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Abstract
Metronidazole (MTNZ) is an antiprotozoa drug, could be labeled with the 99mTc. MTZL could be used as an ideal vehicle to deliver radioactive decay energy of 99mTc to the sites of tumor, thus facilitate tumor imaging. The process of labeling was done using tin chloride as reducing agent. The optimum conditions required to label 25 μg MTZL were 100 μg stannous chloride, 30 min reaction time, room temperature at pH 7–9 using 0.5 M phosphate buffer. The radiochemical purity of the labeled compound, at the above conditions, was determined using paper chromatography. The yield was about 93%. About 2.5 × l06 of Ehrlich Ascites Carcinoma (EAC) was injected intrapritoneally (i.p) to produce ascites and intramuscularly (i.m) in the right thigh to produce solid tumor in female mice. Biodistribution studies were carried out by injecting solution of 99mTc-MTZL in normal and tumor bearing mice. The uptake in ascites was over 5% of the injected dose per gram tissue body weight, at 4 h post injection and above 4% in solid tumor. These data revealed localization of the tracer in the tumor tissues with high percentage sufficient to use 99 mTc MTZL as promising tool for diagnosis of tumor.
Normal-phase TLC with densitometric detection at 220 nm has been used for analysis of clotrimazole and metronidazole in combined-dose tablets and cream. The compounds were separated on silica gel plates with toluene-ethyl acetate-methanol-acetic acid 5.5:2:0.6:0.1 ( v/v ) as mobile phase. Regression analysis showed response was a linear function of the amounts of the drugs in the ranges 0.4–0.8 and 2–4 μg per band for clotrimazole and metronidazole, respectively. Quantification was achieved by measurement of peak area and comparison with calibration standards. The method was successfully applied to pharmaceutical formulations. There was no chromatographic interference from common excipients present in the tablets and cream. The method was validated for accuracy, precision, and specificity.
Abstract
A conjugate of 6-hydrazinopyridine-3-carboxylic acid (HYNIC) with the amino analogue of metronidazole (MN) was synthesized through a multiple-step reaction. HYNIC-MN could be labeled easily and efficiently with 99mTc using N-(2-hydroxy-1,1-bis(hydroxymethyl)ethyl)glycine (tricine) and ethylenediamine -N,N′-diacetic acid (EDDA) as coligands to form the 99mTc–HYNIC–MN complex in high yield (>95%). Its partition coefficient indicated that it was a good hydrophilic complex. The tumor cell experiment showed that the 99mTc–HYNIC–MN complex had a certain hypoxic selectivity. The biodistribution studies of 99mTc–HYNIC–MN in Kunming mice bearing S180 tumor showed a favorable tissue distribution profile with high tumor uptake, and low or negligible accumulation in non-target organs, suggesting 99mTc–HYNIC–MN would be a novel potential tumor hypoxia imaging agent.
A selective densitometric analysis has been adopted for the determination of pantoprazole sodium sesquihydrate, metronidazole, and clarithromycin as they play an important rule as co-administrated drugs in the treatment of helicobacter infection. The aim of this work was to find greener thin-layer chromatographic (TLC) solvents to follow the environmental safety measurements. The three drugs are vastly different in chemical structure, so it was very challenging to carry out the simultaneous separation and quantitation by TLC technique at R F values 0.49 ± 0.01, 0.72 ± 0.01, and 0.83 ± 0.01, respectively. In the developed method, chromatography was performed on TLC plates with pre-coated silica gel 60 F254 using ethyl acetate and absolute ethanol (3:1)‒heptane‒ammonia 33% (14:5:1, v/v) as the developing system with calculated polarity (3.535). Densitometric measurements were carried out using CAMAG Linomat 5 TLC scanner at 280 nm. Regression line data were evaluated by the least square method within the concentration range of pantoprazole sodium sesquihydrate, metronidazole, and clarithromycin 0.8–8, 4–40, and 5–50 μg band−1, and the detection limits of the drugs were 0.15, 0.76, and 0.88 μg band−1, respectively. The suitability of this TLC method for the quantity determination of three compounds in drug substances and drug products was proved by validation in accordance with the International Conference on Harmonization (ICH) guidelines (Q2R1). Statistical analysis was performed using Student’s t and F test, revealing no significant difference between the TLC method and the official ones concerning accuracy and precision.
Introduction Metronidazole (2-methyl-5-nitroimidazole-1-ethanol, MET) is classified therapeutically as an antibacterial and antiprotozoal agent, indicated for the treatment of bacterial vaginosis [ 1 ]. For the treatment of
, a broad-spectrum fluoroquinolone antibacterial agent, is commonly employed in the treatment of urinary and genital tract infections [4–6] . Metronidazole (MTZ) is the prototype nitroimidazole used for trichomoniasis and later found to be a highly
Abstract
The objective of this work was to develop and validate a fast and reproducible method to determine the concentration of metronidazole in drug substance and tablets. The samples were analyzed by dynamic thermogravimetry, using 10, 20, 40, 60 and 80C min–1 heating rates in nitrogen and in nitrogen with synthetic air. Obtained data were used in the Antoine and Langmuir equations in order to have the pressure curves. Vapor pressure curves of drug and tablet of metronidazole were evaluated using the mathematical indexes of difference factor, f 1, and similarity factor, f 2, to compare their profiles. The data showed that there is no significant difference between the vapor pressure profiles of drug and tablet of metronidazole in both environmental conditions, which confirms that the process is really vaporization. The concentration of metronidazole was determined in the raw material and tablets of the drug.
-07-6), cephalexin·H 2 O (CAS No. 23325-78-2), ciprofloxacin HCl (CAS No. 86393-32-0), levofloxacin (CAS No. 100986-85-4), and metronidazole (CAS No. 443-48-1). All of these compounds are antimicrobial pharmaceuticals. In addition, ciprofloxacin HCl and levofloxacin
Abstract
The purpose of the present work was to study the compatibility of metronidazole with different pharmaceutical excipients (hydroxypropyl methylcellulose, poly(ethylene oxide), microcrystalline cellulose, dicalcium phosphate dihydrate, and anhydrous dicalcium phosphate) using differential scanning calorimetry and diffuse reflectance spectroscopy. Dicalcium phosphate dihydrate was the only excipient that showed interaction with metronidazole even before storage. Changes referring to a possible transition to dihydrate form were observed in the thermal curves of anhydrous dicalcium phosphate after four weeks of storage. Although dicalcium phosphate dihydrate can be replaced by the anhydrous form in pharmaceutical formulations, the observed transition might negatively influence the stability of dosage forms.
Abstract
Compatibility studies between active drugs and excipients are substantial in the pharmaceutical technology. The objective of the present work was to develop pre-formulated mixtures of metronidazole (MT) obtained by spray drying (SPDR) and their thermoanalytical characterization. Dynamic and isothermal TG, conventional DSC and DSC coupled to a photovisual system were used. DSC experiments with both techniques confirmed the homogeneity of the conventional and pre-formulated mixtures. The TG data made possible the comparison the thermal stability of the different mixtures. Similar thermal stabilities were found of the conventional and pre-formulated mixtures, with slower particles sizes of MT.
