Bioequivalence study of postcoital emergency contraceptions containing levonorgestrel.

OBJECTIVE: The progestogen-only method of emergency contraception, levonorgestrel, is one of the effectiveness in preventing expected pregnancies. The comparative bioavailability was carried out on levonorgestrel tablets (0.75 mg) from two different sources (Hungarian and Thai made). METHOD: Eighteen healthy female volunteers were given a single oral dose of 0.75 mg tablets in a crossover design. Serum levonorgestrel concentration was determined by radio-immunoassay. The pharmacokinetic analysis of serum levonorgestrel concentration from each treatment was established. The comparative bioavailability of the two products was determined by the analysis of variance (ANOVA) for two way crossover design. RESULTS: The results found that the mean peak (X +/- SD) serum concentration (Cmax) of the Thai-made pill and Hungarian-pill were 1.18 +/- 0.12 and 1.14 +/- 0.10 ng/ml, respectively. The 90% confidence intervalfor the difference of log Cmax mean was 99.54-120.78%. The time to peak serum concentration (Tmax) of the Thai-made pill and Hungarian-pill were 1.56 +/- 0.73 and 1.58 +/- 0.67 hrs, respectively. The different time of peak serum levonorgestrel concentration was 1.27%. The mean area under the curve (AUC) of Thai-made pill and Hungarian-pill were 2.14 +/- 0.21 and 2.09 +/- 0.16 ng.h/ml, respectively. The 90% confidence interval for the difference of log AUC mean was 103.27 - 121.89%. CONCLUSION: The present study revealed that the 90% confidence interval for the difference of log Cmax mean and log AUC mean were in the criteria of acceptance, which should be within 80-125%. So, the authors can conclude that the Thai-made pill was bioequivalent to the Hungarian-pill.

Interferencia endometrial de los estrógenos sintéticos en la regulación de la fertilidad / Endometrial interference of synthesis estrogens in fertility regulation

Inicialmente la actividad antiovulatoria de algunos preparados estrógeno/progestacional, era la acción requerida para controlar la fertilidad. A la fecha se ha conseguido una notable reducción en la dosis de ambos componentes hormonales, ofreciendo menos efectos colaterales, con una eficacia anticonceptiva aceptable. Actualmente se dispone de una variedad de esas combinaciones, en donde el estrógeno sintético concentra de 80 a 20 µg/tableta y la prescripción se inicia o el 1er. día o el 5o. día del ciclo menstrual. Al analizar el plasma y el endometrio simultáneamente obtenida de usuarias crónicas que incluían en la tableta dosis de 30 o 50 µg del estrógeno sintético, se observó un perfil de 17B-estradiol como el de la maduración folicular de los ciclos ovulatorios sólo en las mujeres que tomaban la dosis más baja. Sin embargo, este fenómeno de ciclicidad no se obtuvo a nivel local; paralelamente la progesterona circulante en ambos grupos nunca fue > 5.0 ng/ml. La observación indica que se debe buscar un periodo crítico local durante el ciclo menstrual ovulatorio, con mucho menores dosis hormonales para controlar la fertilidad