Formulation and delivery method to enhance antioxidant potency of vitamin E
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-009/48
A61K-009/66
출원번호
US-0680042
(2000-10-04)
발명자
/ 주소
Udell, Ronald G.
Hari, Siva P.
Rich, Mel
출원인 / 주소
Soft Gel Technologies, Inc.
대리인 / 주소
Dorsey & Whitney LLP
인용정보
피인용 횟수 :
19인용 특허 :
2
초록▼
A formulation to deliver a full-spectrum of Vitamin E isomers for improved antioxidant capacity, bioavailability, dissolution and efficacy. The formulation includes dl-α-tocopheryl acetate or dl-α-tocopheryl succinate (synthetic Vitamin E), natural Vitamin E and mixed tocopherols, such as α-, β-, γ-
A formulation to deliver a full-spectrum of Vitamin E isomers for improved antioxidant capacity, bioavailability, dissolution and efficacy. The formulation includes dl-α-tocopheryl acetate or dl-α-tocopheryl succinate (synthetic Vitamin E), natural Vitamin E and mixed tocopherols, such as α-, β-, γ- and δ-tocopherol, as well as four isomers (α, β, γ and δ) of tocotrienols. This formulation is designed to deliver at least 17-times the antioxidant capacity of synthetic Vitamin E (dl-α-tocopheryl acetate), and at least twice the antioxidant capacity of natural Vitamin E (d-α-tocopherol) as measured by oxygen radical absorbance capacity (ORAC) assay. The potent antioxidant capacity of this formula affords protection against oxidative damage of cell membranes, heart disease, cancer and eye and skin disease.
대표청구항▼
A formulation to deliver a full-spectrum of Vitamin E isomers for improved antioxidant capacity, bioavailability, dissolution and efficacy. The formulation includes dl-α-tocopheryl acetate or dl-α-tocopheryl succinate (synthetic Vitamin E), natural Vitamin E and mixed tocopherols, such as α-, β-, γ-
A formulation to deliver a full-spectrum of Vitamin E isomers for improved antioxidant capacity, bioavailability, dissolution and efficacy. The formulation includes dl-α-tocopheryl acetate or dl-α-tocopheryl succinate (synthetic Vitamin E), natural Vitamin E and mixed tocopherols, such as α-, β-, γ- and δ-tocopherol, as well as four isomers (α, β, γ and δ) of tocotrienols. This formulation is designed to deliver at least 17-times the antioxidant capacity of synthetic Vitamin E (dl-α-tocopheryl acetate), and at least twice the antioxidant capacity of natural Vitamin E (d-α-tocopherol) as measured by oxygen radical absorbance capacity (ORAC) assay. The potent antioxidant capacity of this formula affords protection against oxidative damage of cell membranes, heart disease, cancer and eye and skin disease. troms. 4. The implantable medical device of claim 1, wherein said barrier is a homogeneous layer. 5. The implantable medical device of claim 1, wherein said barrier comprises a plurality of discrete deposits. 6. The implantable medical device of claim 1, wherein said barrier is intermixed with an outer portion of said coating. 7. The implantable medical device of claim 1, wherein said inorganic material is selected from the group consisting of silicides of: niobium, tantalum, titanium, tungsten, vanadium, and zirconium. 8. The implantable medical device of claim 1, wherein said inorganic material is selected from the group consisting of oxides of: aluminum, barium, calcium, hafnium, niobium, silicon, tantalum, titanium, tungsten, and zirconium. 9. The implantable medical device of claim 1, wherein said inorganic material is selected from the group consisting of nitrides of: chromium, silicon, titanium, and zirconium. 10. The implantable medical device of claim 1, wherein said inorganic material is a metal selected from the group consisting of aluminum, chromium, gold, hafnium, iridium, niobium, palladium, platinum, tantalum, titanium, tungsten, zirconium, and alloys thereof. 11. The implantable medical device of claim 1, wherein said drug is selected from the group consisting of antineoplastic, anti-inflammatory, antiplatelet, anticoagulant, fibrinolytic, thrombin inhibitor, antimitotic, antiallergic, and antiproliferative substances. 12. The implantable medical device of claim 1, wherein said drug is selected from the group consisting of paclitaxel, docetaxel, methotrexate, sodium heparin, hirudin, estradiol, actinomycin D, angiopeptin, captopril, nitroprusside, and nitric oxide. 13. The implantable medical device of claim 1, wherein said drug is selected from the group consisting of azathioprine, vincristine, vinblastine, agratroban, forskolin, vapiprost, mitomycin, cilazipril, lisinopril, phosphodiesterase inhibitors, and trizaolopyrimidine. 14. The implantable medical device of claim 1, wherein said device is a stent. 15. The implantable medical device of claim 1, wherein said device is a graft. 16. An implantable medical device comprising: a substrate; a polymer coating containing a drug said polymer disposed on said substrate; and a barrier overlaying at least a portion of said coating, wherein said barrier comprises an inorganic material and is adapted to reduce a rate of release of said drug from said coating after insertion of said device into a body of a patient, wherein said inorganic material is selected from the group consisting of carbides of silicon, carbides of titanium, molybdenum disulfide, amorphous diamond, diamondlike carbon, pyrolytic carbon, ultra low temperature isotropic carbon, amorphous carbon, strontium titanate, and barium titanate. 17. An implantable medical device comprising: a substrate; a polymer coating containing a drug said polymer disposed on said substrate; and a barrier overlaying at least a portion of said coating, said drug having significantly lower diffusivity in said barrier than in said coating. 18. An implantable medical device comprising: a substrate; a polymer coating containing a drug said polymer disposed on said substrate; and a barrier overlaying at least a portion of said coating, said drug having significantly lower degree of solubility in said barrier than in said coating. 19. A method for making an implantable medical device, the method comprising: forming a first layer comprising a polymer and a drug on said device; and forming a barrier over at least a portion of said first layer, wherein said barrier comprises an inorganic material and is adapted to reduce a rate of release of said drug from said first layer after insertion of said device into a body of a patient. 20. The method of claim 19, wherein said barrier is applied by a process selected from the group consisting of plasma enhanced chemical vapor deposition, cathodic are physical vapor
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