RT Journal Article
T1 Clarithromycin laurate salt: physicochemical properties and pharmacokinetics after oral administration in humans
A1 Alkhalidi, Bashar A.
A1 Alkhatib, Hatim S.
A1 Saleh, Mohammad
A1 Hamed, Saja
A1 Bustanji, Yasser
A1 Al Bujuq, Nader
A1 Najib, Naji
A1 Torrado Durán, Susana
A1 Sallam, Al-Sayed
AB Objective: To prepare and characterize the physicochemical and pharmacokinetic properties of clarithromycin laurate (CLM-L), a fatty acid salt of clarithromycin (CLM).Methods: CLM-L was prepared by a simple co-melting process. The formation of CLM-L was confirmed using FTIR, 1H NMR, and 13C NMR. Solubility, intrinsic dissolution rate (IDR), and partitioning properties of CLM-L were determined and compared to those of CLM. Bioavailability of CLM from CLM-L tablets was evaluated in healthy volunteers and compared to immediate release CLM tablets.Results: CLM-L showed lower aqueous solubility, higher partitioning coefficient, and slower dissolution rate. Tablets of CLM-L also showed a significantly slower in vitro release in comparison to CLM tablets. Cmax, Tmax and AUC of CLM-L tablets and immediate release CLM tablets did not show a significant difference. However, the AUC0!1 for the CLM-L tablets tended to be higher than that of CLM tablets at all-time points.Conclusion: CLM-L was successfully prepared and its formation was confirmed. CLM-L was more hydrophobic than CLM. It exhibited a slight in vivo absorption enhancement in comparison to CLM. However, its pharmacokinetic behavior was comparable to that of CLM.
PB Taylor & Francis On Line
SN 1083-7450
YR 2018
FD 2018-12-07
LK https://hdl.handle.net/20.500.14352/98820
UL https://hdl.handle.net/20.500.14352/98820
LA eng
DS Docta Complutense
RD 6 abr 2025