| Full text | |
| Author(s): |
Moreira, Fernanda de Lima
[1]
;
Marques, Maria Paula
[1]
;
Duarte, Geraldo
[2]
;
Lanchote, Vera Lucia
[1]
Total Authors: 4
|
| Affiliation: | [1] Univ Sao Paulo, Dept Anal Clin Toxicol & Bromatol, Fac Ciencias Farmaceut Ribeirao Preto, Ribeirao Preto, SP - Brazil
[2] Univ Sao Paulo, Fac Med Ribeirao Preto, Dept Obstet & Ginecol, Ribeirao Preto, SP - Brazil
Total Affiliations: 2
|
| Document type: | Journal article |
| Source: | Journal of Pharmaceutical and Biomedical Analysis; v. 177, JAN 1 2020. |
| Web of Science Citations: | 0 |
| Abstract | |
Raltegravir (RAL) is a HIV-integrase inhibitor recommended for treatment of HIV type 1 infection during pregnancy. The elimination of RAL to RAL glucuronide (RAL GLU) is mediated primarily by UDP glucuronosyltransferase 1A1 (UGT1A1). The present study shows the development and validation of 4 different methods for the analysis of RAL and RAL GLU in plasma and in urine samples. The methods were applied to evaluate the maternal-fetal pharmacokinetics of RAL and RAL GLU in a HIV-infected pregnant woman receiving RAL 400 mg twice daily. The sample preparation for RAL and RAL GLU analysis in 25 mu L plasma and 100 mu L diluted urine (10-fold with water containing 0.1% formic acid) were carried out by protein precipitation procedure. RAL and RAL GLU generate similar product mass fragments and require separation in the chromatographic system, so a suitable resolution was achieved for unchanged RAL and RAL GLU employing Ascentis Express C18 (75 x 4.6 mm, 2.7 mu m) for both plasma and urine samples. The methods showed linearities at the ranges of 0.1-13.5 mu g/mL RAL and 0.15-19.5 mu g/mL RAL GLU in urine and 10-2000 ng/mL RAL and 2.5-800 RAL GLU in plasma. Precise and accurate evaluation showed coefficients of variation and relative errors <= 15%. The methods have been successfully applied in a maternal-fetal pharmacokinetic study. (C) 2019 Published by Elsevier B.V. (AU) | |
| FAPESP's process: | 18/05616-3 - Clinical pharmacokinetics in infectious diseases |
| Grantee: | Vera Lúcia Lanchote |
| Support Opportunities: | Research Projects - Thematic Grants |
| FAPESP's process: | 16/23938-2 - Influence of pregnancy associated with HIV on the activity of OATP drug transporter in patients under treatment with Efavirenz |
| Grantee: | Fernanda de Lima Moreira |
| Support Opportunities: | Scholarships in Brazil - Post-Doctoral |