scholarly journals Plasma pharmacokinetic profile of fluralaner (Bravecto™) and ivermectin following concurrent administration to dogs

2015 ◽  
Vol 8 (1) ◽  
Author(s):  
Feli M. Walther ◽  
Mark J. Allan ◽  
Rainer KA Roepke
Keyword(s):  
Pharmacokinetic Profile ◽  
Concurrent Administration ◽  
Plasma Pharmacokinetic

scholarly journals Plasma pharmacokinetic profile and efficacy of meloxicam administered subcutaneously and intramuscularly to sheep

PLoS ONE ◽  
2019 ◽  
Vol 14 (4) ◽  
pp. e0215842 ◽  
Author(s):  
Alyssa N. Woodland ◽  
Dominique Van der Saag ◽  
Benjamin Kimble ◽  
Peter J. White ◽  
Merran Govendir ◽  
...  
Keyword(s):  
Pharmacokinetic Profile ◽  
Plasma Pharmacokinetic

Significance of In-Vitro and In-Vivo Correlation in Drug Delivery System

2018 ◽  
Vol 4 (4) ◽  
pp. 523-531
Author(s):  
Hina Mumtaz ◽  
Muhammad Asim Farooq ◽  
Zainab Batool ◽  
Anam Ahsan ◽  
Ashikujaman Syed
Keyword(s):  
Dosage Form ◽  
Pharmaceutical Preparations ◽  
Pharmacokinetic Profile ◽  
In Vitro Dissolution ◽  
Time Saving ◽  
Pharmaceutical Dosage Form ◽  
Short Period ◽  
Form Development

The main purpose of development pharmaceutical dosage form is to find out the in vivo and in vitro behavior of dosage form. This challenge is overcome by implementation of in-vivo and in-vitro correlation. Application of this technique is economical and time saving in dosage form development. It shortens the period of development dosage form as well as improves product quality. IVIVC reduce the experimental study on human because IVIVC involves the in vivo relevant media utilization in vitro specifications. The key goal of IVIVC is to serve as alternate for in vivo bioavailability studies and serve as justification for bio waivers. IVIVC follows the specifications and relevant quality control parameters that lead to improvement in pharmaceutical dosage form development in short period of time. Recently in-vivo in-vitro correlation (IVIVC) has found application to predict the pharmacokinetic behaviour of pharmaceutical preparations. It has emerged as a reliable tool to find the mode of absorption of several dosage forms. It is used to correlate the in-vitro dissolution with in vivo pharmacokinetic profile. IVIVC made use to predict the bioavailability of the drug of particular dosage form. IVIVC is satisfactory for the therapeutic release profile specifications of the formulation. IVIVC model has capability to predict plasma drug concentration from in vitro dissolution media.

Development and Oral Bioavailability of Self-Emulsifying Formulation of Ketoconazole

2013 ◽  
Vol 5 (4) ◽  
pp. 1858-1865
Author(s):  
Arundhati Bhattacharyya ◽  
M Bajpai
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Oral Absorption ◽  
Aqueous Suspension ◽  
Droplet Diameter ◽  
Tween 80 ◽  
Concurrent Administration ◽  
System Maintenance ◽  
Pure Drug ◽  
Ph Dependent

Ketoconazole is an imidazole antifungal drug belonging to the class II of Biopharmaceutic Classification System. Maintenance of gastric acidity is essential for adequate dissolution and absorption of ketoconazole. Concurrent administration of antacid and antiulcer preparations decreases the oral absorption of ketoconazole often causing therapeutic failure.  The aim of this study was to evaluate whether a self-emulsifying formulation of ketoconazole would be able to overcome the pH dependent dissolution and oral bioavailability. Self-emulsifying drug delivery system (SEDDS) was prepared after selecting the oil, surfactant and co-surfactant by solubility analysis. Optimum ratio of the components was finalized on the basis of drug content, self-emulsification and mean droplet diameter. The effect of pH on dissolution was studied in comparison to the pure drug. Oral bioavailability was determined in comparison to aqueous suspension in rats and the effect of co-administration of ranitidine hydrochloride solution and a commercially available liquid antacid preparation was studied. The optimized formulation containing 20% Capryol 90 and 40% each of Carbitol and Tween 80, exhibited 100% drug release regardless of the pH whereas the pure drug exhibited a highly pH dependent dissolution. The AUC0-24 resulted with oral administration of the SEDDS formulation was about 34%, 43% and 60% higher compared to the aqueous suspension when administered alone, administered with ranitidine and administered with antacid respectively. The results of the present study demonstrate that self-emulsifying formulations can be utilized for oral delivery of weakly basic drugs like ketoconazole which exhibit pH dependent dissolution.

Improved Pharmacokinetic Profile and Anti-Inflammatory Property of a Novel Curcumin Derivative, A50

2013 ◽  
Vol 10 (6) ◽  
pp. 535-542
Author(s):  
Xiangjian Chen ◽  
Luqing Ren ◽  
Xiuhua Zhang ◽  
Lu Guo ◽  
Jianmin Zhou ◽  
...  
Keyword(s):  
Pharmacokinetic Profile ◽  
Anti Inflammatory ◽  
Curcumin Derivative

Hybrids of Coumarin Derivatives as Potent and Multifunctional Bioactive Agents: A Review

2020 ◽  
Vol 16 (3) ◽  
pp. 272-306
Author(s):  
Ioannis Fotopoulos ◽  
Dimitra Hadjipavlou-Litina
Keyword(s):  
Pharmacological Activity ◽  
Biological Activities ◽  
Structural Characteristics ◽  
Pharmacokinetic Profile ◽  
Biologically Active ◽  
Hybridization Technique ◽  
Coumarin Derivatives ◽  
Hybrid Molecules ◽  
Pharmacokinetic Properties ◽  
Bioactive Agents

