Application of an In Vitro Dissolution/Permeation System to Early Screening of Oral Formulations of Poorly Soluble, Weakly Basic Drugs Containing an Acidic pH-Modifier

2018 ◽  
Vol 107 (9) ◽  
pp. 2404-2410 ◽  
Author(s):  
Masashi Mizoguchi ◽  
Makoto Kataoka ◽  
Kazutoshi Yokoyama ◽  
Risa Aihara ◽  
Koichi Wada ◽  
...  
Keyword(s):  
In Vitro Dissolution ◽  
Acidic Ph ◽  
Basic Drugs ◽  
Early Screening ◽  
Oral Formulations ◽  
Ph Modifier ◽  
Poorly Soluble

scholarly journals In vitro and in vivo Evaluation of Ibuprofen Nanosuspensions for Enhanced Oral Bioavailability

2021 ◽  
Author(s):  
Mohsen Hedaya ◽  
Farzana Bandarkar ◽  
Aly Nada
Keyword(s):  
Particle Size ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
In Vivo Evaluation ◽  
Poorly Soluble ◽  
Extent Of Absorption ◽  
Better Than

Introduction: The objectives were to prepare, characterize and in vivo evaluate different ibuprofen (IBU) nanosuspensions prepared by ultra-homogenization, after oral administration to rabbits. Methods: The nanosuspensions produced by ultra-homogenization were tested and compared with a marketed IBU suspension for particle size, in vitro dissolution and in vivo absorption. Five groups of rabbits received orally 25 mg/kg of IBU nanosuspension, nanoparticles, unhomogenized suspension, marketed product and untreated suspension. A sixth group received 5 mg/kg IBU intravenously. Serial blood samples were obtained after IBU administration. Results: The formulated nanosuspensions showed significant decrease in particle size. Polyvinyl Pyrrolidone K30 (PP) was found to improve IBU aqueous solubility much better than the other tested polymers. Addition of Tween 80 (TW), in equal amount as PP (IBU: PP:TW, 1:2:2 w/w) resulted in much smaller particle size and better dissolution rate. The Cmax achieved were 14.8±1.64, 11.1±1.37, 9.01±0.761, 7.03±1.38 and 3.23±1.03 μg/ml and the tmax were 36±8.2, 39±8.2, 100±17.3, 112±15 and 105±17 min for the nanosuspension, nanoparticle, unhomogenized suspension, marketed IBU suspension and untreated IBU suspension in water, respectively. Bioavailability of the different formulations relative to the marketed suspension were the highest for nanosuspension> unhomogenized suspension> nanoparticles> untreated IBU suspension. Conclusion: IBU/PP/TW nanosuspensions showed enhanced in vitro dissolution as well as faster rate and higher extent of absorption as indicated from the higher Cmax, shorter tmax and larger AUC. The in vivo data supported the in vitro results. Nanosuspensions prepared by ultra-high-pressure-homogenization technique can be used as a good formulation strategy to enhance the rate and extent of absorption of poorly soluble drugs.

In Vitro and In Vivo Assessment of the Potential of Supersaturation to Enhance the Absorption of Poorly Soluble Basic Drugs

2019 ◽  
Vol 15 (4) ◽  
pp. 591-602
Author(s):  
Jibin Li ◽  
Yuri Bukhtiyarov ◽  
Nicole Spivey ◽  
Christopher Force ◽  
Carlos Hidalgo ◽  
...  
Keyword(s):  
Basic Drugs ◽  
Poorly Soluble ◽  
In Vivo Assessment

scholarly journals Development and Validation of a Discriminating In Vitro Dissolution Method for a Poorly Soluble Drug, Olmesartan Medoxomil: Comparison Between Commercial Tablets

