Crystalline polymorphic forms of monosodium N-[-8-(2-hydroxybenzoyl)amino]caprylate
AssigneeEmisphere Technologies, Inc.
InventorsHalina Levchik, Shingai Majuru, Brahma Singh, Jamila Harris
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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.
Claims13
A method for administering an active agent to a human subject in need thereof comprising administering to the subject 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° 2Θ and (b) at least one active agent, wherein the active agent is a peptide.
A method for administering an active agent to a human subject in need thereof comprising administering to the subject 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° 2Θ and an active agent,
- wherein the active agent is a peptide, and
- wherein the pharmaceutical composition is prepared by a process 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° 2Θ, and
- (iii) directly compressing the second mixture to form the pharmaceutical composition.
A method for administering an active agent to a human subject in need thereof comprising administering to the subject a pharmaceutical composition comprising a milled mixture of (a) crystalline anhydrous monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate exhibiting an X-ray powder diffraction pattern having a peak at 2.98±0.2° 2Θ and (b) at least one active agent, wherein the active agent is a peptide.
Dependencies are inferred from the claim text.