FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to an emulsion composition for treating cardiopathy, autoimmune disease, sepsis, septic shock, severe sepsis, organopathy, septicemia, endotoxic shock, shock, inflammatory disease, central nervous system disease or infectious disease. The composition contains (A) a compound stable in sour conditions which represents (a) a compound presented by formula:
where R represents an optionally substituted aliphatic hydrocarbon group, an optionally substituted aromatic hydrocarbon group, an optionally substituted heterocyclic group, a group presented by formula -OR1 where R1 represents hydrogen atom or an optionally substituted aliphatic hydrocarbon group, or a group presented by formula: where R1b represents hydrogen atom or an optionally substituted aliphatic hydrocarbon group, R1c has the same value as R1b, or differs, and represents hydrogen atom or an optionally substituted aliphatic hydrocarbon group, R0 represents hydrogen atom or an optionally substituted aliphatic hydrocarbon group, or R and R0 are combined to form a bond; the ring A1 represents cycloalkene optionally substituted by 1-4 substitutes selected from a group consisting of (1) an aliphatic hydrocarbon group optionally having substitutes, (2) an aromatic hydrocarbon groups optionally having substitutes, (3) a groups presented by formula; -OR1 where R1 represents hydrogen atom or an aliphatic hydrocarbon group optionally having substitutes, and (4) halogen atom, Ar represents an optionally substituted aromatic hydrocarbon group, and a group presented by formula represents a group presented by formula or n represents an integer from 1 to 4, or (b) a compound presented by formula: where R1 represents an optionally substituted aliphatic hydrocarbon group, an optionally substituted aromatic hydrocarbon group, an optionally substituted heterocyclic group, a group presented by formula: OR1a' where R1a' represents hydrogen atom or an optionally substituted aliphatic hydrocarbon group, or a group presented by formula: where R1b' and R1c are equal or different and represent hydrogen atom or an optionally substituted aliphatic hydrocarbon group, X represents a methylene group, nitrogen atom, sulphur atom or oxygen atom, Y represents an optionally substituted methylene group or an optionally substituted nitrogen atom, the ring A represents a 5-8-member ring which is optionally substituted additionally by 1-4 substitutes selected from a group consisting of (1) an aliphatic hydrocarbon group optionally having substitutes, (2) an aromatic hydrocarbon groups optionally having substitutes, (3) a group presented by formula: OR2' where R2' represents hydrogen atom or an aliphatic hydrocarbon group optionally having substitutes, and (4) halogen atom, Ar' represents an optionally substituted aromatic hydrocarbon group presented by formula, and a group presented by formula: presents a group presented by formula: or m represents an integer from 0 to 2, n' represents an integer from 1 to 3, and the sum m and n' is equal to 4 or less provided when X represents a methylene group, Y represents an optionally substituted methylene group, or their salt or a prodrug, (B) a buffer, (C) oil, (D) an emulsifier and (E) water. The pH value of the compositions is reduced approximately to 3.7-5.5. Also, offered are a method for preparing the emulsion compositions and a method for long-term stabilisation of the emulsion composition.
EFFECT: preparing the composition of improved stability.
28 cl, 10 ex, 24 tbl
Authors
Dates
2011-09-10—Published
2006-04-27—Filed