TY - JOUR
T1 - Comparative bioavailability of two estazolam tablet formulations in Indonesian healthy volunteers
AU - Harahap, Yahdiana
AU - Sasongko, Lucy
AU - Prasaja, Budi
AU - Indriati, Ega
AU - Lusthom, Windy
AU - Lipin,
PY - 2008
Y1 - 2008
N2 - Aim: To compare the bioavailability of two estazolam (CAS 29975-16-4) tablet formulations (Estalin® 2 mg tablets as test formulation and 2 mg tablets of the originator product as reference formulation). Methods: The study was conducted according to an open label, randomized two-way cross-over design with a two-week washout period. Twenty-four subjects received each of the two estazolam formulations. Blood samples for pharmacokinetic profiling were taken up to 72 h after drug administration in fasting condition. Plasma concentrations of estazolam were determined with a validated HPLC method with ultraviolet detection. Pharmacokinetic parameters were calculated from observed plasma concentration-time profiles. Results: The mean AUC0-t, AUC 0-∞ and Cmax were 2581.38 ng·h/mL, 2934.37 ng· h/mL and 95.25 ng/mL, respectively for the test formulation and 2835.75 ng·h/ mL, 3207.73 ng·h/mL and 99.32 ng/mL, respectively, for the reference formulation. The median Tmax for both formulations was 1 h. The point estimates and 90 % confidence intervals for AUC0-t, AUC0-∞ and Cmax were 91.03% (87.48-94.72%), 91.48% (86.67-96.55%) and 95.90% (92.60-99.31 %) respectively, satisfying the bioequivalence criteria of the European Committee for Proprietary Medicinal Products and the US Food and Drug Administration guidelines. Conclusion: These results indicate that two formulations of estazolam are bioequivalent and, thus, may be prescribed interchangeably.
AB - Aim: To compare the bioavailability of two estazolam (CAS 29975-16-4) tablet formulations (Estalin® 2 mg tablets as test formulation and 2 mg tablets of the originator product as reference formulation). Methods: The study was conducted according to an open label, randomized two-way cross-over design with a two-week washout period. Twenty-four subjects received each of the two estazolam formulations. Blood samples for pharmacokinetic profiling were taken up to 72 h after drug administration in fasting condition. Plasma concentrations of estazolam were determined with a validated HPLC method with ultraviolet detection. Pharmacokinetic parameters were calculated from observed plasma concentration-time profiles. Results: The mean AUC0-t, AUC 0-∞ and Cmax were 2581.38 ng·h/mL, 2934.37 ng· h/mL and 95.25 ng/mL, respectively for the test formulation and 2835.75 ng·h/ mL, 3207.73 ng·h/mL and 99.32 ng/mL, respectively, for the reference formulation. The median Tmax for both formulations was 1 h. The point estimates and 90 % confidence intervals for AUC0-t, AUC0-∞ and Cmax were 91.03% (87.48-94.72%), 91.48% (86.67-96.55%) and 95.90% (92.60-99.31 %) respectively, satisfying the bioequivalence criteria of the European Committee for Proprietary Medicinal Products and the US Food and Drug Administration guidelines. Conclusion: These results indicate that two formulations of estazolam are bioequivalent and, thus, may be prescribed interchangeably.
KW - Benzodiazepines
KW - CAS 29975-16-4
KW - Estalin®
KW - Estazolam, bioequivalence, pharmacokinetics
KW - Hypnotics
KW - Sedatives
UR - http://www.scopus.com/inward/record.url?scp=55949131572&partnerID=8YFLogxK
U2 - 10.1055/s-0031-1296548
DO - 10.1055/s-0031-1296548
M3 - Article
C2 - 19025059
AN - SCOPUS:55949131572
VL - 58
SP - 501
EP - 504
JO - Drug Research
JF - Drug Research
SN - 2194-9379
IS - 10
ER -