2010 ◽  
Vol 11 (2) ◽  
pp. 637-644 ◽  
Author(s):  
Lisiane Bajerski ◽  
Rochele Cassanta Rossi ◽  
Carolina Lupi Dias ◽  
Ana Maria Bergold ◽  
Pedro Eduardo Fröehlich
Keyword(s):  
Olmesartan Medoxomil ◽  
In Vitro Dissolution ◽  
Dissolution Method ◽  
Poorly Soluble ◽  
Poorly Soluble Drug ◽  
Development And Validation

scholarly journals FORMULATION AND OPTIMIZATION OF CURCUMIN SOLID DISPERSION PELLETS FOR IMPROVED SOLUBILITY

2019 ◽  
pp. 36-46
Author(s):  
SANJEEVANI DESHKAR ◽  
ARUN SATPUTE
Keyword(s):  
Solid Dispersion ◽  
Weight Ratio ◽  
Poloxamer 407 ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Phase Solubility ◽  
Dsc Studies ◽  
Poorly Soluble ◽  
Extrusion Spheronization

Objective: The present study was aimed at designing of solid dispersion based pellets of curcumin (Cu) for improving its solubility. Methods: Solid dispersion (SD) of Cu was prepared by the melt method using Poloxamer 407 (Pol 407) at a different weight ratio of Cu-Pol 407 (1:2, 1:3, 1:5, 1:7, 1:10). The solid dispersion was characterised by FTIR, SEM, DSC, XRD and evaluated for saturation solubility in water, drug content and in vitro dissolution. The pellets of Cu solid dispersion were prepared by extrusion spheronization technique and optimization was performed by 32full factorial design. The pellets were evaluated for size distribution, flow properties, hardness, disintegration and in vitro drug dissolution. Results: From the phase solubility analysis, Pol 407 was selected as a Solid dispersion carrier. The formation of Cu-SD by melt method using Pol 407, was confirmed from FTIR and DSC studies. XRD studies indicated a change of Cu from crystalline to amorphous form. There was a significant increase of Cu when formulated as SD compared to plain Cu. The optimization of extrusion spheronization process revealed the significant effect of Cu-Pol 407 ratio (p<0.0001) on in vitro dissolution of pellets. Higher Cu dissolution was obtained with Cu-SD pellets compared to plain Cu pellets. Conclusion: The present study demonstrated the potential of Cu-SD pellets in improving the solubility of poorly soluble Cu.

scholarly journals Physicochemical characterization and in vitro dissolution behaviour of celecoxib-β-cyclodextrin inclusion complexes

2007 ◽  
Vol 57 (1) ◽  
pp. 47-60 ◽  
Author(s):  
Vivek Sinha ◽  
R. Anitha ◽  
Soma Ghosh ◽  
Rachana Kumria ◽  
Jayant Bhinge ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Cyclodextrin Inclusion Complexes ◽  
Cyclodextrin Inclusion ◽  
Dissolution Behaviour ◽  
Poorly Soluble

Physicochemical characterization and in vitro dissolution behaviour of celecoxib-β-cyclodextrin inclusion complexes In this study, attempts were made to investigate the effects of β-cyclodextrin (β-CD) on the aqueous solubility and dissolution rate of celecoxib. Inclusion complexes were prepared by the kneading method and characterized by SEM, NMR, IR, DSC, and X-ray powder diffraction. Dissolution rate of the complexes was significantly greater than that of the corresponding physical mixtures and pure drug, indicating that the formation of inclusion complex increased the solubility of the poorly soluble drug celecoxib.

scholarly journals Development and Validation of a Discriminating In Vitro Dissolution Method for Oral Formulations Containing Satranidazole

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Harshal Ashok Pawar ◽  
Pooja Rasiklal Joshi
Keyword(s):  
Water Solubility ◽  
Spectroscopic Method ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
Solution Stability ◽  
Dissolution Medium ◽  
Drug Release Profile ◽  
Drug Products ◽  
Oral Formulations

