Comparative pharmacokinetic study of hesperetin after oral administration in normal and hyperuricemia rats by UPLC-MS/MS

2020 ◽  
Vol 15 ◽  
Author(s):  
Kexin Li ◽  
Li Wei ◽  
Zhigang Han ◽  
Huarong Xiong ◽  
Fengmei Zhang ◽  
...  
Keyword(s):  
Oral Administration ◽  
High Performance ◽  
Pharmacokinetic Parameters ◽  
Specific Method ◽  
Sprague Dawley ◽  
Post Dose ◽  
Pharmacokinetic Profiles ◽  
Group A ◽  
Tandem Mass Spectrometric ◽  
Group B

Backgrounds: Hesperetin has antihyperuricemia activity, and the pharmacokinetic profiles of hesperetin may be altered by hyperuricemia. This study aimed to develop a highly sensitive and specific method for the determination of hesperetin in normal and hyperuricemia rats, and to compare pharmacokinetic profiles of hesperetin after oral administration between normal and hyperuricemia rats. Methods: Sprague-Dawley (SD) rats were randomly divided into one normal group (group A) and four hyperuricemia groups (group B, C, D, and E). Groups A, B, C, and D received a single dose (9–81 mg/kg) of hesperetin on Day 28, respectively, while group E received multiple doses (27 mg/kg) of hesperetin once daily for 28 days. Blood samples were collected at 10 different time points post-dose, and hesperetin was determined by ultra-high performance liquid chromatography-tandem mass spectrometric (UPLC-MS/MS). Results: Compared with normal condition of group A, hyperuricemia of group C induced 48.19% and 19.57% decreases in Cmax and CL/F, and resulted in 58.25% and 19.48% increases in Tmax and AUC0-t for hesperetin, respectively. After 28 days of hesperitin treatment, Cmax of group E was significantly elevated than that of group C (p < 0.05). Hesperetin exhibited nonlinear pharmacokinetic properties in the range of 9–81 mg/kg in hyperuricemia rats. Conclusions: The pharmacokinetic parameters of hesperetin in hyperuricemia rats were reported for the first time. Intestinal injury may be ameliorated by hesperetin in hyperuricemia rats after 28 days’ treatment. These findings could provide more beneficial information to the mechanism and clinical applications of hesperetin.

scholarly journals Artemisinin Pharmacokinetics and Efficacy in Uncomplicated-Malaria Patients Treated with Two Different Dosage Regimens

2002 ◽  
Vol 46 (4) ◽  
pp. 1026-1031 ◽  
Author(s):  
Toufigh Gordi ◽  
Dinh Xuan Huong ◽  
Trinh Ngoc Hai ◽  
Nguyen Thi Nieu ◽  
Michael Ashton
Keyword(s):  
High Performance ◽  
Parasite Clearance ◽  
Oral Dosage ◽  
Pharmacokinetic Parameters ◽  
Oral Clearance ◽  
Dosage Regimens ◽  
Drug Concentrations ◽  
Group A ◽  
Group B ◽  
Pass Metabolism

ABSTRACT The immediate efficacies of two oral dosage regimens of artemisinin were investigated in 77 male and female adult Vietnamese falciparum malaria patients randomly assigned to treatment with either 500 mg of artemisinin daily for 5 days (group A; n = 40) or artemisinin at a dose of 100 mg per day for 2 days, with the dose increased to 250 mg per day for 2 consecutive days and with a final dose of 500 mg on the fifth day (group B; n = 37). Parasitemia was monitored every 4 h. The average parasite clearance time was longer in group B than in group A (means ± standard deviations, 50 ± 23 and 34 ± 14 h, respectively; P < 0.01). Artemisinin concentrations in saliva samples obtained on days 1 and 5 were quantified by high-performance liquid chromatography. The average oral clearance, based on saliva drug concentrations in group B patients, was twofold higher than that in group A patients on day 1 (P < 0.01), with no differences in drug half-lives (P = 0.40), indicating a saturable first-pass metabolism. Female patients had higher oral clearance values on day 1. Artemisinin's pharmacokinetic parameters were similar on day 5 in both groups, although a significant increase in oral clearance from day 1 to day 5 was evident. Thus, artemisinin exhibited both dose- and time-dependent pharmacokinetics. The escalating dose studied did not result in higher artemisinin concentrations toward the end of the treatment period.

scholarly journals Pharmacokinetics Interaction between Imatinib and Genistein in Rats

