Complete dataset for 2-treatment, 2-sequence, 2-period efavirenz bioequivalence study conducted with nightly dosing

The efavirenz pharmacokinetic raw data presented in this article was obtained in an average bioequivalence study between a local brand and Stocrin (Merck Sharp & Dohme, purchased from Australia, batch H009175, expiration date November 2013). Dose was administered at night (9:00 p.m.) two hours after food intake. Fourteen healthy subjects, 8 women and 6 men, completed the study. For each subject, 15 data points until 96 h post-administration are included. Subject demographic characteristics and sequences of administration are provided along with individual pharmacokinetic profiles of efavirenz obtained for both formulations after a single oral dose of 600 mg. This data provides information in support of the research article “Sex-by-formulation interaction assessed through a bioequivalence study of efavirenz tablets” [1].


a b s t r a c t
The efavirenz pharmacokinetic raw data presented in this article was obtained in an average bioequivalence study between a local brand and Stocrin (Merck Sharp & Dohme, purchased from Australia, batch H009175, expiration date November 2013). Dose was administered at night (9:00 p.m.) two hours after food intake. Fourteen healthy subjects, 8 women and 6 men, completed the study. For each subject, 15 data points until 96 h postadministration are included. Subject demographic characteristics and sequences of administration are provided along with individual pharmacokinetic profiles of efavirenz obtained for both formulations after a single oral dose of 600 mg. This data provides information in support of the research article "Sex-by-formulation interaction assessed through a bioequivalence study of efavirenz tablets" [1].
& Data collected for the Reference formulation could be managed with the objective of comparing its performance in different populations.
Development of in vitro-in vivo correlations. Efavirenz is classified as Class II drug in the Biopharmaceutical Classification System (BCS), its oral absorption is limited by its dissolution. Appropriate in vitro assays could help to explain and predict dosage bioavailability.

Data
In this article, raw pharmacokinetic data obtained in an efavirenz average bioequivalence study carried out on 14 healthy subjects is presented. Venous plasma efavirenz concentrations were obtained after a 600 mg oral dose of a local brand (Test) and the Reference, Stocrin (Merck Sharp & Dohme).

Experimental design, materials and methods
A randomized two-treatment, two-period, two-sequence, single-dose crossover study with a washout period of 28 days was performed for bioequivalence evaluation of Test formulation. Sixteen healthy Caucasian subjects were initially recruited, 8 males and 8 females. Dose (600 mg) was administered at night (9:00 p.m.) two hours after the intake of a standardized dinner. Blood samples were obtained up to 96 h post-dosing. Efavirenz concentrations were measured in venous plasma by high performance liquid chromatography with UV detection at 205 nm (HPLC-UV), using a validated analytical method with a lower limit of quantification of 50 ng/mL. Detailed information regarding this method was previously described [1]. The study protocol followed the tenets of the Declaration of Helsinki adopted by the World Medical Association in 1964 and its successive amendments, being previously approved by the Institutional Ethics Review Committee of the Faculty of Chemistry -Universidad de la República. All volunteers received a leaflet with study details and efavirenz information and signed a consent form before their entry to the study. Table 1 summarizes the demographic characteristics of participating volunteers, along with the assigned sequence of product administration. Fourteen volunteers finished the study. Subject 16 did not show up the first day of the study. Subject 11 presented rash after administration of Test formulation. Fortunately, both individuals belonged to different sequence of administration, and so replacement was not necessary to maintain the crossover balanced.  Pharmacokinetic data of efavirenz after single oral dose of Test and Reference is presented in Figs. 1 and 2. For subject 11, only Test data is available. Individual efavirenz plasma concentration from both formulations could be retrieved from a previously published article [2].