| 摘要 |
1,258,352. Erythromycin salts. ABBOTT LABORATORIES. 3 Sept., 1969 [4 Sept., 1968], No. 43710/69. Heading C2A. Novel erythromycin aliphatic sulphate salts having the general formula wherein Ery represents the erythronolide and cladinose moieties of erythromycin A or B and n is zero or an integer from 1 to 4, are prepared by adding to a solution of erythromycin A or B in a suitable solvent (e.g. aqueous acetone) a molar equivalent of an alkali metal salt of an aliphatic sulphate, of formula CH 3 (CH 2 ) (10 +2n) .CH 2 OSO 2 (O-Alkali metal) wherein n is as above, together with an excess of an acid or acid salt over that required to react with the alkali metal from said alkali metal salt. The acid or acid salt (e.g. acetic acid, HC1, sodium dihydrogen phosphate or sodium hydrogen sulphate) is preferably added in sufficient quantity to bring the pH to 5.5 to 6.5. The mixture is preferably warmed to aid the reaction, and the product is precipitated by adding water to the reaction mixture. Pharmaceutical compositions having antibiotic activity comprise an erythromycin aliphatic sulphate salt of Formula I as defined above together with a pharmaceutically acceptable carrier. They are preferably in forms for oral administration, e.g. tablets, chewable tablets or reconstitutable powders or granules. |
