Pharmaceutical composition, a method of preparing it and a method of treatment by use thereof
AssigneeBusulipo AB
InventorsZuzana Hassan, Moustapha Hassan
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Abstract
Pharmaceutically acceptable liposome-encapsulated busulphan formulations for parenteral administration are provided, as well as such formulations furthermore comprising glutathione and/or at least one glutathione precursor and a process for manufacture of the preparations. The formulations are stable, have improved biodistribution and significantly reduced side effects over those produced by oral administration or parenteral administration of free drug. The formulations are useful as part of stem cell and/or bone marrow transplant conditioning regimens. A method of treatment of a mammal by use of such formulations.
Claims20
A liposome composition for myelosuppressive treatment comprising
- busulphan encapsulated in liposomes having a size of from 50 to 300 nm;
- said liposome composition having a character that, when administered to a mammalian patient, does not accumulate in the patient's liver;
- said liposomes having membranes comprising lipids,
- wherein the lipids are L-α-phosphatidylcholine, 1,2-dioleolyl-sn-glycero-3-phosphate and cholesterol,
- said lipids being present in a molar ratio of about 9.45:1:9.4.
A liposome composition for myelosuppressive treatment comprising
- busulphan encapsulated in liposomes having a size of from 50 to 300 nm;
- said liposome composition having a character that, when administered to a mammalian patient, does not accumulate in the patient's liver;
- said liposomes having membranes comprising lipids,
- wherein the lipids are at least one of phosphatidylserine, phosphatidylcholine and cholesterol,
- said lipids being present in a molar ratio of about 3:7:10.
A liposome composition for myelosuppressive treatment comprising
- busulphan encapsulated in liposomes having a size of from 50 to 300 nm;
- said liposome composition having a character that, when administered to a mammalian patient, does not accumulate in the patient's liver;
- said liposomes having membranes comprising lipids,
- wherein the lipids are cardiolipin, phosphatidylcholine and cholesterol,
- said lipids being present in a molar ratio of about 1:4:1.5.
A liposome composition for myelosuppressive treatment comprising
- busulphan encapsulated in liposomes having a size of from 50 to 300 nm;
- said liposome composition having a character that, when administered to a mammalian patient, does not accumulate in the patient's liver;
- said liposomes having membranes comprising lipids,
- wherein the lipids are phosphatidylcholine, cholesterol and stearylamine,
- said lipids being present in a molar ratio of about 7:1:1.
Dependencies are inferred from the claim text.