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.

Oral administration of a microencapsulated low-molecular-weight heparin to rabbits: Anti-Xa and anti-IIa profiles

2010 ◽  
Vol 103 (06) ◽  
pp. 1254-1267 ◽  
Author(s):  
Lucie Javot ◽  
Anne Sapin ◽  
Julien Scala-Bertola ◽  
Claude Vigneron ◽  
Thomas Lecompte ◽  
...  
Keyword(s):  
Oral Administration ◽  
Subcutaneous Injection ◽  
Double Emulsion ◽  
Oral Dosage ◽  
Pharmacokinetic Parameters ◽  
Low Molecular Weight ◽  
Eudragit Rs ◽  
Long Time

SummaryThe development of heparin oral form has been a subject of international research for a long time. Promising results have been obtained in vivo in terms of anti-Xa activity with different strategies and notably microparticles but studies concerning the anti-IIa activity and the anti-Xa/anti-IIa ratio have never been presented. Anti-Xa activities, anti-IIa activities and anti-Xa/anti-IIa ratios provided by nadroparin Eudragit→ RS and poly (D,L-lactic-co-glycolic acid) (PLGA) microparticles were determined in vitro and in vivo and an evaluation of their pharmacokinetic parameters compared to subcutaneous injection was performed. Nadroparin was encapsulated into microparticles prepared by the double emulsion method using Eudragit→ RS alone or in mixture with PLGA of two kinds, i.e. with (PLGA S) or without (PLGA H) esterification of the acid ending. Microparticles characterisation was performed (size, anti-Xa and anti-IIa activities entrapped and released) before their oral administration in rabbits. In vitro anti-Xa/anti-IIa ratios released from nadroparin microparticles were higher than the ratio of the commercial solution. After oral administration, whatever the formulation, sustained anti-Xa and anti-IIa activities were obtained compared to the subcutaneous injection with a peak concentration at 4 hours (up to 0.59 anti-Xa U/ml and 0.11 anti-IIa U/ml for PLGA S 50% / ERS 50% formulation). Anti-Xa and anti-IIa relative bioavailabilities were high, up to 40% (ERS 100% formulation). Anti-Xa/anti-IIa ratios were within range already obtained for subcutaneous injection, i.e. between 5 and 15. Nadroparin microparticles of nadroparin are promising oral dosage form performing sustained and well controlled anti-Xa, anti-IIa activities and anti-Xa/anti-IIa ratio.

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 White Pepper and Piperine Have Different Effects on Pharmacokinetics of Puerarin in Rats

2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Yong-Zhuo Liang ◽  
Hai-Ming Chen ◽  
Zu-Qing Su ◽  
Shao-Zhen Hou ◽  
Xiao-Ying Chen ◽  
...  
Keyword(s):  
Oral Administration ◽  
Drug Interactions ◽  
Intravenous Injection ◽  
Oral Absorption ◽  
The Other ◽  
Pharmacokinetic Parameters ◽  
Control Group ◽  
White Pepper ◽  
Combined Application ◽  
Combined Use

This study attempted to explore the effects of white pepper and its major component piperine on puerarin administered to rats. Pharmacokinetic parameters of puerarin in rats were determined by oral administration (400 mg/kg) or intravenous injection (40 mg/kg) of puerarin, pretreated with or without white pepper and piperine given orally. Compared to the control group given oral puerarin only, the combined use of piperine (10 or 20 mg/kg) increased theCmaxof puerarin by 1.30-fold or 1.64-fold and theAUC0–∞by 133% or 157%, respectively. In contrast, coadministration of white pepper (125 or 250 mg/kg) decreased oral absorption of puerarin to 83% or 74%, respectively. On the other hand, pretreatment with piperine orally did not alter the intravenous pharmacokinetics of puerarin, while the AUC of puerarin after intravenous administration was increased by pretreatment with white pepper. The results indicate that pretreatment with piperine or pepper exerts different effects on pharmacokinetics of puerarin administrated via intragastric and intravenous routes. Therefore, it is suggested that the combined application of piperine or white pepper with puerarin should be carefully monitored for potential diet-drug interactions.

