IPC분류정보
| 국가/구분 |
United States(US) Patent
등록
|
| 국제특허분류(IPC7판) |
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| 출원번호 |
US-0317499
(1999-05-24)
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발명자
/ 주소 |
- Lambert, Karel J.
- Constantinides, Panayiotis P.
- Tustian, Alexander K.
- Quay, Steven C.
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| 출원인 / 주소 |
- Sonus Pharmaceuticals, Inc.
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| 대리인 / 주소 |
Christensen O'Connor Johnson Kindness PLLC
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| 인용정보 |
피인용 횟수 :
29 인용 특허 :
32 |
초록
▼
An emulsion of tocopherol incorporating a co-solvent and, stabilized by biocompatible surfactants, as a vehicle or carrier for therapeutic drugs, which is substantially ethanol free and which can be administered to animals or humans by various routes is disclosed. Also included in the emulsion is PE
An emulsion of tocopherol incorporating a co-solvent and, stabilized by biocompatible surfactants, as a vehicle or carrier for therapeutic drugs, which is substantially ethanol free and which can be administered to animals or humans by various routes is disclosed. Also included in the emulsion is PEGylated vitamin E. PEGylated α-tocopherol includes polyethylene glycol subunits attached by a succinic acid diester at the ring hydroxyl of vitamin E and serves as a primary surfactant, stabilizer and a secondary solvent in emulsions of α-tocopherol.
대표청구항
▼
1. A composition, comprising: one or more tocopherols or derivatives thereof; a co-solvent; a tocopherol polyethylene glycol succinate; an aqueous phase; and a chemotherapeutic agent, wherein the chemotherapeutic agent is at least one of a taxoid, a taxine, a microtubule-binding agent, or a t
1. A composition, comprising: one or more tocopherols or derivatives thereof; a co-solvent; a tocopherol polyethylene glycol succinate; an aqueous phase; and a chemotherapeutic agent, wherein the chemotherapeutic agent is at least one of a taxoid, a taxine, a microtubule-binding agent, or a taxane; wherein the composition is substantially free of any monohydric alcohol, wherein the composition is an emulsion or a microemulsion having an oil and a water phase, and wherein all of the chemotherapeutic agent is in the oil phase. 2. The composition of claim 1, wherein the co-solvent is at least one of dimethylsulfoxide, dimethylamide, ethylene glycol, propylene glycol, glycerol, sorbitol, mannitol, polyethylene glycol, N-methyl-2-pyrrolidone, or pylyvinyl-pyrrolidone. 3. The composition of claim 2, wherein the polyethylene glycol has a molecular weight between 100 to 10,000. 4. The composition of claim 1, wherein the tocopherol is at least one of α-tocotrienol, β-tocotrienol, γ-tocotrienol, δ-tocotrienol, α-tocopherol, α-tocopherol acetate, α-tocopherol phosphate, α-tocopherol succinate, α-tocopherol nicotinate, or α-tocopherol linoleate. 5. The composition of claim 1, wherein the tocopherol polyethylene glycol succinate is an ester or an ether of α-tocopherol and polyethylene glycol. 6. The composition of claim 1, wherein the tocopherol polyethylene glycol succinate is D-α-tocopherol polyethylene glycol 1000 succinate. 7. The composition of claim 1, wherein the ratio of tocopherol to tocopherol polyethylene glycol derivative is from about 1:1 to about 10:1 w/w. 8. The composition of claim 1 further comprising a surfactant having an HLB of at least 10. 9. The composition of claim 8, wherein the surfactant is at least one of an anionic, cationic, a nonionic, or a zwitterionic surfactant. 10. The composition of claim 8, wherein the surfactant is at least one of a polyoxypropylene-polyoxyethylene glycol nonionic block polymer, ascorbyl-6-palmitate, stearylamine, or a sucrose fatty ester. 11. The composition of claim 8, wherein the surfactant is pegylated. 12. The composition of claim 8, wherein the surfactant has the structure: H(OCH2CH2)a(OC3H6)b(OCH2CH2)aOH wherein a is 101 and b is 56. 13. The composition of claim 1, wherein the taxane is paclitaxel. 14. The composition of claim 1, wherein the monohydric alcohol is at least one of ethanol, butanol, or isopropanol. 15. A pharmaceutical composition, consisting essentially of: paclitaxel, one or more tocopherols or derivatives thereof, a tocopherol polyethylene glycol derivative, polyethylene glycol, a polyoxypropylene-polyoxyethylene glycol nonionic block polymer, and an aqueous phase. 16. The composition of claim 15, wherein the tocopherol is at least one of α-tocotrienol, β-tocotrienol, γ-tocotrienol, δ-tocotrienol, α-tocopherol, α-tocopherol acetate, α-tocopherol phosphate, α-tocopherol succinate, α-tocopherol nicotinate, or α-tocopherol linoleate. 17. The composition of claim 15, wherein the tocopherol is α-tocopherol. 18. The composition of claim 15, wherein the tocopherol polyethylene glycol derivative is a tocopherol polyethylene glycol succinate. 19. The composition of claim 18, wherein the tocopherol polyethylene glycol succinate is an ester or an ether of α-tocopherol and polyethylene glycol. 20. The composition of claim 18, wherein the tocopherol polyethylene glycol succinate is D-α-tocopherol polyethylene glycol 1000 succinate. 21. The composition of claim 15, wherein the polyethylene glycol has a molecular weight between 100 to 100,000. 22. The composition of claim 15, wherein the block polymer has the structure: H(OCH2CH2)a(OC3H6)b(OCH2CH2)aOH wherein a is 101 and b is 56.
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