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Effects of bile salts on the lovastatin pharmacokinetics following oral administration to rats

Title
Effects of bile salts on the lovastatin pharmacokinetics following oral administration to rats
Authors
Kim K.Yoon I.Chun I.Lee N.Kim T.Gwak H.S.
Ewha Authors
곽혜선
SCOPUS Author ID
곽혜선scopus
Issue Date
2011
Journal Title
Drug Delivery
ISSN
1071-7544JCR Link
Citation
vol. 18, no. 1, pp. 79 - 83
Indexed
SCIE; SCOPUS WOS scopus
Abstract
This study aimed to examine the effects of bile salts on pharmacokinetics of lovastatin, which has low bioavailability. Lovastatin solid dispersions were prepared using sodium deoxycholate (NaDC) and sodium glycholate (NaGC) at ratios of 1:19, 1:49, and 1:69. The formulated solid dispersions and control (commercial tablet) were administered to rats and plasma concentrations were determined by a validated LC-MS/MS method. Statistically significant differences were found in C max, AUC 010, and AUC 0∞ values among lovastatin formulations (p<0.05). NaDC-containing formulations revealed higher bioavailabilities than NaGC-containing solid dispersions at ratios of 1:19 and 1:49. Especially, NaDC-containing formulation at a ratio of 1:19 (NaDC19) showed the highest bioavailability. The AUC (both AUC 010 and AUC 0∞) of NaDC19 was statistically higher than control and NaDC69 (p<0.05). The AUC values decreased as bile salt concentrations increased. Overall, formulations containing bile salts showed higher AUC values than control, even though all formulations did not show significantly higher AUC. In conclusion, the addition of bile salts to lovastatin could enhance drug bioavailabilities. However, too high concentrations of bile salts could decrease bioavailabilities of lovastatin. © 2011 Informa Healthcare USA, Inc.
DOI
10.3109/10717544.2010.512024
Appears in Collections:
약학대학 > 약학과 > Journal papers
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