Claims for Patent: 8,241,670

Summary for Patent: 8,241,670

Title:	Compositions capable of facilitating penetration across a biological barrier
Abstract:	This invention relates to novel penetrating compositions including one or more effectors included within a water soluble composition, immersed in a hydrophobic medium The invention also relates to methods of treating or preventing diseases by administering such penetrating compositions to affected subjects.
Inventor(s):	Ben-Sasson; Shmuel A. (Jerusalem, IL)
Assignee:	Chiasma Inc. (Newton Centre, MA)
Application Number:	11/547,568
Patent Claims:	1. A method for producing an oral administration composition, the method comprising: (i) providing a therapeutically effective amount of at least one effector in an aqueous composition, wherein said aqueous composition comprises a fatty acid salt selected from: sodium octanoate, sodium decanoate, sodium dodecanoate, and combinations thereof and wherein said effector comprises a peptide; (ii) evaporating the aqueous composition by lyophilizing said aqueous composition to produce a lyophilizate comprising a water soluble composition comprising the fatty acid salt; (iii) suspending the lyophilizate comprising a water soluble composition comprising the fatty acid salt in a hydrophobic medium to produce a suspension, wherein said hydrophobic medium is selected from the group consisting of aliphatic molecules, cyclic molecules, aromatic molecules and combinations thereof; and (iv) further comprising a lecithin, a bile salt or a non-ionic detergent. 2. The method of claim 1, wherein said at least one peptide effector comprises an impermeable molecule selected from the group consisting of: insulin; erythropoietin (EPO); glucagon-like peptide 1 (GLP-1); melanocyte stimulating hormone (.alpha.MSH); parathyroid hormone (PTH); peptide YY amino acids 3-36 (PYY(3-36)); interleukin-2 (IL-2); a 1-antitrypsin; granulocyte/monocyte colony stimulating factor (GM-CSF); granulocyte colony stimulating factor (G-CSF); T20; anti-TNF antibodies; interferon .alpha.; interferon .beta.; interferon .gamma.; luteinizing hormone releasing hormone (LHRH) analog; brain-derived natriuretic peptide (BNP); a hormone; a growth factor; an incretin; a neurotrophic factor; an antibody; a monoclonal antibody; an antibody fragment; an immunomodulator; a soluble receptor; an enzyme; and Caspofungin. 3. The method of claim 1, wherein said fatty acid salt is sodium octanoate. 4. The method of claim 1, wherein said aliphatic molecules are selected from the group consisting of: mineral oil, paraffin, fatty acids, mono-glycerides, di-glycerides, tri-glycerides, such as long chain triglycerides, medium chain triglycerides, short chain triglycerides, ethers, and esters, wherein said cyclic hydrophobic medium is selected from the group consisting of: terpenoids, cholesterol, cholesterol derivatives such as cholesterol sulfate, and cholesterol esters of fatty acids, or wherein said aromatic hydrophobic medium is benzyl benzoate. 5. The method of claim 4, wherein said aliphatic molecules are medium chain triglycerides. 6. The method of claim 4, wherein said long chain triglyceride is castor oil. 7. The method of claim 4, wherein said short chain triglyceride is glyceryl tributyrate. 8. The method of claim 1, wherein said water soluble composition further comprises a stabilizer. 9. The method of claim 8, wherein said water soluble composition further comprises polyvinylpyrrolidone. 10. The method of claim 8, wherein said water soluble composition further comprises polyvinylalcohol. 11. The method of claim 1, wherein said at least one peptide effector comprises an impermeable molecule selected from the group consisting of: parathyroid hormone amino acids 1-34 (PTH 1-34); growth hormone; calcitonin; luteinizing hormone (LH); follicle-stimulating hormone (FSH); enkephalin; dalargin; kytotorphin; basic fibroblast growth factor (bFGF); hirudin and hirulog. 12. An oral administration composition obtained by the method of claim 1, the composition comprising: (i) a therapeutically effective amount of at least one effector in an aqueous composition, wherein said aqueous composition comprises a fatty acid salt selected from: sodium octanoate, sodium decanoate, sodium dodecanoate, and combinations thereof, and wherein said effector comprises a peptide; (ii) a lyophilizate comprising a water soluble composition comprising the fatty acid salt; (iii) a hydrophobic medium, wherein said hydrophobic medium is selected from the group consisting of aliphatic molecules, cyclic molecules, aromatic molecules and combinations thereof; and (iv) a lecithin, a bile salt or a non-ionic detergent. 13. The therapeutic composition of claim 12, comprising a non-ionic detergent. 14. The therapeutic composition of claim 13, wherein the non-ionic detergent is a cremophore, a polyethylene glycol fatty alcohol ether, Solutol HS15, a poloxamer or a sorbitan fatty acid ester. 15. The therapeutic composition of claim 14, wherein the non-ionic detergent is a sorbitan fatty acid ester. 16. The therapeutic composition of claim 12, wherein the composition further comprises a monoglyceride. 17. The therapeutic composition of claim 16, wherein the monoglyceride is glyceryl monooctanoate. 18. The therapeutic composition of claim 12, which further comprises an alcohol selected from the group consisting of linear alcohols, branched alcohols, cyclical alcohols, aromatic alchohols and combinations thereof. 19. The therapeutic composition of claim 12, wherein said composition is contained within a capsule. 20. The therapeutic composition of claim 12, wherein said composition is in the form of a tablet. 21. The therapeutic composition of claim 12, further comprising a pharmaceutically acceptable excipient, a pharmaceutically acceptable carrier, or combinations thereof. 22. The therapeutic composition of claim 16, wherein the monoglyceride is glyceryl monooctanoate, glyceryl monodecanoate, glyceryl monolaurate, glyceryl monomyristate, glyceryl monostearate, glyceryl monopalmitate or glyceryl monooleate.

Details for Patent 8,241,670

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Nps Pharmaceuticals, Inc.	NATPARA	parathyroid hormone	For Injection	125511	01/23/2015		2039-02-26