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Zhe Wang ◽  
Li Wang ◽  
Meng-ming Xia ◽  
Wei Sun ◽  
Cheng-ke Huang ◽  
...  
Keyword(s):  
Single Dose ◽  
Multiple Dose ◽  
Pharmacokinetic Parameters ◽  
Control Group ◽  
Sprague Dawley ◽  
Sprague Dawley Rats ◽  
Significant Difference ◽  
Group A ◽  
Group B ◽  
Group Control Group

The objective of this work was to investigate the effect of orally administered genistein on the pharmacokinetics of imatinib and N-desmethyl imatinib in rats. Twenty-five healthy male SD (Sprague-Dawley) rats were randomly divided into five groups: A group (control group), B group (multiple dose of 100 mg/kg genistein for consecutive 15 days), C group (multiple dose of 50 mg/kg genistein for consecutive 15 days), D group (a single dose of 100 mg/kg genistein), and E group (a single dose of 50 mg/kg genistein). A single dose of imatinib is administered orally 30 min after administration of genistein (100 mg/kg or 50 mg/kg). The pharmacokinetic parameters of imatinib and N-desmethyl imatinib were calculated by DAS 3.0 software. The multiple dose of 100 mg/kg or 50 mg/kg genistein significantly (P<0.05) decreased theAUC0-tandCmaxof imatinib.AUC0-tand theCmaxof N-desmethyl imatinib were also increased, but without any significant difference. However, the single dose of 100 mg/kg or 50 mg/kg genistein has no effect on the pharmacokinetics of imatinib and N-desmethyl imatinib. Those results indicated that multiple dose of genistein (100 mg/kg or 50 mg/kg) induces the metabolism of imatinib, while single dose of genistein has no effect.

Study on Integrated Pharmacokinetics of Gardenia Acid and Geniposide: Time-Antioxidant Efficacy after Oral Administration of Huanglian–Zhizi Couplet Medicine from Huang–Lian–Jie–Du–Tang in MCAO Rats

2014 ◽  
Vol 42 (02) ◽  
pp. 393-407 ◽  
Author(s):  
Linmei Pan ◽  
Jing Zhou ◽  
Huaxu Zhu ◽  
Wenzhe Wang ◽  
Meng Zhang ◽  
...  
Keyword(s):  
Oral Administration ◽  
High Performance ◽  
Artery Occlusion ◽  
Pharmacokinetic Parameters ◽  
Sprague Dawley ◽  
Concentration Time ◽  
Analysis System ◽  
Data Analysis System ◽  
Index Components ◽  
Cerebral Artery Occlusion

Huanglian–Zhizi couplet medicine comes from classical prescription Huang–Lian–Jie–Du–Tang (HLJDT), which has been proven by previous researches to be an effective compound for cerebral ischemia. This paper explores the integrated pharmacokinetics of gardenia acid and geniposide-time-antioxidant efficacy after the oral administration of Huanglian–Zhizi couplet medicine from HLJDT in rats with middle cerebral artery occlusion (MCAO). To investigate the differences in pharmacokinetics and antioxidant effect of Huanglian–Zhizi and HLJDT in MCAO rats, which have been scarcely reported, an oral dose, 24 crud drug g/kg, of Huanglian–Zhizi and 40 crud drug/kg of HLJDT were administered in two groups of normal rats and two groups of Sprague–Dawley (SD) MCAO rats, respectively. At different time points, concentrations of gardenia acid and geniposide were determined by high performance liquid chromatography (HPLC), and levels of superoxide dismutase (SOD) were calculated by ELIASA. Pharmacokinetic parameters including AUC, MRT, t1/2, T max , C max were estimated by statistical moment analysis using a data analysis system (DAS) 2.0. An AUC based on weighting approach was used for integrating gardenia acid and geniposide. Finally, the concentration-time efficacy profiles were obtained. The integrated pharmacokinetics profiles of index components could reveal the pharmacokinetics behavior of Huanglian–Zhizi and HLJDT, corresponding to the antioxidant efficacy.