The development of a meaningful dissolution procedure for drug products with limited water solubility has been a challenge to the pharmaceutical industry. Satranidazole (BCS Class II drug) is a new nitroimidazole derivative with potent antiamoebic action. There is no official dissolution medium available in the literature. In the present study, parameters such as saturation solubility in different pH medium, dissolution behavior of formulations, influence of sink conditions, stability, and discriminatory effect of dissolution testing were studied for the selection of a proper dissolution medium. Results of solubility data revealed that solubility of Satranidazole decreases with an increase in pH. Satranidazole showed better sink condition in 0.1 N HCl as compared to other media. The drug and marketed formulations were stable in the dissolution media used. An agitation speed of 75 rpm showed a more discriminating drug release profile than 50 rpm. Using optimized dissolution parameters (paddle at 75 rpm, 900 mL 0.1 N HCl) greater than 80% of the label amount is released over 60 minutes. UV-spectroscopic method used was validated for the specificity, linearity, precision, robustness, and solution stability. The method was successfully applied to granular formulations and also to marketed tablets containing 300 mg Satranidazole.

scholarly journals A REVIEW ON FLOATING MICROSPHERES

2019 ◽  
Vol 7 (3) ◽  
Author(s):  
T. S. SHINDE ◽  
A. N. BARHATE
Keyword(s):  
Retention Time ◽  
In Vitro Dissolution ◽  
Current Status ◽  
Special Focus ◽  
Gastric Retention ◽  
Oral Formulations ◽  
Floating Drug Delivery ◽  
Floating Drug Delivery System ◽  
Gastric Retention Time

The purpose of writing this review on floating microspheres is to compile the recent literature with special focus on the principle mechanism of floatation to achieve gastric retention. Recent advances indicate that floating microspheres are especially suitable for achieving sustained or delayed release oral formulations with flexibility of blending to attain different release patterns, low risk of dose dumping as well as reproducible and short gastric retention time. One of the approaches toward this goal is to develop the floating microspheres so as to increase the gastric retention time. In this review, the current status of floating microspheres including hollow microspheres (micro balloons) and their characterization, advantages, disadvantages, mechanism and method of preparation for gastric retention of drug are discussed. This review also summarizes the in-vitro dissolution study to evaluate the performance and applications of floating microspheres. Keywords: Floating microspheres, Floating Drug Delivery System, Gastro Retention, Bioavailability, Hydro dynamically Balanced Systems.

Development and Characterization of Aspirin-Phospholipid Complex for Improved Drug Delivery

2010 ◽  
Vol 3 (2) ◽  
pp. 940-947 ◽  
Author(s):  
A Semalty ◽  
M Semalty ◽  
D Singh ◽  
M S M Rawat
Keyword(s):  
In Vitro Dissolution ◽  
Molar Ratio ◽  
X Ray Diffraction ◽  
Phospholipid Complex ◽  
Scanning Calorimetry ◽  
Dissolution Study ◽  
Drug Content ◽  
Poorly Soluble ◽  
Gi Toxicity

Aspirin (acetylsalicylic acid) is one of the most widely used analgesic.  Aspirin is poorly soluble in water and causes gastrointestinal (GI) irritation. To improve the solubility (and hence the bioavailability) and minimize the GI irritation, its complexes with soya-phospholipid-80 % (in  1: 1 molar ratio) were prepared in an organic solvent and evaluated for solubility, drug content, scanning electron microscopy (SEM), FT-IR spectra, X ray diffraction, differential scanning calorimetry (DSC) and in vitro dissolution study. Aspirin-phospholipid complex were found to be disc shaped with rough surface in SEM. Drug content in the complex was found to be 95.6 %. DSC thermograms, XRD and FTIR confirmed the formation of phospholipid complex. Solubility of the prepared complex was found to be improved. Aspirin complex and aspirin showed 90.93 % and 69.42 % of drug release at the end of 10 h in dissolution study in pH 1.2 acid buffer. It was concluded that the phospholipid complex of aspirin may be of potential use for improving the solubility of aspirin and hence its bioavailability. The complexes may also reduce GI toxicity of the drug.  

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