Claims for Patent: 11,129,869

Summary for Patent: 11,129,869

Title:	Pharmaceutical compositions
Abstract:	The present invention relates to an ionic complex comprising a cationic polypeptide and an anionic excipient selected from: a PEG-carboxylic acid; a fatty acid having 10 or more carbon atoms; an anionic phospholipid; and a combination thereof. The invention also relates to a pharmaceutical composition comprising the ionic complex of the invention and a pharmaceutically acceptable carrier. The cationic polypeptide of the ionic complex has pharmacological activity and the complex can provide a more desirable pharmacokinetic profile for the cationic polypeptide of the complex as compared to the cationic polypeptide alone following administration. As such, the invention also relates to the use of the ionic complex and pharmaceutical composition comprising same to treat a subject suffering from a disease or disorder that is responsive to the cationic polypeptide of the ionic complex.
Inventor(s):	Sharma; Shubh (Cranbury, NJ), Van Der Ploeg; Leonardus H. T. (Newton, MA), Henderson; Bart (Belmont, MA)
Assignee:	RHYTHM PHARMACEUTICALS, INC. (Boston, MA)
Application Number:	14/775,911
Patent Claims:	1. An ionic complex comprising: i) a cationic polypeptide represented by the following structural formula: ##STR00027## ii) methoxy(polyethylene glycol 2,000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine (mPEG-2,000-DSPE), and iii) carboxymethylcellulose (CMC), wherein the molar ratio of the cationic peptide to the mPEG-2,000-DSPE is between 1:3 to 1:6. 2. The ionic complex of claim 1, wherein the concentration of the cationic polypeptide is 10 mg/mL. 3. The ionic complex of claim 1, wherein the concentration of the mPEG-2,000-DSPE is 100 mg/mL. 4. The ionic complex of claim 1, wherein the concentration of the CMC is 8 mg/mL. 5. The ionic complex of claim 1, wherein the molar ratio of the cationic peptide to the mPEG-2,000-DSPE is 1:3. 6. The ionic complex of claim 1, wherein the molar ratio of the cationic peptide to the mPEG-2,000-DSPE is 1:4. 7. The ionic complex of claim 1, wherein the concentration of the cationic polypeptide is between 0.01 mg/mL to about 100 mg/mL. 8. The ionic complex of claim 1, wherein the concentration of the cationic polypeptide is between 1 mg/mL to about 50 mg/mL. 9. The ionic complex of claim 1, wherein the molar ratio of the cationic peptide to the mPEG-2,000-DSPE is 1:5. 10. The ionic complex of claim 1, wherein the molar ratio of the cationic peptide to the mPEG-2,000-DSPE is 1:6. 11. The pharmaceutical composition of claim 1, further comprising a preservative. 12. The pharmaceutical composition of claim 11, wherein the preservative comprises phenol or benzyl alcohol. 13. A pharmaceutical composition comprising the ionic complex of claim 1 and a pharmaceutically acceptable carrier. 14. The pharmaceutical composition of claim 13, wherein the concentration of the cationic polypeptide is between 0.01 mg/mL to about 100 mg/mL. 15. The pharmaceutical composition of claim 13, wherein the concentration of the cationic polypeptide is between 1 mg/mL to about 50 mg/mL. 16. The pharmaceutical composition of claim 13, wherein the ionic complex forms a drug depot in a physiological environment. 17. The ionic complex of claim 13, having the property that it forms a drug depot when delivered subcutaneously. 18. The pharmaceutical composition of claim 13, further comprising D-mannitol. 19. The pharmaceutical composition of claim 18, wherein the concentration of the D-mannitol is 22 mg/mL. 20. An ionic complex comprising: i) a cationic polypeptide represented by the following structural formula: ##STR00028## ii) methoxy(polyethylene glycol 2,000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine (mPEG-2,000-DSPE), and iii) carboxymethylcellulose (CMC), wherein the molar ratio of the cationic peptide to the mPEG-2,000-DSPE is between 1:3 to 1:6, and wherein the ionic complex has the property that it forms a drug depot in a physiological environment or when delivered subcutaneously. 21. The ionic complex of claim 20, having the property that it forms a drug depot in a physiological environment. 22. The ionic complex of claim 20, having the property that it forms a drug depot when delivered subcutaneously. 23. An ionic complex comprising: i) a cationic polypeptide represented by the following structural formula: ##STR00029## ii) methoxy(polyethylene glycol 2,000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine (mPEG-2,000-DSPE), and iii) carboxymethylcellulose (CMC), wherein the molar ratio of the cationic peptide to the mPEG-2,000-DSPE is between 1:3 to 1:6, and the ionic complex is made in a process consisting essentially of: a) preparing a mixture of mPEG-2,000-DSPE and CMC in an aqueous solution; and b) adding the cationic polypeptide to the mixture of step a); to thereby make the ionic complex. 24. An ionic complex comprising: i) a cationic polypeptide represented by the following structural formula: ##STR00030## ii) methoxy(polyethylene glycol 2,000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine (mPEG-2,000-DSPE), and iii) carboxymethylcellulose (CMC), and iv) D-mannitol, wherein the molar ratio of the cationic peptide to the mPEG-2,000-DSPE is between 1:3 to 1.6.