scholarly journals Prediction of In-vivo Performance of Naproxen and Esomeprazole Magnesium Delayed-Release Tablets using Biorelevant Dissolution Tests

2020 ◽  
Vol 12 (2) ◽  
pp. 12-23
Author(s):  
Devi Thamizhanban ◽  
Gampa Tulja Rani ◽  
Kathiresan Krishnasamy ◽  
◽  
◽  
...  
Keyword(s):  
Delayed Release ◽  
Biorelevant Dissolution ◽  
Dissolution Tests ◽  
Esomeprazole Magnesium

scholarly journals Biorelevant dissolution of candesartan cilexetil

ADMET & DMPK ◽  
2017 ◽  
Vol 5 (1) ◽  
pp. 39 ◽  
Author(s):  
Lucie Gruberová ◽  
Bohumil Kratochvil
Keyword(s):  
Dosage Form ◽  
Candesartan Cilexetil ◽  
Drug Formulation ◽  
Biorelevant Media ◽  
Solid Dosage ◽  
Biorelevant Dissolution ◽  
Dissolution Tests ◽  
Poorly Soluble ◽  
Form Development

<p class="ADMETabstracttext">The choice of an appropriate medium for dissolution tests is an essential step during a dosage form development. The adequate design of dissolution testing enables forecasting in vivo behavior of drug formulation. Biorelevant media were developed for this purpose because dissolution media described in the International Pharmacopoeia are not thoroughly suitable. Therefore, we carried out solubility and dissolution tests in biorelevant media and we compared the results with data measured in compendial dissolution media. A shake-flask method and standard paddle apparatus were used. The concentration was measured by a UV-Vis spectrophotometer. An oral solid dosage form with poorly soluble drug candesartan cilexetil was tested. Significant differences in the solubility and dissolution profiles of candesartan cilexetil were observed. The study offers the overview of compendial and biorelevant media simulating fasted state that can be analyzed by a spectrophotometric technique.</p>

Application of biorelevant dissolution tests to the prediction of in vivo performance of diclofenac sodium from an oral modified-release pellet dosage form

2009 ◽  
Vol 37 (3-4) ◽  
pp. 434-441 ◽  
Author(s):  
Ekarat Jantratid ◽  
Vincenzo De Maio ◽  
Emanuela Ronda ◽  
Valentina Mattavelli ◽  
Maria Vertzoni ◽  
...  
Keyword(s):  
Dosage Form ◽  
Diclofenac Sodium ◽  
Modified Release ◽  
Biorelevant Dissolution ◽  
Dissolution Tests

Impact of Acid-Reducing Agents on Gastrointestinal Physiology and Design of Biorelevant Dissolution Tests to Reflect These Changes

2019 ◽  
Vol 108 (11) ◽  
pp. 3461-3477 ◽  
Author(s):  
Domagoj Segregur ◽  
Talia Flanagan ◽  
James Mann ◽  
Andrea Moir ◽  
Eva M. Karlsson ◽  
...  
Keyword(s):  
Reducing Agents ◽  
Gastrointestinal Physiology ◽  
Biorelevant Dissolution ◽  
Dissolution Tests

scholarly journals FORMULATION, OPTIMIZATION, CHARACTERIZATION AND IN VIVO ANTI-ULCER ACTIVITY OF ESOMEPRAZOLE MAGNESIUM TRIHYDRATE GASTRORESISTANT MICROSPHERES

2016 ◽  
Vol 9 (1) ◽  
pp. 273
Author(s):  
Krutika Sawant ◽  
Mitali Patel ◽  
Jiten Patel ◽  
Piyush Mundada
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Intestinal Absorption ◽  
Ulcer Formation ◽  
Scanning Calorimetry ◽  
Aqueous Solvent ◽  
Release Study ◽  
Esomeprazole Magnesium

