US 2017/0304190 A1 · pH DEPENDENT CARRIERS FOR TARGETED RELEASE OF PHARMACEUTICALS ALONG THE GASTROINTESTINAL TRACT, COMPOSITIONS THEREFROM, AND MAKING AND USING SAME

Abstract

Novel drug carriers capable of targeted and/or pH dependent release of biologically active agents into selected pH environments including the gastrointestinal (GI), ophthalmic, urinary, or reproductive tracts. Unexpectedly, carriers including free fatty acids (FFA) are able to deliver biologically active agents to various pH environments. Such targeted delivery is tailorable and useful for active agents that are: (a) injurious to the upper GI tract (esophagus, stomach, and duodenum), (b) acid labile, (c) impermeable/insoluble compounds in GI fluids, (d) susceptible to first pass metabolism, and/or (e) cause stomach irritation, upset, or dyspepsia.

Claims25

Dependent claims

1-23. (canceled)

A method of targeting release of a biologically active agent to the small intestine of a subject, comprising orally administering to the subject an ingestible pharmaceutical composition, wherein:

(i) the pharmaceutical composition comprises a suspension of a crystalline solid, biologically active agent in a non-aqueous liquid carrier, (ii) the weight ratio of the active agent to the non-aqueous liquid carrier is between about 50:1 and about 1:10, (iii) the pharmaceutical composition is a solid-in-oil suspension that is substantially free of water, and (iv) the non-aqueous carrier is an oil, wherein:
(a) the carrier comprises at least 10 wt % of free monocarboxylic acid having at least 8 carbons, wherein the monocarboxylic acid is liquid at room temperature;
(b) the carrier comprises from about 0.0001 wt. % to about 5 wt. % of zwitterionic phospholipids;
and
(c) the pharmaceutical composition releases a lesser amount of active agent at a pH of <3 than at pH>3,
wherein the composition is formulated in the absence of a solvent.

3 more elements

A method of targeting release of a biologically active agent to the small intestine of a subject, comprising orally administering to the subject an ingestible pharmaceutical composition, wherein:

(i) the pharmaceutical composition is made by admixing a solid biologically active agent into a non-aqueous liquid carrier, (ii) the composition is formulated for oral administration, (iii) the weight ratio of the active agent to the non-aqueous liquid carrier is between about 50:1 and about 1:10, and (iv) the non-aqueous liquid carrier is an oil, wherein:
(a) the carrier comprises at least about 10 wt % of a free monocarboxylic acid having at least 8 carbons, wherein the monocarboxylic acid is liquid at room temperature;
(b) the carrier is substantially free of water;
(c) the carrier comprises from about 0.0001 wt. % to about 5 wt. % of zwitterionic phospholipids;
and
(d) the pharmaceutical composition releases a lesser amount of active agent at a pH of <3 than at pH>3,
wherein the composition is formulated in the absence of a solvent.

4 more elements

Dependencies are inferred from the claim text.

Facts

Application

15/644,694Filed 7 Jul 2017

Priority

29 Sep 2011

Published

26 Oct 2017

Term ends

Not estimatedThe source records don’t support an estimate.

Classification16 codes

A61K 9/0002
Medicinal preparations characterised by special physical form: galenical forms characterised by the drug release technique; Application systems…
A61K 9/4858
Filling excipients; Inactive ingredients: organic compounds
A61K 31/192
Carboxylic acids, e.g. valproic acid: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 31/196
Having an amino group: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil

Family

Application61/540,699Us provisional application · filed 29 Sep 2011

Application13/631,963Continuation · filed 29 Sep 2012

Application15/644,694Continuation

US 10,179,104 B2Related patent

US 2013/0090313 A1Published application

US 9,730,884 B2Related patent

US 2017/0304190 A1This patent

From the US filing history. Foreign family members aren’t listed.

pH DEPENDENT CARRIERS FOR TARGETED RELEASE OF PHARMACEUTICALS ALONG THE GASTROINTESTINAL TRACT, COMPOSITIONS THEREFROM, AND MAKING AND USING SAME

Life of this patent

pH DEPENDENT CARRIERS FOR TARGETED RELEASE OF PHARMACEUTICALS ALONG THE GASTROINTESTINAL TRACT, COMPOSITIONS THEREFROM, AND MAKING AND USING SAME

Life of this patent

Abstract

Claims25