Diversity-Oriented Synthesis of Spiropyrrolo[1,2-a]isoquinoline Derivatives via Diastereoselective and Regiodivergent Three-Component 1,3-Dipolar Cycloaddition Reactions: In Vitro and in Vivo Evaluation of the Antidiabetic Activity of Rhodanine Analogues

2021 ◽  
Author(s):  
Amani Toumi ◽  
Sarra Boudriga ◽  
Khaled Hamden ◽  
Ismail Daoud ◽  
Moheddine Askri ◽  
...  
Keyword(s):  
Antidiabetic Activity ◽  
Dipolar Cycloaddition ◽  
Cycloaddition Reactions ◽  
In Vivo Evaluation ◽  
Diversity Oriented Synthesis ◽  
Isoquinoline Derivatives

scholarly journals ETHYLCELLULOSE FLOATING MICROSPHERES OF ANTIDIABETIC AGENT: IN VITRO AND IN VIVO EVALUATION

2016 ◽  
Vol 9 (1) ◽  
pp. 44 ◽  
Author(s):  
Seema Kohli ◽  
Megha Sharma ◽  
Abhisek Pal
Keyword(s):  
Average Particle Size ◽  
Insulin Dependent Diabetes Mellitus ◽  
Treated Group ◽  
Antidiabetic Activity ◽  
Dependent Diabetes Mellitus ◽  
Average Particle ◽  
In Vivo Evaluation ◽  
Gastro Retentive

Objective: To develop and evaluate floating type gastro-retentive dosage form, appropriate for controlled release of repaglinide (RG) having a narrow therapeutic window.Methods: Repaglinide loaded microspheres (MS) using biological macromolecule ethylcellulose (EC) was prepared by a solvent diffusion-evaporation technique using polyvinyl alcohol (PVA) emulsifier. Compatibility of drug and polymer was studied by Fourier-transform infrared spectroscopy (FTIR). During formulation, various process optimisation parameters studied were stirring speed, the concentration of drug, polymer and emulsifier. Characterization and in vitro evaluation was performed. In vivo antidiabetic activity was performed on alloxan induced diabetic rats followed by histopathological screening.Results: The average particle size was in the range of 174-243 µm. Yield, entrapment and buoyancy of microspheres were 68.4­­-79.8, 58.6-73.1 and 71.8-84.1% respectively. 65.1% release of drug from optimised formulation was obtained which follows first-order kinetics (r2 = 0.989). Optimised formulation treated group shows significant (p<0.01) decrease in glucose level of blood as compared to pure drug treated group during the later hours of study with satisfactory results of histology.Conclusion: The investigation revealed the promising potential of gastro retentive microspheres for delivering RG for the treatment of non-insulin dependent diabetes mellitus (NIDDM).

In vitro and in vivo evaluation of the antidiabetic activity of ursolic acid derivatives

2014 ◽  
Vol 80 ◽  
pp. 502-508 ◽  
Author(s):  
Pan-Pan Wu ◽  
Kun Zhang ◽  
Yu-Jing Lu ◽  
Ping He ◽  
Su-Qing Zhao
Keyword(s):  
Ursolic Acid ◽  
Antidiabetic Activity ◽  
In Vivo Evaluation

scholarly journals Evaluation of Aqueous Extract of Alphonsea sclerocarpa for in vivo and in vitro Antidiabetic Potentials in Wistar Rats

2021 ◽  
Vol 70 (2) ◽  
Author(s):  
Ravi Shankar N ◽  
Ram Kishore ◽  
Puranik SB
Keyword(s):  
Blood Glucose ◽  
Glucose Uptake ◽  
Aqueous Extract ◽  
Insulin Level ◽  
Antidiabetic Activity ◽  
Albino Rats ◽  
Oral Glucose ◽  
In Vivo Evaluation

The purpose of current investigation was to investigate in vivo and in vitro anti-diabetic potentials of aqueous extract of Alphonsea sclerocarpa leaves against alloxan induced diabetes in albino rats. Two in vivo and one in vitro methods were performed for the evaluation of aqueous extract for antidiabetic activity. For in-vivo evaluation, diabetes was induced in albino rats by administering a single dose of alloxan. The study was designed to test the acute effect of aqueous extract of Alphonsea sclerocarpa (AEAS) to reduce blood glucose in OGTT. The chronic study of 21 days was performed against diabetic rats and blood glucose was determined at 1st , 7 th, 14th and 21st day. In chronic in vivo study, serum parameters insulin, urea, creatinine, total cholesterol, triglycerides, ALT and AST were also estimated at 21st day to determine the effects of aqueous and aqueous extracts on complications of diabetes mellitus. Glucose uptake by hemidiaphragm assay was performed to test the ability of extract to utilize glucose. In Oral Glucose Tolerance Test, standard glibenclamide and aqueous extract (200mg/kg and 400mg/kg) treated animals have shown significant reduction in blood glucose at 90 mins but at 120 mins. In chronic model the aqueous extract effectively reduced blood glucose levels (P<0.001) at 14th and 21st day of study in therapeutic groups and effect was comparable to that of standard. The extract could also significantly (P<0.001) reduce concentrations of SGOT, triglycerides, cholesterol and urea in serum and significantly (P<0.001) increased the insulin level in blood which proves beneficial effects of the extract in diabetes. The change in concentrations of SGPT and urea were less significant (P>0.01). The presence of extract in glucose uptake assay could significantly increase utilization of the glucose by rat hemidiaphragm. The aqueous extract of Alphonsea sclerocarpa possess significant antidiabetic properties against alloxan induced diabetic animals.

