Claims for Patent: 10,188,621

Summary for Patent: 10,188,621

Title:	Crystalline polymorphic forms of monosodium N-[-8-(2-hydroxybenzoyl)amino]caprylate
Abstract:	The present invention relates to crystalline polymorphic forms of monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate (\"SNAC\"), including two hydrates, a methanol solvate, and an ethanol solvate, of SNAC. More specifically, the present invention provide six polymorphic forms of SNAC (hereafter referred to as Forms I-VI). The present invention also provides an amorphous form of SNAC.
Inventor(s):	Levchik; Halina (Croton On Hudson, NY), Majuru; Shingai (Brewster, NY), Singh; Brahma (Jamaica, NY), Harris; Jamila (Flushing, NY)
Assignee:	EMISPHERE TECHNOLOGIES, INC. (Roseland, NJ)
Application Number:	15/668,236
Patent Claims:	1. A method for preparing a pharmaceutical composition comprising a monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate exhibiting an X-ray powder diffraction pattern having a peak at 2.98.+-.0.2.degree. 2.THETA. and at least one active agent, wherein the active agent is a peptide, the method comprising (i) wet granulating monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate, in the presence of the at least one active agent and one or more pharmaceutically acceptable excipients, to yield a first mixture comprising a trihydrate of monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate, (ii) drying the first mixture comprising the trihydrate of monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate to obtain a second mixture comprising monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate exhibiting an X-ray powder diffraction pattern having a peak at 2.98.+-.0.2.degree. 2.THETA. , and (iii) directly compressing the second mixture to form the pharmaceutical composition. 2. The method of claim 1, wherein the dried monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate formed in step (ii) exhibits an X-ray powder diffraction pattern having peaks at both 2.98.+-.0.2.degree. 2.THETA. and 15.72.+-.0.2.degree. 2.THETA.. 3. A pharmaceutical composition comprising a directly compressed mixture of (a) monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate exhibiting an X-ray powder diffraction pattern having a peak at 2.98.+-.0.2.degree. 2.THETA. and (b) at least one active agent, wherein the active agent is a peptide. 4. The pharmaceutical composition of claim 3, wherein the pharmaceutical composition is a tablet. 5. The pharmaceutical composition of claim 3, wherein the pharmaceutical composition comprises from 50 to 98% by weight of crystalline anhydrous monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate, based on the total weight of monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate in the pharmaceutical composition. 6. The pharmaceutical composition of claim 3, wherein the mixture is not prepared by or subjected to wet granulation. 7. The pharmaceutical composition of claim 3, wherein the peptide is insulin. 8. The pharmaceutical composition of claim 3, wherein the peptide is parathyroid hormone. 9. The method of claim 1, wherein the pharmaceutical composition is a tablet. 10. The method of claim 1, wherein the pharmaceutical composition comprises from 50 to 98% by weight of crystalline anhydrous monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate, based on the total weight of monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate in the pharmaceutical composition. 11. The method of claim 1, wherein the peptide is insulin. 12. The method of claim 1, wherein the peptide is parathyroid hormone.

Details for Patent 10,188,621

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Nps Pharmaceuticals, Inc.	NATPARA	parathyroid hormone	For Injection	125511	01/23/2015		2024-05-06