US 5,624,914 A · Lipophilic oligosaccharide antibiotic salt compositions

Abstract

Pharmaceutically acceptable compositions of matter comprising a lipophilic oligosaccharide antibiotic, e.g., the everninomicin-type antibiotic of Formula III, at least a stoichiometric amount of a base, e.g., N-methylglucamine, an amount of, e.g., hydroxypropyl-.beta.-cyclodextrin, and optionally a pharmaceutically acceptable non-ionic surfactant, e.g., Tween-80, pharmaceutical compositions containing such compositions of matter, methods of treating and preventing susceptible bacterial infections in animals especially human beings as well as a method of preventing adverse reaction syndrome while simultaneously delivering an antiinfective amount of a lipophilic oligosaccharide antibiotic such as that of Formula III to said animals as well as the use of the compositions of matter for the preparation of a medicament for such treating or preventing are disclosed. ##STR1##

Claims22

Dependent claims

A composition comprising:

(a) a lipophilic oligosaccharide antibiotic represented by Formula I;
##STR15## wherein ##STR16## X is one of NO.sub.2, NO, NH.sub.2, NHCOCH.sub.3, NHOH, NH(C.sub.2 H.sub.5), N(C.sub.2 H.sub.5).sub.2, OH or H;
R.sub.2 is one of CH.sub.3, COCH(CH.sub.3).sub.2, COCH.sub.3, CO(CH.sub.2).sub.3 CH.sub.3, COCH.sub.2 CH.sub.3 or H;
R.sub.3 is CH.sub.3 or H;
R.sub.4 is one of COCH.sub.3, CH(OCH.sub.3)(CH.sub.3);
CH(OH)CH.sub.3, CHO, or H;
##STR17## R.sub.6 is CH.sub.3 or H;
R.sub.7 is CH.sub.3 or H;
R.sub.8 is CH.sub.3, CH.sub.2 OH or H;
R.sub.9 is CH.sub.3 or H;
Y is OH, H or CH.sub.3
W is Cl or H;
and
Z is Cl or H;
(b) at least about a stoichiometric amount of a base capable of forming a pharmaceutically acceptable salt with a lipophilic oligosaccharide antibiotic of Formula I;
(c) a hydroxypropyl-.alpha.-.beta.- or -.gamma.-cyclodextrin wherein the average number of hydroxypropyl substituents on said -.alpha., .beta.- and .gamma.-cyclodextrin is in the range of about 2 to about 15, and said amount is sufficient to achieve efficacious delivery of said lipophilic oligosaccharide antibiotic to the serum of an animal while simultaneously avoiding occurrence of adverse reaction syndrome;
and
(d) 0 to 6.0 by weight (basis an antibiotic of Formula I) of a pharmaceutically acceptable non-ionic surfactant.

15 more elements

Dependencies are inferred from the claim text.

Lipophilic oligosaccharide antibiotic salt compositions

Life of this patent

Lipophilic oligosaccharide antibiotic salt compositions

Life of this patent

Abstract

Claims22