IPC분류정보
국가/구분 |
United States(US) Patent
등록
|
국제특허분류(IPC7판) |
|
출원번호 |
US-0501500
(2011-03-30)
|
등록번호 |
US-8652511
(2014-02-18)
|
국제출원번호 |
PCT/AU2011/000358
(2011-03-30)
|
§371/§102 date |
20120412
(20120412)
|
국제공개번호 |
WO2011/120084
(2011-10-06)
|
발명자
/ 주소 |
- Cottrell, Jeremy
- Gaetano, Giacinto
- El-Tamimy, Mahmoud
- Kennedy, Nicholas
- Gavin, Paul David
|
출원인 / 주소 |
|
대리인 / 주소 |
Michael Best & Friedrich LLP
|
인용정보 |
피인용 횟수 :
10 인용 특허 :
85 |
초록
A composition suitable for use in a transdermal delivery patch for administration of a biologically active compound, the composition comprising a phosphate compound of tocopherol and a polymer carrier.
대표청구항
▼
1. A matrix layer suitable for use in a transdermal delivery patch for administration of a biologically active compound, the matrix layer comprising a mixture of a mono-tocopheryl phosphate compound and a di-tocopheryl phosphate compound and a polymer carrier comprising polymers selected from the gr
1. A matrix layer suitable for use in a transdermal delivery patch for administration of a biologically active compound, the matrix layer comprising a mixture of a mono-tocopheryl phosphate compound and a di-tocopheryl phosphate compound and a polymer carrier comprising polymers selected from the group consisting of polyacrylates, rubber-based polymers, polysiloxanes and amine-resistant polysiloxanes, wherein the polymer carrier is present in an amount within the range of about 30% w/w to about 95% w/w of the total concentration of the matrix layer. 2. The matrix layer of claim 1, wherein the mono-tocopheryl phosphate compound is selected from the group consisting of mono-(tocopheryl)phosphate, mono-(tocopheryl)phosphate monosodium salt, mono-(tocopheryl)phosphate disodium salt, mono-(tocopheryl)phosphate monopotassium salt and mono-(tocopheryl)phosphate dipotassium salt, and the di-tocopheryl phosphate compound is selected from the group consisting of di-(tocopheryl)phosphate, di-(tocopheryl)phosphate monosodium salt and di-(tocopheryl)phosphate monopotassium salt. 3. The matrix layer of claim 1, wherein the ratio (% w/w) of the mixture of the mono-tocopheryl phosphate compound and the di-tocopheryl phosphate compound is at least 2:1. 4. The matrix layer of claim 1, wherein the mixture of the mono-tocopheryl phosphate compound and the di-tocopheryl phosphate compound is present in an amount within a range of about 0.01% w/w to about 10% w/w of the total concentration of the matrix layer. 5. The matrix layer of claim 1, wherein the mixture of the mono-tocopheryl phosphate compound and the di-tocopheryl phosphate compound is present in an amount within a range of about 0.5% w/w to about 1.5% w/w of the total concentration of the matrix layer. 6. The matrix layer of claim 1, wherein the polymer carrier is present in an amount within the range of about 30% w/w to about 80% w/w of the total weight of the matrix layer. 7. The matrix layer of claim 1, wherein the polymer carrier is present in an amount within the range of about 85% w/w to about 95% w/w of the total weight of the matrix layer. 8. The matrix layer of claim 1, wherein the polymer carrier further comprises inert carrier components selected from the group consisting of anti-tacking agents, tackifiers, and plasticizers. 9. The matrix layer of claim 8, wherein the anti-tacking agent is succinic acid. 10. The matrix layer of claim 8, wherein the anti-tacking agent is present in an amount of up to about 5% w/w of the total weight of the matrix layer. 11. The matrix layer of claim 8, wherein the tackifier is insoluble in water and composed of a monomer which contains partly or wholly a (meth)acrylic alkyl ester. 12. The matrix layer of claim 8, wherein the tackifier is selected from the group consisting of acrylic, N-butyl-methacrylic copolymer, acrylic methyl, acrylic 2-ethylhexyl copolymer, polyacrylic acid, methacrylic copolymer L, aminoalkylmethacrylate copolymer E, rosin esters, hydrogenated rosins, dipropylene glycol dibenzoate, mixed hydrocarbons, and acrylic copolymers. 