ABSTRACT
The seeds of Nigella sativa Linn. (Ranunculaceae), commonly known as Black cumin, are predominantly used as carminative, antispasmodic, and stimulant. The main objective of the present study was to evaluate the effect of N. sativa seed extract on the permeation of co-infused amoxicillin across the gut wall. The methanolic extract of N. sativa improved intestinal permeability of amoxicillin in in-vitro experiments in a dose-dependent manner. Two new glycosides, decanyl nigelloic acid diglucoside [n-decanyl-3-aldehydic-4-methoxy-5-hydroxy benzoate-5-β-D-glucofuranosyl (2→1)-β-D-glucopyranosyl-(2→1)-β-D-glucopyranoside]] and nigelabdienoyl triglucoside [homo-labd-5, 9(11)-dien-16-onyl-β-D-glucopyranosyl (2→1)-β-D-glucopyranosyl (2→1)-β-D-glucopyranoside], along with seven known fatty acid glycerides/esters, were isolated from the gut permeation enhancing extract. The structures of these new glycosides were elucidated by detailed spectroscopic analyses.
Subject(s)
Animals , Male , Rats , Amoxicillin , Pharmacokinetics , Anti-Bacterial Agents , Pharmacokinetics , Intestine, Small , Metabolism , Molecular Structure , Nigella sativa , Chemistry , Phytochemicals , Chemistry , Metabolism , Plant Extracts , Chemistry , Metabolism , Rats, Wistar , Seeds , ChemistryABSTRACT
The seeds of Nigella sativa Linn. (Ranunculaceae), commonly known as Black cumin, are predominantly used as carminative, antispasmodic, and stimulant. The main objective of the present study was to evaluate the effect of N. sativa seed extract on the permeation of co-infused amoxicillin across the gut wall. The methanolic extract of N. sativa improved intestinal permeability of amoxicillin in in-vitro experiments in a dose-dependent manner. Two new glycosides, decanyl nigelloic acid diglucoside [n-decanyl-3-aldehydic-4-methoxy-5-hydroxy benzoate-5-β-D-glucofuranosyl (2→1)-β-D-glucopyranosyl-(2→1)-β-D-glucopyranoside]] and nigelabdienoyl triglucoside [homo-labd-5, 9(11)-dien-16-onyl-β-D-glucopyranosyl (2→1)-β-D-glucopyranosyl (2→1)-β-D-glucopyranoside], along with seven known fatty acid glycerides/esters, were isolated from the gut permeation enhancing extract. The structures of these new glycosides were elucidated by detailed spectroscopic analyses.
Subject(s)
Animals , Male , Rats , Amoxicillin , Pharmacokinetics , Anti-Bacterial Agents , Pharmacokinetics , Intestine, Small , Metabolism , Molecular Structure , Nigella sativa , Chemistry , Phytochemicals , Chemistry , Metabolism , Plant Extracts , Chemistry , Metabolism , Rats, Wistar , Seeds , ChemistryABSTRACT
Background & objectives: Nigella sativa Linn. is extensively used in the Indian diasporas as spice, which may interact with co-administered drugs and affect their intestinal availability. The purpose of this study was to investigate the effect of Nigella on bioavailability of amoxicillin in animal model. Methods: Everted rat intestinal sacs were used for in vitro experiment to study the transfer of amoxicillin across the gut. Amoxicillin (6 mg/ml) was co-infused with 3 and 6 mg of methanol and hexane extract of Nigella seeds separately. The amount of amoxicillin that traversed the gut was followed spectrophotometrically at 273 nm. For in vivo studies Wistar albino rats were used. Amoxicillin (25 mg/kg, po) was co-administered with hexane extract of Nigella seeds (25 mg/kg, po). The amount of amoxicillin in rat plasma was determined by UPLC-MS/MS method. Results: The in vitro studies both with methanol and hexane extracts of Nigella increased the permeation of amoxicillin significantly (P<0.001) as compared to control. Permeation was also found to be significantly higher for the hexane extract (P<0.001) in comparison to methanol extract at the same dose levels. In vivo experiments revealed that Cmax of amoxicillin in rat plasma when administered orally alone and in combination with hexane extract increased correspondingly from 4138.251 ± 156.93 to 5995.045 ± 196.28 ng/ml while as AUC0→t increased from 8890.40 ± 143.33 to 13483.46 ± 152.45 ng/ml.h. Interpretation & conclusions: Nigella enhanced amoxicillin availability in both in vivo and in vitro studies. As the increase in bioavailability is attributed, in part, to enhanced diffusivity across intestine, our study indicated that Nigella increased intestinal absorption of amoxicillin.