Claims for Patent: 6,485,707

Summary for Patent: 6,485,707

Title:	Modulated release particles for aerosol delivery
Abstract:	A modulated release aerosol formulation is disclosed. The formulation comprises a polymer, e.g. Silica gel, fumed silica gel, having a selected medicament associated therewith, and a fluid carrier for carrying and delivering the construct.
Inventor(s):	Zhu; Yaping (Highland Park, NJ), Adjei; Akwete L. (Bridgewater, NJ)
Assignee:	Aeropharm Technology Incorporated (Edison, NJ)
Application Number:	09/784,671
Patent Claims:	1. A modulated release aerosol formulation, which consists essentially of: a. a polymeric construct comprising a polymer selected from the group consisting of silica gel, fumed silica gel, silicic acid, disilicic acid, trisilicic acid, metasilicic acid, and orthosilicic acid, in their free or salt forms; silicon dioxide in either of its amporphous, crystalline, or precipitated forms; talc; attapulgite; micas; montmorilonite; kaolin; aluminum oxide; bentonite; pumice; silanes; siloxanes and a mixture of any of the foregoing polymers; and b. a biotherapeutic medicament associated with said construct. 2. A modulated release aerosol formulation, which consists essentially of: a. a selected particulate medicament; b. a polymer selected from the group consisting of silica gel, fumed silica gel, silicic acid, disilicic acid, trisilicic acid, metasilicic acid, and orthosilicic acid, in their free or salt forms; silicon dioxide in either of its amporphous, crystalline, or precipitated forms; talc; attapulgite; micas; montmorilonite; kaolin; aluminum oxide; bentonite; pumice; silanes; siloxanes, having said medicament associated therewith; and c. a fluid carrier for carrying and transporting said particles of said associated polymer. 3. The formulation as defined in claim 1 wherein said polymer is present in an amount ranging from about 0.000001 to about 10 percent by weight of the total weight of the formulation. 4. The formulation as defined in claim 1 wherein said medicament is a protein or peptide medicament having a molecular size ranging from about 1 K Dalton to about 150 K Daltons. 5. The formulation as defined in claim 4 wherein said medicament is selected from the group consisting of an insulin, an insulin analog, an amylin, an immunodilating protein, an interleukin, an inteferon, an erythropoietan, a heparin, a thrombolytic, an antitrypsin, an anti-protease, a hormone, a growth factor, an enzyme, a nucleic acid, an immunoglobulin, an antibiotic, an antiinfective, a calcitonin, a hematopoietic factor, a vaccine, a vasoactive peptide, an antisense agent, an oligonucleotide, DNase, a cyclosporin, ribavirin or a mixture of any of the foregoing medicaments. 6. The formulation as defined in claim 4 wherein said medicament is selected from the group consisting of an insulin, an insulin analog, an amylin, glucagon, LH-RH, deltirex, leuprolide, gosorelin, nafarelin, octreotide, somatostatin, a calcitonin, parathyroid hormone, TRH, growth hormone-releasing hormone, G-CSF, G-SF, a cytokine, rhDNAse, a heparin, an oligoneucleotide, ribavarin, glucagon, acetohexamide, chlorpropamide, tolazemide, tolbutamide, glipizide, glyburide, metformin, phentolamine, tumor neurosis factor (TNF), nerve growth factor (NGF), macrophage-colony stimulating factor (M-CSF), heparinase, bone morphogenic protein (BMP), hANP, glucagon-like peptide (GLP-1), renin, bradykinin, a bacitracin, a polymyxin, a colistin, tyrocidine, a gramicidin, a monoclonal antibody, a vaccine or a mixture of any of the foregoing medicaments. 7. The formulation as defined in claim 2 wherein said fluid carrier is selected from the group of propellants consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane or a mixture thereof. 8. The formulation as defined in claim 2 wherein said fluid carrier is a compressed gas selected from the group consisting of air, carbon dioxide nitrogen and a mixture of any of the foregoing compressed gasses. 