pH dependent carriers for targeted release of pharmaceuticals along the gastrointestinal tract, compositions therefrom, and making and using same
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/192
A61K-031/196
A61K-031/405
A61K-031/60
A61K-031/616
A61K-045/06
A61K-047/12
A61K-047/14
A61K-047/24
A61K-009/00
A61K-009/48
출원번호
US-0791189
(2013-03-08)
등록번호
US-9226892
(2016-01-05)
발명자
/ 주소
Marathi, Upendra K.
Childress, Susann Edler
Gammill, Shaun L.
Strozier, Robert W.
출원인 / 주소
PLX PHARMA INC.
대리인 / 주소
Foley & Lardner LLP
인용정보
피인용 횟수 :
1인용 특허 :
43
초록▼
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 a
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.
대표청구항▼
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
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 pH3. 5. The method of claim 4, wherein less than 20% of the NSAID is released from the carrier at pH3. 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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이 특허에 인용된 특허 (43)
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Lichtenberger Lenard M. (Houston TX), Methods and compositions employing unique mixtures of polar and neutral lipids for protecting the gastrointestinal tract.
Lichtenberger Lenard M. (Houston TX), Methods and compositions employing unique mixtures of polar and neutral lipids for protecting the gastrointestinal tract.
Lichtenberger Lenard M. (Houston TX), Methods and compositions employing unique mixtures of polar and neutral lipids for protecting the gastrointestinal tract.
Lichtenberger Lenard M. (Houston TX 4), Methods and compositions employing unique mixtures of polar and neutral lipids for surfactant replacement therapy.
Lichtenberger Lenard ; Butler Bruce D, Methods of enhancing the therapeutic activity of NSAIDS and compositions of zwitterionic phospholipids useful therein.
Lichtenberger Lenard M. ; Butler Bruce D., Methods of enhancing the therapeutic activity of NSAIDS and compositions of zwitterionic phospholipids useful therein.
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Liversidge Gary G. (West Chester PA) Conzentino ; Jr. Philip (West Chester PA) Cundy Kenneth C. (Pottstown PA) Sarpotdar Pramod P. (Malvern PA), Surface modified NSAID nanoparticles.
Liversidge Gary G. (West Chester PA) Cundy Kenneth C. (Pottstown PA) Bishop John F. (Rochester NY) Czekai David A. (Honeoye Falls NY), Surface modified drug nanoparticles.
Marathi, Upendra K.; Childress, Susann Edler; Gammill, Shaun L.; Strozier, Robert W., PH dependent carriers for targeted release of pharmaceuticals along the gastrointestinal tract, compositions therefrom, and making and using same.
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