IPC분류정보
| 국가/구분 |
United States(US) Patent
등록
|
| 국제특허분류(IPC7판) |
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| 출원번호 |
US-0424258
(2003-04-28)
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| 등록번호 |
US-7390502
(2008-06-24)
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|
발명자
/ 주소 |
- Ahmad,Imran
- Zhang,Jia Ai
- Rahman,Aquilur
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| 출원인 / 주소 |
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| 대리인 / 주소 |
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| 인용정보 |
피인용 횟수 :
0 인용 특허 :
116 |
초록
▼
The present invention is for novel compositions and methods for treating diseases caused by cellular proliferation, particularly, for treating cancer in mammals and more particularly in humans. The therapeutic compositions of the present invention include SN-38 lipid complexes in which the complexes
The present invention is for novel compositions and methods for treating diseases caused by cellular proliferation, particularly, for treating cancer in mammals and more particularly in humans. The therapeutic compositions of the present invention include SN-38 lipid complexes in which the complexes can contain any of a variety of neutral or charged lipids and, desirably, cardiolipin. The compositions are capable of efficiently incorporating SN-38 into complexes and are capable of solubilizing relatively high concentrations of SN-38.
대표청구항
▼
What is claimed is: 1. A method of forming a lipid composition comprising SN-38 and liposomes, said method comprising: forming a lipid phase comprising cardiolipin; hydrating the lipid phase with an aqueous solution of SN-38 having an alkaline pH so as to form said lipid composition with about 70 w
What is claimed is: 1. A method of forming a lipid composition comprising SN-38 and liposomes, said method comprising: forming a lipid phase comprising cardiolipin; hydrating the lipid phase with an aqueous solution of SN-38 having an alkaline pH so as to form said lipid composition with about 70 wt. % or more of non-precipitated SN-38 entrapped in the liposomes; and reducing the pH of the lipid phase to an acidic pH. 2. The method of claim 1, further comprising adding a nonreducing sugar to the lipid composition, wherein the lipid phase is formed in an organic solvent, and said hydrating the lipid phase is carried out after removing the organic solvent. 3. The method of claim 1, wherein the lipid phase comprises at least one lipid selected from the group consisting of phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylglycerol, phosphatidic acid, phosphatidylinositol, sphingomyelin, sterol, tocopherol, fatty acid, and mixture thereof. 4. The method of claim 1, wherein the lipid phase further comprises a phosphatidylcholine, a sterol and a tocopherol. 5. The method of claim 1, wherein the lipid phase further comprises a phosphatidylglycerol selected from the group consisting of dimyristoylphosphatidylglycerol, dioleoylphosphatidylglycerol, distearoylphosphatidylglycerol, dipalmitoylphosphatidylglycerol, diarachidonoylphosphatidylglycerol, or mixture thereof. 6. The method of claim 1, wherein the lipid phase further comprises a phosphatidylcholine selected from the group consisting of dimyristoylphosphatidylcholine, distearoylphosphatidylcholine, dioleoylphosphatidylcholine, dipalmitoylphosphatidylcholine, diarachidonoylphospatidylcholine, egg phosphatidylcholine, soy phosphatidylcholine, hydrogenated soy phosphate, dylcholine, and mixture thereof. 7. The method of claim 1, wherein the lipid phase further comprises a sterol selected from the group consisting of cholesterol, polyethylene glycol derivatives of cholesterol, coprostanol, cholestane, cholesterol hemisuccinate, cholesterol sulfate, and mixtures thereof. 8. A lipid composition comprising SN-38 prepared in accordance with the method of claim 1. 9. The method of claim 1, wherein the lipid phase further comprises cholesterol, a tocopherol, and dioleoylphosphatidylcholine, and wherein the lipid phase is formed in ethanol. 10. A liposomal composition prepared according to the method of claim 4. 11. A liposomal composition prepared according to the method of claim 5. 12. A liposomal composition prepared according to the method of claim 6. 13. A liposomal composition prepared according to the method of claim 7. 14. A liposomal composition prepared according to the method of claim 1, wherein the concentration of SN-38 in the composition is between about 0.1 mg/ml and about 2.0 mg/ml.
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