Abbreviations: BA, bioavailability; BV, bacterial vaginosis; TLC, thin layer chromatography; HPLC, high performance liquid chromatography; LOD, limit of detection; LOQ, limit of quantification; LLOQ, lower limit of quantification; ULOQ, upper limit of quantification; QCs, quality control samples; CV, coefficient of variation; AUC, area under curve
IntroductionBioavailability (BA) is defined as the rate and extent to which the active ingredient or active moiety is absorbed from a drug product and becomes available at the site of action. For drug products that are not intended to be absorbed into the bloodstream, bioavailability may be assessed by measurements intended to reflect the rate and extent to which the active ingredient or active moiety becomes available at the site of action.1 Some drugs have poor bioavailability and hence take a longer time to act. These drugs therefore do not pass the phase 1 of the clinical trials as these do not meet the necessary criteria of having the maximum bioavailability and hence show a delayed onset of action. In such cases of bioavailability issues, one of the optimal solutions can be bioenhancement of that drug with a suitable bioenhancer to augment its bioavailabilty and hence a dose reduction. There are some drugs, however, which have a moderate bioavailability but only when given in higher doses. One such drug is Secnidazole.Secnidazole is a 5-nitroimidazole. It has a spectrum of activity against anaerobic micro-organisms and it is particularly effective in the treatment of amoebiasis, giardiasis, trichomoniasis and bacterial vaginosis. Secnidazole is rapidly absorbed after oral administration and it has a bioavailability of about 80%.
2The major advantages of Secnidazole are as follows: 3,4 a. Secnidazole is the longest acting medicine with a half-life of 17-29 hours in the category of nitroimidazole drugs.b. As such, available clinical data suggest that the main place of one-dose Secnidazole is as an alternative to multiple-dose metronidazole for treatment of mild or moderate intestinal amoebiasis, particularly in rural endemic regions lacking extensive medical facilities and follow-up capability.c. Oral doses of Secnidazole have produced clinical cure and parasitological eradication in 80 to 100% of adults and children with intestinal amoebiasis, mostly of mild or moderate severity.d. It has a broad spectrum of activity against anaerobic bacteria as compared to other drugs in the same class.In patients with intestinal amoebiasis or giardiasis, clinical or parasistological cure rates of 80 to 100% are achieved after treatment with a 2g dose of Secnidazole. This high dose of Secnidazole causes a lot of side effects even with a single dose. The symptomatic side effects produced by Secnidazole include dizziness, abdominal pain, urticaria, glossitis, stomatitis, taste disturbances, paresthesias. There are cases where the therapy has been withdrawn after a single administration due to these effects. If they become severe, they can be treated symptomatically. 5 The severe o...