|Title:||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.|
|Inventor(s):||Marathi; Upendra K. (Houston, TX), Childress; Susann Edler (Houston, TX), Gammill; Shaun L. (Houston, TX), Strozier; Robert W. (Houston, TX)|
|Assignee:||PLX PHARMA INC. (Houston, TX)|
1. A method of targeting release of a non-steroidal anti-inflammatory drug (NSAID) to the small intestine of a subject, comprising: orally administering to the subject an ingestible
composition consisting of a non-aqueous solid-in-oil suspension of an effective amount of the solid NSAID in a carrier, wherein the carrier comprises at least one free fatty acid having at least 8 carbon atoms in an amount greater than about 10 wt. %,
and wherein the carrier comprises from about 0.0001 wt. % to about 5 wt. % of zwitterionic phospholipids, whereby the composition displays less gastrointestinal toxicity than the NSAID alone.
2. The method of claim 1, wherein at least one free fatty acid is present in the carrier at a level greater than 14 wt. % of the carrier.
3. The method of claim 2, wherein the carrier further comprises triglycerides.
4. The method of claim 1, wherein the carrier releases a minimal amount of the NSAID at pH<3 as compared to at pH>3.
5. The method of claim 4, wherein less than 20% of the NSAID is released from the carrier at pH<3 and greater than 50% of the NSAID is released from the carrier at pH>3.
6. The method of claim 1, wherein the NSAID is selected from the group consisting of ibuprofen, piroxicam, salicylate, aspirin, naproxen, indomethacin, diclofenac, mefenamic acid, COX2 inhibitors and any mixture thereof.
7. The method of claim 6, wherein the NSAID is selected from the group consisting of ibuprofen, aspirin, naproxen, indomethacin, mefenamic acid, and any mixture thereof.
8. The method of claim 1, wherein the amount of zwitterionic phospholipids is selected from the group consisting of about 0 wt. %, about 0.5 wt. %, about 1 wt. %, about 2 wt. %, about 2.5 wt. %, about 5 wt. %, less than 2.5 wt. %, and less than 5 wt. %.
9. The method of claim 1, wherein the amount of zwitterionic phospholipids is from about 0.5 wt. % up to about 2.5 wt. %.
10. The method of claim 1, wherein the amount of zwitterionic phospholipids is selected from the group consisting of about 0.5 wt. %, about 1 wt. %, about 2 wt. %, about 2.5 wt. %, and about 5 wt. %.
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