US 10,646,431 B2 · 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/soluble compounds in GI fluids, (d) susceptible to first pass metabolism, and/or (e) cause stomach irritation, upset, or dyspepsia.

Claims21

Dependent claims

A pharmaceutical composition formulated for oral administration comprising a suspension of solid particles of a biologically active agent in a non-aqueous liquid carrier, wherein the non-aqueous liquid carrier is an oil, and wherein the carrier comprises:

(a) at least about 10 wt. % of free monocarboxylic acid having at least 8 carbons, wherein the monocarboxylic acid is liquid at room temperature;
and
(b) less than about 10 wt. % zwitterionic phospholipid;
wherein the pharmaceutical composition releases a lesser amount of active agent at a pH of <3 than at pH >3, and
wherein the pharmaceutical composition is formulated in the absence of a solvent.

2 more elements

Dependencies are inferred from the claim text.

Facts

Application

16/183,616Filed 7 Nov 2018 · continuation

Priority

29 Sep 2011

Published

US 2019/0070099 A17 Mar 2019

Granted

12 May 2020

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

Application13/631,963Parent of this continuation · filed 29 Sep 2012

Application15/644,694Parent of this continuation · filed 7 Jul 2017

US 2019/0070099 A1Pre-grant publication · published 7 Mar 2019

US 10,179,104 B2Parent of this continuation

US 9,730,884 B2Parent of this continuation

US 2013/0090313 A1Published application

US 2017/0304190 A1Published application

US 10,646,431 B2This 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

Claims21