Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Liposomes
Patent
1995-06-19
1997-09-30
Mullis, Jeffrey C.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Liposomes
424484, 424502, A61K 9107, A61K 9127
Patent
active
056723580
ABSTRACT:
A controlled release aqueous emulsion is disclosed, as are its method of manufacture and use as a vehicle for delivering medicaments in liquid form. A contemplated emulsion comprises an oil-in-water emulsion having an average oil particle size of about 100 nm to about 250 nm, a pH value of about 4.5 to about 8.0 and a viscosity at 20.degree.-25.degree. C. of 1 to about 1000 cps. The water phase constitutes at least 25 weight percent of the total composition. The oil phase is a wax matrix that is a wax having a melting point of about 40.degree. to about 80.degree. C. and is present in an amount of about 3 to about 30 percent of the total composition. A pharmaceutically effective amount of a pharmacologically active compound that is free from decomposition at a temperature below about 90.degree. C. is dissolved or dispersed in the wax matrix. The oil and water phases are emulsified by an emulsifying agent that provides freedom from phase separation at a pH value of about 4.5 to about 8, while also providing phase separation at a pH value below about 2.0. The emulsifier, based on lecithin, is present at about 2 to about 20 weight percent of the total composition. The composition can also contain zero to about 35 weight percent additional excipient.
REFERENCES:
patent: 4952402 (1990-08-01), Sparks et al.
patent: 5188837 (1993-02-01), Domb
patent: 5444041 (1995-08-01), Owen et al.
Domb, Proceed, Intern. Symp. Control. Rel. Bioact. Mat., 20:121-122 (Jul. 1993).
The Lecithin Book, Central Soya, Chemurgy Division, Forth Wayne, IN (1993).
PCT/US95/07908 International Search Report.
Mendes Robert W.
Pathak Nitin P.
Tabibi S. Esmail
Ascent Pharmaceuticals, Inc.
Mullis Jeffrey C.
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