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Q1: How does Diloxanide furoate exert its effects within the body?

A1: While the precise mechanism of action remains not fully elucidated, research suggests Diloxanide furoate primarily targets the lumen of the intestine, exerting its effects directly on luminal amoebae. [] It is considered a luminal amoebicide, primarily active against Entamoeba histolytica trophozoites residing within the gut. [, ] This targeted action makes it particularly effective for treating asymptomatic intestinal amoebiasis. [, ]

Q2: What is the molecular formula and weight of Diloxanide furoate?

A2: Diloxanide furoate has the molecular formula C14H11Cl2NO4 and a molecular weight of 328.15 g/mol. []

Q3: Are there any spectroscopic data available for Diloxanide furoate?

A3: Yes, several studies employ spectroscopic techniques for analysis:

• PMR Spectroscopy: A PMR spectroscopy method using tetramethylsilane (TMS) as an internal standard was developed to quantify Diloxanide furoate in both pure powder and tablet formulations. The method relies on the N-CH3 protons singlet peak at δ = 3.23 for quantitative measurement. []
• UV Spectrophotometry: UV spectrophotometry plays a crucial role in analyzing Diloxanide furoate. Studies use specific wavelengths for detection and quantification, including 258 nm, 270 nm, 280 nm, and 311 nm, depending on the analytical method and the other compounds present in the sample. [, , , , , ]

Q4: How does the presence of carbohydrates affect the stability of Diloxanide furoate?

A4: Research indicates that certain carbohydrates can influence Diloxanide furoate stability. In alkaline conditions, sucrose, glucose, fructose, and lactose were found to accelerate the hydrolysis of Diloxanide furoate at 40°C. [] Interestingly, Diloxanide furoate exhibited better stability in fructose, lactose, and sorbitol solutions at room temperature. []

Q5: How does light exposure impact the stability of Diloxanide furoate?

A5: Studies reveal Diloxanide furoate is susceptible to photodegradation. Exposure to UV irradiation, artificial room light, and sunlight leads to degradation. The photodegradation process follows first-order kinetics in both quartz cells and glass bottles. Solvent choice also influences the rate of photodegradation. []

Q6: What strategies can enhance Diloxanide furoate's photostability?

A6: The addition of photoprotective agents like para-aminobenzoic acid (PABA) and ascorbic acid significantly improves the photostability of Diloxanide furoate solutions exposed to 254 nm UV irradiation. Commercially available Tang® preparation, containing sugars, buffers, stabilizers, and artificial colors, also demonstrated a photoprotective effect. []

Q7: What formulation strategies are explored to enhance Diloxanide furoate's delivery and performance?

A7: Several approaches are under investigation to optimize Diloxanide furoate delivery:

• Cyclodextrin Complexation: Complexation with β-cyclodextrin (βCD), methyl-β-cyclodextrin (MβCD), and hydroxypropyl-β-cyclodextrin (HPβCD) has been shown to significantly improve the solubility and dissolution rate of Diloxanide furoate. [] This strategy holds promise for enhancing its bioavailability and therapeutic efficacy.
• pH-Dependent Polymers: Studies explore colon-targeted delivery using pH-sensitive polymers like Eudragit S100, Eudragit L 100, and Cellulose acetate phthallate. These polymers aim to control drug release in specific intestinal regions for optimal therapeutic effect. []

Q8: What analytical techniques are commonly employed in Diloxanide furoate research?

A8: A range of analytical techniques are utilized to characterize and quantify Diloxanide furoate:

• High-Performance Liquid Chromatography (HPLC): This versatile technique is frequently used to assay Diloxanide furoate in pharmaceutical formulations, study its stability, and analyze its presence in biological samples. Different variations of HPLC, including RP-HPLC, are employed. [, , , , , , , , , , , , , ]
• Thin-Layer Chromatography (TLC): This method provides a rapid and cost-effective way to separate and quantify Diloxanide furoate in mixtures. High-performance TLC (HPTLC) offers enhanced sensitivity and resolution for analysis. [, ]
• UV Spectrophotometry: This technique utilizes the absorption properties of Diloxanide furoate at specific wavelengths to determine its concentration in various samples. [, , , ]
• Difference Spectrophotometry: This technique measures the absorbance difference at specific wavelengths, allowing the determination of Diloxanide furoate in the presence of other components. []

Q9: How is the validity of these analytical methods ensured?

A9: The analytical methods employed in Diloxanide furoate research undergo rigorous validation procedures following guidelines set by organizations like the International Conference on Harmonisation (ICH). [, , , , , , , ] The validation process typically involves assessing parameters like linearity, accuracy, precision, specificity, limit of detection (LOD), and limit of quantitation (LOQ). [, , , , , , ] This rigorous validation process ensures the reliability and reproducibility of the results obtained from these analytical methods.

Q10: What is the clinical significance of distinguishing pathogenic from non-pathogenic Entamoeba histolytica strains?

A10: The identification of distinct pathogenic and non-pathogenic Entamoeba histolytica strains has important implications for treatment decisions. While both strains can colonize the human gut, only pathogenic strains cause invasive disease. [] Therefore, treatment with Diloxanide furoate, a luminal amebicide, is typically recommended only for infections confirmed to be caused by pathogenic strains. [, , ]

Q11: What challenges are associated with treating intestinal amoebiasis in specific populations?

A11: Difficulties in treatment can arise in settings where hygiene and sanitation are compromised, potentially leading to reinfection. This has been observed in institutions housing mentally disabled individuals. In such cases, combined therapeutic approaches, including metronidazole followed by Diloxanide furoate, have proven effective in controlling the spread of infection. []

Q12: How does Diloxanide furoate compare to other available treatments for amoebiasis?

A12: While Diloxanide furoate effectively targets luminal amoebae, it might not be sufficient to completely eliminate amoebae residing within tissues. [, , , ] In such cases, a combination therapy approach, often involving metronidazole or other nitroimidazole derivatives followed by Diloxanide furoate, is recommended. [, , , ] The choice of treatment often depends on the clinical presentation, the severity of infection, and the presence or absence of extraintestinal involvement.