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A composition and liposome technology, applied in the directions of liposome delivery, pharmaceutical formulations, active ingredients of heterocyclic compounds, etc., can solve the problem of high leakage rate
Inactive Publication Date: 2001-05-16
ALZA CORP
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[0030] However, a noteworthy issue with remote loading is that not all ionized drugs are aggregated on liposomes in response to ion gradients (Chakrabarti et al., 1995; Madden et al., 1990)
Another problem is that some reagents aggregated in liposomes are released immediately after aggregation
A further problem is that some agents that are successfully loaded and retained in liposomes in vitro have a high leakage rate from liposomes in vivo, which negates the advantages of liposomal agent delivery in an encapsulated form
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Embodiment 2
[0131] Preparation of Glycyl-Ciprofloxacin and Lysyl-Ciprofloxacin
[0132] A. Synthesis of Glycyl-Ciprofloxacin and Lysyl-Ciprofloxacin
[0133] N-TBOC protected amino acids are commercially available. The compound was reacted with an equimolar amount of N-hydroxysuccinamide and a 10% excess of dicyclohexylcarbodiimide (DCC) in dichloromethane to form the N-hydroxysuccinamide ester.
[0134] The ester is reacted with 2 moles of triethylamine and 1 mole of anhydrous carboxy-protected ciprofloxacin HCl in anhydrous solvent to form the ciprofloxacin amide of the TBOC-protected amino acid.
[0135] Ciprofloxacin-amide was deprotected with trifluoroacetic acid and isolated by methods appropriate to the physical and chemical properties of the product. For example, L-threonine-ciprofloxacin is recovered by adjusting the pH of the aqueous suspension to 7 to separate the crystalline conjugate. The L-leucine-ciprofloxacin conjugate was recovered by extraction of the pH 7-8 aqueous ...
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Abstract
A liposome composition for treating a bacterial infection is described. The composition includes liposomes having a surface coating of hydrophilic polymer chains and an entrapped drug-conjugate composed of a quinolone compound conjugated to an amino acid.
Description
field of invention [0001] The present invention relates to compositions for the administration of quinolones for the treatment of bacterial infections, and more particularly to liposomal compositions for the administration of drug-conjugates of quinolones covalently linked to amino acids. [0002] references [0003] Chakrabarti, A. et al., US Patent 5,380,532, issued 1995, 1,10. [0004] Cramer, J. et al., Biochemical and Biophysical Research Communications 75(2):295-301 (1977). [0005] Culbertson, T.P. et al., J. Med. Chem. 33: 2270-2275 (1990). [0006] Deamer, D.W. et al., Biochim. et Biophys Acta 274:323 (1972). [0007] Domagala, J.M. et al., J. Medicinal Chemistry 29: 448-453 (1986). [0008] Greene, T.W. et al., Protecting Groups in Organic Synthesis, 2nd ed., John Wiley & Sons, New York, USA (1991). [0009] Hagen, S.E., et al., J. Medicinal Chemistry 33: 849-845 (1990). [0010] Hagen, S.E., et al., J. Medicinal Chemistry 34: 1155-1161 (1991). [0011] Hope, ...
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