Claims
- 1. A stable, rapidly soluble, lyophilised injectable composition comprising an anthracycline glycoside selected from the group consisting of 4'-epi-doxorubicin, 4'-desoxydoxorubicin, daunorubicin, 4-demethoxy danunorubicin and their pharmaceutically acceptable salts, and a cosolubilizing agent selected from the group consisting essentially of a hydroxy-, mercapto-, or amino-substituted benzoic acid, an alkali metal salt thereof, a C.sub.1 -C.sub.4 alkyl ester thereof, a ringhalogenated methyl-substituted phenol, an amino acid, and mixtures thereof.
- 2. The composition of claim 1, wherein the salt of the anthracycline glycoside is the hydrochloride.
- 3. The composition of claim 1, wherein the cosolubilizing agent is selected from the group consisting of p-hydroxy-benzoic acid and the methyl ester thereof, p-aminobenzoic acid and the methyl ester thereof, o-hydroxybenzoic acid and the methyl ester thereof, 3-methyl-4-chlorophenol, 3,5-dimethyl-4-chlorophenol, and mixtures thereof.
- 4. The composition of claim 3, wherein said cosolubilizing agent is p-hydroxy-benzoic acid methyl ester.
- 5. The composition of claim 1, further including an inert excipient.
- 6. The composition of claim 5, wherein said inert excipient is lactose.
- 7. A sterile solution comprising water, an anthracycline glycoside selected from the group consisting of 4'-epi-doxorubicin, 4'-desoxy-doxorubicin, daunorubicin, 4-demethoxy daunorubicin and their pharmaceutically acceptable salts, and a cosolubilizing agent selected from the group consisting essentially of a hydroxy-, mercapto-, or amino-substituted benzoic acid, an alkali metal salt thereof, a C.sub.1 -C.sub.4 alkyl ester thereof, a ring-halogenated methyl-substituted phenol, an amino acid, and mixtures thereof.
- 8. A sterile injectable solution obtained upon reconstitution of the lyophilised composition of claim 1 in an aqueous medium.
- 9. The solution of claim 8, wherein the solution is obtained upon reconstitution with physiological saline solution.
- 10. A method of improving the solubility of a lyophilised preparation containing an anthracycline glycoside selected from the group consisting of 4'-epi-doxorubicin, 4'-desoxy-doxorubicin, daunorubicin, 4-demethoxy-daunorubicin, and their pharmaceutically acceptable salts, in an aqueous medium, said method comprising combining the said anthracycline glycoside or a salt thereof with a cosolubilizing agent selected from the group consisting essentially of a hydroxy-, mercapto-, or amino-substituted benzoic acid, an alkali metal salt thereof, a C.sub.1 -C.sub.4 alkyl ester thereof, a ring-halogenated methyl-substituted phenol, an amino acid, and mixtures thereof, and freeze drying the resulting combination, with said anthracycline glycoside or salt thereof remaining in the presence of said cosolubilizing agent.
- 11. The method of claim 10, wherein said preparation further includes an inert excipient.
Priority Claims (1)
Number |
Date |
Country |
Kind |
8426672 |
Oct 1984 |
GBX |
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Parent Case Info
This is a divisional application of Ser. No. 788,158, filed Oct. 16, 1985, now U.S. Pat. No. 4,675,311.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
4177264 |
Wu et al. |
Dec 1979 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
21242244 |
Feb 1984 |
GBX |
Non-Patent Literature Citations (1)
Entry |
Chemical Abstracts, vol. 104, No. 6, Feb. 10, 1986, p. 382 No. 39716d Columbus, Ohio & JP-A-60 92 212 (Kyowa Hakko Kogyo Co., Ltd.) 23-05-1985. |
Divisions (1)
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Number |
Date |
Country |
Parent |
788158 |
Oct 1985 |
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