Pharmacokinetic and pharmacodynamic interaction of Rosuvastatin calcium with guggulipid extract in rats.
Guggulipid
Interaction
Lipid
Pharmacodynamic
Pharmacokinetic
Rosuvastatin
Journal
Saudi journal of biological sciences
ISSN: 1319-562X
Titre abrégé: Saudi J Biol Sci
Pays: Saudi Arabia
ID NLM: 101543796
Informations de publication
Date de publication:
Jun 2021
Jun 2021
Historique:
received:
03
02
2021
revised:
03
03
2021
accepted:
03
03
2021
entrez:
14
6
2021
pubmed:
15
6
2021
medline:
15
6
2021
Statut:
ppublish
Résumé
Rosuvastatin calcium (RC) is a potent and competitive synthetic inhibitor of HMG-CoA reductase used for the treatment of dyslipidemia. Guggulipid obtained from The guggulipid extract was standardized for the presence of guggulsterones. The pharmacokinetic interaction was determined after a single dose administration of RC alone or in combination with the guggulipid extract or after multiple-dose administration of RC alone or RC along with the guggulipid extract for 14 days. To determine the pharmacodynamic interaction, RC and guggulipid extract were administered to hyperlipidemic rats for 14 days. The level of significance was determined using unpaired student's Standardization of guggulipid extract showed it contains 7.5%w/w of guggulsterones. Guggulipid extract increased the bioavailability of RC in both single-dose and multiple-dose studies. Guggulipid extract reduced the rate of absorption (Ka) of RC but showed an increase in maximum serum concentration (Cmax). An in-vitro study using isolated rat intestine revealed that guggulipid extract decreased the rate of absorption of RC in the intestinal lumen. The hypolipidemic activity of RC was augmented by the guggulipid extract in hyperlipidemic rats. Therefore it is concluded that guggulipid extract increases the bioavailability of RC by delaying its Ka and augments its hypolipidemic action. However, it is recommended that a combination of RC with guggulipid extract should be used only after an adverse effect(s) of this combination are determined.
Sections du résumé
BACKGROUND & OBJECTIVES
OBJECTIVE
Rosuvastatin calcium (RC) is a potent and competitive synthetic inhibitor of HMG-CoA reductase used for the treatment of dyslipidemia. Guggulipid obtained from
MATERIALS AND METHODS
METHODS
The guggulipid extract was standardized for the presence of guggulsterones. The pharmacokinetic interaction was determined after a single dose administration of RC alone or in combination with the guggulipid extract or after multiple-dose administration of RC alone or RC along with the guggulipid extract for 14 days. To determine the pharmacodynamic interaction, RC and guggulipid extract were administered to hyperlipidemic rats for 14 days. The level of significance was determined using unpaired student's
RESULTS
RESULTS
Standardization of guggulipid extract showed it contains 7.5%w/w of guggulsterones. Guggulipid extract increased the bioavailability of RC in both single-dose and multiple-dose studies. Guggulipid extract reduced the rate of absorption (Ka) of RC but showed an increase in maximum serum concentration (Cmax). An in-vitro study using isolated rat intestine revealed that guggulipid extract decreased the rate of absorption of RC in the intestinal lumen. The hypolipidemic activity of RC was augmented by the guggulipid extract in hyperlipidemic rats.
INTERPRETATION & CONCLUSION
CONCLUSIONS
Therefore it is concluded that guggulipid extract increases the bioavailability of RC by delaying its Ka and augments its hypolipidemic action. However, it is recommended that a combination of RC with guggulipid extract should be used only after an adverse effect(s) of this combination are determined.
Identifiants
pubmed: 34121889
doi: 10.1016/j.sjbs.2021.03.015
pii: S1319-562X(21)00183-2
pmc: PMC8176130
doi:
Types de publication
Journal Article
Langues
eng
Pagination
3490-3496Informations de copyright
© 2021 The Author(s).
Déclaration de conflit d'intérêts
The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
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