Citation
Li, Yuan, et al. "Improving Oral Bioavailability of Metformin Hydrochloride Using Water-in-oil Microemulsions and Analysis of Phase Behavior After Dilution." International Journal of Pharmaceutics, vol. 473, no. 1-2, 2014, pp. 316-25.
Li Y, Song J, Tian N, et al. Improving oral bioavailability of metformin hydrochloride using water-in-oil microemulsions and analysis of phase behavior after dilution. Int J Pharm. 2014;473(1-2):316-25.
Li, Y., Song, J., Tian, N., Cai, J., Huang, M., Xing, Q., Wang, Y., Wu, C., & Hu, H. (2014). Improving oral bioavailability of metformin hydrochloride using water-in-oil microemulsions and analysis of phase behavior after dilution. International Journal of Pharmaceutics, 473(1-2), 316-25. https://doi.org/10.1016/j.ijpharm.2014.07.011
Li Y, et al. Improving Oral Bioavailability of Metformin Hydrochloride Using Water-in-oil Microemulsions and Analysis of Phase Behavior After Dilution. Int J Pharm. 2014 Oct 1;473(1-2):316-25. PubMed PMID: 25014370.
TY - JOUR
T1 - Improving oral bioavailability of metformin hydrochloride using water-in-oil microemulsions and analysis of phase behavior after dilution.
AU - Li,Yuan,
AU - Song,Jiaqi,
AU - Tian,Ning,
AU - Cai,Jie,
AU - Huang,Meihong,
AU - Xing,Qiao,
AU - Wang,Yalong,
AU - Wu,Chuanbin,
AU - Hu,Haiyan,
Y1 - 2014/07/08/
PY - 2014/04/02/received
PY - 2014/06/26/revised
PY - 2014/07/07/accepted
PY - 2014/7/12/entrez
PY - 2014/7/12/pubmed
PY - 2015/5/15/medline
KW - Lymphatic transport
KW - Metformin hydrochloride
KW - Oral bioavailability
KW - Phase behaviors
KW - W/O microemulsions
SP - 316
EP - 25
JF - International journal of pharmaceutics
JO - Int J Pharm
VL - 473
IS - 1-2
N2 - Microemulsions show significant promise for enhancing the oral bioavailability of biopharmaceutics classification system (BCS) class II drugs, but how about class III drugs remains unclear. Here we employed metformin hydrochloride (MET) as the model drug and prepared drug-loaded water-in-oil (W/O) microemulsions selecting different hydrophile-lipophile balance (HLB) surfactant systems, using HLB 8 as a cut-off. We examined the phase behaviors of microemulsions after dilution and attempted to correlate these behaviors to drug oral bioavailability. ME-A, including a lower content of surfactants (35%), underwent a transition of W/O emulsion and then became a stable O/W emulsion in a light milky appearance; ME-B, in contrast, introducing a higher content of surfactants (45%), still remained transparent or semitransparent upon dilution. Unexpectedly, ME-A showed significantly higher oral bioavailability, which can be reduced by blocking the lymphatic absorption pathway. Comparatively, the AUC of ME-B is lower, close to MET solution. Both microemulsions behaved similarly in intestinal perfusion test because of the dilution before perfusion, lacking of the important phase transition of W/O emulsion. These findings suggest that W/O microemulsions improve oral bioavailability of BCS class III drug by promoting lymphatic absorption. Analyzing the phase behavior of microemulsions after dilution may help predict the drug oral bioavailability and optimize formulations.
SN - 1873-3476
UR - https://www.unboundmedicine.com/medline/citation/25014370/Improving_oral_bioavailability_of_metformin_hydrochloride_using_water_in_oil_microemulsions_and_analysis_of_phase_behavior_after_dilution_
L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(14)00501-8
DB - PRIME
DP - Unbound Medicine
ER -
