Effect of Oral Administration of Crude Aqueous Extract of Garlic on Pharmacokinetic Parameters of Isoniazid and Rifampicin in Rabbits

Pharmacology ◽  
2006 ◽  
Vol 77 (2) ◽  
pp. 100-104 ◽  
Author(s):  
P. Dhamija ◽  
S. Malhotra ◽  
P. Pandhi
Keyword(s):  
Oral Administration ◽  
Aqueous Extract ◽  
Pharmacokinetic Parameters ◽  
Crude Aqueous Extract

scholarly journals Alteration of the Pharmacokinetics of Theophylline by Paullinia cupana Kunth in Rats

2021 ◽  
pp. 12-18
Author(s):  
Nayana Yared Batista ◽  
Ádley Antonini Neves de Lima ◽  
José Wilson do Nascimento Corrêa ◽  
Tatiane Pereira De Souza ◽  
Igor Rafael dos Santos Magalhães
Keyword(s):  
Oral Administration ◽  
Aqueous Extract ◽  
Drug Clearance ◽  
The Other ◽  
Pharmacokinetic Parameters ◽  
Herbal Drug ◽  
Oral Gavage ◽  
Once Daily ◽  
Paullinia Cupana ◽  
Long Time

Aims: Paullinia cupana Kunth has been popularly used to prepare different beverages by the Amazonian inhabitants for a long time ago mainly due to its stimulant properties. Although the utilization of this herbal drug has been increasing lately, little is known regarding the possibility of drug interactions. Therefore, this research tried to investigate the effects of the aqueous extract of P. cupana on the pharmacokinetics of theophylline (TPH), a CYP1A marker in rats. Methodology: The extract was prepared according to the popular recipe and subjects received different once daily doses of extract (vehicle, 82.1 mg/Kg and 821 mg/Kg) by oral gavage during two weeks. Non-compartimental analysis was carried out to obtain the pharmacokinetic parameters. Results: Animals treated with P. cupana (AUC: 1,197.2 ± 284.4 and 346.6 ± 37.0 µg.h/mL for 82.1 and 821 mg/Kg, respectively) had lower exposition to TPH than controls (3,539.48 ± 278.4 µg.h/mL). On the other hand, drug clearance was higher in treated subjects (2.44 ± 0.4 and 7.27 ± 0.7 L/h/kg for 82.1 and 821 mg/Kg, respectively) than controls (0.71 ± 0.0 L/h/kg). Conclusion: Therefore, the multiple oral administration of an aqueous extract of P. cupana caused a significant effect on the pharmacokinetics of TPH in rats.

scholarly journals Simultaneous Determination of Luteoloside, Apigetrin, And Hesperidin In Rat Plasma By UHPLC-MS/MS: Application to A Comparative Pharmacokinetic Investigation After Oral Administration Of Schizonepeta Tenuifolia Aqueous Extract With And Without Its Volatile Oil

2020 ◽  
Author(s):  
Siting Liu ◽  
Yulan Jiang ◽  
Mingqiu Shan ◽  
Sheng Yu ◽  
Fangfang Cheng ◽  
...  
Keyword(s):  
Oral Administration ◽  
Aqueous Extract ◽  
Matrix Effects ◽  
Volatile Oil ◽  
Rat Plasma ◽  
Flavonoid Glycosides ◽  
Pharmacokinetic Parameters ◽  
Ionization Source ◽  
Strong Basis ◽  
Schizonepeta Tenuifolia

