Clarithromycin laurate salt: physicochemical properties and pharmacokinetics after oral administration in humans. (28th May 2019)

• Record Type: Journal Article
• Authors: Alkhalidi, Bashar A.; AlKhatib, Hatim S.; Saleh, Mohammad; Hamed, Saja; Bustanji, Yasser; Al Bujuq, Nader; Najib, Naji; Torrado-Susana, Susana; Sallam, Al-Sayed
• Is Part Of: Pharmaceutical development and technology. Volume 24:Number 5(2019)
• Page Start: 607
• Page End: 615
• Publication Date: 2019-05-28
• Subjects: Clarithromycin laurate -- fatty acid salt -- bioavailability -- physicochemical characterization; Drug delivery systems -- Periodicals; Pharmaceutical technology -- Periodicals; Drugs -- Administration -- Research -- Periodicals; Drug Delivery Systems -- Periodicals; Pharmaceutical Preparations -- Periodicals; Technology, Pharmaceutical -- Periodicals; 615
• DOI: 10.1080/10837450.2018.1547749
• Languages: English
• ISSNs: 1083-7450

Abstract

Abstract: 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, 1 H NMR, and 13 C 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. C max, T max and AUC 0→∞ of CLM-L tablets and immediate release CLM tablets did not show a significant difference. However, the AUC 0→∞ 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.