Claims for Patent: 9,533,048

Summary for Patent: 9,533,048

Title:	Mucosal delivery of drugs
Abstract:	The present invention provides a composition comprising or consisting of components (a) (i) at least one mono-alkanoyl glycerol ester, wherein alkanoyl is selected from C.sub.4 to C.sub.21 alkanoyl, preferably from octanoyl and decanoyl; and (b) (i) at least one compound selected from cholesterol, phosphatidyl cholines and phosphatidyl glycerols, wherein the acyl moieties of the phosphatidyl moieties are independently selected from C.sub.6 to C.sub.21 alkanoyl and C.sub.6 to C.sub.21 alkenoyl.
Inventor(s):	Botti; Paolo (Vessy/Geneva, CH), Tchertchian; Sylvie (Monnetier-Mornex, FR)
Assignee:	ARISGEN SA (Plan-les-Ouates, CH)
Application Number:	14/122,182
Patent Claims:	1. A pharmaceutical or diagnostic composition, comprising as a pharmaceutically or diagnostically active agent, a peptide, or polypeptide, and, as a delivery system for mucosal delivery of the pharmaceutically or diagnostically active agent, components (a) and (b) comprising (a) (i) at least one mono-alkanoyl glycerol ester, wherein alkanoyl is selected from C.sub.8 to C.sub.10 alkanoyl; (ii) an alkanoic acid selected from C.sub.2 to C.sub.21; and (b) (i) at least one compound selected from cholesterol, phosphatidyl cholines, lysophosphatidylcholines and phosphatidyl glycerols, wherein the acyl moieties of the phosphatidyl moieties are independently selected from C.sub.6 to C.sub.21 alkanoyl and C.sub.6 to C.sub.21 alkenoyl, and wherein the delivery system contains no water other than as an impurity. 2. The pharmaceutical or diagnostic composition according to claim 1, wherein said (a)(ii) alkanoic acid is selected from C.sub.6 to C.sub.12. 3. The pharmaceutical or diagnostic composition according to claim 1, wherein said (a)(ii) alkanoic acid is selected from C.sub.8 to C.sub.10. 4. A pharmaceutical or diagnostic composition, comprising as a pharmaceutically or diagnostically active agent, a peptide or polypeptide, and as a delivery system for mucosal delivery of the pharmaceutically or diagnostically active agent, as components (a) and (b) comprising (a) (i) at least one mono-alkanoyl glycerol ester, wherein alkanoyl is selected from C.sub.8 to C.sub.10 alkanoyl; (ii) an alkenoic acid selected from oleic, linoleic and elaidic acid; and (b) (i) at least one compound selected from cholesterol, phosphatidyl cholines, lysophosphatidylcholines and phosphatidyl glycerols, wherein the acyl moieties of the phosphatidyl moieties are independently selected from C.sub.6 to C.sub.21 alkanoyl and C.sub.6 to C.sub.21 alkenoyl, and wherein the delivery system contains no water other than as an impurity. 5. The composition according to claim 1, wherein component (a) comprises two mono-alkanoyl glycerol esters. 6. A pharmaceutical or diagnostic composition according to claim 1 or 4, further comprising, as a component (c)(i) a cyclic compound of formula (I), formula (I) being defined as follows ##STR00009## wherein A, B independently in each occurrence is alkane-i,j-diyl having k carbon atoms, i and independently j being less than or equal k and k being selected from 1 to 10, wherein said alkane-i,j-diyl (1) may comprise one or more double bonds; (2) is optionally substituted; and/or (3) comprises a cycle, wherein the total number of cycles being cyclic sugars in said compound is selected from 0 to 4 and is less than p(n+m); X,Y independently in each occurrence is a biocompatible functional group comprising at least one oxygen atom or two sulfur atoms; n, m independently of each other are selected from 0 to 20; p is selected from 1 to 10; n+m is equal or greater than 1; and p(n+m) is selected from 3 to 30; wherein said cyclic compound is capable of forming a complex with a protonated primary amino group, a protonated secondary amino group, a protonated guanidinium group, and/or a metal ion. 7. The pharmaceutical or diagnostic composition according to claim 6, wherein component (c) has a log P value that differs from the log P value of a mixture of components (a) and (b). 8. The pharmaceutical or diagnostic composition according to claim 6, wherein said pharmaceutically active agent is exendin-4, parathyroid hormone, calcitonin, desmopressin and/or insulin. 9. The composition according to claim 5, wherein the two mono-alkanoyl glycerol esters are mono-octanoyl glycerol ester and mono-decanoyl glycerol ester. 10. A method of mucosal delivery to a human or other mammal of a pharmaceutically or diagnostically active agent, the method comprising orally administering the composition of claim 5 to the human or other mammal. 11. A method of mucosal delivery to a human or other mammal of a pharmaceutically or diagnostically active agent, the method comprising orally administering the composition of claim 6 to the human or other mammal. 12. A method of mucosal delivery to a human or other mammal of a pharmaceutically or diagnostically active agent, the method comprising orally administering the composition of claim 7 to the human or other mammal. 13. A method of mucosal delivery to a human or other mammal of a pharmaceutically or diagnostically active agent, the method comprising orally administering the composition of claim 8 to the human or other mammal. 14. A method of mucosal delivery to a human or other mammal of a pharmaceutically or diagnostically active agent, the method comprising orally administering the composition of claim 9 to the human or other mammal. 15. A method of mucosal delivery to a human or other mammal of a pharmaceutically or diagnostically active agent, the method comprising orally administering the composition of claim 1 to the human or other mammal. 16. A method of mucosal delivery to a human or other mammal of a pharmaceutically or diagnostically active agent, the method comprising orally administering the composition of claim 4 to the human or other mammal.

Details for Patent 9,533,048

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Nps Pharmaceuticals, Inc.	NATPARA	parathyroid hormone	For Injection	125511	01/23/2015		2031-05-25