Bioequivalence evaluation of two marketed brands of stavudine 40mg capsules in healthy human South African volunteers

A Combined‐Formulation Tablet of Lamivudine/Nevirapine/Stavudine: Bioequivalence Compared With Concurrent Administration of Lamivudine, Nevirapine, and Stavudine in Healthy Indian Subjects

“…It is noted that race, ethnicity, and disease state may have profound effects on the antiretroviral drug disposition of the generic formulation. Although there are insufficient data on the effects of gender, race, and concurrent underlying conditions on the PK of d4T, a recent study suggested that the PK profile of d4T in healthy South African volunteers 34 was similar in nature to that presented in the present study. As antiretrovirals exhibit similar PK profiles in healthy subjects and in asymptomatic and symptomatic HIV‐infected individuals, disposition of d4T is likely to be similar in nature in asymptomatic and symptomatic South African patients.…”

Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Stavudine

“…No dissolution testing was performed. The composition of formulation was not reported 49. All the results meet the current BE criteria.…”

“…Two reports in the literature have demonstrated the BE of products containing d4T as the single API and Zerit® 40 mg (manufactured by Bristol‐Myers Squib, NJ, USA) as the reference drug product 48,49. In the first one, 40 healthy volunteers were enrolled and 90% confidence intervals (CIs) for log‐transformed C max and AUC 0– t were 93.9%–106.0% and 98.4%–101%, respectively.…”

Stavudine delivery in an extended release formulation: Will it provide the right in vivo pharmacokinetics - Some key observations

“…[2] No data are available in literature pertaining to the likely absorption sites of stavudine after oral administration, although all published pharmacokinetic data, including the 14 C oral dose data, strongly suggest that the absorption of stavudine is likely to happen in the upper gastrointestinal tract itself. [2][3][4] However, there has been a suggestion that stavudine may be subject to carrier-mediated absorption in the preclinical model. [5] Even as the relevance of such preclinical work to human subjects is not clearly understood, such data appear to be inconsequential, [5] as stavudine has excellent permeability and poses no challenges for passive absorption across a wide dose range, in human subjects.…”