This trial evaluated the pharmacokinetic interaction between fixed doses of lidocaine (2.5%), prilocaine (2.5%) or the association of both (Nanorap®) in healthy volunteers. The drug safety and tolerability was also evaluated.
This study was performed as a monocentric, open, randomized, double-blind, with 3 treatment regimen (lidocaine, prilocaine, or Nanorap®) in 3 periods design. Volunteers were submitted to clinical and laboratory examination before enrollment. Treatments were carried out on 3 different days with a washout period of 7 days between each dose. After a fasting period (8 h), volunteers received topically 2g of the formulation in a delimited area of 16 cm2 in the volar surface of the forearm. The product was applied to the left arm and venous blood was collected from the right arm. The remaining product was removed with a cotton swab 10 minutes after application. Blood samples (3.5 mL) were collected into heparinized tubes before (0:00) and at 1.0, 2.0, 3.0, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 7.5, 8.0, 8.5, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0 and 24.0 h after the hydrogel application. Blood samples were centrifuged at 2000 g (4 ⁰C) for 10 minutes and the obtained plasma samples were stored at -20 °C until analysis. Following dosing, volunteers were monitored for 36 h in a clinical setting safety and tolerability (signs, symptoms, adverse events, and laboratory parameters). The vital signs (blood pressure and pulse rate) were evaluated. ECGs were obtained before (30 min) and at drug Cmax (6 h) for each product application. QT interval corrected by heart rate (QTc) data were obtained from a Bionet Cardiocare 2000 and BMS-Plus software program, using Bazett's formula: QTc = QT/(sqrt RR Interval).
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
48
Single topical dose of 2g lidocaine + prilocaine 2.5 % formulation.
Single topical dose of 2g lidocaine 2.5 % formulation.
Single topical dose of 2g prilocaine 2.5 % formulation.
Galeno Desenvolvimento de Pesquisas Clinicas Ltda. - ME
Campinas, São Paulo, Brazil
Measurement of lidocaine and prilocaine plasma levels
Blood sampling for the determination of plasma levels of lidocaine and prilocaine in participants of each treatment group.
Time frame: 0-24 h
Maximum Plasma Concentration (Cmax) of lidocaine and prilocaine
Determination of Cmax for lidocaine and prilocaine based on plasma concentrations of samples obtained.
Time frame: 0-24 h
Area Under the Curve (AUC) of lidocaine and prilocaine
Determination of AUC for lidocaine and prilocaine based on plasma concentrations of samples obtained.
Time frame: 0-24 h
Number of adverse events per participant
Determination of the number of adverse events, in each treatment group, including clinically relevant alterations of vital signs and laboratory tests results.
Time frame: Up to 36 h after treatment
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