<p><strong>Objective: </strong>The objective of the present investigation was to prepare gastro-resistant microspheres of esomeprazole magnesium trihydrate (EMT) to prevent its degradation in the acidic environment of the stomach and enhance its bioavailability via intestinal absorption.</p><p><strong>Methods: </strong>EMT loaded gastro-resistant microspheres were prepared using hypromellose acetate succinate (HPMCAS) as the gastro-resistant polymer by ‘non-aqueous solvent evaporation’ technique. A 3-factor 3 level factorial design was used to optimise EMT: HPMCAS ratio, the concentration of Span 80 and stirring speed with respect to percent entrapment efficiency and particle size. Further characterization was carried out using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), <em>In vitro</em> release study and <em>In vivo</em> anti-ulcer activity.</p><p><strong>Results: </strong>Fourier transform infrared <strong>(</strong>FTIR) study indicated compatibility between drug and polymer. DSC study revealed that the drug was molecularly dispersed in the polymer. The optimised batch showed 49.63±1.23% drug entrapment and 170.12±3.36 μm particle size. SEM study showed that microspheres were spherical in shape<strong>. </strong><em>In vitro</em> drug release study showed only 4.28±1.23% drug release in simulated gastric media in 2 hr and 93.46±1.20% release in simulated intestinal media after 1 hr from the optimised batch.</p><p><strong>Conclusion: </strong>Results of <em>in vitro </em>release studies indicated the gastro-resistant nature of the developed microspheres. <em>In vivo</em> anti-ulcer activity demonstrated that EMT loaded microspheres were able to significantly reduce ethanol-induced ulcer formation in rats’ stomach as compared to the aqueous solution of EMT. So it can be concluded that the developed gastro-resistant microspheres of EMT prevented drug release in the stomach which would lead to a significant improvement in its bioavailability through enhanced intestinal absorption</p>

In-situ Intestinal Absorption and Pharmacokinetic Investigations of Carvedilol Loaded Supersaturated Self-emulsifying Drug System

2020 ◽  
Vol 8 (3) ◽  
pp. 207-224
Author(s):  
Vamshi M. Krishna ◽  
Vijaya B. Kumar ◽  
Narendar Dudhipala
Keyword(s):  
Oral Administration ◽  
Oral Delivery ◽  
In Vivo Studies ◽  
Absolute Bioavailability ◽  
Delivery Vehicle ◽  
Biorelevant Dissolution ◽  
Alternative Delivery ◽  
Biorelevant Dissolution Media ◽  
Sem Studies

Background: Carvedilol (CD), a non-selective beta-blocker, is indicated for the management of mild to moderate congestive heart failure. After oral administration, CD is rapidly absorbed with an absolute bioavailability of 18-25% because of low solubility and extensive first-pass metabolism. Objective: The present investigation focused on enhanced oral delivery of CD using supersaturated self-emulsifying drug delivery (SEDDS) system. Methods: Optimized SEDDS consisted of a blend of Oleic acid and Labrafil-M2125 as an oil-phase, Cremophor-RH40, polyethylene glycol-400 and HPMC-E5 as a surfactant, co-surfactant and supersaturation promoter respectively. Formulations were characterized for physical characteristics, invitro release in simulated and biorelevant dissolution media, intestinal permeability and bioavailability studies in Wistar rats. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis, scanning electron microscopy (SEM) studies were used to confirm the crystalline nature and shape of the optimized formulation. Results: DSC and XRD, SEM studies showed that the drug was in amorphous form, and droplets were spherical in shape. Dissolution studies clearly showed distinct CD release in compendial and biorelevant dissolution media. The results from permeability and in-vivo studies depicted 2.2-folds and 3.2-folds increase in permeability and bioavailability, respectively from supersaturated SEDDS in comparison with control. Conclusions: The results conclusively confirmed that the SEDDS formulation could be considered as a new alternative delivery vehicle for the oral supply of CD. Lay Summary: Carvedilol (CD) is a non-selective antihypertensive drug with poor oral bioavailability. Previously, various lipid delivery systems were reported with enhanced oral delivery. We developed suprsaturable SEDDS formulation with immediate onset of action. SEDDS formulation was developed and optimized as per the established protocols. The optimized SEDDS formulation was stable over three months and converted to solid and supersaturated SEDDS. The results from permeability and in-vivo studies demonstrated an enhancement in permeability and bioavailability from supersaturated SEDDS in comparison with control. The results conclusively confirmed that the SEDDS formulation could be considered as a new alternative delivery vehicle for the oral administration of CD.

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