scholarly journals Antidiabetic Potential of Selected Medicinal Plants: A Literature Review

2021 ◽  
pp. 1-11
Author(s):  
Abdulrahman Altalhi ◽  
Mashhour Alsufyani ◽  
Khalid Alqurashi ◽  
Hussain Alshalwi ◽  
Abdullah Althobaiti ◽  
...  
Keyword(s):  
Plant Species ◽  
Scientific Evidence ◽  
Tolerance Test ◽  
Protein Glycation ◽  
Antidiabetic Activity ◽  
In Vivo Evaluation ◽  
Traditional Use ◽  
Alpha Glucosidase

Aims: To investigated for any scientific evidence indicating traditional use of different plant species in the management of diabetes. Study Design: Review Article. Place and Duration of Study: Conducted in Saudi Arabia from December 2020 to August 2021. Methodology: The literature was thoroughly investigated for any scientific evidence indicating traditional use of different plant species in the management of diabetes. The search was done in databases of Google Scholar, Saudi Digital Library and PubMed. Accordingly, the used plant species are classified into six groups. These are: Plants with antidiabetic activity, Plants with hypoglycemic activity, plants with alpha-glucosidase activity, Plants with alpha-amylase activity, Plants with glucose tolerance test, Plants with hypolipemic, anti-cholesterol, LDL and HDL activity. Conclusion: We have done in vitro and in vivo evaluation of M. arvensis L. for antidiabetic activity.  The leaves extracts of M. arvensis L. showed significant antioxidant potential and significantly inhibited protein glycation, which correlated well with its phenolics along with other phytoconstituents. the methanolic extract of M. arvensis L.

In vitro and in vivo evaluation of the anti-inflammatory effects of Arzanol from Helichrysum italicum

Planta Medica ◽  
2010 ◽  
Vol 76 (12) ◽  
Author(s):  
J Bauer ◽  
F Dehm ◽  
A Koeberle ◽  
F Pollastro ◽  
G Appendino ◽  
...  
Keyword(s):  
In Vivo Evaluation ◽  
Anti Inflammatory

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

Design and In vivo Evaluation of Palonosetron HCl Mouth Dissolving Films in the Management of Chemotherapy-Induced Vomiting

2017 ◽  
Vol 10 (6) ◽  
pp. 3929-3936
Author(s):  
Y. Srinivasa Rao ◽  
K. Adinarayana Reddy
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Onset Of Action ◽  
In Vivo Evaluation ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Drug Content

Fast dissolving oral delivery systems are solid dosage forms, which disintegrate or dissolve within 1 minute in the mouth without drinking water or chewing. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use and the consequent patient compliance. The purpose of this work was to develop mouth dissolving oral films of palonosetron HCl, an antiemetic drug especially used in the prevention and treatment of chemotherapy-induced nausea and vomiting. In the present work, the films were prepared by using solvent casting method with various polymers HPMC E3, E5 & E15 as a film base synthetic polymer, propylene glycol as a plasticizer and maltodextrin and other polymers. Films were found to be satisfactory when evaluated for thickness, in vitro drug release, folding endurance, drug content and disintegration time. The surface pH of all the films was found to be neutral. The in vitro drug release of optimized formulation F29 was found to be 99.55 ± 6.3 7% in 7 min. The optimized formulation F29 also showed satisfactory surface pH, drug content (99.38 ± 0.08 %), disintegration time of 8 seconds and good stability. FTIR data revealed that no interaction takes place between the drug and polymers used in the optimized formulation. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Palonosetron Hydrochloride. Therefore, the mouth dissolving film of palonosetron is potentially useful for the treatment of emesis disease where quick onset of action is desired, also improved patient compliance.

Formulation and In Vivo Evaluation of Mucoadhesive Micro-spheres of Rebamipide, a Mucoprotective Drug for GIT Disorders

2018 ◽  
Vol 11 (3) ◽  
pp. 4089-4097
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Kanteepan P
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Amino Acid Derivative ◽  
Release Mechanism ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Percentage Yield

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel  were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.  

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