9. The formulation as defined in claim 2 wherein said fluid carrier is a hydrocarbon selected from the group consisting of n-butane, propane, isopentane and a mixture of any of the foregoing hydrocarbons. 10. A method of preparing a stable medicinal aerosol formulation according to claim 1, which comprises, (a) combining said selected medicament with said polymer to form said polymeric construct, wherein said medicament is associated with said polymer in an amount sufficient to provide a plurality of therapeutically effective doses; (b) combining said construct with a fluid carrier, where said carrier is present in an amount sufficient to transport and deliver a plurality of said therapeutically effective doses, to form a mixture; and (c) dispersing said mixture. 11. A method of treating in a human being or another animal a condition capable of treatment by dermal, sublingual, buccal, oral application or by oral or nasal inhalation, which comprises; administering a formulation according to claim 2 in an aerosol canister equipped with a metered dose vale. 12. A formulation according to claim 2 in an aerosol canister equipped with a metered dose valve. 13. A metered dose formulation containing a medicinal formulation, the formulation consisting essentially of: a. a particulate medicament in a therapeutically effective amount; b. a polymer selected from the group consisting of silica gel, fumed silica gel, silicic acid, disilicic acid, trisilicic acid, metasilicic acid, and orthosilicic acid, in their free or salt forms; silicon dioxide in either of its amporphous, crystalline, or precipitated forms; talc; attapulgite; micas; montmorilonite; kaolin; aluminum oxide; bentonite; pumice; silanes; siloxanes, or any mixture of the foregoing polymers with which said particulate medicament is associated to form a particulate polymeric construct; and c. a fluid carrier for carrying and transporting said particles of said associated polymer. 14. A modulated release formulation, which consists essentially of: a. a polymeric construct comprising a polymer selected from the group consisting of silica gel, fumed silica gel, silicic acid, disilicic acid, trisilicic acid, metasilicic acid, and orthosilicic acid, in their free or salt forms; silicon dioxide in either of its amporphous, crystalline, or precipitated forms; talc; attapulgite; micas; montmorilonite; kaolin; aluminum oxide, bentonite; pumice; silanes; siloxanes and a mixture of any of the foregoing polymers; b. a biotherapeutic medicament associated with said construct; c. a second medicament with which said biotherapeutic medicament is combined; and d. a fluid carrier for carrying and transporting said construct. 15. The formulation as defined in claim 14 wherein said biotherapeutic medicament is combined with a second medicament selected from the group consisting of amylin, insulin, a suitable anti-diabetic agent and a mixture of any of the foregoing medicaments. 16. The formulation as defined in claim 14 wherein said biotherapeutic medicament is combined with a second medicament from the group consisting of an amylin, an insulin, an insulin analog, a suitable anti-diabetic agent, an interleukin, an interferon, an erythropoietan, heparin, a thrombolytic, an antitrypsin, an anti-protease, a hormone, a growth factor, an enzyme, a nucleic acid, an immunoglobulin, an antibiotic, an antiinfective, a calcitonin, a hematopoietic factor, a vaccine, a vasoactive peptide, an antisense agent, an oligonucleotide, DNase, a cyclosporin, ribavirin and a mixture of any of the foregoing medicaments. 17. The formulation as defined in claim 16 wherein said second medicament is a suitable anti-diabetic agent.

Details for Patent 6,485,707

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Hoffmann-la Roche Inc.	PEGASYS COPEGUS COMBINATION PACK	peginterferon alfa-2a and ribavirin		125083	06/04/2004		2039-02-26
Schering Corporation A Subsidiary Of Merck & Co., Inc.	PEGINTRON/ REBETOL COMBO PACK	peginterferon alfa-2b and ribavirin		125196	06/13/2008		2039-02-26
Nps Pharmaceuticals, Inc.	NATPARA	parathyroid hormone	For Injection	125511	01/23/2015		2039-02-26