis Ag)
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InventorsSmith, Dan, Dellamary, Luis, BOT, Adrian
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Application NumberUS11/551,166Publication NumberTime in Patent OfficeDaysField of SearchUS Class Current424/45CPC Class CodesA61K 9/127 LiposomesA61K 9/1617 Organic compounds, e.g. pho...A61P 3/10 for hyperglycaemia, e.g. an...A61P 37/00 Drugs for immunological or ...