Abstract Background: Schizonepeta tenuifolia Briq. (ST) has been used as an aromatic exterior-releasing medicine in clinical practice for thousands of years in China. Previous researches have revealed both volatile oil (STVO) and aqueous extract (STAE) from ST showed significant pharmacological activities. However, the influence between each other was still unknown. Methods: This study was designed to compare the pharmacokinetic profiles of three main flavonoids (luteoloside, apigetrin, and hesperidin) in STAE to illustrate the influence of STVO. So, an ultra-flow liquid chromatography-tandem mass spectrometry (UHPLC-MS) method was established to quantitatively analyze the three absorbed ingredients in the plasma of healthy rats. Biological samples were analyzed on an Agilent Eclipse Plus C18 column (3.0 mm × 150 mm, 3.5 μm) with gradient mobile phase (containing 0.2% formic acid and acetonitrile) at a flow rate of 0.8 mL/min. All the analytes and quercitrin (IS) were investigated with an electrospray ionization source (ESI) using multiple-reaction monitoring (MRM) in negative ionization mode. Results: This quantitative method showed good linearities (r ≥0.9995) and the lower limits of quantification were 0.590~1.19 ng/ml. The intra- and inter-day precisions ranged 3.47~10.45% and 4.29~11.28% for the three analytes. The mean extraction recoveries were in the range of 77.41~109.79% and the average matrix effects were within 83.41~112.67%. The validated method has been fully applied to compare the pharmacokinetic parameters of the three flavonoid glycosides in rat plasma after oral administration of STAE and STAE+STVO. In comparison of luteoloside, apigetrin, and hesperidin in STAE group, it was found that different degree of increasing existed for the time to reach the maximum concentration (Tmax), elimination half-life time (T1/2), the area under the concentration curves (AUC0→t and AUC0→∞) and the maximum concentrations (Cmax) in STAE+STVO group. Conclusions: As can be seen from above, STVO could improve the absorption and bioavailability of the three analytes. These findings would provide some active and strong basis of safe clinical application for ST and further exploitation for STVO from the perspective of drug-drug interaction.

scholarly journals Simultaneous determination of three active flavonoids in rat plasma by HPLC-MS/MS: Application to a comparative pharmacokinetic investigation after oral administration of Schizonepeta tenuifolia aqueous extract with and without its volatile oil

2020 ◽  
Author(s):  
Siting Liu ◽  
Yulan Jiang ◽  
Mingqiu Shan ◽  
Sheng Yu ◽  
Fangfang Cheng ◽  
...  
Keyword(s):  
Oral Administration ◽  
Aqueous Extract ◽  
Matrix Effects ◽  
Volatile Oil ◽  
Rat Plasma ◽  
Flavonoid Glycosides ◽  
Pharmacokinetic Parameters ◽  
Ionization Source ◽  
Strong Basis ◽  
Schizonepeta Tenuifolia

AbstractSchizonepeta tenuifolia Briq. (ST) has been used as an aromatic exterior-releasing medicine in clinical practice for thousands of years in China. Previous researches have revealed both volatile oil (STVO) and aqueous extract (STAE) from ST showed significant pharmacological activities, such as anti-virus, anti-inflammation, anti-oxidation, and immunoregulation. However, the influence between each other was still unknown. The purpose of this study was to compare the pharmacokinetic profiles of three main flavonoids (luteoloside, apigetrin, and hesperidin) in STAE to illustrate the influence of STVO. A liquid chromatography-tandem mass spectrometry (HPLC-MS) method was established to quantitatively analyze the three absorbed ingredients in the plasma of healthy rats. Biological samples were analyzed on an Agilent Eclipse Plus C18 column (3.0 mm × 150 mm, 3.5 μm) with gradient mobile phase (containing 0.2% formic acid and acetonitrile) at a flow rate of 0.8 mL/min. All the analytes and quercitrin (IS) were investigated with an electrospray ionization source (ESI) using multiple-reaction monitoring (MRM) in negative ionization mode. In addition, this quantitative method showed good linearities (r ≥ 0.9995) and the lower limits of quantification were 0.590–1.19 ng/mL. The intra- and inter-day precisions ranged 3.47–10.45% and 4.29–11.28% for the three analytes. The mean extraction recoveries were in the range of 77.41–109.79% and the average matrix effects were within 83.41–112.67%. The validated method has been fully applied to compare the pharmacokinetic parameters of the three flavonoid glycosides in rat plasma after oral administration of STAE and STAE+STVO. In comparison of luteoloside, apigetrin, and hesperidin in STAE group, it was found that different degree of increasing existed for the time to reach the maximum concentration (Tmax), elimination half-life time (T1/2), the area under the concentration curves (AUC0→t and AUC0→∞) and the maximum concentrations (Cmax) in STAE+STVO group. As can be seen from above results, STVO could improve the absorption and bioavailability of the three analytes. These findings would provide some active and strong basis of safe clinical application for ST and further exploitation for STVO from the perspective of drug–drug interaction.