13. The matrix layer of claim 8, wherein the plasticizer is selected from the group consisting of phthalates, esters of polycarboxylic acids with linear or branched aliphatic alcohols of moderate chain length, acetylated monoglycerides, alkyl citrates, triethyl citrate (TEC), acetyl triethyl citrate (ATEC), tributyl citrate (TBC), acetyl tributyl citrate (ATBC), trioctyl citrate (TOC), acetyl trioctyl citrate (ATOC), trihexyl citrate (THC), acetyl trihexyl citrate (ATHC), butyryl trihexyl citrate (BTHC, trihexyl o-butyryl citrate), trimethyl citrate (TMC), methyl laurate, lauric acid, lauryl lactate, lauryl alcohol, alkyl sulphonic acid phenyl ester, diethylene glycol monoethyl ether, bis(2-ethylhexyl)phthalate (DEHP), diisooctyl phthalate (DIOP), bis(n-butyl)phthalate (DnBP, DBP), diisobutyl phthalate (DIBP), bis(2-ethylhexyl)adipate (DEHA), dimethyl adipate (DMAD), monomethyl adipate (MMAD), dioctyl adipate (DOA), ethyl oleate, sorbitan monooleate, glycerol monooleate, dibutyl sebacate (DBS), dibutyl maleate (DBM), diisobutyl maleate (DIBM), benzoates, epoxidized vegetable oils, tris(tromethamine), N-ethyl toluene sulfonamide (o/p ETSA), N-(2-hydroxypropyl)benzene sulfonamide (HP BSA), N-(n-butyl)benzene sulfonamide (BBSA-NBBS), tricresyl phosphate (TCP), tributyl phosphate (TBP), triethylene glycol dihexanoate (3G6, 3 GH), tetraethylene glycol diheptanoate (4G7), 1,3-butyleneglycol, dipropylene glycol, PEG400, Span 80, and polyvinylpyrrolidone. 14. The matrix layer of claim 8, wherein the inert carrier components are present in an amount within the range of 0.001% w/w to about 50% w/w of the total weight of the matrix layer. 15. The matrix layer of claim 1, wherein the matrix layer comprises an anti-tacking agent and a plasticizer in a total amount of about 35% w/w of the total weight of the matrix layer. 16. The matrix layer of claim 15, wherein the anti-tacking agent is succinic acid and the plasticizer is dibutyl sebacate. 17. The matrix layer of claim 1, wherein the polymer carrier and optional inert carrier components is present in an amount within the range of about 50% w/w to about 99% w/w of the total weight of the matrix layer. 18. The matrix layer of claim 1, further comprising one or more excipients. 19. A transdermal delivery patch for administration of a biologically active compound comprising a matrix layer as defined in claim 1. 20. The transdermal delivery patch of claim 19, wherein the matrix layer is a solid or semi-solid layer. 21. The transdermal delivery patch of claim 19, further comprising one or more occlusive or impermeable layers, and/or one or more non-occlusive layers. 22. The transdermal delivery patch of claim 21, wherein an impermeable or occlusive layer is a backing layer. 23. The transdermal delivery patch of claim 21, wherein a non-occlusive layer is a backing layer. 24. The transdermal delivery patch of claim 22, wherein the thickness of the backing layer is about 0.0005 inches to about 0.01 inches. 25. The transdermal delivery patch of claim 21, wherein an impermeable layer is a removable release liner. 26. The transdermal delivery patch of claim 21, wherein the impermeable layers are made from metal foil, Mylar, polyethylene terephthalate, siliconized polyester, fumed silica in silicone rubber, polytretrafluoroethylene, cellophane, siliconized paper, aluminized paper, polyvinyl chloride film, composite foils or films containing polyester such as polyester terephthalate, polyester or aluminized polyester, polytetrafluoroethylene, polyether block amide copolymers, polyethylene methyl methacrylate block copolymers, polyurethanes, polyvinylidene chloride, nylon, silicone elastomers, rubber-based polyisobutylene, styrene, styrene-butadiene, and styrene-isoprene copolymers, polyethylene, polypropylene, or a combination thereof. 