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Details for Patent: 6,916,489

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Details for Patent: 6,916,489

Title: Active agent transport systems
Abstract:Methods for transporting a biologically active agent across a cellular membrane or a lipid bilayer. A first method includes the steps of: (a) providing a biologically active agent which can exist in a native conformational state, a denatured conformational state, and an intermediate conformational state which is reversible to the native state and which is conformationally between the native and denatured states; (b) exposing the biologically active agent to a complexing perturbant to reversibly transform the biologically active agent to the intermediate state and to form a transportable supramolecular complex; and (c) exposing the membrane or bilayer to the supramolecular complex, to transport the biologically active agent across the membrane or bilayer. The perturbant has a molecular weight between about 150 and about 600 daltons, and contains at least one hydrophilic moiety and at least one hydrophobic moiety. The supramolecular complex comprises the perturbant non-covalently bound or complexed with the biologically active agent. In the present invention, the biologically active agent does not form a microsphere after interacting with the perturbant. A method for preparing an orally administrable biologically active agent comprising steps (a) and (b) above is also provided as are oral delivery compositions. Additionally, mimetics and methods for preparing mimetics are contemplated.
Inventor(s): Milstein; Sam J. (Larchmont, NY), Barantsevitch; Evgueni (New Rochelle, NY), Leone-Bay; Andrea (Ridgefield, CT), Wang; Nai Fang (Long Island City, NY), Sarubbi; Donald J. (Bronxville, NY), Santiago; Noemi B (Hawthorne, NY)
Assignee: Emisphere Technologies, Inc. (Tarrytown, NY)
Filing Date:Sep 25, 2002
Application Number:10/255,237
Claims:1. A method for preparing a composition, said method comprising mixing: (A) at least one biologically-active agent; and (B) a compound having the formula:

wherein: Ar is a substituted or unsubstituted phenyl or naphthyl, ##STR25## R.sup.15 has the formula ##STR26## R.sup.15 is C.sub.1 to C.sub.24 alkyl, C.sub.2 to C.sub.24 alkenyl, phenyl, naphthyl, (C.sub.1 to C.sub.10 alkyl) phenyl, (C.sub.2 to C.sub.10 alkenyl) phenyl, (C.sub.1 to C.sub.10 alkyl) naphthyl, (C.sub.2 to C.sub.10 to alkenyl) naphthyl, phenyl (C.sub.1 to C.sub.10 alkyl), phenyl (C.sub.2 to C.sub.10 alkenyl), naphthyl (C.sub.1 to C.sub.10 alkyl), and naphthyl (C.sub.2 to C.sub.10 alkenyl); R.sup.15 is optionally substituted with C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkenyl, C.sub.1 to C.sub.4 alkoxy, --OH, --SH, --CO.sub.2 R.sup.17, cycloalkyl, cycloalkenyl, heterocyclic alkyl, alkaryl, heteroaryl, heteroalkaryl, or any combination thereof; R.sup.17 is hydrogen, C.sub.1 to C.sub.4 alkyl or C.sub.2 to C.sub.4 alkenyl; R.sup.15 is optionally interrupted by oxygen, nitrogen, sulfur or any combination thereof; and R.sup.16 is hydrogen, C.sub.1 to C.sub.4 alkyl or C.sub.2 to C.sub.4 alkenyl; and n is from 1 to 5.

2. An oral delivery composition comprising: (a) a biologically active agent in an intermediate conformational state non-covalently complexed with (b) a complexing perturbant having the formula:

wherein: Ar is a substituted or unsubstituted phenyl or naphthyl; ##STR27## R.sup.14 has the formula ##STR28## R.sup.15 is C.sub.1 to C.sub.24 alkyl, C.sub.2 to C.sub.24 alkenyl, phenyl, naphthyl, (C.sub.1 to C.sub.10 alkyl) phenyl, (C.sub.2 to C.sub.10 alkenyl) phenyl, (C.sub.1 to C.sub.10 alkyl) naphthyl, (C.sub.2 to C.sub.10 alkenyl) naphthyl, phenyl (C.sub.1 to C.sub.10 alkyl), phenyl (C.sub.2 to C.sub.10 alkenyl), naphthyl (C.sub.1 to C.sub.10 alkyl), and naphthyl (C.sub.2 to C.sub.10 alkenyl); R.sup.15 is optionally substituted with C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkenyl, C.sub.1 to C.sub.4 alkoxy, --OH, --SH, --CO.sub.2 R.sup.17, cycloalkyl, cycloalkenyl, heterocyclic alkyl, alkaryl, heteroaryl, heteroalkaryl, or any combination thereof; R.sup.17 is hydrogen, C.sub.1 to C.sub.4 alkyl or C.sub.2 to C.sub.4 alkenyl; R.sup.15 is optionally interrupted by oxygen, nitrogen, sulfur or any combination thereof; and R.sup.16 is hydrogen, C.sub.1 to C.sub.4 alkyl or C.sub.2 to C.sub.4 alkenyl; and n is from 1 to 5.

3. The composition according to claim 2, wherein Ar is substituted or unsubstituted phenyl, Y is ##STR29##

--C--, R.sup.15 is C.sub.1 to C.sub.24 alkyl, (C.sub.1 to C.sub.10 alkyl) phenyl; or phenyl (C.sub.1 to C.sub.10 alkyl) and n is equal to 1.

4. The composition according to claim 2, wherein said biologically-active agent is a pharmacological agent or a therapeutic agent.

5. The composition according to claim 2, wherein said biologically-active agent is selected from the group consisting of a peptide, a polysaccharide, a mucopolysaccharide, a carbohydrate, a lipid, a pesticide or any combination thereof.

6. The composition according to claim 2, wherein said biologically-active agent is a peptide.

7. The composition according to claim 6, wherein said biologically-active agent is a hormone.

8. The composition according to claim 2, wherein said biologically-active agent is a mucopolysaccharide.

9. The composition according to claim 2, wherein said biologically-active agent is a lipid.

10. The composition according to claim 2, wherein said biologically-active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-I, interleukin-II, insulin, heparin, low molecular weight heparin, calcitonin, erythropoetin, atrial naturetic factor, an antigen, a monoclonal antibody, somatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, cromolyn sodium, vancomycin, desferrioxamine, an anti-fungal, an anti-microbial agent or any combination thereof.

11. The composition according to claim 10, wherein said biologically-active agent is selected from the group consisting of an interferon, insulin, human growth hormone, heparin, low molecular weight heparin, calcitonin, cromolyn sodium, anti-fungal, and an anti-microbial agent.

12. The composition according to claim 10, wherein said biologically-active agent is an interferon.

13. The composition according to claim 10, wherein said biologically-active agent is insulin.

14. The composition according to claim 10, wherein said biologically-active agent is human growth hormone.

15. The composition according to claim 10, wherein said biologically-active agent is heparin.

16. The composition according to claim 15, wherein said biologically-active agent is low molecular weight heparin.

17. The composition according to claim 10, wherein said biologically-active agent is calcitonin.

18. The composition according to claim 10, wherein said biologically-active agent is cromolyn sodium.

19. The composition according to claim 10, wherein said biologically-active agent is an anti-microbial.

20. A dosage unit form comprising (A) a composition according to claim 2, and (B) (a) an excipient, (b) a diluent, (c) a disintegrant, (d) a lubricant, (e) a plasticizer, (f) a colorant, (g) a dosing vehicle, or (h) any combination thereof.

21. A dosage unit form according to claim 20, comprising a tablet, a capsule, or a liquid.

22. A method for administering a biologically-active agent to an animal in need of said agent said method comprising administering orally to said animal the composition as defined in claim 2.
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