Comparative Pharmacokinetic Study of Mangiferin in Normal and Alloxan-Induced Diabetic Rats after Oral and Intravenous Administration by UPLC-MS/MS

Pharmacology ◽  
2018 ◽  
Vol 103 (1-2) ◽  
pp. 30-37 ◽  
Author(s):  
Peng-Cheng Gu ◽  
Lan Wang ◽  
Mei-Na Han ◽  
Jun Peng ◽  
Jing-Chuan Shang ◽  
...  
Keyword(s):  
Intravenous Administration ◽  
Internal Standard ◽  
Ultra Performance Liquid Chromatography ◽  
Diabetic Rats ◽  
Pharmacokinetic Parameters ◽  
Sprague Dawley ◽  
Triple Quadrupole Mass Spectrometer ◽  
Post Dose ◽  
Pharmacokinetic Profiles ◽  
Administration Methods

Backgrounds: Diabetes mellitus (DM)-induced morphological and/or functional complications may alter the pharmacokinetic profiles of mangiferin. This study aims to compare pharmacokinetic profiles of mangiferin in normal and alloxan-induced diabetic rats after oral and intravenous administration. Methods: Mangiferin was administered orally (10 mg/kg) and intravenously (2 mg/kg) to normal and alloxan-induced diabetic Sprague-Dawley (SD) rats (n = 8). Blood samples were collected at different time points post-dose. Mangiferin and esculentoside (internal standard)  were analyzed by Waters Acquity ultra-performance liquid chromatography system and TSQ Quantum Ultra triple quadrupole mass spectrometer (UPLC-MS/MS). Results: Mangiferin in normal and alloxan-induced diabetic rats experienced serious first-pass effect, which resulted in 1.71 and 0.80% of oral bioavailability respectively. Meanwhile, mangiferin was predominantly restricted to blood but not extensively distributed to organ tissues after intravenous administration. Compared with normal rats, the diabetic condition induced 53.26 and 50.90% decreases in Cmax and AUC0–t, respectively, for mangiferin after oral administration, and 63.08% decreases in Cmax after intravenous administration. Conclusions: Compared to normal rats, pharmacokinetic parameters of mangiferin were altered in diabetic condition induced by alloxan. The findings might help to provide useful evidence for modeling of diabetic rats and the clinical applications of mangiferin.

scholarly journals The effect of nano-hydroxyapatite/chitosan scaffolds on rat calvarial defects for bone regeneration

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Emmanouil Chatzipetros ◽  
Spyros Damaskos ◽  
Konstantinos I. Tosios ◽  
Panos Christopoulos ◽  
Catherine Donta ◽  
...  
Keyword(s):  
Bone Regeneration ◽  
Mean Value ◽  
Parietal Bone ◽  
Female Rats ◽  
Sprague Dawley ◽  
Post Surgery ◽  
Group A ◽  
The Mean ◽  
Group B ◽  
The Right

Abstract Background This study aims at determining the biological effect of 75/25 w/w nano-hydroxyapatite/chitosan (nHAp/CS) scaffolds on bone regeneration, in terms of fraction of bone regeneration (FBR), total number of osteocytes (Ost), and osteocyte cell density (CD), as well as its biodegradability. Methods Two critical-size defects (CSDs) were bilaterally trephined in the parietal bone of 36 adult Sprague-Dawley rats (18 males and 18 females); the left remained empty (group A), while the right CSD was filled with nHAp/CS scaffold (group B). Two female rats died postoperatively. Twelve, 11, and 11 rats were euthanized at 2, 4, and 8 weeks post-surgery, respectively. Subsequently, 34 specimens were resected containing both CSDs. Histological and histomorphometric analyses were performed to determine the FBR, calculated as [the sum of areas of newly formed bone in lateral and central regions of interest (ROIs)]/area of the original defect, as well as the Ost and the CD (Ost/mm2) in each ROI of both groups (A and B). Moreover, biodegradability of the nHAp/CS scaffolds was estimated via the surface area of the biomaterial (BmA) in the 2nd, 4th, and 8th week post-surgery. Results The FBR of group B increased significantly from 2nd to 8th week compared to group A (P = 0.009). Both the mean CD and the mean Ost values of group B increased compared to group A (P = 0.004 and P < 0.05 respectively). Moreover, the mean value of BmA decreased from 2nd to 8th week (P = 0.001). Conclusions Based on histological and histomorphometric results, we support that 75/25 w/w nHAp/CS scaffolds provide an effective space for new bone formation.