27. The transdermal delivery patch of claim 25, wherein the thickness of the release liner is about 0.01 mm to about 2 mm. 28. The transdermal delivery patch of claim 19, further comprising an adhesive layer. 29. The transdermal delivery patch of claim 28, wherein the adhesive layer is a polymeric adhesives selected from the group consisting of include polyacrylate polymers, rubber-based adhesives and polysiloxane adhesives; a commercially available adhesive selected from the group consisting of polyacrylate adhesives. 30. The transdermal delivery patch of claim 19, wherein the biologically active compound is selected from the group of pharmaceuticals including drugs, cosmeceuticals, nutraceuticals, and nutritional agents. 31. The transdermal delivery patch of claim 30, wherein the biologically active compound is selected from the group consisting of cardiovascular drugs, antihypertensive agents and antiarrhythmic agents; congestive heart-failure pharmaceuticals; inotropic agents; vasodilators; ACE inhibitors; diuretics; carbonic anhydrase inhibitors; cardiac glycosides; phosphodiesterase inhibitors; α blockers; β-blockers; sodium channel blockers; potassium channel blockers; β-adrenergic agonists; platelet inhibitors; angiotensin II antagonists; anticoagulants; thrombolytic agents; treatments for bleeding; treatments for anaemia; thrombin inhibitors; antiparasitic agents; antibacterial agents; insulin; human growth hormone and peptides; vaccines; antiinflammatory agents, steroidal antiinflammatory agents; prophylactic antiinflammatory agents; antiglaucoma agents; mast cell stabilisers; mydriatics; agents affecting the respiratory system; allergic rhinitis pharmaceuticals; alpha-adrenergic agonists; corticosteroids; chronic obstructive pulmonary disease pharmaceuticals; xanthine-oxidase inhibitors; antiarthritis agents; gout treatments; autacoids and autacoid antagonists; antimycobacterial agents; antifungal agents; antiprotozoal agents; anthelmintic agents; antiviral agents, herpes, cyto-megalovirus, human immunodeficiency virus and hepatitis infections; treatments for leukemia and kaposi's sarcoma; pain management agents, anaesthetics and analgesics; neuroleptics; sympathomimetic pharmaceuticals; adrenergic agonists; drugs affecting neurotransmitter uptake or release; anticholinergic pharmaceuticals; antihaemorrhoid treatments; agents to prevent or treat radiation or chemotherapeutic effects; liopgenisis drugs; fat reducing treatments; anti-obesity peptides; antiobesity agents; sympathomimetic agents; treatments for gastric ulcers and inflammation; prostaglandins; VEGF inhibitors; antihyperlipidemic agents, drugs that affect the central nervous system (CNS), psychoactive drugs, stimulants, antianxiety and hypnotic drugs, antidepressant drugs; antiparkinson's pharmaceuticals; hormones and fragments thereof; growth hormone antagonists; gonadotropin releasing hormones and analogues thereof; steroid hormones and their antagonists; selective estrogen modulators; growth factors; antidiabetic pharmaceuticals H1, H2, H3 and H4 antihistamines; peptide, protein, polypeptide, nucleic acids and oligonucleotide pharmaceuticals; analogues, fragments and varients of natural proteins, polypeptides, oligonucleotides and nucleic acids; agents used to treat migraine headaches; asthma pharmaceuticals; cholinergic antagonists; glucocorticoids; androgens; antiandrogens; inhibitors of adrenocorticoid biosynthesis; osteoporosis treatments; antithyroid pharmaceuticals; suncreens, sun protectants and filters; cytokine agonists; cytokine antagonists; anticancer drugs; antialzheimer drugs; HMGCoA reductase inhibitors; fibrates; cholesterol absorption inhibitors; HDL cholesterol elevating agents; triglyceride reducing