TY - JOUR
T1 - Development and validation of a sensitive LC-MS/MS method for determination of betamethasone in human plasma. Application to a pharmacokinetic study of healthy Mexican subjects
AU - Patiño-Rodríguez, Omar
AU - Escobedo-Moratilla, Abraham
AU - Martínez-Medina, Rosa María
AU - Torres-Roqu, Irma
AU - Martínez-Delgado, Maricela
AU - Pérez-Urizar, José
N1 - Publisher Copyright:
© 2019 Bentham Science Publishers.
PY - 2019
Y1 - 2019
N2 - Background: Synthetic glucocorticoids like Betamethasone (BE) are used in the treatment of inflammatory diseases due to its effective and potent effect. BE is available in three different esters: Dipropionate (BD), sodium phosphate (BP), and acetate (BA). BD/BP combined in suspension has anti-inflammatory, anti-allergic, and anti-rheumatic effects. The aim of this study was to describe the bioavailability of a single-dose of the injectable formulation of BP/BD in healthy Mexican subjects. Methods: This was a randomized, open-label, longitudinal, not therapeutic, single-dose trial of an intramuscular administration of BD/BP (5 mg/2 mg), in healthy Mexican subjects under fasting condition. Twenty-six healthy Mexicans volunteers of both genders who were between the ages of 18 and 45 were enrolled in the study. Results: From non-compartmental estimation of data, it was observed that the BE highest mean concentration was 15.70 ± 3.93 ng/mL reaching it in 2.83 ± 1.35 h. The values of elimination half-life were 10.89 ± 2.02 h. No clinically significant adverse effects were presented during the study. Conclusion: The reported PK parameters for BE suggest that the BD/BP suspension has a similar release velocity in Mexican healthy subjects compared with previous studies.
AB - Background: Synthetic glucocorticoids like Betamethasone (BE) are used in the treatment of inflammatory diseases due to its effective and potent effect. BE is available in three different esters: Dipropionate (BD), sodium phosphate (BP), and acetate (BA). BD/BP combined in suspension has anti-inflammatory, anti-allergic, and anti-rheumatic effects. The aim of this study was to describe the bioavailability of a single-dose of the injectable formulation of BP/BD in healthy Mexican subjects. Methods: This was a randomized, open-label, longitudinal, not therapeutic, single-dose trial of an intramuscular administration of BD/BP (5 mg/2 mg), in healthy Mexican subjects under fasting condition. Twenty-six healthy Mexicans volunteers of both genders who were between the ages of 18 and 45 were enrolled in the study. Results: From non-compartmental estimation of data, it was observed that the BE highest mean concentration was 15.70 ± 3.93 ng/mL reaching it in 2.83 ± 1.35 h. The values of elimination half-life were 10.89 ± 2.02 h. No clinically significant adverse effects were presented during the study. Conclusion: The reported PK parameters for BE suggest that the BD/BP suspension has a similar release velocity in Mexican healthy subjects compared with previous studies.
KW - Betamethasone
KW - Dipropionate
KW - Glucocorticoid
KW - Human plasma
KW - LC-MS/MS
KW - Pharmacokinetics
KW - Sodium phosphate
UR - http://www.scopus.com/inward/record.url?scp=85059256693&partnerID=8YFLogxK
U2 - 10.2174/1573412913666170912111945
DO - 10.2174/1573412913666170912111945
M3 - Artículo
SN - 1573-4129
VL - 15
SP - 2
EP - 8
JO - Current Pharmaceutical Analysis
JF - Current Pharmaceutical Analysis
IS - 1
ER -