Background: Dienogest is a potential treatment for pelvic pain associated with endometriosis, a condition of significant concern in gynaecology. The current study was conducted as a crossover-randomized bioequivalence...Background: Dienogest is a potential treatment for pelvic pain associated with endometriosis, a condition of significant concern in gynaecology. The current study was conducted as a crossover-randomized bioequivalence assessment of two oral Dienogest 2 mg formulations, aiming to provide valuable insights for healthcare professionals and researchers in this field. Objective: The primary aim of this research was to evaluate and compare the pharmacokinetic characteristics of Dienogest 2 mg tablets. Dinogest (Dienogest 2 mg) tablets, manufactured by Nuvista Pharma Limited in Bangladesh, and Visanne (Dienogest 2 mg) tablets, manufactured by Bayer Pharma in Germany, were the test and reference formulations, respectively. Materials and Method: The study was an open-label, balanced, randomized, two treatments, two sequences, two periods, two-way crossover, laboratory blind, single oral dose bioequivalence study conducted in healthy adult females under fasting conditions. The study was carried out on 13 healthy, non-pregnant female subjects, and all the subjects completed both study periods with a 15-day washout in between. Randomization was used to assign the test and reference formulations to the subjects. Following each oral administration, a series of blood samples were obtained at different time intervals from pre-dose to 72 hours post-dose and analyzed for Dienogest concentrations using a validated bio-analytical method. A standard non-compartmental model was used to analyze the pharmacokinetic parameters. The primary pharmacokinetic parameters were peak plasma drug concentration (C<sub>max</sub>), the area under the plasma concentration-time curve from time zero to time t (AUC<sub>0–t</sub>), and AUC from t = 0 to infinity (AUC<sub>0–∞</sub>). The other PK parameters included time to reach C<sub>max</sub> (T<sub>max</sub>), terminal elimination rate constant (K<sub>el</sub>), and half-life (t<sub>1/2</sub>). Result: The ratios and 90% CI for the geometric mean test/reference were 95.53% (86.70% - 105.26%) for C<sub>max</sub>, 101.75% (95.42% - 108.49%) for AUC<sub>0</sub><sub>−</sub><sub>t</sub>, and 101.54% (95.59%% - 107.87%) for AUC<sub>0</sub><sub>−</sub><sub>∞</sub>. The formulations were bioequivalent since the 90% CIs for the geometric mean test/reference ratios were 80% to 125%, according to the predetermined range of US Food and Drug Administration (FDA) requirements. Conclusion: This single-dose investigation shows that the Dienogest test and reference formulations exhibited a rate and degree of absorption that met the regulatory requirements for bioequivalence.展开更多
文摘Background: Dienogest is a potential treatment for pelvic pain associated with endometriosis, a condition of significant concern in gynaecology. The current study was conducted as a crossover-randomized bioequivalence assessment of two oral Dienogest 2 mg formulations, aiming to provide valuable insights for healthcare professionals and researchers in this field. Objective: The primary aim of this research was to evaluate and compare the pharmacokinetic characteristics of Dienogest 2 mg tablets. Dinogest (Dienogest 2 mg) tablets, manufactured by Nuvista Pharma Limited in Bangladesh, and Visanne (Dienogest 2 mg) tablets, manufactured by Bayer Pharma in Germany, were the test and reference formulations, respectively. Materials and Method: The study was an open-label, balanced, randomized, two treatments, two sequences, two periods, two-way crossover, laboratory blind, single oral dose bioequivalence study conducted in healthy adult females under fasting conditions. The study was carried out on 13 healthy, non-pregnant female subjects, and all the subjects completed both study periods with a 15-day washout in between. Randomization was used to assign the test and reference formulations to the subjects. Following each oral administration, a series of blood samples were obtained at different time intervals from pre-dose to 72 hours post-dose and analyzed for Dienogest concentrations using a validated bio-analytical method. A standard non-compartmental model was used to analyze the pharmacokinetic parameters. The primary pharmacokinetic parameters were peak plasma drug concentration (C<sub>max</sub>), the area under the plasma concentration-time curve from time zero to time t (AUC<sub>0–t</sub>), and AUC from t = 0 to infinity (AUC<sub>0–∞</sub>). The other PK parameters included time to reach C<sub>max</sub> (T<sub>max</sub>), terminal elimination rate constant (K<sub>el</sub>), and half-life (t<sub>1/2</sub>). Result: The ratios and 90% CI for the geometric mean test/reference were 95.53% (86.70% - 105.26%) for C<sub>max</sub>, 101.75% (95.42% - 108.49%) for AUC<sub>0</sub><sub>−</sub><sub>t</sub>, and 101.54% (95.59%% - 107.87%) for AUC<sub>0</sub><sub>−</sub><sub>∞</sub>. The formulations were bioequivalent since the 90% CIs for the geometric mean test/reference ratios were 80% to 125%, according to the predetermined range of US Food and Drug Administration (FDA) requirements. Conclusion: This single-dose investigation shows that the Dienogest test and reference formulations exhibited a rate and degree of absorption that met the regulatory requirements for bioequivalence.
