Preparation and in vitro-in vivo Evaluation of Elagolix Sodium Tablets
In this study,elagolix sodium self-developed tablets were formulated by optimizing three key formulation process parameters,namely the particle size of active pharmaceutical ingredient(API),the aperture of sieve screen in the dry granulation process,and the tablet hardness.The similarity factor(f2)values between the dissolution curves of the self-developed and reference tablets were calculated as a criterion for evaluation.The results indicated that when the API particle size[d(0.9)]was 250 μm,the aperture of sieve screen was 1.4 mm,and the tablet hardness was 80 N,the in vitro dissolution behavior of the self-developed tablets was similar to that of the reference formulations.Subsequently,bioequivalence was investigated using relevant permeation parameters from the parallel artificial membrane permeation assay(PAMPA)and pharmacokinetic characteristics in Beagle dogs.The results revealed that the permeation rates of the self-developed tablets and the reference formulations were 8.698 8 and 8.161 6 μg·mL-1·min-1 respectively,with membrane permeabilities of 2.24× 10-4 and 2.10× 10-4 cm/s.The confidence interval for the self-developed tablets ranged from 100.82％to 104.54％.There was no statistically significant difference in the pharmacokinetic parameters between the two groups(P＞0.05).The relative bioavailability of the self-developed tablets was found to be(95.4±8.69)％,demonstrating the bioequivalence with the reference formulations.
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