Behaviour of Uniaxial Reinforced Concrete Columns Strengthened with Ultra-High Performance Concrete and Fiber Reinforced Polymers

2021 ◽  
Vol 28 (2) ◽  
pp. 54-72
Author(s):  
Abd-al-Salam Al-Hazragi ◽  
Assim Lateef
Keyword(s):  
Reinforced Concrete ◽  
High Performance ◽  
High Performance Concrete ◽  
Concrete Columns ◽  
Fiber Reinforced Concrete ◽  
Fiber Reinforced Polymers ◽  
Tension Zone ◽  
Fiber Reinforced ◽  
Group A ◽  
Group B

This article investigates the behaviour of strengthened concrete columns using jacketing ultra-high-performance fiber reinforced concrete (UHPFRC) and carbon fiber-reinforced polymer (CFRP) under uniaxial loaded. The jacket was connected to the column core using shear connectors and (CFRP) fixed as a strip on the tension zone between the column cores and the jacketing. Seven column samples of square cross-section (120 x120) mm at the midsection with overall length of 1250 mm were cast using normal strength concrete (NSC) and having similar longitudinal and transverse reinforcement. The samples were made and tested under axial load at eccentricity equal to 120 mm up to failure. Test parameters were the thickness of jackets (25 and 35) mm and the width of CFRP (0,8, and 12) cm. Column specimens were tested, one of them was reference without any strengthening, and the other specimens divided into two groups (A, and B), and each group included three specimens based on the parameters. Group (A) has UHPFRC jacket thickness 25 mm and CFRP width (0,8, and 12) cm respectively, and group (B) has UHPFRC jacket thickness 35 mm and CFRP width (0,8, and 12) cm respectively. The outcomes of the article show that increasing the thickness of jacket, and width of CFRP lead to increase in the load carrying capacity about (110.5%,168.4%, and 184.2%) for group A, and (157.9%,226.3%, and 263.2%) for group B compared with the reference column due to delay in the appearance of cracks and their distribution. The mid-height lateral displacement of columns was decreased about (66.6%,42.3%, and 35.9%) for group A, and (46.15%,38.46%, and 32.3%) for group B, also the axial deformation of specimens decreased about (71.7%,60.86%, and 55.86%) for group A, and (65.5%,60.5%, and 53.4) for group B compared with the reference column. The ductility of columns that were strengthened with UHPFRC jacket only was increased about (13.67%,19.66%) for thickness(25,35) mm respectively, because of that UHPFRC jacket was contented on steel fibers, and the percentage decrease of ductility was about (5.1%,and 12%) for group (A), (1%,and 9.4%) for group (B) when bonded CFRP in the tension zone with width (8 ,and 12) cm respectively. The results show improvement in the initial and secant stiffness when, increased the thickness of jacket, and width of CFRP because of increase in the size of columns and improvement in the modulus of elasticity. The toughness increase was about (273.97%,301.55%, and 304.5%) for group A, and (453.69%,511.93%, and 524.28%) for group B compared with the reference column because of increase in the size of specimens and delay the appearance of cracks.

scholarly journals Ameliorative effects of Spinacia oleracea on sperm morphology, count, and motility by normalizing the obesity-induced oxidative stress in Sprague Dawley rats

2020 ◽  
Vol 14 (03) ◽  
pp. 124-127
Author(s):  
Somia Iqbal ◽  
Noman Sadiq ◽  
Saad Siddiqui ◽  
Hira Iqbal
Keyword(s):  
Sperm Concentration ◽  
Treated Group ◽  
Sperm Parameters ◽  
Control Group ◽  
Sprague Dawley ◽  
Normal Morphology ◽  
Sprague Dawley Rats ◽  
Group A ◽  
Group B ◽  
Experimental Group

Background: Obesity is a prevailing metabolic disorder that affects the functioning of the male reproductive system. Excessive adipose tissue enhances reactive oxygen species generation and is linked with male infertility. Spinach has demonstrated antioxidant effects. The present study was conducted to determine the antioxidant effects of spinach on sperm parameters in obese Sprague Dawley rats. Subjects and methods: This randomized control study was conducted at the animal house of the National Institute of Health Islamabad, Islamic International Medical College, Cosmesurge International Hospital, Rawalpindi, and Apollo lab, Islamabad, Pakistan from April 2016 to March 2017. Forty male Sprague Dawley rats having an age of 8 weeks and weight 160-200g were tagged from number 1 to 40. Every third rat was randomly allocated to control Group A (n=13) and remaining into the Experimental group (n=27). Rats of control Group A was given a standard diet while a high-fat diet was given to Experimental group rats to induce obesity for the duration of six weeks. Weight (g) was measured weekly and obesity was confirmed when rats attain more than 20% weight when compared with that of rats of control Group A. Then, after obesity induction, the experimental group was alienated into the obesity control group (Group B) and spinach treated group (Group C). For sample, rats of Group A and Group B were sacrificed, and the cauda epididymis of each rat was placed in a Petri dish containing normal saline and cut into pieces to allow the release of sperm and then sperm parameters (sperms concentration, motility, and morphology) were recorded under the microscope. Then, spinach (5% hot water extract) along with the persistence of fat diet was administered to Group C for 4 weeks and finally, sperm parameters were measured in this group. Results: Sperm concentration/ml, motility (%), and normal morphology (%) of Group B rats were significantly decreased as compared to Group A rats. However, sperm concentration/ml, motility (%), and normal morphology (%) of Group C (spinach treated group) rats was significantly increased (p<0.001) as compared to Group B (obesity control group) rats after administering spinach. Conclusion: The addition of Spinach in a normal diet regimen restores normal sperm morphology, improves sperm motility and concentration.

