Metronidazole phosphate

On the other hand, formation of a prodrug such as a phosphate ester may increase hydrophilicity, thus enhancing solubility. For example, the solubility and dissolution rate of the 77-hydroxymethyl derivative of lomefloxacin is higher than those of the parent compound, and it can be converted readily back to the original molecule. Commonly used prodrugs are procaine penicillin metronidazole phosphate and chloramphenicol sodium succinate. 

Cho MJ, Kurtz RR, Lewis C, Machkovech SM, Houser DJ (1982) Metronidazole phosphate-a water-soluble prodrag for parenteral solutions of metronidazole. J Pharm Sci 71 410-414... 

Extraintestiaal (eg, hepatic) amebiasis is treated with metronidazole and can be followed by iodoquiaol or a combination of dehydroemetiae or emetine hydrochloride with chloroquiae phosphate. Iodoquiaol is the dmg of choice for asymptomatic amebiasis, whereas ddoxanide furoate (9, Furamide) has been used successftiUy to treat symptomatic and asymptomatic intestinal amebic cyst carriers. 

The hypoxia-targeting potential of 99mTc(CO)3 core labelled with 2-nitro and 4-nitroimidazoles has been studied. Phosphate coupled metronidazole gave fast clearout from major organs but high accumulation in bone. There is no tumor uptake study to date or... 

El-gizawy reported the analysis of diloxanide furoate in its dosage forms by a HPLC method [40]. Furazol tablets containing 200 mg of metronidazole and 250 mg of diloxanide furoate were treated with 50 mL of methanol, sonicated for 10 minutes, and diluted to 100 mL with methanol. A portion of the resulting solution was centrifuged, and a 20 pL portion of the clear supernatant solution diluted to 10 mL with the mobile phase. This process yielded a final analyte concentration equivalent to 5 pg/mL. 20 pL aliquots of the solution were annualized by HPLC using a stainless steel column (10 cm x 4.6 mm) packed with Cyclobond I. The mobile phase consisted of 13 7 0.05 M phosphate buffer (pH 7) methanol (flow rate of 1 mL/min), and detection was performed at 254 nm. 

Drugs that are not absorbed from the gastrointestinal tract of the baby, such as warfarin, are safe for the mother to take. The administration of antibiotics to a breast-feeding mother usually poses no concern for the newborn infant. However, metronidazole, which has mutagenic properties, reaches concentrations in milk that equal or exceed maternal plasma levels. Caution is also advised with sulphonamides, nitrofurantoin, or naladixic acid since these can cause haemolysis in infants with glucose-6-phosphate dehydrogenase deficiency. 

Several systemic antibiotics that have traditionally been used in the treatment of acnevulgaris have been shown to be effective when applied topically. Currently, four antibiotics are so utilized clindamycin phosphate, erythromycin base, metronidazole, and sulfacetamide. The effectiveness of topical therapy is less than that achieved by systemic administration of the same antibiotic. Therefore, topical therapy is generally suitable only in mild to moderate cases of inflammatory acne. 

Nemutlu et al. [22] determined lomoxicam in pharmaceutical preparations by a liquid chromatographic method. The separation was achieved on a reversed phase (Nucleosil 100-5 Cis 25 cm x 4.6 mm, 5 gm) column kept at room temperature. The flow rate of mobile phase was 1 ml / min. The mobile phase consisted of 0.1 M phosphate buffer (pH 6)-acetonitrile (60 40) and UV detection at 293 nm. The retention times for the drug and the internal standard, metronidazole, were 5.65 and 3.95 min, respectively. Quantitative analysis of the drug in tablets and injections were performed. The method is fast, simple, inexpensive and applicable over a wide range of concentrations with high precision and accuracy. 

Citrate and phosphate ions were found to catalyze the photodegradation of sulfacetamide and sulfanilamide (63). Adriamycin is most stable in a citrate buffer, followed by phosphate and then acetate buffer (47). The order of the catalytic effect of buffer species for metronidazole was found to be citrate > acetate > phosphate buffer (68). Acetate ions were found to be most detrimental to the photostability of... 

Figure 11 Zero-order photodegradation of metronidazole in phosphate buffer of pH 7. without sodium urate O with sodium urate. Source From Ref. 68.

Antimicrobials. Metronidazole is present in milk in moderate amounts avoid prolonged exposure. Nalidixic acid and nitrofurantoin should be avoided where glucose-6-phosphate dehydrogenase deficiency is prevalent. Avoid clindamycin, dapsone, Uncomycin, sulphonamides. Regard chloramphenicol as unsafe. 

Acute intestinal amebic dysentery is most commonly treated with metronidazole (1, Flagyl) (Table 1). An alternative drug is iodoquinol (2, diiodohydroxyquin, diiodohydroxyquinoline [83-73-8]), which has also been used advantageously in combination with metronidazole or oxytetracydine (3, Terramycin [79-57-2]). For patients too sick to take iodoquinol orally, emetine (4) or dehydroemetine (5, 2,3-dehydroemetine) hydrochloride is administered either subcutaneously or intramusculady. The latter sometimes is followed by chloroquine (6, Aralen) phosphate or iodoquinol. Because emetine and dehydroemetine cause cardiac arrhythmias, muscle weakness, and inflammation at the injection site, these toxic compounds are used primarily for patients whose lives are threatened by the disease. Antibiotics, such as tetracycline (7, Achromycin [60-54-8]) and paromomycin (8, Humatin), are also effective against moderate intestinal amebiasis. 

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