Chain length affects pancreatic lipase activity and the extent and pH-time profile of triglyceride lipolysis.

摘要: Triglycerides (TG) are one of the most common excipients used in oral lipid-based formulations. The chain length TG plays an important role bioavailability co-administered drug. Fatty acid (FA) chain-length specificity porcine pancreatic lipase was studied by means vitro lipolysis model under bio-relevant conditions at pH 6.80. In order to determine total extent lipolysis, back-titration experiments 11.50 were performed. Results suggest that there is a specific range (C2–C8) for which shows higher activity. This could result from combination physicochemical properties TGs, 2-monoglycerides (2-MGs) and FAs, namely droplet size solubility 2-MGs within mixed micelles, relative stability FAs as leaving groups hydrolysis reaction. During experimentation, it evident optimisation needed tighter control over levels so better mimic vivo conditions. 1 M NaOH, 3.5 mL/min maximum dosing rate, 3 μL/min minimum rate optimised set allowed control, well differentiation different lipid loads.