Moxifloxacin salts

Concurrent use of the fluoroquinolones with theophylline causes an increase in serum theophylline levels. When used concurrently with cimetidine, the cimetidine may interfere with the elimination of the fluoroquinolones. Use of the fluoroquinolones with an oral anticoagulant may cause an increase in the effects of the oral coagulant. Administration of the fluoroquinolones with antacids, iron salts, or zinc will decrease absorption of the fluoroquinolones. There is a risk of seizures if fluoroquinolones are given with the NSAIDs. There is a risk of severe cardiac arrhythmias when the fluoroquinolones gatifloxacin and moxifloxacin are administered with drains that increase the QT interval (eg, quini-dine, procainamide, amiodarone, and sotalol). 

The synthesis of the moxifloxacin core (de Souza, 2006 Martel et al., 1997 Seidel et al., 2000) proceeds from a Grohe-Heitzer sequence as described earlier in the chapter. Unlike the traditional Grohe-Heitzer sequence, however, the opening step involved the reaction between acid chloride 101 with the mono potassium salt of malonic acid monoethyl ester (102) in the presence of triethylamine to deliver ketoester 103 (Scheme 4.18). Treatment of 103 with ethyl orthoformate furnished acrylate 104, which reacted with cyclopropyl amine to afford 105. Cyclization of 105 in the presence of sodium fluoride in DMF gave the moxifloxicin core 106. 

Sample preparation for tests in solutions 60pgmL water solution of moxifloxacin hydrochloride were measured off on quartz dishes of 4 cm diameter with the addition of water or of the appropriate water salt solution (CUSO4 5H2O, ZnS04-71120, Fe2(S04)3 -H20, Al2(S04)3 I8H2O). The dishes were sealed with a quartz lid. 

Sample preparation for tests in solid phase Samples were prepared by measuring off 60- J,g mL" methanol solution of moxifloxacin hydrochloride with the addition of water or the appropriate salt aqueous solution on Petri dishes of 5 cm diameter. Samples were mixed and evaporated in a water bath until dry matter was obtained. After irradiation, the content of individual dishes was dissolved in methanol. 

---