Antihyperglycemic, Antihyperlipidemic and Antioxidant Effects of Cotula cinerea (Del) in Normal and Streptozotocin-Induced Diabetic Rats

2020 ◽  
Vol 20 (9) ◽  
pp. 1504-1513 ◽  
Author(s):  
Ayoub Amssayef ◽  
Mohamed Eddouks
Keyword(s):  
Antioxidant Activity ◽  
Glucose Tolerance ◽  
Oral Administration ◽  
Beneficial Effect ◽  
Aqueous Extract ◽  
Aerial Part ◽  
Diabetic Rats ◽  
Histopathological Analysis ◽  
Phytochemical Screening ◽  
Cotula Cinerea

Aims: The current investigation aimed to assess the antioxidant, antidiabetic and antilipidemic effects of the aqueous extract of aerial part of Cotula cinerea (C. cinerea). Background: Cotula cinerea (Del). which belongs to the Asteraceae family is commonly used traditionally for the treatment of diabetes. Objective: The objective of the study was to study the effect of the aqueous C. cinerea extract on glucose and lipid metabolism in normal and streptozotocin-induced diabetic rats using a single and repeated oral administration. Methods: A preliminary phytochemical screening and the quantification of phenolic and flavonoid contents as well as the antioxidant activity using three methods (DPPH, FRAP and ABTS) were carried out. The effect of a single and repeated (15 days of treatment) oral administration of the aqueous extract of aerial part of Cotula cinerea (AEAPCC) at a dose of 20 mg/kg on glucose and lipid profile was examined in normal and streptozotocin-induced diabetic rats. Additionally, histopathological examination of the pancreas and liver was carried out according to the Hematoxylin-Eosin method. Results: AEAPCC (20 mg/kg) showed a significant blood glucose-lowering activity in both normal and diabetic rats after a single and repeated oral administration during 15 days. The aqueous extract was also able to decrease the plasma triglycerides levels in both normal and diabetic rats after 15 days of oral treatment at a dose of 20 mg/Kg while no effect was observed on plasma cholesterol levels. In addition, the results show that AEAPCC exhibits an in vitro antioxidant activity using different tests. Histopathological analysis of the pancreas and liver of AEAPCC-treated diabetic rats has revealed that AEAPCC had a beneficial effect on the architecture of these organs while no improvement of glucose tolerance was noticed using the glucose tolerance test. Furthermore, the results showed that the extract is rich in several phytochemical compounds and exhibited an important antioxidant activity. The phytochemical screening revealed that AEAPCC contains polyphenolic compounds, flavonoids, tannins, alkaloids, saponins, quinones, sterols, terpenoids, anthroquinones and reducing sugars. Whereas, it is free from glycosides. Conclusion: In conclusion, this study demonstrates that Cotula cinerea possesses a beneficial effect on diabetes. Further investigations are required to study the mechanism of action of the antidiabetic effect of this plant.

scholarly journals Effects of Diabetes Mellitus Induced by Alloxan on the Pharmacokinetics of Metformin in Rats: Restoration of Pharmacokinetic Parameters to the Control State by Insulin Treatment

2008 ◽  
Vol 11 (1) ◽  
pp. 88 ◽  
Author(s):  
Myung G. Lee ◽  
Young H Choi ◽  
Inchul Lee
Keyword(s):  
Diabetes Mellitus ◽  
Oral Administration ◽  
Protein Expression ◽  
Intravenous Administration ◽  
Insulin Treatment ◽  
Pharmacokinetic Parameters ◽  
Mrna Levels ◽  
Altered Pharmacokinetic ◽  
Intravenous And Oral Administration ◽  
Control State

