Claims
- 1. Crystalline 1,1-dioxopenicillanoyloxymethyl 6-(D-.alpha.-amino-.alpha.-phenylacetamido)penicillanate tosylate hydrates.
- 2. A compound according to claim 1, characterized in having a water content corresponding to a dihydrate.
- 3. A compound according to claim 1, characterized in having a water content corresponding to a monohydrate.
- 4. Method for producing a compound according to claim 1, characterized in that 1,1-dioxopenicillanoyloxymethyl 6-(D-.alpha.-amino-.alpha.-phenylacetamido)penicillanate or a salt thereof is reacted with p-toluenesulfonic acid or one of its salts in a suitable medium with a view to accomplishing the formation of the crystalline compound, which is recovered and optionally recrystallized in order to obtain a product with the desired water content.
- 5. Method for producing a compound of claim 1, characterized in that an amino-protected derivative of 1,1-dioxopenicillanoyloxymethyl 6-(D-.alpha.-amino-.alpha.-phenylacetamido)penicillanate is reacted with p-toluenesulfonic acid resulting in cleavage of the protecting group and formation of a compound of claim 1.
- 6. Method for producing a compound of claim 1, characterized in subjecting 1,1-dioxopenicillanoyloxymethyl 6-(D-.alpha.-amino-.alpha.-phenylacetamido)penicillanate tosylate to crystallization from a suitable solvent or a mixture of solvents containing a sufficient amount of water to accomplish formation of the desired crystalline hydrate.
- 7. An antimicrobial or antibacterial composition, comprising as an active ingredient an effective amount of a compound according to claim 1 together with a pharmaceutically acceptable, non-toxic carrier.
- 8. A composition according to claim 7 in dosage unit form for enteral, parenteral or topical administration to patients suffering from bacterial infections.
- 9. A composition according to claim 8 for oral treatment of patients, containing from 50 mg to 2500 mg of the active ingredient.
- 10. A composition according to claim 9, in which the active ingredient has a water content approximately corresponding to a dihydrate.
- 11. A composition according to claim 9, in which the active ingredient has a water content approximately corresponding to a monohydrate.
- 12. A composition according to claim 8 in the form of slow release tablets, effervescent tablets, pills, or capsules.
- 13. A composition according to claim 7 in form of a suspension.
- 14. A composition according to claim 7 in form of a powder.
- 15. A composition according to claim 7 in form of an intramammary preparation.
- 16. A composition according to claim 7 in form of an ointment.
- 17. A composition according to claim 8 in which the active ingredient constitutes from 1% to 95% of the composition.
- 18. A compounded composition according to claim 8 which contains one or more additional active compounds selected from the group consisting of .beta.-lactam antibiotics, antiviral agents, antifungal drugs, antitussives, pain-relieving drugs and probenecid.
- 19. A composition according to claim 18 in form of a multilayer tablet or a core tablet.
- 20. A process for the treatment of patients suffering from microbial or bacterial diseases which comprises administering thereto an effective amount of a compound according to claim 1.
- 21. A treatment according to claim 20, comprising the administration of an amount of the active compound of 3-200 mg/kg body weight of the patient/day.
- 22. A treatment according to claim 21 of an adult human being, comprising a daily administration of from 0.5 g to 5 g of the active compound.
- 23. A process for the treatment of a patient suffering from a microbial or bacterial disease which comprises administering thereto one or more additional active compounds selected from the group consisting of -lactam antibiotics, antiviral agents, antifungal drugs, antitussives, pain-relieving drugs, and probenecid, the additional administration being undertaken simultaneously with the administration of a compound according to claim 1, or at spaced intervals with respect to the administration of said compound.
Priority Claims (1)
Number |
Date |
Country |
Kind |
8035156 |
Oct 1980 |
GBX |
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Parent Case Info
This is a continuation of application Ser. No. 314,021, filed Oct. 22, 1981, which was abandoned upon the filing hereof.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
4244951 |
Bigham |
Jan 1981 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
881675 |
Aug 1980 |
BEX |
Continuations (1)
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Number |
Date |
Country |
Parent |
314021 |
Oct 1981 |
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