A stability-indicating HPLC assay method has been developed to quantify metronidazole benzoate in suspensions. A study of the stabilities of two suspensions (16.0 mg/ml) of metronidazole benzoate in commercially available vehicles, Ora-Plus and a mixture of Ora-Plus and Ora-Sweet, showed that both suspensions were stable for at least 90 days at room temperature. The mobile phase required to elute metronidazole benzoate contained 40% acetonitrile versus approximately 10% for the free base. The solubility of the ester in water at 25 degrees C was found to be approximately 0.1 mg/ml versus 10 mg/ml for the free base. The ester did not hydrolyse significantly to the free base after storage for 8 h at 37 degrees C in simulated gastric fluid, and 5 h at 37 degrees C in simulated intestinal fluid. The bitter tasting metronidazole may not be satisfactorily substituted with its tasteless ester in the treatment of local gastrointestinal infections.
A range of isatin-thiazolidinone hybrid analogues were synthesized and their cytotoxicity was evaluated against several cancer cell lines in vitro. The acute toxicity studies in mice models revealed that these analogues possess low systemic toxicity and are safe up to 1600mg/Kg. Among the compounds synthesized, 5-(2-nitrobenzylidene)-2-(isatin-3-azino)-thiazolidin-4-one (CI) has been shown to be the most active, highly promising compound which induced S phase arrest in cell cycle in a time dependent manner. Our initial analysis indicate that incorporation of electron withdrawing group at ortho position of the ring favors over the meta and para positions for eliciting its cytostatic effect. Overall, the in vitro biological evaluation suggests that the growth inhibitory effect of CI is promising and can be studied further.
The stability of piperacillin sodium in the presence of tazobactam sodium in 5% dextrose and normal saline i.v. admixtures has been determined using a modified stability-indicating high performance liquid chromatography assay method reported in the literature. The solutions were stored at room and refrigerator temperatures in plastic bags. They remained clear throughout the study although the pH values decreased slightly during storage. The solutions were stable for 2 days at 25 degrees C and for 28 days at 5 degrees C. Tazobactam sodium appears to have a slight adverse effect on the stability of piperacillin sodium.
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