agents; antiageing or antiwrinkle agents; precursor molecules for the generation of hormones; proteins; antibacterial agents; anti acne agents; antioxidants; hair treatments and skin whitening agents; suncreens, sun protectants and filters; variants of human apolipoprotein; precursor molecules for generation of hormones; proteins and peptides thereof; amino acids; plant extracts; DHEA; isoflavones; nutritional agents, phytosterols and iridoid gylcosides, sesquiterpene lactones, terpenes, phenolic glycosides, triterpenes, hydroquinone derivatives, phenylalkanones; antioxidants; omega-3-fatty acids; glucosamine; nucleic acids, oligonucleotides, antisense pharmaceuticals; enzymes; cytokines; cytokine analogues; cytokine agonists; cytokine antagonists; immunoglobulins; antibodies; antibody pharmaceuticals; gene therapies; lipoproteins; erythropoietin; vaccines; small and large molecule therapeutic agents for the treatment, of human and animal diseases. 32. The transdermal delivery patch of claim 31, wherein the biologically active compound is selected from the group consisting of alprazolam, donepazil, rispiredone, lorazepam, nicotine, lidocaine, diclofenac, felodipine, insulin, ketoralac, prilocalne, halobetasol, hydrocortisol, opioids, oxycodone, and dihydrohydroxycodeinone. 33. The transdermal delivery patch of claim 19, wherein the biologically active compound is present in an amount of the total concentration of the matrix layer. 34. The transdermal delivery patch of claim 33, wherein the amount of biologically active compound is present in an amount within the range of about 3.0% w/w to about 15.0% w/w of the total concentration of the matrix layer. 35. The transdermal delivery patch of claim 19, wherein the ratio (% w/w) of biologically active compound:tocopheryl phosphate mixture is within the range of about 5:5 to about 5:0.5. 36. The transdermal delivery patch of claim 19, wherein the ratio (% w/w) of polymer carrier:biologically active compound and tocopheryl phosphate mixture is within the range of about 1:1 to about 3:1. 37. The matrix layer of claim 1, wherein the polymer carrier is present in an amount within the range of about 55% w/w to about 65% w/w of the total weight of the matrix layer. 38. The matrix layer of claim 1, wherein the polymer carrier is present in an amount within the range of about 90% w/w to about 95% w/w of the total weight of the matrix layer. 39. The transdermal delivery patch of claim 31, wherein the biologically active compound is selected from the group consisting of calcium channel blockers, calcium antagonists, non-steroidal anti-inflammatory agents (NSAIDs), COX-2 inhibitors, lipase inhibitors, proton pump inhibitors, statins, antipsychotic drugs, antiepileptic drugs, antiseizure drugs, anticonvulsants, sex hormones, hypoglycaemic agents, bisphosphonates, collagen, elastin, grape seed extract, vitamins, retinol, retinoids, retinoic acid and co-enzyme Q10. 40. The transdermal delivery patch of claim 19, wherein the biologically active compound is present in an amount within the range of about 0.1% w/w to about 20% w/w of the total concentration of the matrix layer. 41. The transdermal delivery patch of claim 19, wherein the biologically active compound is present in an amount within the range of about 0.1% w/w to about 10% w/w of the total concentration of the matrix layer. 42. The transdermal delivery patch of claim 19, wherein the ratio (% w/w) of the biologically active compound:tocopherol phosphate mixture is within the range of about 5:1. 43. The transdermal delivery patch of claim 19, wherein the ratio (% w/w) of polymer carrier:biologically active compound and tocopherol phosphate mixture is within the range of about 7:6 to about 7:3. 44. The transdermal delivery patch of claim 32, wherein the oxycodone is oxycodone base.
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