scholarly journals Pain Markers and Epidural Fibrosis Caused by Repeated Spinal Surgery in Sprague–Dawley Rats

2020 ◽  
Author(s):  
Meiling Quan ◽  
Jae-Hoon Kim ◽  
Won-Ha Hwang ◽  
Young-Yul KIM
Keyword(s):  
Western Blotting ◽  
Spinal Surgery ◽  
Immunohistochemical Analysis ◽  
Epidural Fibrosis ◽  
Sprague Dawley ◽  
Sprague Dawley Rats ◽  
Mitogen Activated Protein ◽  
Repeated Surgery ◽  
Group A ◽  
Group B

Abstract Background Epidural fibrosis is one of the aetiologies of pain following spinal revision surgery. However, roles of epidural fibrosis caused by repeated spinal surgery and pain-related proteins in causing the post spinal surgery syndrome remain unknown. In this study, using a rat spinal surgery epidural fibrosis and adhesion model, we evaluate and investigated the relationship between pain marker and epidural fibrosis caused by repeated spinal surgery in Sprague-Dawley rats. Methods Sprague–Dawley rats that underwent repeated spinal surgery were divided into three groups: group A (single laminectomy), group B (two repeated surgeries) and group C (three repeated surgeries). Dural thickness was measured in each experimental group, and immunohistochemical analysis and western blotting of mitogen-activated protein kinases were performed (ERK, p38 and JNK). Results Dural thickness was 6.363 ± 1.911 µm in group A, 13.238 ± 2.123 µm in group B and 19.4 ± 2.115 µm in group C. In western blotting, phosphorylated ERK expression was higher in groups B (1.77 fold) and C (2.42 fold) than in group A. Phosphorylated p38 expression was higher in groups B (1.17 fold) and C (1.33 fold) than in group A. Immunohistochemical analysis revealed that phosphorylated ERK and p38 expression gradually increased with the number of repeated surgeries, as evidenced by western blotting. Conclusions Repeated spinal surgery may increase dural thickness and expression of phosphorylated ERK and p38 in the spinal dorsal horn, suggesting that pain increases with repeated surgery.

Pharmacokinetic Interaction between Asari Radix et Rhizoma and Dried Ginger (Zingiber officinalis) in Rats

2021 ◽  
Vol 17 ◽  
Author(s):  
Xingxing Zhuang ◽  
Li Zhou ◽  
Renhua Miao ◽  
Shoudong Ni ◽  
Meng Li
Keyword(s):  
High Performance ◽  
Pharmacokinetic Interaction ◽  
Raw Material ◽  
Pharmacokinetic Parameters ◽  
Sprague Dawley ◽  
Active Components ◽  
Sprague Dawley Rats ◽  
Liquid Chromatography Tandem Mass ◽  
Student’S T ◽  
Student’S T Test

