Biphasic Effect of Rifampicin on Bilirubin- A Case Report

Manigandan, Gopi

doi:10.7860/jcdr/2016/18040.7614

Cited by 4 publications

(2 citation statements)

References 5 publications

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“…Rabbits that received the oral RF suspension showed significant ( p < 0.05) changes in ALT (80.3 ± 0.16 U/L), AST (37.97 ± 5.9 U/L), albumin (3.41 ± 0.18 mg/dL) and total bilirubin (0.61 ± 0.06 mg/dL) when compared to the control group. The mechanism by which RF can induce liver toxicity is not fully established, but it can be partially explained by two mechanisms: the first is that the liver is the major site for metabolizing antitubercular drugs [ 40 ] and for the production of RF metabolites, which may have direct toxicity or induce immunological liver injury [ 41 ]; and the second is hepatic enzyme induction, which enhances the metabolism of other co-administered drugs. However, the toxicity is mainly accompanied by a significant increase in liver enzymes [ 42 ] and decrease in albumin [ 43 ] and cholestasis [ 44 ].…”

Section: Resultsmentioning

confidence: 99%

Mucoadhesive In Situ Rectal Gel Loaded with Rifampicin: Strategy to Improve Bioavailability and Alleviate Liver Toxicity

et al. 2021

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Although it is a front-line in tuberculosis treatment, rifampicin (RF) exhibits poor oral bioavailability and hepatotoxicity. Rectal mucoadhesive and in situ rectal gels were developed to overcome drug drawbacks. A RF/polyethylene glycol 6000 co-precipitate was first prepared in different ratios. Based on the drug solubility, the selected ratio was investigated for drug/polymer interaction and then incorporated into in situ rectal gels using Pluronic F127 (15%) and Pluronic F68 (10%) as a gel base and mucoadhesive polymers (HPMC, sodium alginate and chitosan). The formulations were assessed for gelation temperature and gel strength. The selected formulation was investigated for in vivo assessments. The results showed that a 1:1 drug/polymer ratio exhibited satisfying solubility with the recorded drug/polymer interaction. Depending on their concentrations, adding mucoadhesive polymers shifted the gelation temperature to lower temperatures and improved the gel strength. The selected formulation (F4) did not exhibit any anal leakage or marked rectal irritation. Using a validated chromatographic analytical method, F4 exhibited higher drug absorption with a 3.38-fold and 1.74-fold higher bioavailability when compared to oral drug suspension and solid suppositories, respectively. Toxicity studies showed unnoticeable hepatic injury in terms of biochemical, histopathological and immunohistochemical examinations. Together, F4 showed a potential of enhanced performance and also offered lower hepatic toxicity, thus offering an encouraging therapeutic alternative.

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Section: Resultsmentioning

confidence: 99%

Mucoadhesive In Situ Rectal Gel Loaded with Rifampicin: Strategy to Improve Bioavailability and Alleviate Liver Toxicity

et al. 2021

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“…However, the most severe is a toxic liver damage [13,20,21]. The risk of a toxic liver damage is the highest on the background of the present chronic hepatitis and HIV infection [22].…”

Section: Drug Therapymentioning

confidence: 99%