To test the effect of insulin treatment on the pharmacokinetics of metformin in rats with diabetes mellitus induced by alloxan (DMIA rats). The following results were reported from other studies. Metformin was metabolized via hepatic CYP2C11, 2D1, and 3A1/2 in rats. In DMIA rats, the protein expression and mRNA levels of hepatic CYP2C11 and 3A1/2 decreased and increased, respectively. In rat model of diabetes mellitus induced by streptozotocin, the protein expression of hepatic CYP2D1 was not changed. The increase in hepatic CYP1A2, 2B1, and 2E1, and decrease in hepatic CYP2C11 in DMIA rats was returned to the controls by insulin treatment. METHODS. Metformin (100 mg/kg) was administered intravenously and orally to the control rats, DMIA rats, and DMIA rats with insulin treatment for 3 weeks (DMIA rats with insulin). RESULTS. After intravenous administration of metformin to the DMIA rats, the CLR and CLNR of the drug were significantly slower than the controls. After oral administration of metformin to the DMIA rats, the AUC of the drug was also significantly greater than the controls. After intravenous administration of metformin to the DMIA rats with insulin, the significantly slower CLNR of the drug in the DMIA rats was returned to the controls. The altered pharmacokinetic indices observed following intravenous and oral administration of metformin to DMIA rats returned to the control values in the DMIA rats with insulin. CONCLUSIONS. The significantly slower CLNR of metformin in the DMIA rats could be due to the decrease in hepatic CYP2C11 than the controls. The comparable CLNR of metformin between the DMIA rats with insulin and the control rats could be due to restoration of hepatic CYP enzyme changes in DMIA rats to the controls.

scholarly journals Experimental determination of the pharmacokinetic properties of trimethoprim and sulfamethoxazole combination in the blood serum of broiler chickens

2021 ◽  
Author(s):  
K Putecova ◽  
K Nedbalcova ◽  
I Bartejsova ◽  
M Zouharova ◽  
K Matiaskova ◽  
...  
Keyword(s):  
Oral Administration ◽  
Broiler Chickens ◽  
Animal Health ◽  
Pharmacokinetic Parameters ◽  
Serum Samples ◽  
Commercial Preparation ◽  
Single Oral Administration ◽  
Thermo Fisher Scientific ◽  
Medicinal Substances

A rapid, simple and highly efficient analytical method for the targeted determination of trimethoprim and sulfamethoxazole in serum samples has been developed and used to measure the pharmacokinetic curve of these medicinal substances after administration to chicken broilers. The pharmacokinetics properties of trimethoprim and sulfamethoxazole were investigated in clinically healthy broiler chickens after the single oral administration of the commercial preparation Methoxasol (Eurovet Animal Health, B.V., The Netherlands) at a dose of 0.275 ml/kg b.w. After a single dose drug administration, the chickens were sacrificed by decapitation under general anaesthesia by Isoflurin 1 000 mg/g (Vetpharma AH, Spain) and the blood was collected at precisely defined intervals: 15, 30, 45, 60, 90, 120, 180, 360 and 720 min after the administration. The serum concentrations of amoxicillin were determined using Q Exactive tandem mass spectrometer (Thermo Fisher Scientific, USA) in conjunction with liquid chromatography. The detected pharmacokinetic parameters of trimethoprim after the oral administration were C<sub>max</sub> = 2.1 ± 1.0 µg/ml; T<sub>max</sub> = 1.5 h; t<sub>½</sub> = 0.88 h; k<sub>el</sub> = 0.009 3 ± 0.001 1 1/h; AUC<sub>t</sub> = 2.901 ± 1.4 µg.h/ml; AUC<sub>∞</sub> = 2.907 ± 1.5 µg.h/ml; V<sub>d</sub> = 2.632 l/kg; Cl = 2.7 l/h. The pharmacokinetic parameters of sulfamethoxazole after the oral administration were C<sub>max</sub> = 47.1 ± 15.3 µg/ml; T<sub>max</sub> = 1 h; t<sub>½</sub> = 1.92 h; k<sub>el</sub> = 0.004 6 ± 0.000 3 1/h; AUC<sub>t</sub> = 89.676 ± 26.9 µg.h/ml; AUC<sub>∞</sub> = 94.612 ± 28.4 µg.h/ml; V<sub>d</sub> = 0.584 l/kg; Cl = 0.21 l/h. To the best of our knowledge, this is the first pharmacokinetic study of the combination of sulfamethoxazole and trimethoprim in broiler chickens.

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