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.

Leading with Pedagogical Tact- a Challenge in Children's Sports in Sweden

2010 ◽  
Vol 19 (1-2) ◽  
pp. 127-147 ◽  
Author(s):  
Krister Hertting
Keyword(s):  
Daily Activity ◽  
The Other ◽  
Competitive Sport ◽  
Sports Clubs ◽  
Youth Politics ◽  
Pedagogical Tact ◽  
Children And Parents ◽  
Swedish Society ◽  
Long Time ◽  
Voluntary Commitment

Leading with Pedagogical Tact- a Challenge in Children's Sports in Sweden The purpose of this article is to elucidate and problemize meetings between children and leaders in children's sport. The competitive sport is high valuated in the Swedish society and sport for children is central in the Swedish youth politics. The foundation in Swedish sport, as well as in the other Nordic countries, has for a long time relied on voluntary commitment. Approximately 650 000 people are voluntary engaged as leaders in sport in Sweden and 70% of children between 7 and 14 years compete in sports clubs. There is, however, a tension in the Swedish sport system. The sports for children has double missions - ‘association nurturing’ and ‘competition nurturing’, missions which are not always in harmony. In the daily activity it is the voluntary leaders who have to deal with these missions, which creates a field of tension. In this article I argue for a bridge between these missions by a leadership based on pedagogical tact. The empirical outlook is a narrative based on statements from leaders, children and parents in a study dealing with voluntary leadership within children's football. In the end I argue that focusing on this bridge is a win-win situation, both for children and sports.

Introduction and overview of the current situation regarding the employment of biomass

2014 ◽  
pp. 691-697
Author(s):  
Suleiman José Hassuani
Keyword(s):  
Sugar Industry ◽  
Energy Generation ◽  
Current Situation ◽  
The Other ◽  
Significant Excess ◽  
Cane Juice ◽  
Energy Needs ◽  
Long Time ◽  
Biomass Availability ◽  
Sugarcane Industry

The sugarcane industry for a long time has focused only on the cane juice, its extraction and conversion to sugar. Bagasse was considered a residue and burnt inefficiently to generate steam and power. In the last decades, bagasse gradually started to be converted into energy in a more efficient way, supplying all the sugar industry energy needs (power, and steam) and, in some cases, significant excess electricity has been exported to the grid, becoming another important source of revenue. This motivated several studies of more advanced energy generation systems to boost energy exports. In more recent years, technologies called 2nd and 3rd generation have taken over the scene with many options, promising to convert biomass into more valuable products such as biofuels, chemicals, fertilisers, pellets, etc. Unfilled expectations and opportunities are rising. On the other hand, these technologies are competing for the same biomass, and this has to be considered. The industry has started to question ‘which way to go’, strategy and investment wise. The present study provides a broad scenario for the biomass availability, and its employment, with a close view to the main processes and products that might have an important role in the future of the biomass in the sugarcane industry.

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 A Discontinuity of the Energy of Quantum Walk in Impurities

Symmetry ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1134
Author(s):  
Kenta Higuchi ◽  
Takashi Komatsu ◽  
Norio Konno ◽  
Hisashi Morioka ◽  
Etsuo Segawa
Keyword(s):  
Unit Circle ◽  
Stationary State ◽  
Discrete Time ◽  
Quantum Walk ◽  
Time Limit ◽  
The Other ◽  
Unitary Matrix ◽  
Initial State ◽  
Time Quantum ◽  
Long Time

We consider the discrete-time quantum walk whose local dynamics is denoted by a common unitary matrix C at the perturbed region {0,1,⋯,M−1} and free at the other positions. We obtain the stationary state with a bounded initial state. The initial state is set so that the perturbed region receives the inflow ωn at time n(|ω|=1). From this expression, we compute the scattering on the surface of −1 and M and also compute the quantity how quantum walker accumulates in the perturbed region; namely, the energy of the quantum walk, in the long time limit. The frequency of the initial state of the influence to the energy is symmetric on the unit circle in the complex plain. We find a discontinuity of the energy with respect to the frequency of the inflow.

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