We found a match
Your institution may have rights to this item. Sign in to continue.
- Title
Comparative Pharmacokinetic Profiles of a Novel Low‐Dose Micronized Formulation of Raloxifene 45 mg (AD‐101) and the Conventional Raloxifene 60 mg in Healthy Subjects.
- Authors
Lee, Hae Won; Kang, Woo Youl; Gwon, Mi‐Ri; Park, Soo‐Jin; Cho, Kyunghee; Seong, Sook Jin; Yoon, Young‐Ran
- Abstract
Raloxifene hydrochloride shows poor bioavailability (only 2%) when orally administered because of its poor aqueous solubility and its extensive first‐pass metabolism. A new micronized formulation of raloxifene was developed to improve bioavailability via enhanced gastrointestinal absorption. The primary objective of this study was to evaluate the pharmacokinetic characteristics of a new micronized raloxifene formulation (AD‐101) in comparison with the conventional raloxifene formulation. This study was designed as an open‐label, randomized, 2‐treatment‐period, crossover study with a 2‐week washout period. Two treatments consisted of micronized raloxifene 45 mg daily; and conventional raloxifene 60 mg daily administered in fasting conditions. Plasma raloxifene concentrations were determined by a validated method using ultra‐fast liquid chromatography–tandem mass spectrometry, and pharmacokinetic parameters were calculated using a noncompartmental model. In total, 49 subjects completed the study. The geometric mean ratio (micronized/conventional) of the maximum concentration and the area under the plasma concentration–time curve from time zero to the last concentration values were 1.08 (90% CI, 0.95‐1.24) and 0.97 (90% CI, 0.89‐1.05), respectively. The adverse event profile did not differ between the 2 formulations. The results demonstrate that micronized formulation of raloxifene 45 mg is equivalent to conventional formulation of raloxifene 60 mg when administered at the single dose in the fasted state. After single oral dosing of AD‐101, there were no serious or unexpected adverse events.
- Subjects
BIOAVAILABILITY; RALOXIFENE; LIQUID chromatography-mass spectrometry; PHARMACOKINETICS
- Publication
Clinical Pharmacology in Drug Development, 2023, Vol 12, Issue 12, p1204
- ISSN
2160-763X
- Publication type
Article
- DOI
10.1002/cpdd.1319