TY - JOUR
AU - Spampinato, S
AB - Gastric tolerability, absorption and pharmacological activity of the non-steroidal anti-inflammatory drug 4-biphenylacetic acid (BPAA), as an inclusion complex with β-cyclodextrin (β-CyD) or chemically modified β-CyDs: 2,6-di-O-methyl-β-CyD (DM-β-CyD), 2,3,6-tri-O-methyl-β-CyD (TM-β-CyD) and 2-hydroxypropyl-β-CyD (HP-β-CyD), were investigated in the rat after oral administration.BPAA absorption, determined from area under the plasma concentration-time curve (AUC), was increased by complexation with all β-CyDs in the following order: DM-β-CyD > TM-β-CyD > HP-β-CyD > β-CyD. The carrageenan paw oedema test demonstrated a significant increase in anti-inflammatory activity of BPAA and the ED50 values, compared with BPAA alone, were reduced to about a third for the BPAA-DM-βCyD complex and halved for the others. BPAAA complexed with DM-β-CyD, HP-β-CyD or β-CyD showed better gastric tolerability compared with uncomplexed drug, whereas the BPAA-TM-β-CyD complex produced marked gastric lesions similar in extent to BPAA alone. TM-β-CyD (500mg kg−1) and DM-β-CyD (1000mg kg−1) caused gastric erosions 21 h after oral administration.The pharmacokinetic profiles of BPAA-β-CyD complexes have shown that DM-β-CyD is the most effective in enhancing the bioavailability of BPAA.
TI - Differential Effects of Modified β-Cyclodextrins on Pharmacological Activity and Bioavailability of 4-Biphenylacetic Acid in Rats after Oral Administration
JF - Journal of Pharmacy and Pharmacology
DO - 10.1111/j.2042-7158.1995.tb05762.x
DA - 1995-02-01
UR - https://www.deepdyve.com/lp/oxford-university-press/differential-effects-of-modified-cyclodextrins-on-pharmacological-RApv3CbZYF
SP - 120
EP - 123
VL - 47
IS - 2
DP - DeepDyve
ER -