Introduction:: Asari Radix et Rhizoma (ARR) and dried ginger (Zingiber officinalis) (DG) are often used together in drug preparations in traditional Chinese medicine (TCM) to treat respiratory diseases including cold, bronchitis and pneumonia. Previous studies suggested that ARR and/or DG may influence the pharmacokinetics of other herbal components. In the current study, we examined pharmacokinetic interactions between ARR and DG in rats after oral administration. Methods:: We developed a method based on ultra-high-performance liquid chromatography-tandem mass spectrometry to simultaneously measure serum concentrations of two active components each in ARR (L-asarinin and sesamin) and DG (6-gingerol and 6-shogaol). Adult Sprague-Dawley rats were starved overnight, then given ARR extract, DO extract, or a co-decoction of ARR and DG by gastric gavage (6 g raw material per kg body weight; n = 6 per group). Blood samples were collected prior to drug administration and at the following times (h) afterward: 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 6.0, 8.0, 12.0 and 24.0. Pharmacokinetic parameters were compared using Student’s t test for independent samples. Results:: A simple, rapid, sensitive analytical method has been developed to detect four bioactive components simultaneously in the ARR-DG herbal pair. Pharmacokinetic parameters including Cmax, Tmax, T1/2 and AUC(0~t) were calculated using the non-compartmental model with the DAS 2.0 pharmacokinetic software. For L-asarinin, Tmax was 2.00 ± 0.00 h in ARR animals and 1.67±0.26 h in ARR-DG animals (P<0.05), T1/2 was 8.58 ± 1.75 h in ARR and 11.93 ± 2.13 h in ARR-DG (P<0.05). For 6-gingerol, Cmax was 350.48 ± 23.85 ng/mL in DG animals and 300.21 ± 20.02 ng/mL in ARR-DG (P<0.01), Tmax was 2.83 ± 0.41 h in DG and 2.17 ± 0.41 h in ARR-DG (P<0.05) and AUC(0~t) was 1.93 ± 0.15 mg/mL•h in ARR and 1.70 ± 0.15 mg/mL•h in ARR-DG (P<0.05). For 6-shogaol, Cmax was 390.28 ± 26.02 ng/mL in DG animals and 455.63 ± 31.01 ng/mL in ARR-DG (P<0.01), Tmax was 2.93 ± 0.10 h in DG and 1.92 ± 0.10 h in ARR-DG (P<0.01), T1/2 was 3.74 ± 0.29 h in DG and 3.28 ± 0.22 h in ARR-DG (P<0.01), and AUC(0~t) was 2.15 ± 0.18 mg/mL•h in DG and 2.73 ± 0.15 mg/mL•h in ARR-DG (P<0.01). Conclusions:: Pharmacokinetic interations between ARR and DG decrease Tmax, increase T1/2 but do not affect overall bioavailability of L-asarinin in ARR. The interactions in ARR-DG decrease Cmax and Tmax but increase T1/2 and AUC(0~t) of 6-gingerol in DG. The interactions increase Cmax and AUC(0~t) but decrease Tmax and T1/2 of 6- shogaol in DG. Interactions in ARR-DG do not affect the pharmacokinetics of sesamin.

scholarly journals Pharmacokinetic Profile of μSMIN Plus™, a new Micronized Diosmin Formulation, after Oral Administration in Rats

2015 ◽  
Vol 10 (9) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Rosario Russo ◽  
Angelo Mancinelli ◽  
Michele Ciccone ◽  
Fabio Terruzzi ◽  
Claudio Pisano ◽  
...  
Keyword(s):  
Oral Administration ◽  
Plasma Concentrations ◽  
Compartmental Analysis ◽  
Pharmacokinetic Profile ◽  
Pharmacokinetic Parameters ◽  
Maximum Plasma ◽  
Sprague Dawley ◽  
Time Curve ◽  
Maximum Plasma Drug Concentration

Diosmin is a naturally occurring flavonoid present in citrus fruits and other plants belonging to the Rutaceae family. It is used for the treatment of chronic venous insufficiency (CVI) for its pheblotonic and vaso-active properties, safety and tolerability as well. The aim of the current in vivo study was to investigate the pharmacokinetic profile of a branded micronized diosmin (μSMIN Plus™) compared with plain micronized diosmin in male Sprague-Dawley rats. After oral administration by gastric gavage, blood samples were collected via jugular vein catheters at regular time intervals from baseline up to 24 hours. Plasma concentrations were assessed by LC/MS. For each animal, the following pharmacokinetic parameters were calculated using a non-compartmental analysis: maximum plasma drug concentration (Cmax), time to reach Cmax (Tmax), area under the plasma concentration-time curve (AUC0-last), elimination half-life (t1/2), and relative oral bioavailability (%F). The results of the current study clearly showed an improvement in the pharmacokinetic parameters in animals treated with μSMIN Plus™ compared with animals treated with micronized diosmin. In particular, μSMIN Plus™ showed a 4-fold increased bioavailability compared with micronized diosmin. In conclusion, the results from the current study provided a preliminary pharmacokinetic profile for μSMIN Plus™, which may represent a new tool for CVI management.

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