Background: Coumarins exhibit a plethora of biological activities, e.g. antiinflammatory and anti-tumor. Molecular hybridization technique has been implemented in the design of novel coumarin hybrids with several bioactive groups in order to obtain molecules with better pharmacological activity and improved pharmacokinetic profile. Objective: Therefore, we tried to gather as many as possible biologically active coumarin hybrids referred in the literature till now, to delineate the structural characteristics in relation to the activities and to have a survey that might help the medicinal chemists to design new coumarin hybrids with drug-likeness and varied bioactivities. Results: The biological activities of the hybrids in most of the cases were found to be different from the biological activities presented by the parent coumarins. The results showed that the hybrid molecules are more potent compared to the standard drugs used in the evaluation experiments. Conclusion: Conjugation of coumarin with varied pharmacophore groups/druglike molecules responsible for different biological activities led to many novel hybrid molecules, with a multitarget behavior and improved pharmacokinetic properties.

Design, Synthesis, and Pharmacokinetic Evaluation of O-Carbamoyl Tizoxanide Prodrugs

2020 ◽  
Vol 16 ◽  
Author(s):  
Xi He ◽  
Wenjun Hu ◽  
Fanhua Meng ◽  
Xingzhou Li
Keyword(s):  
Plasma Concentration ◽  
Broad Spectrum ◽  
Plasma Concentrations ◽  
Antiviral Drug ◽  
Systemic Exposure ◽  
Pharmacokinetic Profile ◽  
Hydroxyl Group ◽  
First Pass

Background: The broad-spectrum antiparasitic drug nitazoxanide (N) has been repositioned as a broad-spectrum antiviral drug. Nitazoxanide’s in vivo antiviral activities are mainly attributed to its metabolitetizoxanide, the deacetylation product of nitazoxanide. In reference to the pharmacokinetic profile of nitazoxanide, we proposed the hypotheses that the low plasma concentrations and the low system exposure of tizoxanide after dosing with nitazoxanide result from significant first pass effects in the liver. It was thought that this may be due to the unstable acyloxy bond of nitazoxanide. Objective: Tizoxanide prodrugs, with the more stable formamyl substituent attached to the hydroxyl group rather than the acetyl group of nitazoxanide, were designed with the thought that they might be more stable in plasma. It was anticipated that these prodrugs might be less affected by the first pass effect, which would improve plasma concentrations and system exposure of tizoxanide. Method: These O-carbamoyl tizoxanide prodrugs were synthesized and evaluated in a mouse model for pharmacokinetic (PK) properties and in an in vitro model for plasma stabilities. Results: The results indicated that the plasma concentration and the systemic exposure of tizoxanide (T) after oral administration of O-carbamoyl tizoxanide prodrugs were much greater than that produced by equimolar dosage of nitazoxanide. It was also found that the plasma concentration and the systemic exposure of tizoxanide glucuronide (TG) were much lower than that produced by nitazoxanide. Conclusion: Further analysis showed that the suitable plasma stability of O-carbamoyl tizoxanide prodrugs is the key factor in maximizing the plasma concentration and the systemic exposure of the active ingredient tizoxanide.

A Comparative Pharmacokinetic Profile of Trahydropalmatine After Oral Administration of its Monomer, Rhizoma Corydalis Alkaloid Extracts and Tong-Bi-Si-Wei-Fang to Rats

2019 ◽  
Vol 15 (4) ◽  
pp. 338-345
Author(s):  
Lijun Ni ◽  
Lu Ding ◽  
Liguo Zhang ◽  
Shaorong Luan
Keyword(s):  
Oral Administration ◽  
Panax Notoginseng ◽  
Pharmacokinetic Profile ◽  
Apparent Volume ◽  
Bone Diseases ◽  
Glycyrrhiza Uralensis ◽  
Pharmacokinetic Property ◽  
Time Curve ◽  
Concentration Time

Background: Tong-Bi-Si-Wei-Fang (TBSWF) is a candidate formula of Traditional Chinese Medicine (TCM) for treating rheumatoid bone diseases, which is composed of rhizoma corydalis alkaloids, saponins of glycyrrhiza uralensis and panax notoginseng, flavonoids of rhizoma drynariae and glycyrrhiza uralensis. </P><P> Objective: Trahydropalmatine (THP), the main active ingredient of rhizoma corydalis alkaloids, was selected to study in vivo pharmacokinetics and druggability of TBSWF. Methods: The plasma concentration-time (C-T) profiles of THP and the pharmacokinetic property parameters after oral administration of THP monomer, extract of corydalis alkaloids (ECA) and TBSWF to rats, respectively were compared by a fully-validated HPLC method. Results: Compared to the THP monomer, the THP in TBSWF is absorbed faster, resides in the plasma longer and has a similar apparent volume of distribution Vz/F (10~20 L/kg). Compared to THP monomer and THP in TBSWF, the area under the concentration-time curve AUC 0-t of THP in ECA decreases two-third; Vz/F of THP in ECA (85.02 L/kg) is significantly higher than that of THP in TBSWF(p <0.05). Unlike THP monomer and THP in ECA, double peaks are observed in the C-T profile of THP after oral administration of TBSWF. THP in TBSWF exhibits slow release to a certain degree. Conclusion: The interactions among the ingredients of TBSWF promote the adsorption and prolong the residence time of THP in vivo, and provide an explanation for the advantages of TBSWF from the point of pharmacokinetics.

Sign in / Sign up

Export Citation Format

Share Document